![logo]()
female maturation, endometrial proliferation, increase bone mass, increase HDL, decrease LDL, increase production factors 2, 7, 9, 10, and fibrinogen, decrease antithrombin III, increase risk thromboembolic events, increase production SHBG, increase NO, increase prostacyclin, Na+ and H2O retention
conjugation by cytochrome enzymes (inducers lead to reduction in efficacy)
uses- decrease risk of osteoporosis, decrease frequency of hot flashes (re-establish feedback on hypothalamic NE secretion), reverse postmenopausal atrophy of vulva, vagina, urethra, bladder trigone, primary hypogonadism (ages 11-13, add progestin after first uterine bleeding), androgen-dependent prostate cancer, OCP, menstrual abnormalities
adverse- bleeding, nausea, boobs hurt, melasma, peripheral edema, increased risk endometrial cancer, migraines, cholestasis, HTN, thromboembolism, depression natural- progesterone
synthetic- medroxyprogesterone, norgestrol, norethindrone, norgestimate, desogestreol, drospirenone
decrease growth and increaes vascularization of endometrium, thicken cervical mucus (inhibit sperm), increase in body temperature, maintain pregnancy
conjugation by cytochrome enzymes
levonorgestrel and norgestrel- highest androgenic activity
drospirenone- anti-androgenic activity
uses- OCP, endometrial cancer, abnormal uterine bleeding, hormone replacement, infertility
adverse- uterine bleeding, weight gain, insulin resistance, depression, changes in libido, headache, decreased HDL male maturation, sexual function, reduce hormone binding and other carrier proteins, increase synthesis of clotting factors, triglyceride lipase, a1AT, haptoglobin, sialic acid
testosterone, methyltestosterone
uses- hypogonadism, wasting (HIV, cancer), burn recovery, increase body mass in endurance athletes
danazol
uses- endometriosis, fibrocystic breast disease
adverse-
female- masculinization, acne, hirsutism, male pattern baldness, menstrual irregularities
male- priapism, impotence, decreased sperm, gynecomastia, gonadal atrophy
children- abnormal sex maturation, growth disturbances
general- increase LDL, decrease HDL, edema benefits- reduce risk of endometrial and ovarian cancer, improved regulation menstruation, relief benign breast disease, prevention ovarian cysts, reduction symptomatic PID, acne control
adverse-cardiovascular toxicity (thromboembolism, thrombophlebitis, HTN, MI), breakthrough bleeding, headache, insulin resistance, hirsutism (androgenic progestins), melasma, amenorrhea, depression
interactions- rifampin reduces efficacy (CYP450 induction)
contraindications- pregnancy, thromboembolic disorders, stroke, CAD, breast cancer, abnormal vaginal bleeding, HTN, liver tumor, DM, smoker, thrombophilia, migraine, hepatitis
start day one-five protected immediately, start after day 5 takes about a week to become effective
progestin only pill- norethrindrone or norgestrel, thickening of cervical mucus, endometrial alterations impair implantation delay labor by 48 hours so we can give glucocorticoids so baby can breathe
adverse overall- pulmonary edema, MI, respiratory arrest, death
MAGNESIUM SULFATE- uncouples excitation contraction in myometrial cells
adverse- flushing, nausea, headache, tired, blurred vision
INDOMETHACIN- inhibit PG (that act to stimulate uterine contractions)
adverse- oligohydramnios, premature closure ductus arteriosus
NIFEDIPINE- inhibit contractility
adverse- maternal tachycardia, flushing, headache, dizziness, nausea
ATOSIBAN- oxytocin antagonist
TERBUTALINE (B2 agonist)- PKA phosphorylates smooth muscle myosin light chain kinase and decreases affinity for calcium-calmodulin complex so no phosphorylation of myosin and smooth muscle relaxation
adverse- palpitations, tremor, nausea, vomiting, hypokalemia, hypoTN, DEATH depolarizing neuromuscular blocker activates nicotinic receptors leading to desensitization and blockade, ultra-rapid onset/ultra-short duration of action, initially causes transient fasiculations, penetrates membranes poorly and does not cross BBB
Phase I block- membrane is depolarized and unresponsive to additional impulses leading to flaccid paralysis, augmented by acetylcholinesterase inhibitors
Phase II block- channels behave as in prolonged closed state, can be reversed by acetylcholinesterase inhibitors
adverse- bradycardia (activation of muscarinic receptors), histamine release, muscle pain (unsynchronized contractions of muscle fibers), hyperkalemia (loss of potassium during depolarization), increased intraocular pressure, increased intra-gastric pressure, malignant hyperthermia
contraindicated- major burns, UMN, extensive denervation respiratory alkalosis (stimulate respiratory centers in medulla), metabolic acidosis, increased ketone bodies, inhibit dehydrogenases (increased pyruvate and lactate), messes with kidneys (increased sulfuric and phosphoric acid), vomiting, tinnitus, lethargy, coma, seizures, hypoglycemia, hyperthermia, pulmonary edema
treat- IV sodium bicarbonate (alkalinize urine for excretion), hemodialysis (severe cases) hyperthermia, myoclonic jerking, muscle rigidity, hyperreflexia, agitation, delirium
causes- linezolid, methylene blue, MAOI, TCAs, SSRIs, SNRIs, cocaine, dextrometorphan, fentanyl, meperidine, pentacozine, tramadol, trazodone, LSD, amphetamines, busiprone, lithium, mirtazapine
treat- cyproheptadine (5HT-2 antagonist) increased cAMP via inhibition of PDE, blocks adenosine receptors
acute- GI, hypokalemia, hypophosphatemia, hyperglycemia, metabolic acidosis, tremor, anxiety, tachycardia, SEIZURES, hypotension, ventricular arrythmias
chronic- dysarrythmias, seizures, minimal GI symptoms
treat- propanolol/esmolol (tachyarrythmias and hypotension), benzo/barb (seizures), oral activated charcoal, bowel irrigation, hemodialysis binds sulfhydryl groups inhibiting enzymes and messing with cell membranes
acute (usually elemental)- chest pain, SOB, nausea, kidney failure, GI distress, CNS toxicity
treat- dimercaprol, unithiol, succimer
chronic (usually vapor)- tremor, neuropsychiatric, gingivostomatitis, acrodynia (painful erythemia, HTN, diaphoresis common in children)
treat- unithiol, succimer, NO dimercaprol use- improve physical and mental performance
mechanism- increase insulin release, increase ACh, NE, DA, 5HT, activate leukocytes, antiplatelet, analgesic, cardioprotective, anticancer
adverse- bleeding, hypoglycemia 