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weak bases neutralise HCl, decrease pepsin activity, relief within 5 minutes, duration 30-60 minutes, take after meals
aluminum hydroxide- adverse constipation, decreased phosphate, muscle weakness, osteodystorphy, seizures, renal excretion
magnesium hydroxide (milk of magnesia)- can cause osmotic diarrhea, Na/K loss, caridac arrest, hypotension, coadminister with aluminum, renal excretion
calcium carbonate- also supplements calcium in osteoporosis and ESRD, can cause belching and metabolic alkalosis
do not give with tetracyclines, fluorquinolones, ifraconazole, iron omeprazole, esomeprazole, lansoprazole, pantoprazole, rabeprazole
irreversibly bind and inhibit H/K ATPase in parietal cells
uses- GERD (fail H2RA therapy), PUD, gastrinoma, nonulcer dyspepsia, prophylaxis stress ulcers
adverse- decreased magnesium, diarrhea, headache, B12 deficiency, osteopenia, increased risk community acquired pneumonia and C diff, hypergastrinemia can lead to carcinoid
omeprazole- CYP2C19 inhibitor (cannot activate clopidogrel) aminosalicylate, 5 ASA (effective in UC/Crohn's) linked to sulfapyridine (effective in RA), partially absorbed in jejunum, activated by bacteria in colon and backwash to terminal ileum
uses- UC, Crohn's, RA (DMARD), AS
adverse- many can't handle due to nausea, GI upset, headache, arthralgia, bone marrow suppression, HS reaction, sulfa toxicity, oligospermia, neutropenia, thrombocytopenia, drug induced lupus aspirin, diclofenac, ibuprofen, indomethacin, ketorolac, naproxen, piroxicam
anti inflammatory, antipyretic, analgesic
uses- chronic post op pain, MSK pain (OA, RA), decrease risk of colon cancer, niacin tolerability, close PDA, gout
adverse-
stomach- depress mucosal cytoprotective PG leading to ulcers (piroxilam highest risk),
kidney- decrease GFR increase Na/H2O retention, edema, increased BP, hyperkalemia
hypersensitivity
interactions- ACEI, diuretics, corticosteroids, warfarin
contraindicated- Reye's, pregnancy mu delta and kappa receptors paired to Gi leading to activation of K channels on postsynaptic neurons (inhibitory depolarization) and inhibition of Ca channels on presynaptic neurons (inhibit NT release)
CNS effects- analgesia, euphoria, sedation, respiratory depression (reduce brainstem response CO2), cough suppression, miosis (excitatory PSNS), truncal rigidity, nausea/vomiting
peripheral- hypotension (vasodilation, inhibit baroreceptor reflex, increase histamine), constipation, biliary colic, decreased RPF, prolong labor, stimulate release ADH, PRL, somatotropin, inhibit release LH, pruritus (histamijne)
uses- analgesia, acute pumonary edema due to L heart failure, cough, diarrhea, anesthesia
contraindications- pure agonist with weak partial agonist, head injury (CO2 retention leads to increased ICP), pregnancy, impaired pulm/hepatic/renal function, Addison's, hypothyroidism induce annexin-1 to inhibit PLA2 blocking release of arachidonic acid
induce MAPK phosphatase 1 inactivating MAPK and inflammatory signalling
inhibit NF-KB a TF that stimualtes cytokines, chemokines and COX-2
uses- prevent and treat transplant rejection, autoimmune diseases, pain, nausea, fatigue, anorexia, gout
adverse-
short term- HTN, hyperglycemia, immunosuppression, psychosis
long term- osteoporosis, weight gain, fluid retention, cataracts, poor wound healing, gastric ulcers, GI bleed, adrenal suppression binds cyclophillin and forms complex that inhibits calcineurin, excreted via biliary system
(calcineurin activates transcription factor NF-AT in T cells allowing for formation of IL-2)
uses- organ transplant, uveitis, RA (DMARD), psoriasis
adverse- nephrotoxicity (limiting), tremor, HTN, hyperglycemia, hyperlipidemia, hyperuricemia osteoporosis, hirsutism, gym hyperplasia binds FK-BP, complex inhibits calcineurin
(calcineurin activates transcription factor NF-AT in T cells allowing for formation of IL-2)
uses- transplant kidney, liver, heart, atopic dermatitis, psoriasis
adverse- nephrotoxicity, neurotoxicity, hyperglycemia, HTN, hyperkalemia, GI upset, pleural effusion, preferred to cyclosporine inhibits AICAR transformylase leading to increased AICAR which competitively inhibits AMP deaminase leading to increased AMP and adenosine, adenosine inhibits inflammation via A2b receptors that suppress NF-KB, leads to suppression WBCs
also inhibits DHF reductase to prevent purine and thymidine synthesis
uses- RA (DMARD, drug of choice), psoriasis, psoriatic arthritis, AS, vasculitis, SLE, graft vs host disease, inflammatory bowel disease
adverse- nausea, ulcers, leukopenia, anemia, alopecia, hepatotoxicity, HS, pneumonitis, teratogen TCAs tertiary amines, inhibit reuptake NE and 5HT, anticholinergic, antihistamine, alpha block
uses- neuropathic pain (diabetic neuropathy, post herpetic neuralgia), fibromyalgia, migraine prophylaxis
adverse- anticholinergic, sexual dysfunction, orthostatic hypotension, weight gain, sedation
contra- glaucoma, BPH, heart block, prolonged QT interval TCAs secondary amines, inhibit reuptake NE and 5HT, anticholinergic, antihistamine, alpha block
uses- neuropathic pain (diabetic neuropathy, post herpetic neuralgia), fibromyalgia, migraine prophylaxis
adverse- fewer than tertiary amines, anticholinergic, sexual dysfunction, orthostatic hypotension, weight gain, sedation
contra- glaucoma, BPH, heart block, prolonged QT interval acute attack NSAID/acetaminophen, triptans, ergotamine and dihydroergotamine
prophylaxis
first line- B blockers, valproate, topirimate
second/third line- tricyclic, venlafaxine, verapamil, gabapentin, ACEI/ARB, Botox, NSAIDs inhibits voltage gated Na+ channels, GABAa agonist, glutamate antagonist
uses- migraine prophylaxis
adverse- tired, slow, nervous, confused, myopia, glaucoma, hyperthermia, renal stones, teratogen once absorbed, reduced by reacting with reduced ferredoxin, binds to proteins and DNA resulting in instability and cell death
uses- Entamoeba histolytica, Giardia, Trichomonas, anaerobic cocci, anaerobic gram negative bacilli, combo for H. pylori
adverse- GI distress, disulfiram-like reaction (no alcohol), metallic taste, tinadazole is better tolerated and has shorter treatment course inhibit microtubule synthesis and glucose uptake, decrease ATP production
albendazole
uses-cestodes (Taenia solium and Echinococcus granulosis)
adverse- hepatotoxicity, agranulocytosis, pancytopenia, inflammatory response to dying parasites in CNS, pregnancy category C
mebendazole
uses- Trichuris trichiuria, Enterobius vermicularis, Necator americanus, Ancyclostoma duodenale, Ascariasis lumbricoides
adverse- pregnancy category C
thiabendazole
uses- Strongyloides, cutaneous larva migrans, trichinosis
adverse- more toxic than others, CNS disturbances, contraindicated in pregnancy 