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Pharmacology-NPLEX 2

Key Concepts:

Terms in this set (170)

"Indications: type 2 diabetes
Actions: biguanide that improves peripheral insulin sensitivity, reduces hepatic glucose
production, decreases intestinal glucose absorption, not hypoglycemic
Adverse Effects: may increase cardiovascular mortality, lactic acidosis (rare but 50% lethality;
primarily occurs if renal function declines); may interfere with vit B12; intervening stress
can reduce efficacy
Contraindications: renal failure, metabolic acidosis, type i diabetes; Preg B
Interactions: synergistic with oral hypoglycemics; toxicity enhanced by ethanol; cimetidine
increases absorption
Monitoring Parameters: urine glucose and ketones, fasting serum glucose, HgbA1C,
hematology, renal function, vitamin B12 and folate if anemia is present, serum creatinine
levels
Rx: oral" "Indications: type 2 diabetes
Actions: biguanide that improves peripheral insulin sensitivity, reduces hepatic glucose
production, decreases intestinal glucose absorption, not hypoglycemic
Adverse Effects: may increase cardiovascular mortality, lactic acidosis (rare but 50% lethality;
primarily occurs if renal function declines); may interfere with vit B12; intervening stress
can reduce efficacy
Contraindications: renal failure, metabolic acidosis, type i diabetes; Preg B
Interactions: synergistic with oral hypoglycemics; toxicity enhanced by ethanol; cimetidine
increases absorption
Monitoring Parameters: urine glucose and ketones, fasting serum glucose, HgbA1C,
hematology, renal function, vitamin B12 and folate if anemia is present, serum creatinine
levels
Rx: oral
"Indications: nausea and vomiting due to cancer, emetogenic drugs, radiation, etc.; gastroparesis; GERD; migraines; insufficient lactation
Actions: dopamine D2 antagonist; 5-HT3/5-HT4 agonist, promusacrinic
Adverse effects: restlessness, drowsiness, dizziness, fatigue, dystonia and other extrapyrami-dal effects, blood pressure abnormalities (rare), hyperprolactinemia (rare), agranulocytosis (very rare), neuroleptic malignant syndrome (very rare), tardive dyskinesia (very rare but now an FDA black-box warning)
Contraindications: pheochromocytoma, Parkinson's disease, depression (chronic use), intestinal obstruction, preg B, use for >12 wk
Interactions: synergistic toxicity with other dopamine antagonists (e. g. promethazine, antipsychotics), synergistic toxicity with sedatives (e.g., propoxyphene), increased seizures with bupropion
Monitoring parameters: csc, prolactin, neuro exam (with long-term use)
Rx: oral" "Indications: nausea and vomiting due to cancer, emetogenic drugs, radiation, etc.; gastroparesis; GERD; migraines; insufficient lactation
Actions: dopamine D2 antagonist; 5-HT3/5-HT4 agonist, promusacrinic
Adverse effects: restlessness, drowsiness, dizziness, fatigue, dystonia and other extrapyrami-dal effects, blood pressure abnormalities (rare), hyperprolactinemia (rare), agranulocytosis (very rare), neuroleptic malignant syndrome (very rare), tardive dyskinesia (very rare but now an FDA black-box warning)
Contraindications: pheochromocytoma, Parkinson's disease, depression (chronic use), intestinal obstruction, preg B, use for >12 wk
Interactions: synergistic toxicity with other dopamine antagonists (e. g. promethazine, antipsychotics), synergistic toxicity with sedatives (e.g., propoxyphene), increased seizures with bupropion
Monitoring parameters: csc, prolactin, neuro exam (with long-term use)
Rx: oral
"Indications: short term treatment of atonic constipation (synthetic cathartic laxative) Actions: promote colonic motility directly in the colon
Adverse effects: nausea and vomiting, cramping, obstipation, chronic use can induce atonic constipation and pseudomelanosis coli (harmless colon wall pigmentation; anthraquinone glycosides only), diarrhea, hypokalemia, abuse potential in anorexia nervous and bulimia
Contraindications: do not use for longer than io days consecutively, GI obstruction, spastic constipation, eating disorder, acute intestinal inflammation/pain, Preg C, lactation, diarrhea
Interactions: Interferes with many drugs and herbs by decreasing transit time thus interfering with absorption. Potentiates toxicity of hypokalemia-inducing agents and agents whose toxicity is increased by hypokalemia, e.g., digoxin, steroids, and diuretics.
Rx: oral at bedtime (takes 6-10 hours to take effect), enema (takes effect in 15-60 min)" "Indications: short term treatment of atonic constipation (synthetic cathartic laxative) Actions: promote colonic motility directly in the colon
Adverse effects: nausea and vomiting, cramping, obstipation, chronic use can induce atonic constipation and pseudomelanosis coli (harmless colon wall pigmentation; anthraquinone glycosides only), diarrhea, hypokalemia, abuse potential in anorexia nervous and bulimia
Contraindications: do not use for longer than io days consecutively, GI obstruction, spastic constipation, eating disorder, acute intestinal inflammation/pain, Preg C, lactation, diarrhea
Interactions: Interferes with many drugs and herbs by decreasing transit time thus interfering with absorption. Potentiates toxicity of hypokalemia-inducing agents and agents whose toxicity is increased by hypokalemia, e.g., digoxin, steroids, and diuretics.
Rx: oral at bedtime (takes 6-10 hours to take effect), enema (takes effect in 15-60 min)
"Similar agent: clemastine
Indications: allergic rhinitis, allergic skin disorders, insomnia, motion sickness (prevention and tx), Parkinson's disease, drug-induced extrapyramidal effects, urticaria
Effects: Hi receptor antagonist that crosses blood-brain barrier; cholinergic muscarinic antagonist activity
Adverse effects: drowsiness (>5096 + people taking it, used therapeutically in insomnia), may shorten menstrual cycle; anticholinergic effects (dry eyes, dry mouth, constipation, blurry vision, etc.), tends to lose efficacy over time, Preg B
Contraindications: BPH, acute glaucoma, PUD, bronchial asthma, pneumonia, seizures, chicken pox, elderly, do not take with MAO inhibitors; tolerance develops long term; useless in/may worsen common cold
Interactions: synergistic with other anticholinergic drugs and sedatives (especially ethanol), MAO inhibitors may increase anticholinergic effects
Monitoring parameters: relief of symptoms, mental alertness
Ibc: oral, topical, elderly (may cause dementia-like syndrome) and children more susceptible to effects.
Rx for Anaphylactic shock: 5omg IV combined with epinephrine for severe or slow-onset anaphylaxis; 25-50 mg by mouth every 8 hours for 24 hours for mild anaphylaxis." "Similar agent: clemastine
Indications: allergic rhinitis, allergic skin disorders, insomnia, motion sickness (prevention and tx), Parkinson's disease, drug-induced extrapyramidal effects, urticaria
Effects: Hi receptor antagonist that crosses blood-brain barrier; cholinergic muscarinic antagonist activity
Adverse effects: drowsiness (>5096 + people taking it, used therapeutically in insomnia), may shorten menstrual cycle; anticholinergic effects (dry eyes, dry mouth, constipation, blurry vision, etc.), tends to lose efficacy over time, Preg B
Contraindications: BPH, acute glaucoma, PUD, bronchial asthma, pneumonia, seizures, chicken pox, elderly, do not take with MAO inhibitors; tolerance develops long term; useless in/may worsen common cold
Interactions: synergistic with other anticholinergic drugs and sedatives (especially ethanol), MAO inhibitors may increase anticholinergic effects
Monitoring parameters: relief of symptoms, mental alertness
Ibc: oral, topical, elderly (may cause dementia-like syndrome) and children more susceptible to effects.
Rx for Anaphylactic shock: 5omg IV combined with epinephrine for severe or slow-onset anaphylaxis; 25-50 mg by mouth every 8 hours for 24 hours for mild anaphylaxis.
"Indications: reflux esophagitis, peptic ulcer disease, dyspepsia, Zollinger-Ellison syndrome
(symptom relief only in all)
Actions: histamine-2 antagonist preventing HCl formation in the stomach
Adverse Effects: headache, fatigue, decreased mineral absorption, decreased vitamin B12
absorption, infectious gastroenteritis, intestinal candidiasis, dysbiosis, small intestinal
bacterial overgrowth, pneumonia, phytobezoar formation, increased food allergies,
confusion, psychosis. Preg B
Contraindications: elderly (increases confusion), gastric cancer, renal failure, lactation
Interactions: none significant reported
Monitoring Parameters: GI symptoms, serum B12, iron status
Rx: oral just after meals, withdraw gradually (to avoid rebound hyperacidity), available OTC " "Indications: reflux esophagitis, peptic ulcer disease, dyspepsia, Zollinger-Ellison syndrome
(symptom relief only in all)
Actions: histamine-2 antagonist preventing HCl formation in the stomach
Adverse Effects: headache, fatigue, decreased mineral absorption, decreased vitamin B12
absorption, infectious gastroenteritis, intestinal candidiasis, dysbiosis, small intestinal
bacterial overgrowth, pneumonia, phytobezoar formation, increased food allergies,
confusion, psychosis. Preg B
Contraindications: elderly (increases confusion), gastric cancer, renal failure, lactation
Interactions: none significant reported
Monitoring Parameters: GI symptoms, serum B12, iron status
Rx: oral just after meals, withdraw gradually (to avoid rebound hyperacidity), available OTC
"Indications: erosive esophagitis, peptic ulcer disease, GERD
Actions: proton pump inhibitor thus blocking HC1 formation in the stomach (more potent
than H2 blockers; these drugs basically cause achlorhydria) .
Adverse Effects: infectious gastroenteritis, intestinal candidiasis, dysbiosis, small intestinal
bacterial overgrowth, malabsorption (particularly of carotenoids, vitamin B12, and some
divalent cations), pneumonia, carcinoid gut tumors, atrophic gastritis, carcinogenic, food
allergies
Contraindications: severe liver disease, gastric cancer, Preg B
Monitoring Parameters: GI symptoms, serum B12, iron status
Interactions: increases clarithromycin, diazepam, phenytoin and warfarin. Reduces
absorption of ketoconazole and ampicillin (seen with all proton pump inhibitors).
Rx: oral" "Indications: erosive esophagitis, peptic ulcer disease, GERD
Actions: proton pump inhibitor thus blocking HC1 formation in the stomach (more potent
than H2 blockers; these drugs basically cause achlorhydria) .
Adverse Effects: infectious gastroenteritis, intestinal candidiasis, dysbiosis, small intestinal
bacterial overgrowth, malabsorption (particularly of carotenoids, vitamin B12, and some
divalent cations), pneumonia, carcinoid gut tumors, atrophic gastritis, carcinogenic, food
allergies
Contraindications: severe liver disease, gastric cancer, Preg B
Monitoring Parameters: GI symptoms, serum B12, iron status
Interactions: increases clarithromycin, diazepam, phenytoin and warfarin. Reduces
absorption of ketoconazole and ampicillin (seen with all proton pump inhibitors).
Rx: oral
"Indications: ulcerative colitis, Crohn's disease of colon; RA (if not helped by safer analgesics) Actions: conjugated salicylate analog and a sulfonamide antibiotic (folate antagonist), anti-inflammatory
Adverse Effects: hypersensitivity, may cause folate deficiency; headache, photosensitivity,
anorexia, nausea, vomiting, diarrhea, oligospermia, drowsiness, dizziness Contraindications: use with caution with renal, hepatic impairment; GI or GU obstruction,
children under 2, pregnancy (at term); Preg B/D
Interactions: decreased effect with iron, digoxin, PABA metabolites, oral hypoglycemic drugs Monitoring Parameters: maintain adequate fluid intake; drowsiness, dizziness, anorexia, abdominal pain and nausea with overdose/toxicity
Rx: oral; enteric coated tablets" "Indications: ulcerative colitis, Crohn's disease of colon; RA (if not helped by safer analgesics) Actions: conjugated salicylate analog and a sulfonamide antibiotic (folate antagonist), anti-inflammatory
Adverse Effects: hypersensitivity, may cause folate deficiency; headache, photosensitivity,
anorexia, nausea, vomiting, diarrhea, oligospermia, drowsiness, dizziness Contraindications: use with caution with renal, hepatic impairment; GI or GU obstruction,
children under 2, pregnancy (at term); Preg B/D
Interactions: decreased effect with iron, digoxin, PABA metabolites, oral hypoglycemic drugs Monitoring Parameters: maintain adequate fluid intake; drowsiness, dizziness, anorexia, abdominal pain and nausea with overdose/toxicity
Rx: oral; enteric coated tablets
"Indications: chronic hepatitis B and C (only about 50% effective; minimally effective for 'icy genotype ib), chronic myelogenous leukemia, Kaposi's sarcoma, renal cell carcinoma, esophageal or colorectal ca (with 5-Fu), metastatic malignant melanoma
Actions: antiviral by inhibiting protein synthesis and inducing apoptosis in host cells before or after infection
Adverse effects: mild bone marrow suppression, insomnia, hair loss, depression, sexual dysfunction, and/or debilitating fatigue (seen in 5096+ of patients treated), neutropenia, thyroid autoimmunity, CHF (rare), seizure (rare), hyperglycemia (rare), renal failure (rare), interstitial pneumonitis (rare), suicidal ideation (rare)
Contraindications: pregnancy, renal insufficiency, hypothyroidism, thrombocytopenia, major depression, diabetes mellitus, <age 16 yr, non-liver organ transplant, seizure disorder, active alcoholic, retinopathy, many autoimmune diseases
Interactions: NSAIDS reduce flu-like adverse effects, synergistic bone marrow suppression with zidovudine
Monitoring parameters: monthly cm, serum transaminases, bilirubin, chemistry panel, ophthalmologic exam, clinical depression inventory
Rx: subQ" "Indications: chronic hepatitis B and C (only about 50% effective; minimally effective for 'icy genotype ib), chronic myelogenous leukemia, Kaposi's sarcoma, renal cell carcinoma, esophageal or colorectal ca (with 5-Fu), metastatic malignant melanoma
Actions: antiviral by inhibiting protein synthesis and inducing apoptosis in host cells before or after infection
Adverse effects: mild bone marrow suppression, insomnia, hair loss, depression, sexual dysfunction, and/or debilitating fatigue (seen in 5096+ of patients treated), neutropenia, thyroid autoimmunity, CHF (rare), seizure (rare), hyperglycemia (rare), renal failure (rare), interstitial pneumonitis (rare), suicidal ideation (rare)
Contraindications: pregnancy, renal insufficiency, hypothyroidism, thrombocytopenia, major depression, diabetes mellitus, <age 16 yr, non-liver organ transplant, seizure disorder, active alcoholic, retinopathy, many autoimmune diseases
Interactions: NSAIDS reduce flu-like adverse effects, synergistic bone marrow suppression with zidovudine
Monitoring parameters: monthly cm, serum transaminases, bilirubin, chemistry panel, ophthalmologic exam, clinical depression inventory
Rx: subQ
"Indications: treatment of mild to moderate dementia, such as occurs in Alzheimer's patients;
possibly ADHD
Action: inhibits acetylcholinesterase reversibly and noncompetitively, increasing
concentrations of acetylcholine available in the cisrs
Adverse effects: headache, nausea, diarrhea, syncope, chest pain, hypertension, atrial
fibrillation, hypotension, hot flashes, bruising, anorexia, frequent urination, arthritis and
muscle cramps, ineffective in up to 50% of patients
Contraindications: Preg C
Interactions: inhibited by ketoconazole and quinidine in vitro; synergistic effect possible
with succinylcholine or cholinergic agonists; anticholinergic agents may inhibit effect;
substrate of CYP2D6, 3A4
Monitoring parameters: behavior, mood, bowel function
Rx: oral" "Indications: treatment of mild to moderate dementia, such as occurs in Alzheimer's patients;
possibly ADHD
Action: inhibits acetylcholinesterase reversibly and noncompetitively, increasing
concentrations of acetylcholine available in the cisrs
Adverse effects: headache, nausea, diarrhea, syncope, chest pain, hypertension, atrial
fibrillation, hypotension, hot flashes, bruising, anorexia, frequent urination, arthritis and
muscle cramps, ineffective in up to 50% of patients
Contraindications: Preg C
Interactions: inhibited by ketoconazole and quinidine in vitro; synergistic effect possible
with succinylcholine or cholinergic agonists; anticholinergic agents may inhibit effect;
substrate of CYP2D6, 3A4
Monitoring parameters: behavior, mood, bowel function
Rx: oral
"Indications: osteoporosis (prevention and treatment), symptoms of menopause (increases breast cancer risk), primary ovarian failure, hypogonadism, abnormal uterine bleeding. The idea that estradiol might reduce the risk of atherosclerosis or Alzheimer's disease has been disproven in recent large clinical trials.
Actions: blocks osteoclasts from breaking down old bone but has very little ability to stimulate formation of new bone by osteoblasts, replaces endogenous estrogens' effects on uterus, vaginal epithelium, etc. to relieve symptoms of menopause.
Adverse effects: nausea, dizziness, chloasma, weight gain, folate deficiency. Major toxicity concerns: stroke, myocardial infarction, thrombophlebitis, migraine headache, hypertension, breast cancer, endometrial cancer, liver cancer, cholelithiasis, fibrocystic breasts, worsening of leiomyomata. Combination with progestin increases risk of dementia and cancer even further i libido. j serum SHBG. Preg X.
Contraindications: current smoker, cardiovascular disease, hypertension, thrombophlebitis, any estrogen-sensitive cancer, lactation, hypercalcemia, headache with focal neurological signs, complicated diabetes, liver disease, major surgery and any cause of prolonged immobilization; age > 35 yr.
Interactions: Combine with progesterone to prevent endometrial cancer. May jeffects of warfarin, ielimination of corticosteroids, and itoxicity of tricyclic antidepressants. Impaired by many antibiotics (by disrupting enterohepatic recirculation), phenytoin and barbiturates. ITGB and T3u without affecting free T4. Folate and other B vitamins may reduce some side effects.
Monitoring parameters: clinical signs of DVT; CBC
Rx: patch preferred (avoids first pass metabolism), oral, vaginal cream, IM. Must combine with progesterone or progestin if uterus present (to prevent uterine hyperplasia, dysplasia and carcinoma)" "Indications: osteoporosis (prevention and treatment), symptoms of menopause (increases breast cancer risk), primary ovarian failure, hypogonadism, abnormal uterine bleeding. The idea that estradiol might reduce the risk of atherosclerosis or Alzheimer's disease has been disproven in recent large clinical trials.
Actions: blocks osteoclasts from breaking down old bone but has very little ability to stimulate formation of new bone by osteoblasts, replaces endogenous estrogens' effects on uterus, vaginal epithelium, etc. to relieve symptoms of menopause.
Adverse effects: nausea, dizziness, chloasma, weight gain, folate deficiency. Major toxicity concerns: stroke, myocardial infarction, thrombophlebitis, migraine headache, hypertension, breast cancer, endometrial cancer, liver cancer, cholelithiasis, fibrocystic breasts, worsening of leiomyomata. Combination with progestin increases risk of dementia and cancer even further i libido. j serum SHBG. Preg X.
Contraindications: current smoker, cardiovascular disease, hypertension, thrombophlebitis, any estrogen-sensitive cancer, lactation, hypercalcemia, headache with focal neurological signs, complicated diabetes, liver disease, major surgery and any cause of prolonged immobilization; age > 35 yr.
Interactions: Combine with progesterone to prevent endometrial cancer. May jeffects of warfarin, ielimination of corticosteroids, and itoxicity of tricyclic antidepressants. Impaired by many antibiotics (by disrupting enterohepatic recirculation), phenytoin and barbiturates. ITGB and T3u without affecting free T4. Folate and other B vitamins may reduce some side effects.
Monitoring parameters: clinical signs of DVT; CBC
Rx: patch preferred (avoids first pass metabolism), oral, vaginal cream, IM. Must combine with progesterone or progestin if uterus present (to prevent uterine hyperplasia, dysplasia and carcinoma)
"Specific agents: estradiol (strongest), estrone, estriol (weakest)
Indications: osteoporosis (prevention and treatment), symptoms of menopause, primary ovarian failure, hypogonadism, abnormal uterine bleeding.
Actions: blocks osteoclasts from breaking down old bone but has very little ability to stimulate formation of new bone by osteoblasts, replaces endogenous estrogens' effects on uterus, vaginal epithelium, etc. to relieve symptoms of menopause.
Adverse effects: less toxic than synthetic estrogens. Nausea, dizziness, chloasma, weight gain, folate deficiency. Major toxicity concerns: stroke, myocardial infarction, thrombophlebitis, migraine headache, hypertension, breast cancer, endometrial cancer, liver cancer, cholelithiasis, fibrocystic breasts, worsening of leiomyomata. Preg X.
Contraindications: current smoker, cardiovascular disease, hypertension, thrombophlebitis, any estrogen-sensitive cancer, lactation, hypercalcemia, headache with focal neurological signs, complicated diabetes, liver disease, major surgery and any cause of prolonged immobilization; age > 35 yr.
Interactions: Combine with progesterone to prevent endometrial cancer. May J. effects of warfarin, ielimination of corticosteroids, and I toxicity of tricyclic antidepressants. Impaired by many antibiotics (by disrupting enterohepatic recirculation), phenytoin and barbiturates. TTGB and T3u without affecting free T4. Folate and other B vitamins may reduce some side effects.
Monitoring parameters: clinical signs of DVT; CBC
Rx: patch preferred (avoids first pass metabolism), oral, vaginal cream, IM. Must combine with progesterone or progestin if uterus present (to prevent uterine hyperplasia, dysplasia and carcinoma)" "Specific agents: estradiol (strongest), estrone, estriol (weakest)
"Similar drugs: drospirenone (used in oscp) and Levonorgestrel IUD
Indications: contraception, to counter deleterious effects of estrogens on endometrium, PMS, dysfunctional uterine bleeding, amenorrhea, endometriosis, menopausal symptoms, insufficient lactation, osteoporosis (multiple negative clinical trials have largely disproven this theory)
Actions: prevent implantation, make cervical mucus impenetrable to sperm, replaces effects of endogenous progesterone
Adverse effects: acne, mastalgia, spotting, breakthrough bleeding, amenorrhea Levonorgestrel turn ectopic or interuterine pregnancy, PID, irregular bleeding, ovarian cyst, breast cancer, uterine or cervical perforation
Contraindications: pregnancy (sometimes used to prevent miscarriage), thrombophlebitis, severe atherosclerosis, liver disease, breast or uterine cancer, missed abortion, undiagnosed vaginal bleeding, uterine fibroids, PID, postpartum endometritis
Interactions: aminoglutethimide and rifampin can reduce efficacy of progestins
Monitoring parameters: physical exam, PAP, blood glucose, pregnancy test (IUD), breast exam, signs and symptoms of depression
Rx: po; subdermal levonorgestrel (Norplant) implant—lasts up to 5 yr. IM (Depo-Provera)—lasts up to 3 mo. Intrauterine implantation (mirena)—lasts up to 5 years" "Similar drugs:rugs:* drospirenone (used in oscp) and Levonorgestrel IUD
Indications: contraception, to counter deleterious effects of estrogens on endometrium, PMS, dysfunctional uterine bleeding, amenorrhea, endometriosis, menopausal symptoms, insufficient lactation, osteoporosis (multiple negative clinical trials have largely disproven this theory)
Actions: prevent implantation, make cervical mucus impenetrable to sperm, replaces effects of endogenous progesterone
Adverse effects: acne, mastalgia, spotting, breakthrough bleeding, amenorrhea Levonorgestrel turn ectopic or interuterine pregnancy, PID, irregular bleeding, ovarian cyst, breast cancer, uterine or cervical perforation
Contraindications: pregnancy (sometimes used to prevent miscarriage), thrombophlebitis, severe atherosclerosis, liver disease, breast or uterine cancer, missed abortion, undiagnosed vaginal bleeding, uterine fibroids, PID, postpartum endometritis
Interactions: aminoglutethimide and rifampin can reduce efficacy of progestins
Monitoring parameters: physical exam, PAP, blood glucose, pregnancy test (IUD), breast exam, signs and symptoms of depression
Rx: po; subdermal levonorgestrel (Norplant) implant—lasts up to 5 yr. IM (Depo-Provera)—lasts up to 3 mo. Intrauterine implantation (mirena)—lasts up to 5 years
"Specific drugs: medroxyprogesterone, norelgestromin, norgestimate, norethindrone acetete
Indications: contraception, to counter deleterious effects of estrogens on endometrium, PMS, dysfunctional uterine bleeding, amenorrhea, endometriosis, menopausal symptoms, insufficient lactation. These drugs are toxic and natural progesterone should always be tried first—these should only be resorted to if it is not working, and then with great caution and for as short a time as possible.
Actions: prevent implantation,make cervical mucus impenetrable to sperm, replaces effects of endogenous progesterone
Adverse effects: hypercholesterolemia, fluid retention, impaired glucose tolerance, acne, photosensitivity, mastalgia, spotting, breakthrough bleeding, amenorrhea, breast cancer, dementia, atherosclerosis
Contraindications: pregnancy (sometimes used to prevent miscarriage), thrombophlebitis, severe atherosclerosis, liver disease, breast cancer, missed abortion, undiagnosed vaginal bleeding
Interactions: aminoglutethimide and rifampin can reduce efficacy of progestins Monitoring parameters: physical exam, PAP, signs or symptoms of depression, blood glucose, breast exam
Rx: oral (norgestimate); IM (medroxyprogesterone)—lasts up to 3 mo; patch (norelgestromin)" "Specific drugs: medroxyprogesterone, norelgestromin, norgestimate, norethindrone acetete
Indications: contraception, to counter deleterious effects of estrogens on endometrium, PMS, dysfunctional uterine bleeding, amenorrhea, endometriosis, menopausal symptoms, insufficient lactation. These drugs are toxic and natural progesterone should always be tried first—these should only be resorted to if it is not working, and then with great caution and for as short a time as possible.
Actions: prevent implantation,make cervical mucus impenetrable to sperm, replaces effects of endogenous progesterone
Adverse effects: hypercholesterolemia, fluid retention, impaired glucose tolerance, acne, photosensitivity, mastalgia, spotting, breakthrough bleeding, amenorrhea, breast cancer, dementia, atherosclerosis
Contraindications: pregnancy (sometimes used to prevent miscarriage), thrombophlebitis, severe atherosclerosis, liver disease, breast cancer, missed abortion, undiagnosed vaginal bleeding
Interactions: aminoglutethimide and rifampin can reduce efficacy of progestins Monitoring parameters: physical exam, PAP, signs or symptoms of depression, blood glucose, breast exam
Rx: oral (norgestimate); IM (medroxyprogesterone)—lasts up to 3 mo; patch (norelgestromin)
"Indications: carcinomas of the breast, colon, head and neck, pancreas, rectum or stomach;
topical for management of actinic or solar keratoses, superficial basal cell carcinomas Actions: pyrimidine antimetabolite, blocks methylation of deoxyuridylic and interferes with
DNA synthesis
Adverse effects: dermatitis, vomiting, diarrhea, alopecia, heartburn, nausea, anorexia, stomatitis, esophagitis, leukopenia, GI ulceration, myelosuppression
Contraindications: poor nutritional status, depressed bone marrow function, thrombocy-
topenia, major surgery within the previous month, pregnancy, enzyme deficiency Interactions: decreased effect from methotrexate; cimetidine, leucovorin increase levels; avoid
ethanol
Monitoring parameters: csc with differential, platelet count, renal and liver function tests Rx: iv or topical, depending on individual treatment protocols" "Indications: carcinomas of the breast, colon, head and neck, pancreas, rectum or stomach;
topical for management of actinic or solar keratoses, superficial basal cell carcinomas Actions: pyrimidine antimetabolite, blocks methylation of deoxyuridylic and interferes with
DNA synthesis
Adverse effects: dermatitis, vomiting, diarrhea, alopecia, heartburn, nausea, anorexia, stomatitis, esophagitis, leukopenia, GI ulceration, myelosuppression
Contraindications: poor nutritional status, depressed bone marrow function, thrombocy-
topenia, major surgery within the previous month, pregnancy, enzyme deficiency Interactions: decreased effect from methotrexate; cimetidine, leucovorin increase levels; avoid
ethanol
Monitoring parameters: csc with differential, platelet count, renal and liver function tests Rx: iv or topical, depending on individual treatment protocols
"Indications: venous thrombosis, hypercoagulation state, atrial fibrillation, artificial heart valves
Actions: vitamin K analog, anticoagulant by inhibiting formation and activity of vitamin K-dependent clotting factors (i.e., prothrombin, VII, ix, X)
Adverse Effects: hemorrhage, necrosis, menorrhagia; overdose can be lethal (antidotes—vit K, prothrombin)
Contraindications: hemorrhagic diathesis, CHF, leukemia, visceral cancers, GI bleeding, aneurysm, diverticulitis, malnutrition, severe HTN, severe renal/hepatic dz, endocarditis; Preg X
Interactions: highly protein bound (any other drug that binds proteins more avidly will knock warfarin off its binding sites, increasing amount available to inhibit coagulation)
Drugs that increase warfarin's effects: acetaminophen, androgens, beta blockers, cimetidine, corticosteroids, disulfiram, erythromycin, influenza vaccine, isoniazid, ketoconazole, lovastatin, omeprazole, phenytoin, quinine, quinidine, quinolones, streptokinase, sulfonamides, tamoxifen, thyroid hormones

Drugs that increase warfarin's effects by decreasing vit K: antibiotics
Agents that increase warfarin's effects by inhibiting platelets: cephalosporins, NSAIDS, penicillins, salicylates, onions, garlic, ginger, ginkgo

Agents decreasing warfarin's effects: barbiturates, carbamazepine, estrogens, ethanol, griseofulvin, rifampin, spironolactone, sucralfate, thiazides, trazodone, vitamin K

Monitoring Parameters: monitor PT or INR regularly (2-3 goal) and adjust doses; hematocrit
Rx: oral"
"Related drugs: didanosine (ddI), lamivudine (3TC), zalcitabine (ddC), stavudine (d4T), abacavir (ABC)
Indications: HIV infection, AIDS, prevention of maternal-fetal transmission, post-exposure prophylaxis of infection (e.g., after needle stick)
Actions: nucleoside analog that inhibits reverse transcriptase of my
Adverse Effects: nausea, bone marrow suppression (anemia in 80% of patients; neutropenia), peripheral neuropathy, headache, muscle wasting, myalgia, insomnia, encephalitis, seizures, all worse the more symptomatic the HIV infection, severe allergic reactions (abacavir), pancreatitis (rare), hepatotoxicty with lactic acidosis (rare), resistance can develop
Contraindications: bone marrow failure, myopathy, myositis, obesity (increases risk of hepatotoxicity, use caution), liver dz; Preg C
Interactions: acetaminophen interferes with NRTIS; synergistic toxicity with bone marrow suppressive drugs, IFN, acyclovir, and ganciclovir; fluconazole potentiates it; some NRTIS can be combined, others can't; unpredictable interaction with phenytoin; trimethoprim increases its levels
Monitoring Parameters: CBC, platelet counts, mcv, serum creatinine lcinase, viral load, co,' count, opportunistic infections
Rx: oral; some must be taken with food, others without" "Related drugs: didanosine (ddI), lamivudine (3TC), zalcitabine (ddC), stavudine (d4T), abacavir (ABC)
Indications: HIV infection, AIDS, prevention of maternal-fetal transmission, post-exposure prophylaxis of infection (e.g., after needle stick)
Actions: nucleoside analog that inhibits reverse transcriptase of my
Adverse Effects: nausea, bone marrow suppression (anemia in 80% of patients; neutropenia), peripheral neuropathy, headache, muscle wasting, myalgia, insomnia, encephalitis, seizures, all worse the more symptomatic the HIV infection, severe allergic reactions (abacavir), pancreatitis (rare), hepatotoxicty with lactic acidosis (rare), resistance can develop
Contraindications: bone marrow failure, myopathy, myositis, obesity (increases risk of hepatotoxicity, use caution), liver dz; Preg C
Interactions: acetaminophen interferes with NRTIS; synergistic toxicity with bone marrow suppressive drugs, IFN, acyclovir, and ganciclovir; fluconazole potentiates it; some NRTIS can be combined, others can't; unpredictable interaction with phenytoin; trimethoprim increases its levels
Monitoring Parameters: CBC, platelet counts, mcv, serum creatinine lcinase, viral load, co,' count, opportunistic infections
Rx: oral; some must be taken with food, others without
"Similar agents: ganciclovir, famciclovir, acyclovir, valaciclovir (oral prodrug of acyclovir) Indications: Hsv infxn (herpes labialis, genital herpes), to prevent herpes outbreaks, vzv
(including herpes zoster) and EBV infxn (esp. in immunosuppressed patients), disseminated
neonatal herpes, cmv infxn (relatively ineffective)
Actions: nucleoside analog inhibiting viral replication (inhibits DNA polymerase), non-curative
Adverse Effects: headache, diarrhea, nausea, delirium, tremor, htn, transient renal dysfunction with high doses, encephalopathy (iv); can promote emergence of resistant strains Contraindications: Preg C
Interactions: synergistic toxicity with zidovudine (AzT)
Monitoring Parameters: urinalysis, BUN, serum creatinine, liver enzymes, csc
Rx: topical, oral, iv" "Similar agents: ganciclovir, famciclovir, acyclovir, valaciclovir (oral prodrug of acyclovir) Indications: Hsv infxn (herpes labialis, genital herpes), to prevent herpes outbreaks, vzv
(including herpes zoster) and EBV infxn (esp. in immunosuppressed patients), disseminated
neonatal herpes, cmv infxn (relatively ineffective)
Actions: nucleoside analog inhibiting viral replication (inhibits DNA polymerase), non-curative
Adverse Effects: headache, diarrhea, nausea, delirium, tremor, htn, transient renal dysfunction with high doses, encephalopathy (iv); can promote emergence of resistant strains Contraindications: Preg C
Interactions: synergistic toxicity with zidovudine (AzT)
Monitoring Parameters: urinalysis, BUN, serum creatinine, liver enzymes, csc
Rx: topical, oral, iv
"Similar drugs: penicillin, amoxicillin + clavulanate. Penicillinase-resistant: methicillin,
oxacillin, dicloxacillin.
Indications:
Gram pos: pneumococci, staphylococci (mostly resistant), streptococci, listeriosis, clostridia,
Bacillus spp.
Gram neg: gonorrhea; ampicillin kills H. influenzae, enterobacteria
Spirochete: syphilis
Actions: cell wall synthesis inhibition, bactericidal. Clavulanic acid is a beta-lactamase
inhibitor to reduce resistance.
Adverse effects: dysbiosis, GI upset, resistance common, allergy relatively common
Contraindications: Preg B, allergy relatively common
Interactions: 1.13y tetracyclines. Unpredictable interaction with erythromycin, aminogly-
cosides and chloramphenicol. May ibioavailability of beta blockers. Synergistic with
heparin.
Monitoring Parameters: none" "Similar drugs: penicillin, amoxicillin + clavulanate. Penicillinase-resistant: methicillin,
oxacillin, dicloxacillin.
Indications:
Gram pos: pneumococci, staphylococci (mostly resistant), streptococci, listeriosis, clostridia,
Bacillus spp.
Gram neg: gonorrhea; ampicillin kills H. influenzae, enterobacteria
Spirochete: syphilis
Actions: cell wall synthesis inhibition, bactericidal. Clavulanic acid is a beta-lactamase
inhibitor to reduce resistance.
Adverse effects: dysbiosis, GI upset, resistance common, allergy relatively common
Contraindications: Preg B, allergy relatively common
Interactions: 1.13y tetracyclines. Unpredictable interaction with erythromycin, aminogly-
cosides and chloramphenicol. May ibioavailability of beta blockers. Synergistic with
heparin.
Monitoring Parameters: none
"Similar drugs:
1st generations: cephalexin, cefacetril, cefadroxil
2nd generation: cephamycin, cefaclor, cefprozil, cefuroxime
3rd generation: cefdinir, cefixime, cefpodoxime
4th generation: cefepime, cefclidine, cefclidine
Actions: cell wall synthesis inhibition, bactericidal
Indications:
1st generation: Gram pos: staphylococci, streptococci, anaerobic streptococci. Gram neg: enterobacteria.
2nd generation: Gram pos: strepto¬cocci (weak), Gram neg: gonorrhea, enterobacteria, H. influenzae
3rd generation: Gram neg: gonor¬rhea, enterobacteria, H. influenzae, Pseudomonas
4th generation: Gram pos: streptococcus pneumoniae, group A and B strepto¬cocci, Gram neg: Enterobacteriaceae,

Pseudomonas aeruginosa
Adverse effects: For all: allergic rxn, ur-ticaria, thrombophlebitis, diarrhea, dysbiosis, pseudomembranous colitis, Preg B
1st generation: hypoprothrombinemia 2nd generation: hypoprothrombinemia and bleeding
3rd generation: rust or red colored stools due to iron binding in pediatric popu¬lations. If accompanied by abdominal pain, weight loss, and diarrhea then rule out Clostridium dif ficile infection.
4th generation: headache, nausea Contraindications: allergy to the drug, penicillin allergy (7% of people allergic to penicilin are allergic to 1st generation cephalopsorins)
Interactions: Disulfiram-like interac-
tion with ethanol (2nd and 3rd gen).
inephrotoxicity with aminoglycosides. Monitoring Parameters: none
Rx: oral" "Similar drugs:
1st generations: cephalexin, cefacetril, cefadroxil
2nd generation: cephamycin, cefaclor, cefprozil, cefuroxime
3rd generation: cefdinir, cefixime, cefpodoxime
4th generation: cefepime, cefclidine, cefclidine
Actions: cell wall synthesis inhibition, bactericidal
Indications:
1st generation: Gram pos: staphylococci, streptococci, anaerobic streptococci. Gram neg: enterobacteria.
2nd generation: Gram pos: strepto¬cocci (weak), Gram neg: gonorrhea, enterobacteria, H. influenzae
3rd generation: Gram neg: gonor¬rhea, enterobacteria, H. influenzae, Pseudomonas
4th generation: Gram pos: streptococcus pneumoniae, group A and B strepto¬cocci, Gram neg: Enterobacteriaceae,

Pseudomonas aeruginosa
Adverse effects: For all: allergic rxn, ur-ticaria, thrombophlebitis, diarrhea, dysbiosis, pseudomembranous colitis, Preg B
1st generation: hypoprothrombinemia 2nd generation: hypoprothrombinemia and bleeding
3rd generation: rust or red colored stools due to iron binding in pediatric popu¬lations. If accompanied by abdominal pain, weight loss, and diarrhea then rule out Clostridium dif ficile infection.
4th generation: headache, nausea Contraindications: allergy to the drug, penicillin allergy (7% of people allergic to penicilin are allergic to 1st generation cephalopsorins)
Interactions: Disulfiram-like interac-
tion with ethanol (2nd and 3rd gen).
inephrotoxicity with aminoglycosides. Monitoring Parameters: none
Rx: oral
"Similar drugs: erythromycin
Indications: Chlamydia
Gram pos: pneumococci, staphylococci (mostly resistant), streptococci, listeriosis, clostridia,
Bacillus spp.
Gram neg: gonorrhea; ampicillin kills H. influenzae, enterobacteria
Spirochete: syphilis
Actions: bacterial protein synthesis inhibition, bacteriostatic
Adverse effects: GI irritation (take w/ food); estolate form can cause reversible hepatitis; Preg
Contraindications: liver disease (estolate form)
Interactions: erythromycin TCYP3A4, with potentially lethal interaction with antihistamines astemizole and terfenadine (both off market), and serious toxicity with bromocriptine, carbamazepine, cyclosporine, digoxin, ergot alkaloids, theophylline and prednisone. Unpredictable interaction with penicillin. Azithromycin can itheophylline. Antacids azithromycin absorption.
Monitoring Parameters: none" "Similar drugs: erythromycin
Indications: Chlamydia
Gram pos: pneumococci, staphylococci (mostly resistant), streptococci, listeriosis, clostridia,
Bacillus spp.
Gram neg: gonorrhea; ampicillin kills H. influenzae, enterobacteria
Spirochete: syphilis
Actions: bacterial protein synthesis inhibition, bacteriostatic
Adverse effects: GI irritation (take w/ food); estolate form can cause reversible hepatitis; Preg
Contraindications: liver disease (estolate form)
Interactions: erythromycin TCYP3A4, with potentially lethal interaction with antihistamines astemizole and terfenadine (both off market), and serious toxicity with bromocriptine, carbamazepine, cyclosporine, digoxin, ergot alkaloids, theophylline and prednisone. Unpredictable interaction with penicillin. Azithromycin can itheophylline. Antacids azithromycin absorption.
Monitoring Parameters: none
"Indications: Gram neg: gonorrhea, H. influenzae, Legionnaire's disease, enterobacteria. jiroveci (formerly P. carinii), malaria
Actions: structural analog of ',ABA, dihydropteroate synthetase bacterial enzyme inhibition (blocks folate synthesis), bacteriostatic. Usually given with trimethoprim.
Adverse effects: folate deficiency (Especially in those with marginal folate nutriture, pregnant women, and infants), photosensitivity, allergic reactions common, crystalluria and kidney damage
Contraindications: porphyria, severe liver or renal disease, G6PD deficiency; Preg C
Interactions: Tnephrotoxicity of cyclosporine, bone marrow suppressive effects of methotrexate, and toxicity of phenytoin. Potentiates oral hypoglycemics. Cross sensitivity seen to sulfonylurea hypoglycemics, thiazide and loop diuretics, carbonic anhydrase inhibitors, PABA and local anesthetics.
Monitoring Parameters: none" "Indications: Gram neg: gonorrhea, H. influenzae, Legionnaire's disease, enterobacteria. jiroveci (formerly P. carinii), malaria
Actions: structural analog of ',ABA, dihydropteroate synthetase bacterial enzyme inhibition (blocks folate synthesis), bacteriostatic. Usually given with trimethoprim.
Adverse effects: folate deficiency (Especially in those with marginal folate nutriture, pregnant women, and infants), photosensitivity, allergic reactions common, crystalluria and kidney damage
Contraindications: porphyria, severe liver or renal disease, G6PD deficiency; Preg C
Interactions: Tnephrotoxicity of cyclosporine, bone marrow suppressive effects of methotrexate, and toxicity of phenytoin. Potentiates oral hypoglycemics. Cross sensitivity seen to sulfonylurea hypoglycemics, thiazide and loop diuretics, carbonic anhydrase inhibitors, PABA and local anesthetics.
Monitoring Parameters: none
"Similar drugs: levofloxacin, norfloxacin, ofloxacin
Indications: Chlamydia, Mycoplasma, Mycobacterium
Gram pos: pneumococcus, staphylococci
Gram neg: enterobacteria, Pseudomonas, Legionnaire's disease
Actions: inhibits DNA gyrase, bactericidal
Adverse effects: damage to connective tissue (ligaments and tendons) with sudden rupture
that can happen weeks after discontinuation, dizziness, agitation, dysbiosis, superinfections
Contraindications: Preg C; ct in children (irreversible cartilage damage)
Interactions: Antacids, didanosine, Fe2+, Zn2+, sucralfate ""absorption. Cimetidine
'excretion. Chemotherapy drugs iquinolone levels. Synergistic nephrotoxicity with
cyclosporine. 'caffeine excretion and effects of phenytoin and theophylline. Mg2+ may
reduce chondrotoxicity.
Monitoring Parameters: none" "Similar drugs: levofloxacin, norfloxacin, ofloxacin
Indications: Chlamydia, Mycoplasma, Mycobacterium
Gram pos: pneumococcus, staphylococci
Gram neg: enterobacteria, Pseudomonas, Legionnaire's disease
Actions: inhibits DNA gyrase, bactericidal
Adverse effects: damage to connective tissue (ligaments and tendons) with sudden rupture
that can happen weeks after discontinuation, dizziness, agitation, dysbiosis, superinfections
Contraindications: Preg C; ct in children (irreversible cartilage damage)
Interactions: Antacids, didanosine, Fe2+, Zn2+, sucralfate ""absorption. Cimetidine
'excretion. Chemotherapy drugs iquinolone levels. Synergistic nephrotoxicity with
cyclosporine. 'caffeine excretion and effects of phenytoin and theophylline. Mg2+ may
reduce chondrotoxicity.
Monitoring Parameters: none
"Indications: giardiasis, trichomoniasis, amebiasis, rosacea, anaerobic bacterial infections, Crohn's disease, Helicobacter pylori infection
Actions: reducing agent inside anaerobic organisms, causing DNA damage
Adverse Effects: nausea, vomiting, headache, dry mouth, metallic taste, stomatitis, dizziness, insomnia, hepatotoxic, neurotoxicity from long-term use (paresthesias, seizure), mild leukopenia, harmless darkening of urine; carcinogenic in animals; Preg B
Contraindications: liver failure, first trimester of pregnancy, lactation, elderly (use caution), blood dyscrasias; can exacerbate candidiasis or other infections by inducing dysbiosis
Interactions: do not combine with ethanol or disulfiram (disulfiram-like action by interfering with ethanol degradation and hence buildup of acetaldehyde); barbiturates interfere with it; potentiates warfarin, lithium and phenytoin
Monitoring Parameters: discontinue if seizures or neuropathies occur
Rx: oral with food" "Indications: giardiasis, trichomoniasis, amebiasis, rosacea, anaerobic bacterial infections, Crohn's disease, Helicobacter pylori infection
Actions: reducing agent inside anaerobic organisms, causing DNA damage
Adverse Effects: nausea, vomiting, headache, dry mouth, metallic taste, stomatitis, dizziness, insomnia, hepatotoxic, neurotoxicity from long-term use (paresthesias, seizure), mild leukopenia, harmless darkening of urine; carcinogenic in animals; Preg B
Contraindications: liver failure, first trimester of pregnancy, lactation, elderly (use caution), blood dyscrasias; can exacerbate candidiasis or other infections by inducing dysbiosis
Interactions: do not combine with ethanol or disulfiram (disulfiram-like action by interfering with ethanol degradation and hence buildup of acetaldehyde); barbiturates interfere with it; potentiates warfarin, lithium and phenytoin
Monitoring Parameters: discontinue if seizures or neuropathies occur
Rx: oral with food
"Indications: prophylaxis of organ rejection in kidney, liver, heart transplants; severe active RA not responsive to methotrexate alone; severe psoriasis in non-immunocompromised adults Actions: immunosuppressant agent
Adverse effects: dose-related nephrotoxicity or hepatotoxicity; must be monitored; hypertension
Contraindications: RA or psoriasis with abnormal renal function; uncontrolled hypertension, malignancies; concomitant treatment with PUVA or uvs therapy, methotrexate, coal tar, or radiation in patients with psoriasis
Interactions: increased toxicity with allopurinol, metoclopramide, octreotide; increases toxi¬city of digoxin, diuretics, methotrexate, nifedipine; decreased effects with carbamazepine, nafcillin, phenobarbital, phenytoin, rifampin, isoniazid; decreases effects of live vaccines; nephrotoxicity increased with aminoglycosides, amphotericin B, acyclovir, cimetidine, ketoconazole, lovastatin, NSAIDS; grapefruit juice increases absorption; avoid Hypericum perforatum.
Monitoring parameters: blood pressure, serum creatinine, plasma concentrations of cyclosporine
Rx: oral or iv, depending on individual treatment protocols" "Indications: prophylaxis of organ rejection in kidney, liver, heart transplants; severe active RA not responsive to methotrexate alone; severe psoriasis in non-immunocompromised adults Actions: immunosuppressant agent
Adverse effects: dose-related nephrotoxicity or hepatotoxicity; must be monitored; hypertension
Contraindications: RA or psoriasis with abnormal renal function; uncontrolled hypertension, malignancies; concomitant treatment with PUVA or uvs therapy, methotrexate, coal tar, or radiation in patients with psoriasis
Interactions: increased toxicity with allopurinol, metoclopramide, octreotide; increases toxi¬city of digoxin, diuretics, methotrexate, nifedipine; decreased effects with carbamazepine, nafcillin, phenobarbital, phenytoin, rifampin, isoniazid; decreases effects of live vaccines; nephrotoxicity increased with aminoglycosides, amphotericin B, acyclovir, cimetidine, ketoconazole, lovastatin, NSAIDS; grapefruit juice increases absorption; avoid Hypericum perforatum.
Monitoring parameters: blood pressure, serum creatinine, plasma concentrations of cyclosporine
Rx: oral or iv, depending on individual treatment protocols
These are not as specific for prostatic alpha receptors, and are much more likely to cause hypotension; they tend to be used for hypertension.
Indications: symptom relief due to BPH (does not prevent complications)
Actions: alpha-adrenergic blocking agent relatively specific for alpha receptors in the prostate Adverse effects: orthostatic hypotension, priapism, headache, dizziness, chest pain, abnormal ejaculation, rhinitis
Contraindications: concurrent use with phosphodiesterase-5 inhibitors including sildenafil, hypotension
Interactions: hypotension increased with alpha-adrenergic blockers and calcium channel blockers; cimetidine decreases clearance; blood-pressure lowering effects additive with sildenafil; fasting increases bioavailability
Monitoring parameters: postural blood pressure, symptoms
Rx: oral" "Similar drugs: doxazosin, prazosin, terazosin. These are not as specific for prostatic alpha receptors, and are much more likely to cause hypotension; they tend to be used for hypertension.
Indications: symptom relief due to BPH (does not prevent complications)
Actions: alpha-adrenergic blocking agent relatively specific for alpha receptors in the prostate Adverse effects: orthostatic hypotension, priapism, headache, dizziness, chest pain, abnormal ejaculation, rhinitis
Contraindications: concurrent use with phosphodiesterase-5 inhibitors including sildenafil, hypotension
Interactions: hypotension increased with alpha-adrenergic blockers and calcium channel blockers; cimetidine decreases clearance; blood-pressure lowering effects additive with sildenafil; fasting increases bioavailability
Monitoring parameters: postural blood pressure, symptoms
Rx: oral
"Similar agents: tadalafil, vardenafil
Indications: erectile dysfunction
Actions: affects sexual response by releasing nitrous oxide in the corpus cavernosum, activating guanylate cyclase and increasing cGMP. This produces smooth muscle relaxation and inflow of blood. Has no response in absence of sexual stimulation or patients with unstable angina. Will not overcome lack of sexual desire.
Adverse effects: headache, flushing, bluish visual tint, stuffy nose, hypotension, increased risk of cystitis in female sexual partners
Contraindications: use with nitroglycerin (potentiates hypotensive effects), congestive heart failure, recent heart attack, retinitis pigmentosa
Interactions: nitrates potentiate hypotension; antihypertensives—combine with caution. Metabolized by CYP3A4—increased by drugs such as amprenavir, cimetidine, ciprofloxacin, digoxin, ethanol, fluconazole, grapefruit juice, isoniazid, rifampin, valproate; increases bleeding in patients on heparin; decreased effect with enzyme inducers such as Hypericum perforatum.
Monitoring parameters: cardiovascular status, predisposition to priapism
Rx: administer 30 minutes to 4 hours before sexual activity (optimal is i hour); tablets" "Similar agents: tadalafil, vardenafil
Indications: erectile dysfunction
Actions: affects sexual response by releasing nitrous oxide in the corpus cavernosum, activating guanylate cyclase and increasing cGMP. This produces smooth muscle relaxation and inflow of blood. Has no response in absence of sexual stimulation or patients with unstable angina. Will not overcome lack of sexual desire.
Adverse effects: headache, flushing, bluish visual tint, stuffy nose, hypotension, increased risk of cystitis in female sexual partners
Contraindications: use with nitroglycerin (potentiates hypotensive effects), congestive heart failure, recent heart attack, retinitis pigmentosa
Interactions: nitrates potentiate hypotension; antihypertensives—combine with caution. Metabolized by CYP3A4—increased by drugs such as amprenavir, cimetidine, ciprofloxacin, digoxin, ethanol, fluconazole, grapefruit juice, isoniazid, rifampin, valproate; increases bleeding in patients on heparin; decreased effect with enzyme inducers such as Hypericum perforatum.
Monitoring parameters: cardiovascular status, predisposition to priapism
Rx: administer 30 minutes to 4 hours before sexual activity (optimal is i hour); tablets
"Similar drug: methyltestosterone
Indications: AIDS wasting, anorchia, hypogonadism, osteoporosis; surreptitiously by athletes; andropause; gender identity dysphoria; female-to-male transsexuals
Actions: anabolic on muscle, stimulates sebaceous gland growth, multiple critical roles in secondary sex characteristic development and maintenance; increase bone density; stimulate erythropoietin production; possibly protective against autoimmune disorders
Adverse effects: aggression, stimulates growth of prostate cancer, acne, virilization (in women), gynecomastia (from conversion of testosterone to estrogens), oligospermia, hypercalcemia, hypercholesterolemia, edema, jaundice, liver cancer (long-term use). Oral synthetic methyltestosterone—hepatotoxicity.
Contraindications: severe cardiac, liver or renal disease, breast or prostate cancer, BPH (can worsen), porphyria. Preg X
Interactions: Warfarin potentiated and imipramine toxicity increased by methyltestosterone. All forms decrease TBG and T3u.
Monitoring parameters: liver function tests, PSA, cholesterol, hemoglobin and hematocrit, serum testosterone levels
Rx: oral, IM, patch (best method)" "Similar drug: methyltestosterone
Indications: AIDS wasting, anorchia, hypogonadism, osteoporosis; surreptitiously by athletes; andropause; gender identity dysphoria; female-to-male transsexuals
Actions: anabolic on muscle, stimulates sebaceous gland growth, multiple critical roles in secondary sex characteristic development and maintenance; increase bone density; stimulate erythropoietin production; possibly protective against autoimmune disorders
Adverse effects: aggression, stimulates growth of prostate cancer, acne, virilization (in women), gynecomastia (from conversion of testosterone to estrogens), oligospermia, hypercalcemia, hypercholesterolemia, edema, jaundice, liver cancer (long-term use). Oral synthetic methyltestosterone—hepatotoxicity.
Contraindications: severe cardiac, liver or renal disease, breast or prostate cancer, BPH (can worsen), porphyria. Preg X
Interactions: Warfarin potentiated and imipramine toxicity increased by methyltestosterone. All forms decrease TBG and T3u.
Monitoring parameters: liver function tests, PSA, cholesterol, hemoglobin and hematocrit, serum testosterone levels
Rx: oral, IM, patch (best method)
"Indications: aging, cardiovascular disease, depression, SLE. Low plasma levels are associated with obesity, RA, some cancers, aging, erectile dysfunction and many other conditions. Replacement therapy may be indicated.
Actions: lower blood lipid levels, antineoplastic, anti-glucocorticoid, immunostimulant, improves glucose tolerance, weak androgen, possibly antiviral
Adverse effects: mild androgenic effects (e.g., acne, hirsutism, aggression) Contraindications: G6PD deficiency (high-doses), prostate cancer
Interactions: Levels decreased by exogenous estrogens.
Monitoring parameters: temperature, swelling, blood pressure, liver function tests, physical exam
Rx: oral 10-50 mg qd (high-dose 200+ mg qd; may be necessary to treat autoimmune diseases and depression)" "Indications: aging, cardiovascular disease, depression, SLE. Low plasma levels are associated with obesity, RA, some cancers, aging, erectile dysfunction and many other conditions. Replacement therapy may be indicated.
Actions: lower blood lipid levels, antineoplastic, anti-glucocorticoid, immunostimulant, improves glucose tolerance, weak androgen, possibly antiviral
Adverse effects: mild androgenic effects (e.g., acne, hirsutism, aggression) Contraindications: G6PD deficiency (high-doses), prostate cancer
Interactions: Levels decreased by exogenous estrogens.
Monitoring parameters: temperature, swelling, blood pressure, liver function tests, physical exam
Rx: oral 10-50 mg qd (high-dose 200+ mg qd; may be necessary to treat autoimmune diseases and depression)
"Note: this is an ester local anesthetic, but it is not commonly used due to its' hypertensive and
local vasoconstriction effect
Similar agents: Benzocaine, chloroprocaine, cyclomethycaine; Amphetamines
Indications: upper respiratory tract local anesthetic (nasal and lacrimal duct surgery most
common)
Actions: euphoria resulting from blockage of reuptake of monoamines of norepinephrine,
serotonin, and dopamine (largest effect) in cortex and brainstem; local norepinephine
reuptake inhibition leads to local anesthesia; peripheral adrenergic stimulation; impairs
sweating and cutaneous vasodilation
Adverse Effects: local vasoconstriction, anxiety, hypertension, tachycardia, paranoia,
irritability, depression following use, seizures, cardiac arrhythmia, necrosis and perforation
of nasal septum with chronic inhalation, Preg X
Contraindications: not studied
Interactions: not studied
Monitoring Parameters: cardiovascular health
Rx: topical for anesthia; IV, intranasal, chewing, or smoking for euphoria in non-medicinal
setting" "Note: this is an ester local anesthetic, but it is not commonly used due to its' hypertensive and
local vasoconstriction effect
Similar agents: Benzocaine, chloroprocaine, cyclomethycaine; Amphetamines
Indications: upper respiratory tract local anesthetic (nasal and lacrimal duct surgery most
common)
Actions: euphoria resulting from blockage of reuptake of monoamines of norepinephrine,
serotonin, and dopamine (largest effect) in cortex and brainstem; local norepinephine
reuptake inhibition leads to local anesthesia; peripheral adrenergic stimulation; impairs
sweating and cutaneous vasodilation
Adverse Effects: local vasoconstriction, anxiety, hypertension, tachycardia, paranoia,
irritability, depression following use, seizures, cardiac arrhythmia, necrosis and perforation
of nasal septum with chronic inhalation, Preg X
Contraindications: not studied
Interactions: not studied
Monitoring Parameters: cardiovascular health
Rx: topical for anesthia; IV, intranasal, chewing, or smoking for euphoria in non-medicinal
setting
"Indications: serotonin agonist for treatment of migraine with or without aura
Actions: selective agonist for serotonin 5-HD 1D receptor in cranial arteries, which causes vasoconstriction
Adverse Effects: coronary artery vasospasm, transient ischemia, MI, ventricular tachycardia, vision changes, tingling sensations, tiredness or weakness, upset stomach, dizziness, warm or cold temperature sensations, pain or tightness in chest, difficulty breathing, sudden or severe stomach pain
Contraindications: ischemic heart disease, including Prinzmetal's angina, angina pectoris, MI, silent MI, stroke, TIA, peripheral vascular syndromes; Preg C
Interactions: increased toxicity with ergot-containing drugs; MAOIS decrease clearance; enhances aqs toxic effects when taken with SSRIS like fluoxetine, sertraline
Monitoring Parameters: monitor for chest tightness or pain, excessive drowsiness, acute abdominal pain, skin rash or burning sensation, muscle weakness, soreness, or respiratory difficulty
Rx: single oral dose, with a second dose after 2 hours if there is no satisfactory improvement; subQ injection for acute treatment; intranasal; do not administer iv; adjust dose with hepatic impairment" "Indications: serotonin agonist for treatment of migraine with or without aura
Actions: selective agonist for serotonin 5-HD 1D receptor in cranial arteries, which causes vasoconstriction
Adverse Effects: coronary artery vasospasm, transient ischemia, MI, ventricular tachycardia, vision changes, tingling sensations, tiredness or weakness, upset stomach, dizziness, warm or cold temperature sensations, pain or tightness in chest, difficulty breathing, sudden or severe stomach pain
Contraindications: ischemic heart disease, including Prinzmetal's angina, angina pectoris, MI, silent MI, stroke, TIA, peripheral vascular syndromes; Preg C
Interactions: increased toxicity with ergot-containing drugs; MAOIS decrease clearance; enhances aqs toxic effects when taken with SSRIS like fluoxetine, sertraline
Monitoring Parameters: monitor for chest tightness or pain, excessive drowsiness, acute abdominal pain, skin rash or burning sensation, muscle weakness, soreness, or respiratory difficulty
Rx: single oral dose, with a second dose after 2 hours if there is no satisfactory improvement; subQ injection for acute treatment; intranasal; do not administer iv; adjust dose with hepatic impairment
"Indications: anesthesia esp pediatric, complex regional pain syndrome (cRPs), status
epilepticus, as component of topical agent for nerve pain, experimental antidepressant use Actions: analgesia, anesthesia, sedation, elevated blood pressure, bronchodilation. Adverse effects: hallucinations, dissociative sxs, dizziness, nausea/vomiting, anorexia,
insomnia, arrhythmia, clonic movements, confusion, increase in cerebrospinal fluid
pressure
Contraindications: dissociative disorder, hypertension (potentially), hypersensitivity to ketamine, pre-anesthetic elevated cerebrospinal fluid pressure, acute alcohol or drug intoxication, chronic alcoholism, acute or severe mental illness
Interactions: accentuates analgesic action of opioids, use of barbiturates or narcotics prolongs recovery time
Monitoring parameters: cardiac and respiratory functions
Rx: iv: 1 mg/kg to 4.5 mg/kg for anesthesia; im: 6.5 to 13 mg/kg for anesthesia" "Indications: anesthesia esp pediatric, complex regional pain syndrome (cRPs), status
epilepticus, as component of topical agent for nerve pain, experimental antidepressant use Actions: analgesia, anesthesia, sedation, elevated blood pressure, bronchodilation. Adverse effects: hallucinations, dissociative sxs, dizziness, nausea/vomiting, anorexia,
insomnia, arrhythmia, clonic movements, confusion, increase in cerebrospinal fluid
pressure
Contraindications: dissociative disorder, hypertension (potentially), hypersensitivity to ketamine, pre-anesthetic elevated cerebrospinal fluid pressure, acute alcohol or drug intoxication, chronic alcoholism, acute or severe mental illness
Interactions: accentuates analgesic action of opioids, use of barbiturates or narcotics prolongs recovery time
Monitoring parameters: cardiac and respiratory functions
Rx: iv: 1 mg/kg to 4.5 mg/kg for anesthesia; im: 6.5 to 13 mg/kg for anesthesia
"Indications: Parkinson's disease, Parkinsonism, herpes zoster pain, restless legs syndrome Action: carbidopa inhibits dopamine carboxylase, thus decreasing peripheral catabolism of
levodopa (L-dopa); levodopa enters civs, then is converted into dopamine (deficient in
Parkinsonism)
Adverse Effects: anorexia, nausea, vomiting, depression, mood changes, anxiety; long-term—hallucinations, dyskinesias, and loss of effect after a few years
Contraindications: glaucoma, use with MAO-A inhibitors, melanoma, liver or renal dz, COPD, peptic ulcer (can activate), psychosis, lactation; Preg C
Interactions: pyridoxine increases peripheral dopa catabolism—carbidopa compensates (except possibly with pyridoxine doses >500 mg qd); anticholinergics and benzodiazepines interfere with L-dopa; avoid alcohol due to cisrs depression
Monitoring Parameters: monitor blood pressure standing, sitting and supine; assess for symptoms of parkinsonism, dyskinesias, mental status changes
Rx: oral; must increase dose over time (which worsens adverse effects); do not take with meals (competitive uptake with amino acids); take protein in pm and drug in am to avoid absorption problems" "Indications: Parkinson's disease, Parkinsonism, herpes zoster pain, restless legs syndrome Action: carbidopa inhibits dopamine carboxylase, thus decreasing peripheral catabolism of
levodopa (L-dopa); levodopa enters civs, then is converted into dopamine (deficient in
Parkinsonism)
Adverse Effects: anorexia, nausea, vomiting, depression, mood changes, anxiety; long-term—hallucinations, dyskinesias, and loss of effect after a few years
Contraindications: glaucoma, use with MAO-A inhibitors, melanoma, liver or renal dz, COPD, peptic ulcer (can activate), psychosis, lactation; Preg C
Interactions: pyridoxine increases peripheral dopa catabolism—carbidopa compensates (except possibly with pyridoxine doses >500 mg qd); anticholinergics and benzodiazepines interfere with L-dopa; avoid alcohol due to cisrs depression
Monitoring Parameters: monitor blood pressure standing, sitting and supine; assess for symptoms of parkinsonism, dyskinesias, mental status changes
Rx: oral; must increase dose over time (which worsens adverse effects); do not take with meals (competitive uptake with amino acids); take protein in pm and drug in am to avoid absorption problems
"Indications: seizure (partial, grand ma!, mixed), trigeminal neuralgia, neuralgia, bipolar disorders, schizophrenia, restless legs syndrome, withdrawal of ethanol, cocaine or benzodiazepines
One you're not likely to see: exaggerated sexual behavior from temporal lobe injuries
Actions: iminostilbene-type anticonvulsant and anti-neuralgic; decreases neuron impulse transmission and reduces neuron excitability in cm; voltage-dependent sodium channels blocked, so repetitive action potentials can't occur (similar to phenytoin); chemical structure similar to tricyclics, but not anti-depressant
Adverse effects: drowsiness, vertigo, ataxia, diplopia, blurred vision, increased seizure frequency (!), edema (interferes with ADH), GI upset, liver toxicity, mild transient (after months of use) leukopenia, aplastic anemia (rare, can be irreversible), agranulocytosis, decreased libido, photosensitivity
Contraindications: use with MAOIS, hepatic failure, petit mal seizures, CHF, bone marrow suppression; Preg C
Interactions: interferes with or is interfered with by most other anti-seizure meds; interferes with haloperidol, OCPS, doxycycline, and warfarin; increases toxicity of acetaminophen and lithium; increased effects or toxicity due to inhibited metabolism when combined with cimetidine, isoniazid, verapamil, propoxyphene, SSRIS, and erythromycin
Monitoring Parameters: csc with platelet count, reticulocytes, serum iron, liver function tests, urinalysis, BUN, serum carbamazepine levels, thyroid function tests, serum sodium; observe patient for excessive sedation when beginning or increasing therapy
Rx: oral; take with food" "Indications: seizure (partial, grand ma!, mixed), trigeminal neuralgia, neuralgia, bipolar disorders, schizophrenia, restless legs syndrome, withdrawal of ethanol, cocaine or benzodiazepines
One you're not likely to see: exaggerated sexual behavior from temporal lobe injuries
Actions: iminostilbene-type anticonvulsant and anti-neuralgic; decreases neuron impulse transmission and reduces neuron excitability in cm; voltage-dependent sodium channels blocked, so repetitive action potentials can't occur (similar to phenytoin); chemical structure similar to tricyclics, but not anti-depressant
Adverse effects: drowsiness, vertigo, ataxia, diplopia, blurred vision, increased seizure frequency (!), edema (interferes with ADH), GI upset, liver toxicity, mild transient (after months of use) leukopenia, aplastic anemia (rare, can be irreversible), agranulocytosis, decreased libido, photosensitivity
Contraindications: use with MAOIS, hepatic failure, petit mal seizures, CHF, bone marrow suppression; Preg C
Interactions: interferes with or is interfered with by most other anti-seizure meds; interferes with haloperidol, OCPS, doxycycline, and warfarin; increases toxicity of acetaminophen and lithium; increased effects or toxicity due to inhibited metabolism when combined with cimetidine, isoniazid, verapamil, propoxyphene, SSRIS, and erythromycin
Monitoring Parameters: csc with platelet count, reticulocytes, serum iron, liver function tests, urinalysis, BUN, serum carbamazepine levels, thyroid function tests, serum sodium; observe patient for excessive sedation when beginning or increasing therapy
Rx: oral; take with food
"Indications: seizure (tonic-clonic, psychomotor, myoclonic, focal), trigeminal neuralgia Actions: hydantoin-type anticonvulsant (slows rate of recovery of voltage-activated sodium
channels in neurons, limiting repetitive neuron firing and their overall excitability);
stimulates fibroblasts, good for wound healing
Adverse effects: hyperplastic gums (excreted partly in the saliva; 20% of patients), hirsutism, impaired intellectual development, sluggishness, fatigue, pink/red or brown urine, decreased libido, Peyronie's dz, hyperglycemia (interferes with insulin secretion), megaloblastic (interferes with folic acid) or aplastic anemia, hypoglycemia, osteomalacia (interferes with vitamin D and increases vitamin K breakdown), lymphadenopathy (due to decreased IgA production), hepatitis (rare), SLE (rare), nephritis; binds TBG, thus creates apparent TBG deficiency (decreases total T4 with normal T7)
Contraindications: arrhythmias, absence (petit mal) seizures (may worsen), Dm; Preg D
Interactions: highly protein bound; may decrease activity of OCPS, corticosteroids, acetaminophen (while increasing hepatotoxicity), digitalis, doxycycline, quinidine, and theophylline; phenytoin and carbamazepine mutually interfere with each other; unpredictable interactions with phenobarbital and ethanol
Folate, vitamin D and vitamin K are critical to prevent nutrient deficiency-related adverse effects (though folate may decrease phenytoin activity).
Decreases phenytoin by increasing its metabolism: theophylline
Increases phenytoin by inhibiting its metabolism: chloramphenicol, dicumarol, disulfiram, isoniazid, cimetidine, sulfonamides, valproic acid, phenylbutazone
Monitoring Parameters: narrow therapeutic window; OD dangerous (rapid saturation of liver phenytoin metabolism); BP, vitals (with I.V.), plasma phenytoin level, cm, liver function tests
Rx: oral with monitoring of blood levels; withdraw slowly to avoid status epilepticus" "Indications: seizure (tonic-clonic, psychomotor, myoclonic, focal), trigeminal neuralgia Actions: hydantoin-type anticonvulsant (slows rate of recovery of voltage-activated sodium
channels in neurons, limiting repetitive neuron firing and their overall excitability);
stimulates fibroblasts, good for wound healing
Adverse effects: hyperplastic gums (excreted partly in the saliva; 20% of patients), hirsutism, impaired intellectual development, sluggishness, fatigue, pink/red or brown urine, decreased libido, Peyronie's dz, hyperglycemia (interferes with insulin secretion), megaloblastic (interferes with folic acid) or aplastic anemia, hypoglycemia, osteomalacia (interferes with vitamin D and increases vitamin K breakdown), lymphadenopathy (due to decreased IgA production), hepatitis (rare), SLE (rare), nephritis; binds TBG, thus creates apparent TBG deficiency (decreases total T4 with normal T7)
Contraindications: arrhythmias, absence (petit mal) seizures (may worsen), Dm; Preg D
Interactions: highly protein bound; may decrease activity of OCPS, corticosteroids, acetaminophen (while increasing hepatotoxicity), digitalis, doxycycline, quinidine, and theophylline; phenytoin and carbamazepine mutually interfere with each other; unpredictable interactions with phenobarbital and ethanol
Folate, vitamin D and vitamin K are critical to prevent nutrient deficiency-related adverse effects (though folate may decrease phenytoin activity).
Decreases phenytoin by increasing its metabolism: theophylline
Increases phenytoin by inhibiting its metabolism: chloramphenicol, dicumarol, disulfiram, isoniazid, cimetidine, sulfonamides, valproic acid, phenylbutazone
Monitoring Parameters: narrow therapeutic window; OD dangerous (rapid saturation of liver phenytoin metabolism); BP, vitals (with I.V.), plasma phenytoin level, cm, liver function tests
Rx: oral with monitoring of blood levels; withdraw slowly to avoid status epilepticus
DELETE NOT ON LIST
Indications: Acute convulsive episodes, tonic-clonic (partial and generalized) seizures, status elipticus, recurrent febril seizures, insomnia (short-term treatment), and sedation
Actions: Depress sensory cortex though increasing GABA action and decreasing glutamine; results in decreased motor activity, drowsiness, sedation, hypnosis, anesthesia, and altered cerebellar function
Adverse Effects: Somnolence, tiredness upon waking, nausea, vertigo, tremors, decreased cognitive performance in children, addictive, Preg D
Contraindications: Porphyria, impaired liver or renal function, severe respiratory disease, Interactions: Depletes Vit D, Vit K, biotin, calcium, and folic acid; alcohol increases CNS depressant effects, MAOI, charcoal, chloramphenicol, rifampin, valproic acid,
Monitoring Parameters: CBC, renal function tests, Liver panel
Rx: oral or IV" "Similar agents: Amobarbital, aprobarbital, butabarbital, mephobarbital, pentobarbital, and secobarbital
Indications: Acute convulsive episodes, tonic-clonic (partial and generalized) seizures, status elipticus, recurrent febril seizures, insomnia (short-term treatment), and sedation
Actions: Depress sensory cortex though increasing GABA action and decreasing glutamine; results in decreased motor activity, drowsiness, sedation, hypnosis, anesthesia, and altered cerebellar function
Adverse Effects: Somnolence, tiredness upon waking, nausea, vertigo, tremors, decreased cognitive performance in children, addictive, Preg D
Contraindications: Porphyria, impaired liver or renal function, severe respiratory disease, Interactions: Depletes Vit D, Vit K, biotin, calcium, and folic acid; alcohol increases CNS depressant effects, MAOI, charcoal, chloramphenicol, rifampin, valproic acid,
Monitoring Parameters: CBC, renal function tests, Liver panel
Rx: oral or IV
"Indications: jetlag, shift work, insomnia due to circadian rhythm disturbance, seasonal affective disorder, cancer (very-high dose)
Actions: methylated and N-acetylated product of serotonin found in pineal gland and released
at night; regulatory molecule of diurnal rhythms (not directly sedative); interacts with
melatonin receptors throughout body; antioxidant, immunomodulating, antineoplastic Adverse Effects: nausea, morning drowsiness, headache, hyperprolactinemia (rare) Contraindications: use in daytime (possibly ok in shift workers)
Interactions: potential serotonin syndrome if combined with SSRIS; SSRIS may lower endogenous melatonin; synergistic benefits with many chemotherapy drugs Monitoring Parameters: monitor for insomnia and sleep disturbances
Rx: oral; 500 mcg-5 mg hs for regulation of diurnal rhythms; 30 mg hs for cancer" "Indications: jetlag, shift work, insomnia due to circadian rhythm disturbance, seasonal affective disorder, cancer (very-high dose)
Actions: methylated and N-acetylated product of serotonin found in pineal gland and released
at night; regulatory molecule of diurnal rhythms (not directly sedative); interacts with
melatonin receptors throughout body; antioxidant, immunomodulating, antineoplastic Adverse Effects: nausea, morning drowsiness, headache, hyperprolactinemia (rare) Contraindications: use in daytime (possibly ok in shift workers)
Interactions: potential serotonin syndrome if combined with SSRIS; SSRIS may lower endogenous melatonin; synergistic benefits with many chemotherapy drugs Monitoring Parameters: monitor for insomnia and sleep disturbances
Rx: oral; 500 mcg-5 mg hs for regulation of diurnal rhythms; 30 mg hs for cancer
"Indications: short-term treatment of insomnia
Actions: structurally dissimilar to benzodiazepines, but much of its actions are explained by its effects on benzodiazepine receptors; has hypnotic properties but reduced effects on skeletal muscle and seizure threshold
Adverse Effects: use only after evaluation of causes of sleep disturbance; use with caution in depression; use with other sedative drugs or alcohol may potentiate effects; other effects include palpitations, headache, drowsiness, lethargy, dizziness, abnormal dreams, amnesia, rash, confusion, impaired concentration, coma and hypotension
Contraindications: long-term use without evaluation of cause of insomnia, abrupt withdrawal, use while operating heavy machinery or in dangerous situations, liver failure
Interactions: ciis depression with other centrally acting drugs; increased effects with erythromycin, ketoconazole, verapamil; reduced effects with rifampin, other enzyme inducers
Monitoring Parameters: daytime alertness, respiratory and cardiac status
Rx: oral; duration of therapy limited to 7-10 days" "Indications: short-term treatment of insomnia
Actions: structurally dissimilar to benzodiazepines, but much of its actions are explained by its effects on benzodiazepine receptors; has hypnotic properties but reduced effects on skeletal muscle and seizure threshold
Adverse Effects: use only after evaluation of causes of sleep disturbance; use with caution in depression; use with other sedative drugs or alcohol may potentiate effects; other effects include palpitations, headache, drowsiness, lethargy, dizziness, abnormal dreams, amnesia, rash, confusion, impaired concentration, coma and hypotension
Contraindications: long-term use without evaluation of cause of insomnia, abrupt withdrawal, use while operating heavy machinery or in dangerous situations, liver failure
Interactions: ciis depression with other centrally acting drugs; increased effects with erythromycin, ketoconazole, verapamil; reduced effects with rifampin, other enzyme inducers
Monitoring Parameters: daytime alertness, respiratory and cardiac status
Rx: oral; duration of therapy limited to 7-10 days
Indications: narcolepsy, shift work sleep disorder, sleepiness due to obstructive sleep apnea, ADHD (controversial)
Actions: enhances CNS catecholamine and histamine release, mild memory enhancer Adverse effects: insomnia, restlessness, hypertension, small risk of addiction with long-term use
Contraindications: use in athletes, liver cirrhosis, severe cardiovascular problems. Schedule iv drug in us.
Interactions: may offset somnolence due to a range of drugs, may interact with alcohol, synergistic toxicity with other stimulants (including Pausinystalia yohimbe and Ephedra sinica), may interfere with OCPS
Monitoring parameters: blood pressure in hypertensive patient, CVD parameters in ADHD cases (heart rate, etc), levels of sleepiness, body mass index and weight loss, exacerbation of psychiatric symptoms
Rx: oral (in morning/afternoon only)" "Indications: narcolepsy, shift work sleep disorder, sleepiness due to obstructive sleep apnea, ADHD (controversial)
Actions: enhances CNS catecholamine and histamine release, mild memory enhancer Adverse effects: insomnia, restlessness, hypertension, small risk of addiction with long-term use
Contraindications: use in athletes, liver cirrhosis, severe cardiovascular problems. Schedule iv drug in us.
Interactions: may offset somnolence due to a range of drugs, may interact with alcohol, synergistic toxicity with other stimulants (including Pausinystalia yohimbe and Ephedra sinica), may interfere with OCPS
Monitoring parameters: blood pressure in hypertensive patient, CVD parameters in ADHD cases (heart rate, etc), levels of sleepiness, body mass index and weight loss, exacerbation of psychiatric symptoms
Rx: oral (in morning/afternoon only)
"Indications: skeletal muscle relaxant; muscle spasm, myalgia, acute painful musculoskeletal conditions w/limited mobility
Action: centrally active muscle relaxant that blocks neuron transmission in the spinal cord Adverse effects: sleepiness, dizziness, vertigo, lack of concentration, insomnia, agitation;
dependence rare with mild withdrawal symptoms; overdose dangerous if combined
w/alcohol or psychoactive drugs
Contraindications: acute intermittent porphyria, liver disease, kidney disease, lactation; Preg: C
Interactions: major substrate of CYP2C19; delaviridine, fluconazole, fluvoxamine, omeprazole may increase effects; alcohol, cisTs depressants, psychotropic drugs may increase toxicity
Monitoring parameters: assess pain relief, avoid excessive drowsiness
Rx: oral; often comes combined with aspirin or codeine (qv)." "Indications: skeletal muscle relaxant; muscle spasm, myalgia, acute painful musculoskeletal conditions w/limited mobility
Action: centrally active muscle relaxant that blocks neuron transmission in the spinal cord Adverse effects: sleepiness, dizziness, vertigo, lack of concentration, insomnia, agitation;
dependence rare with mild withdrawal symptoms; overdose dangerous if combined
w/alcohol or psychoactive drugs
Contraindications: acute intermittent porphyria, liver disease, kidney disease, lactation; Preg: C
Interactions: major substrate of CYP2C19; delaviridine, fluconazole, fluvoxamine, omeprazole may increase effects; alcohol, cisTs depressants, psychotropic drugs may increase toxicity
Monitoring parameters: assess pain relief, avoid excessive drowsiness
Rx: oral; often comes combined with aspirin or codeine (qv).
"Indications: narcolepsy, ADD (ADHD), weight loss, abuse/recreational (as CNS stimulants) Action: release of stored norepinephrine from pre-synaptic terminals
Adverse effects: insomnia, irritability, tremor, paranoia, tachycardia, headache, tolerance, addiction, psychosis (overdose); depression, hypersomnia and fatigue after discontinuation
Contraindications: advanced atherosclerosis, hypertension, hyperthyroid, glaucoma, diabetes mellitus, drug abuse, insomnia, schizophrenia, anorexia nervosa, pregnancy, lactation, MAO inhibitors (increase effects of Ritalin), tricyclic antidepressants (decrease effects of Ritalin); Preg C (avoid in pregnancy and lactation)
Interactions: Major substrate of CYP2D6; hypertensive effects with MAO inhibitors; may increase levels of phenytoin, phenobarbitol, warfarin; increased toxicity with clonidine, sibutramine.
Monitoring parameters: blood pressure, heart rate, csc with differential, platelet counts, signs of c/sTs stimulation, symptoms of depression
Rx: oral; schedule II drug" "Indications: narcolepsy, ADD (ADHD), weight loss, abuse/recreational (as CNS stimulants) Action: release of stored norepinephrine from pre-synaptic terminals
Adverse effects: insomnia, irritability, tremor, paranoia, tachycardia, headache, tolerance, addiction, psychosis (overdose); depression, hypersomnia and fatigue after discontinuation
Contraindications: advanced atherosclerosis, hypertension, hyperthyroid, glaucoma, diabetes mellitus, drug abuse, insomnia, schizophrenia, anorexia nervosa, pregnancy, lactation, MAO inhibitors (increase effects of Ritalin), tricyclic antidepressants (decrease effects of Ritalin); Preg C (avoid in pregnancy and lactation)
Interactions: Major substrate of CYP2D6; hypertensive effects with MAO inhibitors; may increase levels of phenytoin, phenobarbitol, warfarin; increased toxicity with clonidine, sibutramine.
Monitoring parameters: blood pressure, heart rate, csc with differential, platelet counts, signs of c/sTs stimulation, symptoms of depression
Rx: oral; schedule II drug
"Note: lisdexamfetamine is a prodrug
Indications: fatigue, excess appetite, ADHD (particularly as d,1-amphetamine), narcolepsy,
depression (treatment-resistant)
Actions: sympathomimetic by increasing release of dopamine and noradrenaline
Adverse effects: euphoria, anorexia, restlessness, anxiety, hypertension, dry mouth,
insomnia, tachycardia, MI, stroke, death, amphetamine psychosis (overdose), addiction
Contraindications: glaucoma, hypertension, hyperthyroidism, seizure disorder, arterioscle-
rosis (severe)
Interactions: hypertensive crisis with mikois, alkaline urine decreases renal excretion,
synergistic with other sympathomimetics
Monitoring parameters: watch for signs of tolerance and addiction; regularly monitor blood
pressure and body weight
Rx: oral; schedule II drug" "Note: lisdexamfetamine is a prodrug
Indications: fatigue, excess appetite, ADHD (particularly as d,1-amphetamine), narcolepsy,
depression (treatment-resistant)
Actions: sympathomimetic by increasing release of dopamine and noradrenaline
Adverse effects: euphoria, anorexia, restlessness, anxiety, hypertension, dry mouth,
insomnia, tachycardia, MI, stroke, death, amphetamine psychosis (overdose), addiction
Contraindications: glaucoma, hypertension, hyperthyroidism, seizure disorder, arterioscle-
rosis (severe)
Interactions: hypertensive crisis with mikois, alkaline urine decreases renal excretion,
synergistic with other sympathomimetics
Monitoring parameters: watch for signs of tolerance and addiction; regularly monitor blood
pressure and body weight
Rx: oral; schedule II drug
"Similar agents: isocarboxazid, tranylcypromine
Indications: depression, severe anxiety
Actions: inhibits the enzyme monoamine oxidase which breaks down epinephrine, nore-pinephrine, dopamine, and serotonin; with that enzyme halted these neurotransmitters accumulate within the presynaptic cleft
Adverse Effects: hypertension, orthostatic hypotension, hypomania, Preg C Contraindications: pheochromocytoma, congestive heart failure, Liver disease, renal impairment, over 6oyoa,
Interactions: foods with tyramine or tryptophan content (watch for hypertensive crisis), caffeine, alcohol, SSRIS and TCAS (watch for serotonin syndrome) and many other drug interactions (such as methyphenidate, barbiturates, beta blockers, buspirone, carbamazepine, levodopa, sympathomimetics, etc.)
Monitoring Parameters: BP, Liver panel,
Rx: oral (15mg 3 times day starting and increase up to 3 omg 3 times day; will take 4 weeks of 2omg 3 times a day to show improvement)" "Similar agents: isocarboxazid, tranylcypromine
Indications: depression, severe anxiety
Actions: inhibits the enzyme monoamine oxidase which breaks down epinephrine, nore-pinephrine, dopamine, and serotonin; with that enzyme halted these neurotransmitters accumulate within the presynaptic cleft
Adverse Effects: hypertension, orthostatic hypotension, hypomania, Preg C Contraindications: pheochromocytoma, congestive heart failure, Liver disease, renal impairment, over 6oyoa,
Interactions: foods with tyramine or tryptophan content (watch for hypertensive crisis), caffeine, alcohol, SSRIS and TCAS (watch for serotonin syndrome) and many other drug interactions (such as methyphenidate, barbiturates, beta blockers, buspirone, carbamazepine, levodopa, sympathomimetics, etc.)
Monitoring Parameters: BP, Liver panel,
Rx: oral (15mg 3 times day starting and increase up to 3 omg 3 times day; will take 4 weeks of 2omg 3 times a day to show improvement)
"Similar agents: paroxetine, sertraline, citalopram
Indications: major depression, obsessive-compulsive disorder, eating disorders, chronic fatigue syndrome, fibromyalgia, PMS
Actions: inhibits reuptake of serotonin by cisis neurons, leading to increased serotonin levels in cm; a selective serotonin reuptake inhibitor (ssm). The cisis stimulation side effects are not clearly understood, as supposedly high serotonin levels in cisis are calming. Takes 2-4 weeks to achieve equilibrium blood levels and clinical results.
Adverse effects: insomnia, sexual dysfunction, headache, diarrhea, agitation/anxiety Rare but serious: suicide or homicide; serotonin syndrome (rare, acute, anxiety, chills, confusion, insomnia, ataxia, akathisia, hyperreflexia, diaphoresis, tremor, seizures, coma) Contraindications: liver failure, mania (can activate it in bipolar patients), seizure disorders (use caution)
Interactions: don't use with MAO inhibitors or tricyclics-5 wk washout period if using in sequence. May ihypoglycemic agents. Fluoxetine and paroxetine strongly 'some liver enzymes (fluvoxamine and sertraline less so), and can affect many drugs (esp. other antidepressants, phenothiazine neuroleptics, and antiarrhythmics, esp. quinidine). Highly protein bound—may displace other highly bound drugs (e.g., aspirin, warfarin). Synergistic with tryptophan.
Monitoring parameters: symptoms of depression, anxiety, sleep
Rx: oral in morning (due to tendency to stimulate); Half life: 48-72 hrs (longest half-life of the class due to active metabolite). Preg B (other SSRIS are preg C)." "Similar agents: paroxetine, sertraline, citalopram
Indications: major depression, obsessive-compulsive disorder, eating disorders, chronic fatigue syndrome, fibromyalgia, PMS
Actions: inhibits reuptake of serotonin by cisis neurons, leading to increased serotonin levels in cm; a selective serotonin reuptake inhibitor (ssm). The cisis stimulation side effects are not clearly understood, as supposedly high serotonin levels in cisis are calming. Takes 2-4 weeks to achieve equilibrium blood levels and clinical results.
Adverse effects: insomnia, sexual dysfunction, headache, diarrhea, agitation/anxiety Rare but serious: suicide or homicide; serotonin syndrome (rare, acute, anxiety, chills, confusion, insomnia, ataxia, akathisia, hyperreflexia, diaphoresis, tremor, seizures, coma) Contraindications: liver failure, mania (can activate it in bipolar patients), seizure disorders (use caution)
Interactions: don't use with MAO inhibitors or tricyclics-5 wk washout period if using in sequence. May ihypoglycemic agents. Fluoxetine and paroxetine strongly 'some liver enzymes (fluvoxamine and sertraline less so), and can affect many drugs (esp. other antidepressants, phenothiazine neuroleptics, and antiarrhythmics, esp. quinidine). Highly protein bound—may displace other highly bound drugs (e.g., aspirin, warfarin). Synergistic with tryptophan.
Monitoring parameters: symptoms of depression, anxiety, sleep
Rx: oral in morning (due to tendency to stimulate); Half life: 48-72 hrs (longest half-life of the class due to active metabolite). Preg B (other SSRIS are preg C).
"Indications: depression, smoking cessation, obesity, seasonal affective disorder
Actions: norepinephrine reuptake inhibitor (possibly via central alpha-2 adrenergic receptor
blockade, like yohimbine), dopamine reuptake inhibitor
Adverse effects: nausea, dry mouth, insomnia, tremor, sweating, tinnitus, increased
suicidality in youth, anxiety
Rare but serious: mania (or activation of it in bipolar patients), agranulocytosis, overdose
can occur
Contraindications: seizure disorders (lowers seizure threshold mildly), sudden discontinu-
ation
Interactions: mAois Ttoxicity. Bupropioni CYP2D6 thus T serum levels of drugs metabolized
by this enzyme and may /their toxicity (TcA, SSRI, some antipsychotics, some beta-
blockers, esp. metoprolol, and type IC antiarrhythmics such as propafenone, flecanide).
Metabolized by CYP2B6.
Monitoring parameters: none
Rx: oral" "Indications: depression, smoking cessation, obesity, seasonal affective disorder
Actions: norepinephrine reuptake inhibitor (possibly via central alpha-2 adrenergic receptor
blockade, like yohimbine), dopamine reuptake inhibitor
Adverse effects: nausea, dry mouth, insomnia, tremor, sweating, tinnitus, increased
suicidality in youth, anxiety
Rare but serious: mania (or activation of it in bipolar patients), agranulocytosis, overdose
can occur
Contraindications: seizure disorders (lowers seizure threshold mildly), sudden discontinu-
ation
Interactions: mAois Ttoxicity. Bupropioni CYP2D6 thus T serum levels of drugs metabolized
by this enzyme and may /their toxicity (TcA, SSRI, some antipsychotics, some beta-
blockers, esp. metoprolol, and type IC antiarrhythmics such as propafenone, flecanide).
Metabolized by CYP2B6.
Monitoring parameters: none
Rx: oral
"Indications: depression, aggression, panic, anxiety
Actions: primarily 5-HT2A serotonin receptor antagonist but also serotonin reuptake
inhibition, alpha-2 adrenergic receptor antagonist (like yohimbine)
Adverse effects: nausea, weight gain, edema, sedation, dry mouth, loss of libido, sexual
dysfunction, priapism, orthostatic hypotension, anxiety, headache, depression, false
positive urine tests for mnmA, increased suicidality in youths, arrhythmias in those
predisposed to them, hyperprolactinemia
Rare but serious: mania (or activation of it in bipolar patients)
Contraindications: under age 25, suicidal ideation, rapid discontinuation, pregnancy (unless
absolutely necessary)
Interactions: mAcns Ttoxicity, combination with ethanol, photosensitizing. Metabolized by
CYP3A4.
Monitoring parameters: none
Rx: oral" "Indications: depression, aggression, panic, anxiety
Actions: primarily 5-HT2A serotonin receptor antagonist but also serotonin reuptake
inhibition, alpha-2 adrenergic receptor antagonist (like yohimbine)
Adverse effects: nausea, weight gain, edema, sedation, dry mouth, loss of libido, sexual
dysfunction, priapism, orthostatic hypotension, anxiety, headache, depression, false
positive urine tests for mnmA, increased suicidality in youths, arrhythmias in those
predisposed to them, hyperprolactinemia
Rare but serious: mania (or activation of it in bipolar patients)
Contraindications: under age 25, suicidal ideation, rapid discontinuation, pregnancy (unless
absolutely necessary)
Interactions: mAcns Ttoxicity, combination with ethanol, photosensitizing. Metabolized by
CYP3A4.
Monitoring parameters: none
Rx: oral
Indications: manic-depression (bipolar disorders), thyrotoxicosis (with supersaturated potassium iodide)
Actions: antimanic mood-stabilizing agent; stabilizes mood by altering cation transport across cell membrane in nerve and muscle cells; inhibits second messenger systems involving the phosphatidylinositol cycle; suppresses release of thyroid hormone Mostly normalizes mania (rather than elevating depressed mood)
Adverse effects: thirst, weight gain, acne, leukocytosis, drowsiness, polyuria, sexual dysfunction, very narrow therapeutic window, overdose potentially fatal; can cause diabetes insipidus, Dm, long-term kidney damage (nephrogenic diabetes insipidus) and hypothyroidism. Preg D.
Signs of toxicity: confusion, drowsiness, sluggishness, unsteadiness, tremor, muscle twitching, vomiting, diarrhea
Contraindications: Pregnancy, lactation, renal failure, CHF, hypothyroidism, dehydration, hyponatremia, diuretic use concomitantly
Interactions: Diuretics and carbamazepine potentiate toxicity. Do not combine with neuroleptics (may cause encephalopathy). NSAIDS decrease lithium excretion.
Monitoring parameters: serum lithium every 4-5 days during initial therapy; lithium serum concentrations 8-12 hours postdose; renal, thyroid, and cardiovascular function; fluid status, serum electrolytes, cac with differential, urinalysis. Monitor for signs of toxicity. Pregnancy test for females not known to be infertile.
Critical to monitor serum levels due to very narrow therapeutic levels.
Monitor cm, serum creatinine, UA, Na+, K+, fasting glucose, ECG, thyroid tests."
"Indications: anxiety (with or without depression), panic disorder, agoraphobia
Action: enhances action of inhibitory neurotransmitter GABA
Adverse effects: impaired sleep quality thus daytime drowsiness/sedation (worse in elderly), addiction risk (worse with alprazolam), withdrawal symptoms often worse
With Insomnia: >2-4 wk -,REM disturbances and deterioration of sleep quality; removal of
agent -.rebound insomnia -.think must take more to fight insomnia (cycle occurs) Contraindications: acute glaucoma, psychosis, elderly; preg D; do not operate machinery or drive while using
Interactions: substrates of CYP34A; potentiates CNS depressant effects of narcotic analgesics, barbiturates, phenothiazines, ethanol, antihistamines, MAO inhibitors, sedative-hypnotics; inhibitors of CYP3A4 may increase serum levels; carbamazepine, rifampin, cigarette smoking and phenobarbitol may decrease therapeutic effect
Monitoring parameters: signs of dependence/drug-seeking behavior, sleep quality
Rx: oral, short-term use only, taper dose before discontinuing" "Indications: anxiety (with or without depression), panic disorder, agoraphobia
Action: enhances action of inhibitory neurotransmitter GABA
Adverse effects: impaired sleep quality thus daytime drowsiness/sedation (worse in elderly), addiction risk (worse with alprazolam), withdrawal symptoms often worse
With Insomnia: >2-4 wk -,REM disturbances and deterioration of sleep quality; removal of
agent -.rebound insomnia -.think must take more to fight insomnia (cycle occurs) Contraindications: acute glaucoma, psychosis, elderly; preg D; do not operate machinery or drive while using
Interactions: substrates of CYP34A; potentiates CNS depressant effects of narcotic analgesics, barbiturates, phenothiazines, ethanol, antihistamines, MAO inhibitors, sedative-hypnotics; inhibitors of CYP3A4 may increase serum levels; carbamazepine, rifampin, cigarette smoking and phenobarbitol may decrease therapeutic effect
Monitoring parameters: signs of dependence/drug-seeking behavior, sleep quality
Rx: oral, short-term use only, taper dose before discontinuing
"Similar agents: Methylenedioxyamphetamine (mDA)
Indications: used in psychological setting to aid a client in processing deep painful issues in the US until 1985, psychoactive
Actions: increases serotonin and blocks reuptake resulting in increased serotonin within the synaptic cleft
Adverse Effects: tachycardia, tachypnea, hypertension, hyperthermia, sexual dysfunction,
seizures, muscle cramping, dehydration, hyperglycemia, hyponatremia, Preg C Contraindications: decreased serotoninergic receptors functioning (effects are debateable),
decreased memory, temporary sexual dysfunction with high doses
Interactions: fluoxetine may inhibit permanent damage done to serotoninergic receptors Monitoring Parameters: temperature; hydration, sodium, and glucose levels
Rx: oral" "Similar agents: Methylenedioxyamphetamine (mDA)
Indications: used in psychological setting to aid a client in processing deep painful issues in the US until 1985, psychoactive
Actions: increases serotonin and blocks reuptake resulting in increased serotonin within the synaptic cleft
Adverse Effects: tachycardia, tachypnea, hypertension, hyperthermia, sexual dysfunction,
seizures, muscle cramping, dehydration, hyperglycemia, hyponatremia, Preg C Contraindications: decreased serotoninergic receptors functioning (effects are debateable),
decreased memory, temporary sexual dysfunction with high doses
Interactions: fluoxetine may inhibit permanent damage done to serotoninergic receptors Monitoring Parameters: temperature; hydration, sodium, and glucose levels
Rx: oral
"Similar drug: rimantadine
Indications: prevention of influenza A, very early in influenza A infection; early Parkinson's disease or extrapyramidal drug adverse effects; adjunct to levodopa in later disease (often loses effect in months as single agent)
Actions: inhibits viral RNA transcription and/or virus uncoating (after cell entry); augments dopaminergic activity (anti-parkinson)
Adverse Effects: influenza resistance (growing problem), dry mouth, blurred vision, confusion, livedo reticularis, dependent edema
Contraindications: epilepsy, liver or kidney disease, psychosis, CHF, edema; Preg C Interactions: synergism with anticholinergic drugs; increased by thiazide and loop diuretics Monitoring Parameters: renal function, Parkinson's symptoms, mental status, blood pressure, symptoms of flu
Rx: oral; abrupt discontinuation can provoke Parkinsonian crisis" "Similar drug: rimantadine
Indications: prevention of influenza A, very early in influenza A infection; early Parkinson's disease or extrapyramidal drug adverse effects; adjunct to levodopa in later disease (often loses effect in months as single agent)
Actions: inhibits viral RNA transcription and/or virus uncoating (after cell entry); augments dopaminergic activity (anti-parkinson)
Adverse Effects: influenza resistance (growing problem), dry mouth, blurred vision, confusion, livedo reticularis, dependent edema
Contraindications: epilepsy, liver or kidney disease, psychosis, CHF, edema; Preg C Interactions: synergism with anticholinergic drugs; increased by thiazide and loop diuretics Monitoring Parameters: renal function, Parkinson's symptoms, mental status, blood pressure, symptoms of flu
Rx: oral; abrupt discontinuation can provoke Parkinsonian crisis
"Specific agents: belocmethasone, budesonide
Indications: prophylactic treatment of asthma; management of allergic rhinitis; topical relief of inflammation
Actions: inhaled corticosteroid; potent anti-inflammatory and immunosuppressive
Adverse Effects: headache, fever, nausea/vomiting, URI, throat irritation, pharyngitis, nasal congestion, oral candidiasis, growth inhibition, adrenal suppression
Contraindications: do not use for primary treatment of status asthmaticus, acute bronchospams; do not use topically if infection is present; Preg C
Interactions: salmeterol improves response; amiodarone, cimetidine, disulfiram increase
effects; immunostimulant botanicals may antagonize effects
Monitoring Parameters: growth in adolescents and children, symptoms of HPA axis
suppression/adrenal insufficiency, bone density, glucose, electrolytes
Rx: oral inhalation, topical" "Specific agents: belocmethasone, budesonide
Indications: prophylactic treatment of asthma; management of allergic rhinitis; topical relief of inflammation
Actions: inhaled corticosteroid; potent anti-inflammatory and immunosuppressive
Adverse Effects: headache, fever, nausea/vomiting, URI, throat irritation, pharyngitis, nasal congestion, oral candidiasis, growth inhibition, adrenal suppression
Contraindications: do not use for primary treatment of status asthmaticus, acute bronchospams; do not use topically if infection is present; Preg C
Interactions: salmeterol improves response; amiodarone, cimetidine, disulfiram increase
effects; immunostimulant botanicals may antagonize effects
Monitoring Parameters: growth in adolescents and children, symptoms of HPA axis
suppression/adrenal insufficiency, bone density, glucose, electrolytes
Rx: oral inhalation, topical
"Indications: acute bronchospasm
Effects: increased cAMP levels causes smooth muscle relaxes and bronchodilation (minor or short acting betai effects)
Adverse Effects: HA, hypertension, fine hand tremor, arrhythmia, dry mouth, altered taste, nervousness, agitation, fatigue (possibly due to cellular Mg and K leaching); may lead to paradoxical airway resistance (discontinue immediately); may contain sulfites, to which many people with asthma are allergic; prolonged use correlates to decreased life span and decreased effectiveness
Contraindications: cardiovascular disease, hyperthyroidism, Dm, angina, during labor; Preg
Interactions: potentiated by guanethidine; hypertensive crisis with MAOIS, hypertension with reserpine or tricyclic antidepressants; may enhance toxicity of theophylline; inhibition of bronchodilation when taken with beta blocker; depletes magnesium and potassium
Monitoring Parameters: pulmonary function tests, BP, HR, CNS stimulation, serum glucose, serum potassium, asthma symptoms, arterial or capillary blood gases
Rx: oral or inhaler; do not overuse; do not use within 20 min of beclomethasone inhaler" "Indications: acute bronchospasm
Effects: increased cAMP levels causes smooth muscle relaxes and bronchodilation (minor or short acting betai effects)
Adverse Effects: HA, hypertension, fine hand tremor, arrhythmia, dry mouth, altered taste, nervousness, agitation, fatigue (possibly due to cellular Mg and K leaching); may lead to paradoxical airway resistance (discontinue immediately); may contain sulfites, to which many people with asthma are allergic; prolonged use correlates to decreased life span and decreased effectiveness
Contraindications: cardiovascular disease, hyperthyroidism, Dm, angina, during labor; Preg
Interactions: potentiated by guanethidine; hypertensive crisis with MAOIS, hypertension with reserpine or tricyclic antidepressants; may enhance toxicity of theophylline; inhibition of bronchodilation when taken with beta blocker; depletes magnesium and potassium
Monitoring Parameters: pulmonary function tests, BP, HR, CNS stimulation, serum glucose, serum potassium, asthma symptoms, arterial or capillary blood gases
Rx: oral or inhaler; do not overuse; do not use within 20 min of beclomethasone inhaler
"Indications: counter-irritant for rheumatic conditions, painful muscles or joints
Actions: first-pass metabolism through skin with esterases rapidly hydrolyzing salicylate
esters to release salicylate in epidermis and dermis; masks symptoms of pain when
combined with heat or cold
Adverse effects: local irritation, erythema, rash, desquamation, pruritus, skin discoloration. Systemic absorption of topical methyl salicylate can occur and can be fatal.
Contraindications: aspirin, NSAIDS, menthol, linseed oil, or diclofenac sensitivities. Do not use over broken skin. Do not cover large skin areas to avoid systemic absorption and toxicity. Children more sensitive. Internal use.
Interactions: avoid applying heat immediately to the area
Monitoring parameters: monitor for local irritation
Rx: topical" "Indications: counter-irritant for rheumatic conditions, painful muscles or joints
Actions: first-pass metabolism through skin with esterases rapidly hydrolyzing salicylate
esters to release salicylate in epidermis and dermis; masks symptoms of pain when
combined with heat or cold
Adverse effects: local irritation, erythema, rash, desquamation, pruritus, skin discoloration. Systemic absorption of topical methyl salicylate can occur and can be fatal.
Contraindications: aspirin, NSAIDS, menthol, linseed oil, or diclofenac sensitivities. Do not use over broken skin. Do not cover large skin areas to avoid systemic absorption and toxicity. Children more sensitive. Internal use.
Interactions: avoid applying heat immediately to the area
Monitoring parameters: monitor for local irritation
Rx: topical
"Indications: severe pain; detoxification and maintenance treatment of narcotic addiction Actions: binds to opiate receptors in cm, inhibiting ascending pain pathways; produces CNS depression
Adverse effects: bradycardia, peripheral vasodilation, cardiac arrest, syncope, euphoria, dysphoria, headache, agitation, drowsiness, decreased libido, respiratory depression Contraindications: pregnancy: prolonged use or high doses near term
Interactions: inhibits CYP2D6; fluconazole, itraconazole, ketoconazole, amiodarone,
verapamil, paroxetine, and fluoxetine increase serum concentrations of methadone Monitoring parameters: pain relief, respiratory and mental status, blood pressure; doses
accumulate, so may need to adjust dosage downward after 3-5 days to avoid toxic effects. Rx: oral, injection; oral dose may be administered in fruit juice or water" "Indications: severe pain; detoxification and maintenance treatment of narcotic addiction Actions: binds to opiate receptors in cm, inhibiting ascending pain pathways; produces CNS depression
Adverse effects: bradycardia, peripheral vasodilation, cardiac arrest, syncope, euphoria, dysphoria, headache, agitation, drowsiness, decreased libido, respiratory depression Contraindications: pregnancy: prolonged use or high doses near term
Interactions: inhibits CYP2D6; fluconazole, itraconazole, ketoconazole, amiodarone,
verapamil, paroxetine, and fluoxetine increase serum concentrations of methadone Monitoring parameters: pain relief, respiratory and mental status, blood pressure; doses
accumulate, so may need to adjust dosage downward after 3-5 days to avoid toxic effects. Rx: oral, injection; oral dose may be administered in fruit juice or water
"Indications: Available almost exclusively combined w/acetaminophen (e.g., as Vicodin) for use in relief of mild-to-moderate pain or with other medications as an antitussive. Actions: semi-synthetic mild opioid receptor agonist
Adverse effects: euphoria, sedation, miosis (pinpoint pupils), nausea, vomiting, constipation. Cough suppression (can cause problems if not therapeutic intent). Highly addictive with withdrawal symptoms. Tolerance and cross tolerance occur. Overdose can cause dysphoria (nightmares, ""bad trip"") and potentially lethal respiratory depression; antidote is naloxone. Over aggressive use in painful conditions may obscure underlying problem (e.g., acute abdomen). Tend to promote hypotension. Preg C
Contraindications: renal or hepatic failure, respiratory weakness (esp. acute asthma), urinary bladder obstruction (opioids increase sphincter tone), hypovolemia (opioids worsen hypotension)
Interactions: synergistic with barbiturates. May cause false elevations of amylase and lipase. Monitoring parameters: pain relief, respiratory and mental status, blood pressure Rx: oral. Schedule III." "Indications: Available almost exclusively combined w/acetaminophen (e.g., as Vicodin) for use in relief of mild-to-moderate pain or with other medications as an antitussive. Actions: semi-synthetic mild opioid receptor agonist
Adverse effects: euphoria, sedation, miosis (pinpoint pupils), nausea, vomiting, constipation. Cough suppression (can cause problems if not therapeutic intent). Highly addictive with withdrawal symptoms. Tolerance and cross tolerance occur. Overdose can cause dysphoria (nightmares, ""bad trip"") and potentially lethal respiratory depression; antidote is naloxone. Over aggressive use in painful conditions may obscure underlying problem (e.g., acute abdomen). Tend to promote hypotension. Preg C
Contraindications: renal or hepatic failure, respiratory weakness (esp. acute asthma), urinary bladder obstruction (opioids increase sphincter tone), hypovolemia (opioids worsen hypotension)
Interactions: synergistic with barbiturates. May cause false elevations of amylase and lipase. Monitoring parameters: pain relief, respiratory and mental status, blood pressure Rx: oral. Schedule III.
"Indications: severe headache pain, severe dysmenorrhea, cough
Actions: natural opioid, low first pass metabolism means it is effective orally. Weak opioid receptor agonist; 10% of dose metabolizes to morphine, providing analgesic and antitussive effects
Adverse effects: constipation (usually mild), respiratory depression, confusion (usually mild), urinary retention, nausea and vomiting (usually mild), hypotension, dizziness, pruritus. Addictive; tolerance for its effects increase as pain increases. Allergic reactions fairly common. Schedule III (small amounts oTc).
Contraindications: severe renal (due to renal excretion) or pulmonary (due to respiratory depression) disease, acute asthma, use with caution in elderly (effects have longer duration). No major drug interactions.
Monitoring parameters: pain relief, respiratory and mental status, blood pressure, heart rate
Rx: oral, IM, tv (not in children), or subcutaneous. Preg C" "Indications: severe headache pain, severe dysmenorrhea, cough
Actions: natural opioid, low first pass metabolism means it is effective orally. Weak opioid receptor agonist; 10% of dose metabolizes to morphine, providing analgesic and antitussive effects
Adverse effects: constipation (usually mild), respiratory depression, confusion (usually mild), urinary retention, nausea and vomiting (usually mild), hypotension, dizziness, pruritus. Addictive; tolerance for its effects increase as pain increases. Allergic reactions fairly common. Schedule III (small amounts oTc).
Contraindications: severe renal (due to renal excretion) or pulmonary (due to respiratory depression) disease, acute asthma, use with caution in elderly (effects have longer duration). No major drug interactions.
Monitoring parameters: pain relief, respiratory and mental status, blood pressure, heart rate
Rx: oral, IM, tv (not in children), or subcutaneous. Preg C
"Indications: mild pain, acute musculoskeletal pain, osteoarthritis, rheumatoid arthritis, fever
Actions: inhibits cis prostaglandin synthesis, analgesic, anti-pyretic. NOT anti-inflammatory. Does NOT affect platelet aggregation or uric acid metabolism
Adverse effects: May inhibit cartilage formation. Preg B. Overdose can cause poten¬tially lethal hepatotoxicity (overwhelms glutathione detoxification system of liver), nephrotoxicity. Antidote: charcoal (to reduce absorption), N-acetylcysteine (glutathione precursor).
Contraindications: liver disease, liver failure, alcoholism
Interactions: Barbiturates, carbamazepine, phenytoin, isoniazid, OBCP, and rifampin all activate liver breakdown of acetaminophen and may cause it to be more hepatotoxic and less active. Acetaminophen may decrease activity of lamotrigine, zidovudine and loop diuretics. May interfere with home glucose monitors.
Monitoring parameters: relief of pain or fever; hepatotoxicity with ingestion of greater than 4 g per day
Rx: oral, rectal" "Indications: mild pain, acute musculoskeletal pain, osteoarthritis, rheumatoid arthritis, fever
Actions: inhibits cis prostaglandin synthesis, analgesic, anti-pyretic. NOT anti-inflammatory. Does NOT affect platelet aggregation or uric acid metabolism
Adverse effects: May inhibit cartilage formation. Preg B. Overdose can cause poten¬tially lethal hepatotoxicity (overwhelms glutathione detoxification system of liver), nephrotoxicity. Antidote: charcoal (to reduce absorption), N-acetylcysteine (glutathione precursor).
Contraindications: liver disease, liver failure, alcoholism
Interactions: Barbiturates, carbamazepine, phenytoin, isoniazid, OBCP, and rifampin all activate liver breakdown of acetaminophen and may cause it to be more hepatotoxic and less active. Acetaminophen may decrease activity of lamotrigine, zidovudine and loop diuretics. May interfere with home glucose monitors.
Monitoring parameters: relief of pain or fever; hepatotoxicity with ingestion of greater than 4 g per day
Rx: oral, rectal
"Similar agents: ketoprofen
Indications: mild pain relief, inflammation, fever.
Actions: inhibit peripheral cox-i and-2 hence prostaglandin synthesis, analgesic, anti-inflammatory, antipyretic. Inhibits ability of kidney vasculature to vasodilate. Mildly anti-platelet.
Adverse effects: dyspepsia, ulcerogenic by systemic mechanism (thus enteric coating does NOT help); may cause iron deficiency anemia. Increases intestinal permeability and inhibits cartilage synthesis. Account for many deaths due to ulcers and other causes (including increased risk of MI, stroke). Nephrotoxicity. Preg B first and second trimesters. Mechanism of ulcerogenesis: inhibition of systemic prostaglandin synthesis decreases
blood flow to gastric lining hence bicarbonate is not delivered efficiently, compromising mucus production.
Contraindications: PUD, iron deficiency, anemia, renal disease, hepatic failure (with naproxen), use in third trimester can cause premature closure of ductus arteriosus.
Interactions: Highly protein bound. May increase effects of anticoagulants. May decrease efficacy of ACE inhibitors, beta blockers, and loop and thiazide diuretics. Synergistic nephrotoxicity with cyclosporine. Synergistic toxicity with methotrexate. May increase digoxin levels. Increases hypertensive effects of phenylpropanolamine. Do not combine with aspirin.
Monitoring parameters: cuc, occult blood loss, liver function tests, response to symptoms, renal function, bruising, GI effects; periodic ophthalmic exams
Rx: oral" "Similar agents: ketoprofen
Indications: mild pain relief, inflammation, fever.
Actions: inhibit peripheral cox-i and-2 hence prostaglandin synthesis, analgesic, anti-inflammatory, antipyretic. Inhibits ability of kidney vasculature to vasodilate. Mildly anti-platelet.
Adverse effects: dyspepsia, ulcerogenic by systemic mechanism (thus enteric coating does NOT help); may cause iron deficiency anemia. Increases intestinal permeability and inhibits cartilage synthesis. Account for many deaths due to ulcers and other causes (including increased risk of MI, stroke). Nephrotoxicity. Preg B first and second trimesters. Mechanism of ulcerogenesis: inhibition of systemic prostaglandin synthesis decreases
blood flow to gastric lining hence bicarbonate is not delivered efficiently, compromising mucus production.
Contraindications: PUD, iron deficiency, anemia, renal disease, hepatic failure (with naproxen), use in third trimester can cause premature closure of ductus arteriosus.
Interactions: Highly protein bound. May increase effects of anticoagulants. May decrease efficacy of ACE inhibitors, beta blockers, and loop and thiazide diuretics. Synergistic nephrotoxicity with cyclosporine. Synergistic toxicity with methotrexate. May increase digoxin levels. Increases hypertensive effects of phenylpropanolamine. Do not combine with aspirin.
Monitoring parameters: cuc, occult blood loss, liver function tests, response to symptoms, renal function, bruising, GI effects; periodic ophthalmic exams
Rx: oral
"Similar agents: dronabinol, nabilone
Indications: glaucoma, anorexia or appetite loss associated with AIDS, chemotherapy
induced nausea and vomiting, tremors and spasticity associated with MS, and pain Actions: cannabinoids act on the cannabinoid receptors in the central nervous system to
have an antiemetic, anticonvulsive, and psychoactive effect
Adverse Effects: Preg B or C (depending on which agent used)
[Acute:] dry mouth, impaired short-term memory, paranoia, anxiety, panic, hypotension, vasodilation, hallucinations, depression, impaired reaction times and motor coordination [Chronic:] decreased LI-1/FSH, sexual dysfunction, infertility, impaired judgment and concentration, diminished REM sleep, constructive lung disease (with inhaled form) Contraindications: cardiovascular or respiratory disease, patients who are immunocompro-mised or undergoing surgery, epilepsy or seizure disorders
Interactions: increases metabolism of theophylline, decreases metabolism of barbiturates or warfarin; additive or synergistic effects with CNS depressants; hypomania when used concurrently with disulfiram or fluoxetine
Monitoring Parameters: none
Rx: oral or inhaled" "Similar agents: dronabinol, nabilone
Indications: glaucoma, anorexia or appetite loss associated with AIDS, chemotherapy
induced nausea and vomiting, tremors and spasticity associated with MS, and pain Actions: cannabinoids act on the cannabinoid receptors in the central nervous system to
have an antiemetic, anticonvulsive, and psychoactive effect
Adverse Effects: Preg B or C (depending on which agent used)
[Acute:] dry mouth, impaired short-term memory, paranoia, anxiety, panic, hypotension, vasodilation, hallucinations, depression, impaired reaction times and motor coordination [Chronic:] decreased LI-1/FSH, sexual dysfunction, infertility, impaired judgment and concentration, diminished REM sleep, constructive lung disease (with inhaled form) Contraindications: cardiovascular or respiratory disease, patients who are immunocompro-mised or undergoing surgery, epilepsy or seizure disorders
Interactions: increases metabolism of theophylline, decreases metabolism of barbiturates or warfarin; additive or synergistic effects with CNS depressants; hypomania when used concurrently with disulfiram or fluoxetine
Monitoring Parameters: none
Rx: oral or inhaled
"Indications: severe rheumatoid arthritis; psoriasis; severe pneumoconiosis; prevent organ transplant rejection; breast, gastric, esophagus, testes, head, neck, and lung carcinomas; trophoblastic neoplasms; osteosarcoma; non-Hodgkin lymphoma; leukemia
Actions: folic acid analog; inhibits human dihydrofolate reductase, thus folic acid-dependent mechanisms don't function; cytotoxic (folic acid dependent DNA synthesis can't occur); antirheumatic effects are poorly understood
Adverse Effects: low-doses can cause transient asymptomatic elevation of serum liver enzymes (doesn't predict long-term toxicity), GI upset (aggravated by SAID use), photosensitivity. High-doses much more dangerous—ulcerative stomatitis (must stop therapy), rash, nausea, vomiting, diarrhea (must stop therapy), bone marrow suppression with pancytopenia, bone and soft tissue necrosis, long-term toxicity includes liver fibrosis, renal damage (high doses), and neurological damage, can be lethal. Preg X
Contraindications: bone marrow suppression in patients with psoriasis or RA; AIDS, blood dyscrasias, renal failure, liver failure, alcoholism, immune deficiency, blood dyscrasias, anemia, pregnancy and lactation
Interactions: synergistic toxicity with NSAIDs (can be lethal); folic acid reduces side effects in RA patients but interferes with anti-cancer effects
Monitoring Parameters: monitor (qi--3 months) CBC, and liver and kidney function; periodic liver biopsy may be needed to detect onset of cirrhosis
Rx: low-dose for RA (1 dose/week), high-dose for cancer" "Indications: severe rheumatoid arthritis; psoriasis; severe pneumoconiosis; prevent organ transplant rejection; breast, gastric, esophagus, testes, head, neck, and lung carcinomas; trophoblastic neoplasms; osteosarcoma; non-Hodgkin lymphoma; leukemia
Actions: folic acid analog; inhibits human dihydrofolate reductase, thus folic acid-dependent mechanisms don't function; cytotoxic (folic acid dependent DNA synthesis can't occur); antirheumatic effects are poorly understood
Adverse Effects: low-doses can cause transient asymptomatic elevation of serum liver enzymes (doesn't predict long-term toxicity), GI upset (aggravated by SAID use), photosensitivity. High-doses much more dangerous—ulcerative stomatitis (must stop therapy), rash, nausea, vomiting, diarrhea (must stop therapy), bone marrow suppression with pancytopenia, bone and soft tissue necrosis, long-term toxicity includes liver fibrosis, renal damage (high doses), and neurological damage, can be lethal. Preg X
Contraindications: bone marrow suppression in patients with psoriasis or RA; AIDS, blood dyscrasias, renal failure, liver failure, alcoholism, immune deficiency, blood dyscrasias, anemia, pregnancy and lactation
Interactions: synergistic toxicity with NSAIDs (can be lethal); folic acid reduces side effects in RA patients but interferes with anti-cancer effects
Monitoring Parameters: monitor (qi--3 months) CBC, and liver and kidney function; periodic liver biopsy may be needed to detect onset of cirrhosis
Rx: low-dose for RA (1 dose/week), high-dose for cancer
"Specific agents: risedronate
Indications: osteoporosis in postmenopausal women, males; Paget's dz of the bone Actions: inhibits bone resorption by acting on osteoclasts or osteoclast precursors Adverse effects: esophagitis, esophageal ulcers, headache, transient hypocalcemia, GI distress, abdominal pain, acid reflux, nausea
Contraindications: hypocalcemia, esophageal abnormalities, inability to stand or sit upright for at least 30 minutes
Interactions: iv ranitidine doubles bioavailability, estrogen may enhance therapeutic effect;
GI distress increases with aspirin; other medications may interfere with absorption Monitoring parameters: alkaline phosphatase, serum calcium and phosphorus, pain and
fracture rate, hormonal status, bone mineral density
Rx: oral, take with a full glass of water in the morning at least 30 minutes before food and other medications; ensure adequate calcium and vitamin D intake" "Specific agents: risedronate
Indications: osteoporosis in postmenopausal women, males; Paget's dz of the bone Actions: inhibits bone resorption by acting on osteoclasts or osteoclast precursors Adverse effects: esophagitis, esophageal ulcers, headache, transient hypocalcemia, GI distress, abdominal pain, acid reflux, nausea
Contraindications: hypocalcemia, esophageal abnormalities, inability to stand or sit upright for at least 30 minutes
Interactions: iv ranitidine doubles bioavailability, estrogen may enhance therapeutic effect;
GI distress increases with aspirin; other medications may interfere with absorption Monitoring parameters: alkaline phosphatase, serum calcium and phosphorus, pain and
fracture rate, hormonal status, bone mineral density
Rx: oral, take with a full glass of water in the morning at least 30 minutes before food and other medications; ensure adequate calcium and vitamin D intake
"Note: obtained from the corm of Colchicum autumnale (autumn crocus).
Indications: acute gout, herniated discs (by injection), familial Mediterranean fever, pyoderma gangrenosum, primary amyloidosis, primary biliary cirrhosis, Belicet's disease, other autoimmune diseases
Actions: selective inhibitor of microtubule assembly in leukocytes, reducing migration and phagocytosis. Decreases migration of granulocytes into inflamed area; decreases cellular metabolic activity.
Adverse effects: GI irritation, nausea/vomiting, diarrhea (80% of patients); skin sloughing (iv only). Long-term use may cause agranulocytosis, aplastic anemia (via vitamin B12 malabsorption), and myopathies.
Contraindications: renal or hepatic failure, elderly (use caution). Preg C (iv: preg D). Interactions: may cause false positive results on RBC tests during urinalysis.
Monitoring parameters: cac and renal function test
Rx: oral, iv. Dosed acutely every 2 h until pain decreases or diarrhea occurs (indicates tissue saturation)." "Note: obtained from the corm of Colchicum autumnale (autumn crocus).
Indications: acute gout, herniated discs (by injection), familial Mediterranean fever, pyoderma gangrenosum, primary amyloidosis, primary biliary cirrhosis, Belicet's disease, other autoimmune diseases
Actions: selective inhibitor of microtubule assembly in leukocytes, reducing migration and phagocytosis. Decreases migration of granulocytes into inflamed area; decreases cellular metabolic activity.
Adverse effects: GI irritation, nausea/vomiting, diarrhea (80% of patients); skin sloughing (iv only). Long-term use may cause agranulocytosis, aplastic anemia (via vitamin B12 malabsorption), and myopathies.
Contraindications: renal or hepatic failure, elderly (use caution). Preg C (iv: preg D). Interactions: may cause false positive results on RBC tests during urinalysis.
Monitoring parameters: cac and renal function test
Rx: oral, iv. Dosed acutely every 2 h until pain decreases or diarrhea occurs (indicates tissue saturation).
"Indications: inflammatory disorders, autoimmune dz
Actions: anti-inflammatory, immunosuppressive, inhibit PLP-A2, inhibit cartilage synthesis, stimulates gluconeogenesis with rise in blood sugar, stimulation of insulin secretion, catabolic effect on skin, catabolic effects on bone, catabolic effects on muscle, alteration of fat deposition
Adverse effects: mood changes, insomnia, edema, lappetite, acne, iweight, skin thinning, impaired wound healing, GI irritation, PUD, adrenal suppression, Cushing's dz, cataracts, htn, CHF, osteoporosis, growth suppression (in children).
Contraindications: systemic fungal infection, other severe infections (e.g., malaria, hepatitis), vaccine administration (when using full immunosuppressive doses), hypertension, hypocalcemia, PUD, recent MI, renal insufficiency, lactation. Preg C.
Interactions: Estrogens decrease steroid clearance, increase their effects. Phenytoin and rifampin interfere with steroids. Macrolide antibiotics decrease prednisone clearance. Enhance toxicity of potassium-depleting drugs (digoxin, thiazides, licorice). Interferes with aspirin. Unpredictable interactions with anti-coagulants and theophylline. Interferes with T4 binding to TBG giving appearance of decreased TBG levels.
Monitoring parameters: blood pressure, glucose, electrolytes, eye exam
Rx: oral, IM, Iv, inhaled, topical. Do not discontinue suddenly (can cause adrenal failure). Increase protein and potassium intake during therapy to reduce adverse effects. Give before 9 am to reduce risk of adrenal suppression." "Indications: inflammatory disorders, autoimmune dz
Actions: anti-inflammatory, immunosuppressive, inhibit PLP-A2, inhibit cartilage synthesis, stimulates gluconeogenesis with rise in blood sugar, stimulation of insulin secretion, catabolic effect on skin, catabolic effects on bone, catabolic effects on muscle, alteration of fat deposition
Adverse effects: mood changes, insomnia, edema, lappetite, acne, iweight, skin thinning, impaired wound healing, GI irritation, PUD, adrenal suppression, Cushing's dz, cataracts, htn, CHF, osteoporosis, growth suppression (in children).
Contraindications: systemic fungal infection, other severe infections (e.g., malaria, hepatitis), vaccine administration (when using full immunosuppressive doses), hypertension, hypocalcemia, PUD, recent MI, renal insufficiency, lactation. Preg C.
Interactions: Estrogens decrease steroid clearance, increase their effects. Phenytoin and rifampin interfere with steroids. Macrolide antibiotics decrease prednisone clearance. Enhance toxicity of potassium-depleting drugs (digoxin, thiazides, licorice). Interferes with aspirin. Unpredictable interactions with anti-coagulants and theophylline. Interferes with T4 binding to TBG giving appearance of decreased TBG levels.
Monitoring parameters: blood pressure, glucose, electrolytes, eye exam
Rx: oral, IM, Iv, inhaled, topical. Do not discontinue suddenly (can cause adrenal failure). Increase protein and potassium intake during therapy to reduce adverse effects. Give before 9 am to reduce risk of adrenal suppression.
Long acting steroid at 24-72 hours. 30 times stronger than hydrocortisone (7.5x stronger than prednisone). Indications: inflammatory disorders, autoimmune dz
Actions: anti-inflammatory, immunosuppressive, inhibit PLP-A2, inhibit cartilage synthesis, stimulates gluconeogenesis with rise in blood sugar, stimulation of insulin secretion, catabolic effect on skin, catabolic effects on bone, catabolic effects on muscle, alteration of fat deposition
Adverse effects: mood changes, insomnia, edema, Tappetite, acne, tweight, skin thinning, impaired wound healing, GI irritation, PUD, adrenal suppression, Cushing's dz, cataracts, htn, CHF, osteoporosis, growth suppression (in children).
Contraindications: systemic fungal infection, other severe infections (e.g., malaria, hepatitis), vaccine administration (when using full immunosuppressive doses), hypertension, hypocalcemia, PUD, recent MI, renal insufficiency, lactation. Preg C.
Interactions: Estrogens decrease steroid clearance, increase their effects. Phenytoin and rifampin interfere with steroids. Macrolide antibiotics decrease prednisone clearance. Enhance toxicity of potassium-depleting drugs (digoxin, thiazides, licorice). Interferes with aspirin. Unpredictable interactions with anti-coagulants and theophylline. Interferes with T4 binding to TBG giving appearance of decreased TBG levels.
Monitoring parameters: blood pressure, glucose, electrolytes, eye exam
Rx: oral, IM, iv, inhaled, topical. Do not discontinue suddenly (can cause adrenal failure). Increase protein and potassium intake during therapy to reduce adverse effects. Give before 9 am to reduce risk of adrenal suppression.
"Indications: inflammatory disorders, autoimmune dz, low-doses for ""adrenal fatigue""
Actions: anti-inflammatory, immunosuppressive, inhibit PLP-A2, inhibit cartilage synthesis, stimulates gluconeogenesis with rise in blood sugar, stimulation of insulin secretion, catabolic effect on skin, catabolic effects on bone, catabolic effects on muscle, alteration of fat deposition
Adverse effects: mood changes, insomnia, edema, tappetite, acne, iweight, skin thinning, impaired wound healing, GI irritation, PUD, adrenal suppression, Cushing's dz, cataracts, htn, CHF, osteoporosis, growth suppression (in children).
Contraindications: systemic fungal infection, other severe infections (e.g., malaria, hepatitis), vaccine administration (when using full immunosuppressive doses), hypertension, hypocalcemia, PUD, recent MI, renal insufficiency, lactation. Preg C.
Interactions: Estrogens decrease steroid clearance, increase their effects. Phenytoin and rifampin interfere with steroids. Macrolide antibiotics decrease prednisone clearance. Enhance toxicity of potassium-depleting drugs (digoxin, thiazides, licorice). Interferes with aspirin. Unpredictable interactions with anti-coagulants and theophylline. Interferes with T4 binding to TBG giving appearance of decreased TBG levels.
Monitoring parameters: blood pressure, glucose, electrolytes, eye exam
Rx: oral, IM, iv, inhaled, topical. Do not discontinue suddenly (can cause adrenal failure). Increase protein and potassium intake during therapy to reduce adverse effects. Give before 9 am to reduce risk of adrenal suppression." "Indications: inflammatory disorders, autoimmune dz, low-doses for ""adrenal fatigue""
Actions: anti-inflammatory, immunosuppressive, inhibit PLP-A2, inhibit cartilage synthesis, stimulates gluconeogenesis with rise in blood sugar, stimulation of insulin secretion, catabolic effect on skin, catabolic effects on bone, catabolic effects on muscle, alteration of fat deposition
Adverse effects: mood changes, insomnia, edema, tappetite, acne, iweight, skin thinning, impaired wound healing, GI irritation, PUD, adrenal suppression, Cushing's dz, cataracts, htn, CHF, osteoporosis, growth suppression (in children).
Contraindications: systemic fungal infection, other severe infections (e.g., malaria, hepatitis), vaccine administration (when using full immunosuppressive doses), hypertension, hypocalcemia, PUD, recent MI, renal insufficiency, lactation. Preg C.
Interactions: Estrogens decrease steroid clearance, increase their effects. Phenytoin and rifampin interfere with steroids. Macrolide antibiotics decrease prednisone clearance. Enhance toxicity of potassium-depleting drugs (digoxin, thiazides, licorice). Interferes with aspirin. Unpredictable interactions with anti-coagulants and theophylline. Interferes with T4 binding to TBG giving appearance of decreased TBG levels.
Monitoring parameters: blood pressure, glucose, electrolytes, eye exam
Rx: oral, IM, iv, inhaled, topical. Do not discontinue suddenly (can cause adrenal failure). Increase protein and potassium intake during therapy to reduce adverse effects. Give before 9 am to reduce risk of adrenal suppression.
"Indications: typei and late-stage type 2 diabetes
Actions: drives glucose into cells, anabolic
Adverse Effects: initial weight gain, hypoglycemia (potentially fatal; antidote—sugar), diabetic ketoacidosis/coma (from failure to take medicine or intervening metabolic stress, such as an infection), atrophy of injection sites (must rotate)—less common now due to smaller needles, allergic reactions; Preg A
Interactions: interfered with by OCPS, corticosteroids, thyroxine, diltiazem, epinephrine, smoking, and thiazide diuretics; potentiated by ethanol, testosterone, beta blockers, clofibrate, guanethidine, MAOIS, salicylates and tetracyclines
Monitoring Parameters: urine glucose and acetone, serum glucose, electrolytes, HgbAtC, lipids. Spirometry (inhaled insulin)
Rx: all used in combination with rigorous diet and exercise program.
Short-acting insulins: used with meals to handle the rush of carbohydrates. Essential for type I; used by some type 2 diabetics. Regular insulin: subQ or iv (only form usable in a subQ pump). Given 30-45 min before meals but still does not mimic natural insulin secretion kinetics very well. Insulin lispro and aspart are newer versions with more natural kinetics. Inhaled insulin also available (can cause hypoglycemia, weight gain, cough, dyspnea, dry mouth).
Long-acting or basal insulins: subQ; used all day long to maintain baseline insulin levels (0.5-1 unit/hour, less at night, more in the morning). NPH, ultralente, insulin glargine, insulin detemir are major versions available " "Indications: typei and late-stage type 2 diabetes
Actions: drives glucose into cells, anabolic
Adverse Effects: initial weight gain, hypoglycemia (potentially fatal; antidote—sugar), diabetic ketoacidosis/coma (from failure to take medicine or intervening metabolic stress, such as an infection), atrophy of injection sites (must rotate)—less common now due to smaller needles, allergic reactions; Preg A
Interactions: interfered with by OCPS, corticosteroids, thyroxine, diltiazem, epinephrine, smoking, and thiazide diuretics; potentiated by ethanol, testosterone, beta blockers, clofibrate, guanethidine, MAOIS, salicylates and tetracyclines
Monitoring Parameters: urine glucose and acetone, serum glucose, electrolytes, HgbAtC, lipids. Spirometry (inhaled insulin)
Rx: all used in combination with rigorous diet and exercise program.
Short-acting insulins: used with meals to handle the rush of carbohydrates. Essential for type I; used by some type 2 diabetics. Regular insulin: subQ or iv (only form usable in a subQ pump). Given 30-45 min before meals but still does not mimic natural insulin secretion kinetics very well. Insulin lispro and aspart are newer versions with more natural kinetics. Inhaled insulin also available (can cause hypoglycemia, weight gain, cough, dyspnea, dry mouth).
Long-acting or basal insulins: subQ; used all day long to maintain baseline insulin levels (0.5-1 unit/hour, less at night, more in the morning). NPH, ultralente, insulin glargine, insulin detemir are major versions available