Term
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Definition
| r-hGH; used for replacement in children, AIDS wasting syndrome, effects- ↑ IGF-1, protein synthesis, epiphyseal cartilage growth |
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Term
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Definition
| D2 receptor agonist; tx of Parkinson’s and hyperprolactinemia (impotence, infertility, galactorrhea, amenorrhea) |
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Term
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Definition
| somatostatin analogue; tx of acromegaly/gigantism when sx is not option, inhibits all GI hormones → side effects (diarrhea, N/V, abd pain) |
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Term
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Definition
| used to distinguish btw pituitary and hypothalamic dz, if ↑ LH/FSH, then hypothalamic disease dz, tx of infertility as continuous IV pump |
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Term
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Definition
| FSH and LH collected from urine of pregnant women; tx of infertility, ↑ risk of multiple pregnancies (i.e. octuplets) |
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Term
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Definition
| GnRH agonist; work @ pituitary cells, initially ↑ LH then ↓LH due to receptor down-regulation, tx prostate CA and uterine fibroids |
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Term
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Definition
| posterior pituitary hormone; facilitates birth (via positive feedback) and breastfeeding (milk letdown) |
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Term
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Definition
| ADH analogue; used in tx of diabetes insipidus – upregulates aquaporin channels in renal collecting ducts |
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Term
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Definition
| 1st 24 amino acids of ACTH; used to test adrenal function – measure cortisol levels pre- and post- |
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Term
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Definition
| adrenal hormone; anti-inflammatory via downregulation of PLA2, ↑ blood glucose, cross-reactivity w/ aldosterone, fat redistribution, skeletal muscle proteolysis, maintainence of vascular tone, overuse → Cushing’s syndrome |
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Term
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Definition
| potent glucocorticoid; long t1/2, tx of rheumatic diseases, suppresses ACTH and CRH release – TAPER dose |
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Term
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Definition
| inhibitor of P450’s in liver; prevents overproduction of cortisol in Cushing’s disease pts (↑↑↑ ACTH) |
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Term
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Definition
| synthetic estrogen; used commonly in oral contraceptives, inhibits FSH/LH secretions via negative feedback, side effects- DVT/stroke, endometrial tumors, closes epiphyses, breast enlargement |
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Term
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Definition
| synthetic progestin; used commonly in oral contraceptives, side effects- acne, wt gain, effective alone as injection |
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Term
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Definition
| estrogen receptor antagonist; blocks action of estrogen in breast tissue, tx of breast CA, must be activated in tissue in order to be useful |
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Term
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Definition
| estrogen receptor antagonist; blocks action of estrogen in breast tissue, tx of breast CA, must be activated in tissue in order to be useful |
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Term
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Definition
| produced by testes, ovary, and adrenals; development of male structures (DHT) and 2o sex characteristics, converted to estrogens via aromatase, when given as patch – avoids 1st pass metabolism, side effects – virilization, ↓ LH/FSH |
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Term
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Definition
| analogue; given orally, short t1/2 |
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Term
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Definition
| testosterone analogue; long t1/2, used for tx of endometriosis and PMS symptoms, same side effects as testosterone |
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Term
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Definition
| DHT receptor antagonist; tx of acne, baldness, hirsuitism, inhibits libido in sexual deviants |
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Term
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Definition
| androgen receptor antagonist; tx of prostate cancer (DHT-mediated) |
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Term
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Definition
| 5α-reductase inhibitor; prevents conversion of testosterone to DHT, tx of BPH and male pattern baldness |
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Term
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Definition
| aromatase inhibitor; prevents conversion of androgens to estrogens thus preventing growth of estrogen-mediated tumors (breast, endometrial, ovarian), side effects- osteoporosis (esp. in post-menopausal women) |
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Term
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Definition
| 1st generation sulfonylurea; ↑ insulin release by ββ-cells by enhancing glucose uptake via GLUT-2, hypoglycemia due to excess insulin secretion |
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Term
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Definition
| 1st generation sulfonylurea; ↑ insulin release by ββ-cells by enhancing glucose uptake via GLUT-2, hypoglycemia due to excess insulin secretion |
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Term
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Definition
| 2nd generation sulfonylurea; same action as 1st generation except 10-100X more potent |
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Term
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Definition
| ↑ insulin secretion, taken before meal to control post-prandial glucose, side effect- hypoglycemia |
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Term
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Definition
| ↑ insulin sensitivity, ↓ hepatic gluconeogenesis, ↑ uptake and glycolysis in peripheral tissues, ↓ GI glucose absorption, ↓ plasma glucagon levels, side effects- lactic acidosis (liver or renal disease), GI upset |
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Term
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Definition
| ↑ insulin sensitivity by binding PPAR- receptors (fibrates use PPAR-α), ↑ glucose uptake into muscles and fat, inhibit hepatic gluconeogenesis (~metformin) |
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Term
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Definition
| α-glucosidase inhibitor; ↓ intestinal absorption of disacarrhides, ↓ post-prandial glucose elevation, side effect- flatulence and abdominal pain |
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Term
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Definition
| somatostatin analogue; inhibits secretion of GI hormones, tx of glucagonoma/insulinoma in pancreas |
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Term
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Definition
| glucagon-like-peptide analogue; inhibits glucagon-stimulation gluconeogenesis in liver, slows gastric emptying, suppresses appetite |
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Term
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Definition
| synthetic T4; tx of hypothyroidism, must monitor levels during therapy, converted to T3 in tissues |
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Term
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Definition
| mixture of T3 and T4; only T3 is active in tissues |
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Term
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Definition
| inhibits thyroperoxidase reactions (iodination and coupling), tx of hyperthyroidism/Grave’s dz, inhibits peripheral conversion of T4, does not cross placenta - preferred in pregnancy, side effects- agranulocytosis |
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Term
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Definition
| inhibits thyroperoxidase reactions (iodination and coupling), tx of hyperthyroidism/Grave’s dz, 10X more potent than PTU, crosses placenta and concentrates in fetal thyroid (use PTU) |
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Term
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Definition
| radioactive isotope, concentrates in thyroid, used in combo w/ radiation to ablate thyroid in hyperthyroidism |
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Term
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Definition
| contrast media; inhibits conversion of T4 to T3 in liver, kidney, pituitary, and brain |
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Term
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Definition
| precursor to active form of VitD (1,25-OH), ↑ Ca2+ absorption from gut (also renal and bone resorption @ pharmacological doses), tx of rickets, osteomalacia, hypoparathyroidism, osteoporosis (in combo w/ calcium) |
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Term
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Definition
| calcitriol analogue; tx of psoriasis when used topically (> steroids) |
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Term
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Definition
| PTH inhibitor; binds to Calcium sensor in parathyroid and prevents PTH release, tx hyperparathyroidism |
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Term
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Definition
| 1st generation bisphosphonate; inhibits bone resorption, tx of post-menopausal osteoporosis and Paget’s disease, side effects- jaw osteonecrosis (3rd gen.) and esophageal irritaion (take after overnight fast w/ glass of water) |
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Term
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Definition
| 2nd generation bisphosphonate; same effect as etidronate but 10-100X more potent |
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Term
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Definition
| 3rd generation bisphosphonate; tx of Paget’s disease, most likely to cause osteonecrosis |
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Term
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Definition
| 3rd generation bisphosphonate; most likely to cause osteonecrosis, 1000-10000X more potent |
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Term
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Definition
| disrupts DNA structure, needs enzymatic activation, effective against anaerobic bacteria, good BBB penetration, teratogenic, “disulfiram effect” w/ EtOH, DOC for trichomonas, enaemoba, giardia |
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Term
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Definition
| inhibition of mitochondrial transport, 2o tx PCP (AIDS), toxoplasma, amoeba, trichomoas, and p. flaciparum |
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Term
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Definition
| inhibits ornithine decarboxylase (shared enzyme), tx West African trypanosome, side effects- bone marrow suppression, dose-limiting diarrhea orally |
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Term
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Definition
| antimalarial; prevents polymerization of heme by parasite, resistance via p-gp, side effect- visual impairment, tx. P. falciparum and extra-GI amoeba |
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Term
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Definition
| antimalarial; inhibits nucleic acid synthesis, toxic to gamete forms of vivax and malariae (not falciparum), parenteral for drug-resistant falciparum, CN8 toxicity |
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Term
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Definition
| antimalarial; same mechanism as quinine, also prevents polymerization (~chloroquine) |
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Term
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Definition
| antimalarial; alkylates and damage macromolecules in plasmodia, given IV for severe p. falciparum |
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Term
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Definition
| antimalarial; prophylaxis, kills hepatic stages and tissue forms of vivax and ovale, active against falciparum gametes, side effects- hemolytic anemia w/ G-6PD deficiency |
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Term
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Definition
| antimalarial; inhibits DHFR, tx of drug-resistant falciparum w/ sulfadoxine, NEVER used as single agent |
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Term
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Definition
| sulfonamide; inhibits utilization of PABA in synthesis of folic acid, used in combo w/ pyrimethamine for malaria |
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Term
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Definition
| antihelminthic; inhibits microtubule polymerization (~vincristine), immobilization and death of parasites, tx ascaris, enterobius, ancylostoma, necator, teratogenic |
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Term
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Definition
| antihelminthic; inhibits microtubule polymerization (~vincristine), immobilization and death of parasites, tx ascaris, enterobius, ancylostoma, necator, teratogenic |
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Term
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Definition
| antihelminthic; binds nicotinic receptors → spastic paralysis (~succinylcholine), poor absorption = remains in gut lumen (intestinal worms) |
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Term
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Definition
| antihelminthic; inhibits Glut and GABA channels → paralysis, allergic reaction to dead worms, tx strongyloides |
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Term
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Definition
| ↑ Ca2+ permeability → spastic paralysis; tx schistosomiasis, tissue flukes and tapeworms |
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Term
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Definition
| tx for lympathic filiariasis (agent for elephantiasis) |
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Term
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Definition
| bile acid sequestrant; interrupts enterohepatic recycling of cholesterol, given in powder form (fecal impaction), prevents absorption of other drugs (i.e. ezetimibe) |
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Term
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Definition
| HMG-CoA reductase inhibitor; inhibits cholesterol synthesis, ↑ hepatic LDL receptors, ↓ hepatic VLDL secretion, able to reduce LDL by 60%, low potency, contraindicated w/ UGT blockers (gemfibrozil), CYP3A4 inhibitors, and p-gp inhibitors (cyclosporin), side effects- teratogenic , myalgias, myositis, rhabdomyolysis |
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Term
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Definition
| HMG-CoA reductase inhibitor; high potency, use with renal disease, side effects- teratogens, muscle disease |
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Term
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Definition
| inhibits cholesterol absorption in small bowel via, NPC1L1 receptor, ↑ hepatic LDL receptors (statins), often combined w/ statins, interaction w/ bile acid sequestrants – reduced absorption |
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Term
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Definition
| ↓ TG’s by binding PPAR-α, ↑ HDL apolipoproteins, ↓ TG synthesis and ↑ FA oxidation in muscle and liver, primarily used to lower plasma TG’s |
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Term
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Definition
| inhibits FA mobilization from fat, ↓ hepatic TG synthesis, ↓ VLDL secretion (LDL and TG), side effects- flushing (high capacity) and hepatotoxicity (low capacity), gout and pruritis |
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Term
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Definition
| active ingredient is THC, injection of conjunctiva, decreased immune response, side effects- short term memory loss, loss of balance/stability, amotivational syndrome (chronic use), wt gain |
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Term
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Definition
| synthetic THC; approved for antiemetic effect in cancer chemotherapy and AIDS wasting syndrome, Lysergic Acid Diethylamide (LSD)- 5-HT2 partial agonist; sympathomimetic effects- visual illusions, synesthesia, loss of judgement, adverse effects- bad trips and flashbacks (tx with BNZs) |
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Term
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Definition
| 5-HT/DA agonist; visual illusions, time misperceptions, adverse effects- paranoia/fear and N/V |
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Term
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Definition
| agonist, NMDA antagonist, DA/NE reuptake inhibitor; causes restlessness and anxiety, dependence and OD common, toxicities- coma/convulsions (tx BNZs), psychosis (~schizophrenia) |
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Term
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Definition
| GABA-mimetic; metabolized by alcohol dehydrogenase and aldehyde dehydrogenase, facilitates @ GABA receptors, blocks NMDA Glut receptors, depresses cardiac and smooth muscle, BNZ tx for withdrawal, reduced gluconeogenesis in liver, peripheral neuropathy, Thiamine deficiency often present (ataxia, confusion, EOM paralysis), dilated cardiomyopathy, Withdrawal → DT’s (tx BNZ/phenytoin) |
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Term
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Definition
| specific β1 blocker; used to tx sympathomimetic response to acute alcohol withdrawal, slows HR and lowers BP |
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Term
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Definition
| opioid receptor antagonist; used to tx alcoholism and alcohol withdrawal, ↓ cravings and relapses |
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Term
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Definition
| aldehyde dehydrogenase antagonist; tx alcoholism, consumption of EtOH leads to accumulation of acetaldehyde → N/V and general malaise in user |
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Term
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Definition
| alcohol dehydrogenase inhibitor; tx of alcoholism and methanol poisoning, blocks methanol metabolism w/ concurrent EtOH infusion IV |
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Term
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Definition
| found in household cleaners and “canned heat”; metabolized to formaldehyde → severe acidosis, retinal damage, and blindness (“in a snowstorm”), tx w/ EtOH infusion and fomepizole |
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Term
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Definition
| Vit B1; given to all suspected EtOH intoxicated pts to prevent Wernicke-Korsakoff syndrome (ataxia, confusion, nystagmus, opthalmoplegia) |
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Term
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Definition
| nicotine gum; used to tx nicotine addiction (6-12 months duration), contraindicated w/ oral lesion and dental work, best when combined w/ stop smoking program or bupropion |
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Term
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Definition
| atypical antidepressant; ~ NE/DA reuptake inhibitor, interacts with CYP2D6 drugs, contraindicated in pts w/ seizure dsorder, anorexia or bulimia nervosa, most effective when combined w/ behavior therapy |
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Term
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Definition
| nAch receptor partial agonist; side effects- nausea, suicidal ideations, nightmares, depressed mood, 2nd line tx |
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Term
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Definition
| non-selective antagonist @ non-a7 nAchR, crosses BBB and hits CNS and peripheral receptors |
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Term
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Definition
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Term
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Definition
| typical antidepressant; 5-HT/NE reuptake inhibition, also blocks mAch (xerostomia, constipation, urinary retention), α1 (orthostatic hypotension), and histamine receptors (sedation), OD → arrhythmias/myocardial depression, p-gp resistance to cross BBB |
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Term
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Definition
| typical antidepressant; 5-HT/NE reuptake inhibition, also blocks mAch (xerostomia, constipation, urinary retention), α1 (orthostatic hypotension), and histamine receptors (sedation), OD → arrhythmias/myocardial depression |
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Term
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Definition
| atypical antidepressant; moderate inhibition of 5-HT reuptake; useful in depressed pts w/ sleep disorders, CYP3A4 inhibition |
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Term
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Definition
| presynaptic α2 antagonist; increased NE and 5-HT release, potent antihistamine – sedating |
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Term
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Definition
| SSRI; 1st line therapy in MDD, selective inhibition of 5-HT reuptake, long t1/2 (days-wk), contraindicated w/ MAOIs (serotonin syndrome), adverse effects- sexual dysfunction, substrate for p-gp resistance |
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Term
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Definition
| SSRI; 1st line therapy in MDD, selective inhibition of 5-HT reuptake, long t1/2 (days-wk), contraindicated w/ MAOIs (serotonin syndrome), adverse effects- sexual dysfunction |
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Term
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Definition
| MAOI; irreversibly blocks monoamine oxidase in nerve terminals, typically used in pts unresponsive to TCA’s and SSRI’s, adverse effects- sleep disturbance, SSRI interactions, HTN drug interactions |
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Term
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Definition
| mood stabilizer; tx of Bipolar disorder, ~stabilizes membranes bia inositol signaling inhibition, very narrow therapeutic window, adverse effects- neurological, hypothyroidism, arrhythmias, diuretics and NSAIDs ↓ excretion |
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Term
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Definition
| immediate precursor to DA, crosses BBB and is converted to DA, replenishes DA in synaptic terminals of striatal neurons, co-administered w/ carbidopa to prevent peripheral metabolism (99%), adverse effects- N/V, arrhythmias, dyskinesias/akinesia, “on/off phenomenon”, MAOI’s → HTN crisis, psychosis (due to DA stimulation) |
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Term
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Definition
| D2 agonist/D1 partial agonist; enhances activation of indirect pathway (↓ erratic movements) |
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Term
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Definition
| D2 agonist; more effective than bromocriptine |
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Term
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Definition
| D2 agonist; may act as free radical scavenger |
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Term
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Definition
| antiviral; enhances DA secretion and possibly synthesis, OD → psychosis, side effects similar to L-DOPA, contraindicated w/ hx of seizure disorder or CHF |
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Term
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Definition
| COMT inhibitor; inhibits DA metabolism and reduces metabolite production that competes w/ L-DOPA, reduces fluctuations in response to L-DOPA |
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Term
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Definition
| mAch antagonist; blocks excess Ach stimulation in striatum, restores balance of DA/Ach, adjunct to L-DOPA |
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Term
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Definition
| 1st generation antihistamine; strong anticholinergic effects, sedative |
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Term
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Definition
| AchE inhibitor; centrally-active inhibition of Ach metabolism, parasympathomimetic side effects |
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Term
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Definition
| AchE inhibitor; centrally-active inhibition of Ach metabolism, parasympathomimetic side effects |
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Term
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Definition
| SSRI; tx of depression in Huntington’s pts |
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Term
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Definition
| blocks voltage-gated Na+ channels and ↑ GABA, mood stabilizer in HD |
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Term
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Definition
| D2 receptor antagonist; antipsychotic w/ Parkinsonian side effects, “blocks inhibition” in indirect pathway, tx chorea in HD |
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Term
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Definition
| D2 receptor antagonist; antipsychotic w/ Parkinsonian side effects, “blocks inhibition” in indirect pathway, tx chorea in HD |
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Term
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Definition
| Na+/Ca2+ blocker; tx ALS, reduces glutamate release, direct NMDA (Glut) receptor blocker – reduces excitotoxicity, |
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Term
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Definition
| mAB used to tx MS and Crohn’s disease, restores BBB w/ anti-inflammatory actions, adverse effect- PML (~JC v) |
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Term
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Definition
| short-acting BNZ; enhances GABAergic inhibition by increasing frequency of Cl- channel opening, tx acute panic attacks, ↓ sleep onset, ↑ stage 2 NREM sleep and ↓ REM, high risk for rebound anxiety/insomnia, taper withdrawal, anterograde amnesia (while on drug) |
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Term
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Definition
| short-acting BNZ; enhances GABAergic inhibition by increasing frequency of Cl- channel opening, tx acute panic attacks, ↓ sleep onset, ↑ stage 2 NREM sleep and ↓ REM, high risk for rebound anxiety/insomnia, taper withdrawal, anterograde amnesia (while on drug) |
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Term
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Definition
| long-acting BNZ, high risk for morning-after effects (intrinsic tapered withdrawal) |
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Term
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Definition
| GABA agonist; binds to GABAergic Cl- channel and increases duration of opening, linear dose-response curve, profound CNS depression, not 1st line choice for sedation/hypnosis, CYP inducer |
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Term
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Definition
| hypnotic; ↓ sleep latency, ↓ REM sleep, rebound insomnia @ high doses, tolerance w/ extended use |
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Term
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Definition
| hypnotic; ↓ sleep latency, short t1/2 w/ little effect on total sleep time |
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Term
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Definition
| GABA receptor antagonist; tx OD w/ BNZ, can precipitate withdrawal in BNZ-dependent pts |
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Term
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Definition
| HIV fusion inhibitor; binds gp41 on viral envelope and prevents membrane fusion on CD4+ T cells (CXCR4 or CCR5 receptors), resistance if gp41 mutates, ↑ risk of bacterial pneumonia |
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Term
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Definition
| nucleoside reverse transcriptase inhibitor (NRTI); purine analogue, P’ed to TP form to compete w/ dATP for incorporation, side effects- peripheral neuropathy and pancreatitis |
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Term
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Definition
| nucleoside reverse transcriptase inhibitor (NRTI); pyrimidine analogue, P’ed to TP form to compete w/ dCTP for incorporation |
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Term
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Definition
| nucleoside reverse transcriptase inhibitor (NRTI); pyrimidine analogue, P’ed to dTTP in order to compete for incorporation, only NRTI proven to ↓ perinatal HIV transmission, side effect- bone marrow suppression |
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Term
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Definition
| protease inhibitor; prevents cleavage of polyprotein/prevents virion maturation (noninfectious particles), most effect HAART treatment, potent CYP3A4 inhibitor, adverse effects- hyperlipidemia, insulin resistance, and lipodystrophy |
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Term
|
Definition
| protease inhibitor; prevents cleavage of polyprotein/prevents virion maturation (noninfectious particles), most effect HAART treatment, potent CYP3A4 inhibitor, adverse effects- hyperlipidemia, insulin resistance, and lipodystrophy |
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Term
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Definition
| nucleoside analogue; inactivates DNA polymerase via direct binding, resistance occurs due to viral DNAP mutation/absent thymidine kinase, must be activated by viral thymidine kinase (host protected) and cytoplasmic kinases, tx herpes virus infections – HSV, VZV, and CMV+ BMT pts, side effects- reversible renal dysfunction, neurolotoxic (@ high doses) |
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Term
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Definition
| nucleoside analogue; hydrolyzed to acyclovir after oral administration, increased bioavailability |
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Term
|
Definition
| nucleoside analogue; prodrug of penciclovir, used as alternative to acyclovir |
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Term
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Definition
| nucleoside analogue; tx of CMV retinitis in AIDS patients, 100X activity of acyclovir |
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Term
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Definition
| nucleoside analogue; NOT activated by viral thymidine kinase, tx of acyclovir-resistant HSV/VZV, IV to prevent progression of CMV retinitis in AIDS pts, adverse effect- nephrotoxic |
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Term
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Definition
| pyrophosphate analogue; inhibits HSV DNAP and HIV reverse transcriptase, inhibits cleavage of pyrophosphate in chain elongation, tx of nucleoside-resistant HSV, VZV, and CMV, adverse effect- nephrotoxic |
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Term
|
Definition
| nucleoside analog for HBV/HCV; inhibits GTP-mediated 5’ capping of mRNA, concentrates in erythrocytes → hemolytic anemia, teratogenic |
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Term
|
Definition
| influenza uncoating inhibitor; binds to M2 ion channel on virion and prevents H+-mediated uncoating, tx oral prophylaxis for Influenza A, alternative to vaccine for eldery and immunocompromised pts, resistance due to M2 mutations |
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Term
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Definition
| neuraminidase inhibitor; inhibits viral neuraminidase thus preventing spread, tx uncoating agent-resistant Influenza A and B, resistance due to neuraminidase mutations |
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Term
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Definition
| typical antipsychotic; D2 receptor antagonist, largely effects “positive” symptoms (delusions, hallucinations, etc) low potency - unlikely to produce EPS (dystonia, akathesia, parkinsonism, neuroleptic malignant syndrome, tardive dyskinesia), also blocks cholinergic (confusion), H1 (sedation), α-adrenergic (hypotension/tachycardia), and 5-HT2 receptors (< atypicals), impairs glucose tolerance → type 2 DM, ↑↑ PRL levels (removal of tonic inhibition) |
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Term
|
Definition
| typical antipsychotic, low potency, no glucose intolerance |
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Term
|
Definition
| typical antipsychotic, high potency, most likely to cause EPS, less anticholinergic effects |
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Term
|
Definition
| atypical antipsychotic; ↓↓D2 and ↑ 5-HT2 (antagonist) affinity – prevents presynaptic DA release, ↑ PRL levels, also cholinergic, α-adrenergic, and histamine antagonist, ↑ risk of DM2/metabolic syndrome, side effects- lowers seizure threshold in non-epileptics, blood dyscrasias (requires weekly monitoring) |
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Term
|
Definition
| atypical antipsychotic; MoA clozapine, highest risk of developing metabolic syndrome |
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Term
|
Definition
| atypical antipsychotic; MOA clozapine, NO ↑ in PRL levels |
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Term
|
Definition
| atypical antipsychotic; limited EPS, only agent approved for use in children/teens, extreme ↑ PRL levels |
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Term
|
Definition
| atypical antipsychotic; D2 receptor partial agonist, little effect if any on PRL levels, also 5-HT antagonist |
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Term
|
Definition
| atypical antipsychotic; limited EPS |
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Term
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Definition
| stabilizes Na+ channels in inactivated state, voltage-gated Na+ channel blocker, Ca3+ channel blocker; 2nd line tx for simple and generalized seizures (+ tonic-clonic), 2nd line tx for status epilepticus, zero-order kinetics (constant amt metabolized), CYP inducer – warfarin and OC interactions, side effects- gingival hyperplasia, hirsuitism, bone sx (chronic) |
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Term
|
Definition
| barbiturate; enhances GABA-mediated chloride flux by binding GABA receptors, partially blocks Glut channels; highly sedative, CYP inducer |
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Term
|
Definition
| stabilizes Na+ channels in inactivated state (~phenytoin); DOC for partial/generalized tonic-clonic seizures, CYP and UGT inducer (↑ metabolism of other AEDs and OC), side effects- diplopia, ataxia, blood dyscrasias |
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Term
|
Definition
| inhibits low threshold T-type Ca2+ channels in thalamus, DOC for absence seizures |
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Term
|
Definition
| ~ phenytoin on Na+ channels, ~ethosuximide on T-type Ca2+ channels, ↑ GABA synthesis and ↓ GABA metabolism; indicated for all types of seizures (2nd line), inhibits UGTs (own metabolism) and CYPs (AED’s) |
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Term
|
Definition
| BNZ; DOC for status epilepticus, can be given rectally for seizures in children or pts unable to take oral medications |
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Term
|
Definition
| MoA unknown; adjunct for partial seizures, monotherapy for generalized tonic-clonic and myoclonic seizures |
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Term
|
Definition
| mechanism is ambiguous; adjunct or monotherapy in refractory partial seizures, also used for migraines, inhibits carbonic anhydrase → kidney stones |
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Term
|
Definition
| inhibits Na+ channels and may reduce Ca2+ currents; adjunct for partial seizures in adults, broad spectrum |
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Term
|
Definition
| BNZ receptor antagonist; quickly reverses BNZ intoxication, may precipitate withdrawal in dependent pts |
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Term
|
Definition
| binds to Hgb and ↓ affinity for O2 (reduced carrying capacity), tx 100% O2 |
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Term
|
Definition
| non-selective β-blocker; used in stimulant overdose – ephedrine, amphetamines, cocaine; prevents NE-mediated tachycardia and HTN |
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Term
|
Definition
| AchE inhibitor; ↑ Ach levels @ synaptic terminal by inhibiting metabolism, tx of anticholinergic side effects – antihistamines, antidepressants, antipsychotics, and antiemetics (urinary retention, confusion, mydriasis, etc) |
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Term
|
Definition
| organophosphate; inhibits AchE by phophorylation causing neurtotoxicity and paralysis, tx w/ pralidoxime (2PAM) IV which removes Pi group from enzyme |
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Term
|
Definition
| musarinic antagonist; used to inhibit toxicity by AchE inhibitors such as pesticides |
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Term
|
Definition
| converted to glutathione to replace after acetaminophen overdose, given < 8-10 hrs post-OD to prevent hepatic failure |
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Term
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Definition
| chelator; given in mild/asymptomatic lead toxicity to prevent colic/constipation, neurotoxicity, and encephalopathy, also used in arsenic poisoning, lowers blood levels but unable to reverse previous damage |
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Term
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Definition
| chelator; used in severe lead toxicity/encephalopathy, in combination w/ Calcium EDTA, 1st line therapy for arsenic poisoning – produces necrotic abscesses @ injection sites |
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Term
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Definition
| iron chelator; given IV to chelate excess iron and remove in bile, turns body fluids red |
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Term
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Definition
| β-lactam; binds to enzymes required for cell wall synthesis (PBP’s) – bacteriocidal, renally eliminated – adjust in renal dz, given orally (vs. Pen G), tx G+ cocci/some G- cocci/spirochetes, adverse effects- neurotoxic (@ high doses), hypersensitivity rashes 2 days after, acute IgE-mediated allergy (use macrolide), pseudomembranous colitis (wide coverage) |
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Term
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Definition
| antistaphylococcal β-lactam; tx s. aureus and s. epidermis, given parenterally |
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Term
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Definition
| extended spectrum β-lactam; same coverage as Pen G + some G-‘s (H. flu + E. coli), used w/ clavulonic acid to prevent degradation by β-lactamase |
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Term
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Definition
| extended spectrum β-lactam; side effects- diarrhea after oral dosing |
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Term
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Definition
| 1st generation cephalosporin; useful in penicillin-allergic pts, same spectrum as ampicillin |
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Term
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Definition
| 2nd generation cephalosporin; more active against G- (H. flu and B. fragilis), less active against G+ |
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Term
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Definition
| 3rd generation cephalosporin; reserved for serious infections (pneumonia/meningitis), wide G- coverage w/ good Gram+ coverage, crossed BBB into CSF |
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Term
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Definition
| 3rd generation cephalosporin; reserved for serious infections (pneumonia/meningitis), wide G- coverage w/ good Gram+ coverage, crossed BBB into CSF |
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Term
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Definition
| 4th generation cephalosporin; ↑ Gram+ coverage + activity against β-lactamase producing organisms |
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Term
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Definition
| inhibits d-Ala d-Ala production in cell wall synthesis (step before penicillins), Enterococcus is resistant, Gram+ coverage – narrow spectrum, given parenterally for systemic infections/orally for colitis, side effects- ototoxic + “red man syndrome” (histamine release on trunk) w/ rapid infusion, nephrotoxic, tx MRSA, Enterococcus, pseudomembranous colitis |
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Term
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Definition
| inhibits protein synthesis by binding 50S ribosomal subunit; resistance by point mutation in 50S subunit, tx MRSA/E, Vancomycin-resistant Enterococcus |
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Term
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Definition
| tetracycline; inhibition of protein synthesis via 30S ribosomal subunit; enters via porin molecules in G-, effluxed by energy-dependent pump, absorption inhibited by di- and trivalent cations, chelates Ca2+ → discoloration of teeth/depression of bone growth, photosensitivity reactions, tx most zoonoses, Chlamydia, mycoplasma |
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Term
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Definition
| macrolide; inhibits protein synthesis via 50S ribosomal subunit, GI irritation most common, extremely long half-lives, concentrates in cells – campylobacter, legionella (intracellular bugs) |
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Term
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Definition
| macrolide; CYP inhibitor, DOC for MAI complex and H. pylori |
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Term
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Definition
| macrolide; see azithromycin for MoA, DOC for C-AP, legionaire’s diseaes, concentrates in prostate and macrophages, tx Gram+ infections in pen-allergic pts |
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Term
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Definition
| ketolide; 10X higher affinity for 50S than macrolides, CYP3A4 inhibitor, DOC for anaerobic infections, adverse effect- pseudomembranous colitis w/ C. difficile (tx. Vanc or metronidazole), often used in combo w/ antimalarials |
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Term
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Definition
| aminoglycoside; inhibits protein synthesis via 30S ribosomal subunit, must diffuse thru membrane (requires energy – NO anaerobes), only given IM/IV, tx serious Gram- infections (+ penicillin/cephalosporin for Gram+’s) adverse effects- ototoxic, nephrotoxic (cortex), neurotoxic |
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Term
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Definition
| aminoglycoside; inhibits protein synthesis via 30S ribosomal subunit, must diffuse thru membrane (requires energy – NO anaerobes), only given IM/IV, tx serious Gram- infections (+ penicillin/cephalosporin for Gram+’s) adverse effects- ototoxic, nephrotoxic (cortex), neurotoxic |
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Term
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Definition
| aminoglycoside; inhibits protein synthesis via 30S ribosomal subunit, must diffuse thru membrane (requires energy – NO anaerobes), only given IM/IV, tx serious Gram- infections (+ penicillin/cephalosporin for Gram+’s) adverse effects- ototoxic, nephrotoxic (cortex), neurotoxic |
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Term
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Definition
| DHFR inhibitor; prevents reduction of DHF to THF (highly selective for bacterial enzyme), concentrates in vaginal and prostatic secretions – UTI’s and prostate infections, used in combo w/ sulfamethoxazole for UTI’s, adverse effects- megaloblastic anemia (tx w/ folinic acid- reduced form) |
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Term
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Definition
| fluouroquinolone; inhibits DNA gyrase (bacteriocidal), absorption inhibited by di- and trivalent cations, distributes to bone, kidney, urine, prostate, and intracellular, adverse effects- crystalluria, tendon rupture, CYP inhibitor, tx Gram- infections (alternative for aminoglycosides |
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Term
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Definition
| fluouroquinolone; inhibits DNA gyrase (bacteriocidal), absorption inhibited by di- and trivalent cations, distributes to bone, kidney, urine, prostate, and intracellular, adverse effects- crystalluria, tendon rupture, CYP inhibitor, tx Gram- infections (alternative for aminoglycosides |
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Term
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Definition
| anti-TB; inteferes w/ mycobacterial synthesis of mycolic acids (cell wall), -cidal for fast-growing cells, adverse effects- pyridoxine (B6) depletion → peripheral neuropathy and dose-related hepatotoxicity |
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Term
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Definition
| anti-TB; inhibits DNA-dependent RNA polymerase (-cidal), resistance emerges quickly, effective against intra- and extracellular bugs, potent inducer of CYP’s, turns body fluids red, hepatotoxicity, also used prophlactically aginst Neisseria m. |
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Term
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Definition
| anti-TB; hepatotoxicity, optic neuritis → blindness |
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Term
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Definition
| antifungal; binds to ergosterol in fungal membrane → leakage of small molecules, resistance by some Candida spp., tx disseminated fungal infections, use in pregnancy (azoles teratogenic), adverse effect- nephrotoxicity (DL) |
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Term
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Definition
| antimetabolite; inhibits thymidylate synthase, used in combo w/ amphotericin B, tx meningitis caused by Cryptococcus or candida, adverse effects- bone marrow toxicity, colitis |
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Term
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Definition
| azole antifungal; inhibits synthesis of ergosterol, adverse effects- CYP inhibition, teratogenic, male steroid dysfunction (testosterone), inhibition of adrenal steroid synthesis |
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Term
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Definition
| azole antifungal, inhibits synthesis of ergosterol, visual disturbances, hepatic toxicity, tx invasive resistant-aspergillus |
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Term
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Definition
| disrupts fungal mitotic spindle, deposits into keratinized cells, tx dermatophyes (i.e. tineas) |
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Term
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Definition
| interferes w/ fungal ergosterol synthesis, concentrates in hair and nail beds, tx ringworm of nails |
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Term
| Ampethamine/Dextroamphetamine |
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Definition
| enter synaptic terminal and release catecholamines into cleft; tx ADHD, Obesity, and narcolepsy, sympathomimetic response, ↑↑↑ DA in reward pathway – highly addictive, acute toxicity- hyperthermia, tachycardia, seizures, chronic toxicity- wt loss/appetite suppression, dilated cardiomyopathy, anxiety/paranoia/psychosis |
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Term
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Definition
| mild CNS stimulant, similar abuse potential to amphetamines, tx narcolepsy and ADHD |
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Term
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Definition
| used in short-term tx of obesity, less abuse potential than amphetamine, contraindications- advanced atherosclerosis, CVD/HTN, hyperthyroidism, hx drug abuse |
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Term
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Definition
| tx of narcolepsy, little abuse potential – no DA stimulation, microsomal enzyme inducer (OC’s, AEDs) |
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Term
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Definition
| NE reuptake inhibitor; tx ADHD – only drug approved for adult ADHD (addiction prone adolescents), side effects- appetite suppression, insomnia, tachycardia and HTN |
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Term
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Definition
| DA/NE/5-HT reuptake inhibitor; tx obesity and wt loss, high risk of serontonin syndrome w/ SSRIs and triptans |
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Term
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Definition
| natural product containing phytoestrogen; tx menstrual cramps |
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Term
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Definition
| laxative; hepatotoxic effects, possibly carcinogenic |
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Term
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Definition
| natural coumarin derivative; interferes w/ concurrent warfarin and other anticoagulant therapy, contains estrogen-like compounds → risk of uterine/breast cancer |
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Term
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Definition
| anti-platelet action, most often used by surgical candidates, some evidence of ↓ LDL cholesterol |
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Term
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Definition
| ↓ LDL cholesterol and blood glucose, immune system booster – antagonizes immunosuppressant drugs (steroids, azathioprine), CYP inhibitor (↑ amts of other drugs) |
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Term
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Definition
| anti-platelet action, most often used by surgical candidates, CYP inhibitor |
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Term
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Definition
| used for tx of depression, CYP inducer - ↓ activity of HAART medications (protease inhibitors) |
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Term
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Definition
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Term
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Definition
| CYP inhibitor, also induces CYP3A4, immune system booster – antagonizes immunosuppressant drugs (steroids) |
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Term
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Definition
| potent antioxidant; ↓ systolic and diastolic BP, improvements in exercise tolerance, side effect- potential interaction w/ warfarin due to Vit K homology |
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Term
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Definition
| cofactor for multiple enzymes; role in carbohydrate, protein, and lipid metabolism, tx gastric ulcer and sickle cell anemia |
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Term
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Definition
| hormone made naturally by kidney; stimulates BFU and CFU on committed erythrocyte progenitor cells, must monitor pts Hct and supplement iron, tx perioperative sx (↓ tranfusion needs), chemotherapy, chronic inflammatory dz, renal failure |
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Term
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Definition
| r-erythropoietin; stimulates BFU and CFU on committed erythrocyte progenitor cells, must monitor pts Hct and supplement iron, tx perioperative sx (↓ tranfusion needs), chemotherapy, chronic inflammatory dz, renal failure |
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Term
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Definition
| r-erythropoietin; stimulates BFU and CFU on committed erythrocyte progenitor cells, must monitor pts Hct and supplement iron, tx perioperative sx (↓ tranfusion needs), chemotherapy, chronic inflammatory dz, renal failure |
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Term
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Definition
| r-granulocyte colony stimulating factor (G-CSF); tx severe neutropenia following chemotherapy/BMT, bone pain and flu-like symptoms @ high doses, requires frequent monitoring for granulocyte counts |
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Term
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Definition
| r-granulocyte colony stimulating factor (G-CSF); tx severe neutropenia following chemotherapy/BMT, bone pain and flu-like symptoms @ high doses, longer t1/2 |
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Term
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Definition
| recombinant IL-11; tx thrombocytopenia, stimulates myeloid and lymphoid proliferation also |
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Term
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Definition
| iron supplementation; tx of choice for iron-deficient anemia in children, pregnant women, and women w/ heavy menstruation, side effects- heartburn, gastric discomfort, poisoning, monitor Hct and Hgb to determine efficacy |
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Term
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Definition
| Vit B12 supplement; tx of megaloblastic anemia to prevent irreversible neurotoxicity |
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Term
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Definition
| tx of megaloblastic anemia and to prevent NTDs; tx during pregnancy and breastfeeding period |
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Term
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Definition
| GABAB agonist; works at multiple spinal cord levels by ↑ inhibitory signaling and hyperpolarizing neurons, tx of MS, spasms, and cord trauma, avoid in renal impairment, abrupt d/c → “rebound phenomenon”, raises blood glucose levels |
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Term
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Definition
| ryanodine receptor blocker; prevents Ca2+ release from SR in skeletal muscle cells, tx of malignant hyperthermia and neuroleptic malignant syndrome (antipsychotics), side effects - thrombophlebitis @ injection site, interaction w/ concourrent estrogen therapy, CV collapse w/ CCB’s |
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Term
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Definition
| α2 agonist; can produce hypotension/tachycardia with concurrent centreally-acting α2 agonists (clonidine, guanfacine, guanabenz, etc), tx. Spasticity |
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Term
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Definition
| central CNS action in RAS and spinal cord, NO direct effect on nerve conduction, extensive hepatic metabolism - interactions w/ inducers and inhibitors |
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Term
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Definition
| blocks neuronal transmission via Ca2+ channels, tx muscle spasms, neuralgia, and seizures |
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Term
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Definition
| binds α-2- subunit of neuronal Ca2+ channels, reduces neuronal transmission, tx of seizures and fibromyalgia (only one approved), side effects- hand swelling, wt gain |
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Term
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Definition
| irreversible COX inhibitor; ↓ TXA2 synthesis in platelets and PGI2 in endothelial cells, active for lifetime of platelets (4-7 days), side effects- GI bleeding, asthma, tx. MI prophylaxis, contraindicated w/ coumarin derivatives, PUD, and asthmatics |
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Term
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Definition
| reversible COX inhibitor; little antiplatelet effect and may disrupt effect of aspirin, liver toxicity (esp. w/ EtOH), DOC for fever in children |
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Term
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Definition
| PDE inhibitor in platelets; ↑ platelet cAMP levels – inactivating, also blocks adenosine uptake, weak antiplatelet effect when used alone, benefit w/ aspirin in cerebrovascular dz, ↓ TE events in prosthetic valves w/ warfarin |
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Term
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Definition
| ADP receptor blocker on platelet membranes; prevents ADP-mediated chemotaxis and activation of Gp IIb/IIIa receptors, tx stroke, MI, post-angioplasty, aspirin + clopidogrel NOT recommended for stable CHD, risk of post-op bleeding |
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Term
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Definition
| synthetic Gp IIb/IIIa receptor antagonist; blocks fibrinogen and vWF binding to platelet membranes, blocks aggregation, given IV prior to heart cath and angioplasty to prevent in-stent clot |
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Term
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Definition
| mAB fragment against Gp IIb/IIIa receptor on platelets, given IV prior to heart cath and angioplasty to prevent in-stent clot |
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Term
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Definition
| thrombolytic; isolated from hemolytic strep, converts plasminogen to plasmin which dissolves clots, risk of intracranial bleeding, highly immunogenic (exp post-strep infection), one time use only |
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Term
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Definition
| synthetic version of protease secreted by endothelial cells, localizes plasminogen activation to clot, tx acute MI, acute ischemic stroke (<3 hrs), and PE |
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Term
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Definition
| anticoagulant; binds to Antithrombin III and ↑ affinity for clotting factor inactivation (IX-XII, thrombin), given IV for rapid effect, variable effects and t1/2 – requires constant monitoring, Heparin-induced thrombocytopenia (heparin-platelet factor 4 antibody induced), LMW heparins given SQ w/ longer t1/2 and more stable effects |
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Term
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Definition
| direct thrombin inhibitor; inhibits thrombin mediated activation of clotting factors, action against free and clot-bound thrombin, used in pts with HIT from heparin |
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Term
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Definition
| recombinant form of hirudin |
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Term
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Definition
| vitamin K antagonist; inhibits Vit K epoxide reductase in liver preventing carboxylation of clotting factors II, VII, IX, and X, delayed onset (46-72 hrs) – give heparin, prolonged t1/2, procoagulant state early due to PC and PS inactivation, monitor PT/INR biweekly, highly protein bound – drug interactions, tx DVT/PE, AFib, RHD, and prosthetic valve prophylaxis |
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Term
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Definition
| H2 antagonist; acid blocker, ↑ gastric pH prevents absorption of weak acids, no CYP interactions (cimetidine) |
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Term
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Definition
| proton pump inhibitor; ↑ gastric pH prevents absorption of weak acids |
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Term
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Definition
| opioid agonist; antidiarrheal agent, contraindicated in infectious diarrhea (stasis = worsening), paralytic ileus |
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Term
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Definition
| 1st generation antihistamine; very sedating, side effects- anticholinergic, avoid in closed-angle glaucoma, also used as a sleep aid |
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Term
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Definition
| antitussive; blocks cough reflex center in brainstem, non-narcotic with high abuse potential → hallucinations/depersonalization (~PCP) |
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Term
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Definition
| expectorant; ↑amount but ↓ viscosity of nasal/airway secretions, breaks up phlegm, also used in cough syrups to prevent dextromethorphan abuse (N/V) |
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Term
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Definition
| decongestant; used topically to vasoconstrict vessels in nasal cavity; potential hypertensive effect if systemic exposure (α and β agonist) |
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Term
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Definition
| weight loss aid; prevents fat absorption from small bowel; massive steatorrhea and potential hepatotoxicity |
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