Master drugs Flashcards
Epoprostenol
Class: PGI2MOA: relax smooth muscle Use: pulmonary HTNAdverse Effects: GI upset
Methazolamide
Class: carbonic anhydrase inhibitorsMOA: inhibit CA preventing breakdown of carbonic acid and absorption of bicarbonate –> osmotic diuresisUse: promotes urinary alkalinization and prevents acute altitude sicknessPK/PD: admin oral or topical. decreases NH4 secretion*contraindicated in hepatic cirrhosis (b/c alkaline urine traps NH4 as ammonia –> reabsorbed –> hepatic encephalopathy)Adverse Effects: Type II RTA
Mecamylamine
Class: Nicotinic Antagonists - Tertiary Ganglion BlockersMOA: competitive blockage of autonomic nicotinic receptors –> decrease in arteriolar and vasomotor tone.PK/PD: can distribute to CNS
Sorbitol
Class: non-digestible sugars/alcoholsMOA: water retentionUse: acidify lumen, drawing water inPK/PD: contraindicated in CHF, pulmonary edema (because these will expand ECF by drawing fluid out of tissue)Adverse Effects: dehydration, hypernatremia, metabolic acidosis
Glycopyrolate
Class: Muscarinic Antagonists - Quaternary AminesUse: pre-operative, hyperhidrosis*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
Dimenhydrinate
Class: H1 antagonists - first generationMOA: anti-cholinergic. blocks Na channel (anesthesia)Use: allergic rhinitis or urticaria, motion sickness, local anesthesia, nausea, vomiting, insomnia PK/PD: well-absorbed, inhibit CYP450, cross BBBAdverse Effects: sedation (anti-cholinergic), urinary retention (anti-muscarinic)*cyclizine, meclizine have least sedative effect
Terbutaline
Class: Direct Adrenoceptor Agonists - β2 selectiveMOA: increase cAMP –> bronchodilation and smooth muscle relaxationUse: asthma, status asthmaticus, and uterine relaxation in premature laborAdverse effects: tremors
Procainamide
Class: Class 1A anti-arrhythmeticsMOA: moderate Na channel block –> elevating depolarization threshold, decreasing phase 4 for depolarization. Block K channel –> prolonging AP duration. Ganglion blockage –> increase AV node conductionUse: atrial and ventricular arrhythmia, post-MI arrhythmia , wide-complex tachycardiaPK/PD: oral and IV admin, short half life, hepatic metabolism, renal excretion, contraindicated in chronic arthritisAdverse Effects: Cardiotoxic (Torsades de Pointes), lupus-like syndrome*does not elevate digoxin levels
Hydrocortisone
Class: Glucocorticoids - short actingUse: adrenal insufficiency, asthmaPK/PD: admin oral aerosol, or topical. inactivated by placenta –> use to treat motherContraindications: gastric ulcer, anaphylaxis, CML, endotoxic shock, sclerodermaAdverse Effects: abdominal striae, osteoporosis, hyperglycemia, moon facies, typical glucocorticoid effects*sudden withdrawal –> adrenal insufficiency. This is due to suppression of endogenous HPA axis
Echothiophate
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleDistributes to CNSPralidoxime (2-PAM) treats poisoning
Diazoxide
Class: direct vasodilatorsMOA: K channel activation –> hyperpolarization. Arterial dilationUse: HTN Admin IVAdverse Effects: reflex tachycardia, fluid retention, HA, palpitation
Fosaprepitant
Class: Neurokinin-1 receptor antagonistUse: chemo-induced emesis
Norethynodrel
Class: ProgestinsMOA: proliferation of mammary acini. thermogenic. moderately anabolic. growth of endometrium. progestational (esp. norgestrel). estrogenic activity (esp. norethynodrel, ethynodiol diacetate). anti-estrogenic activity. androgenic activity (exc. norgestrel, desogestrel)Use: Oral contraception (combo or alone [not at effective])PK/PD: high first pass metabolism. admin oral (norethindrone, norgesterel), implant (norgesterel), IM (medroxy)Adverse Effects: Increase appetite, fatigue
Cabergoline
Class: dopamine agonistMOA: D2 agonistUse: Parkinsonism, hyperprolactinemia, prolactinomaAdverse Effects: NandV, orthostatic hypotension, fluctuation in efficacy of motor control, abnormal involuntary movements, arrhythmia, hypersexuality, hallucinations, paranoia, anxiety, mania, depression
Phenylephrine
Class: Direct Adrenoceptor Agonists - α1 selectiveUse: mydriasis (eye exams) and nasal decongestion
Valsartan
Class: ARBsMOA: selectively inhibit AT1 receptors –> vasodilationUse: HTNPK/PD: more effective at blocking angiotensin than ACE inhibitors b/c more specific*no effect on bradykinin, thus no cough or edema
Torsemide
Class: Loop diureticsMOA: inhibit NKCC –> decreased Na/Cl/K reabsorption –> osmotic diuresis. Change in potential –> Mg and Ca excretionUse: Pulmonary edema, CHF, HTN, acute hypercalcemia, hyperkalemnia, acute renal failurePK/PD: admin oral, IV, or IM. rapidly absorbed. Elimination = tubular secretion and absorptionAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, ototoxicity, dehydration, hyonatremia, metabolic alkalosis (contraction alkalosis)*hypomagnesemia –> increased PG production and renal blood flow aiding anti-hypertensive effect*Effective when GFR is low*more effective diuretic than thiazide*use ethacrynic acid of pt has sulfa allergy
Soman
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleUse: war gasDistributes to CNSPralidoxime (2-PAM) treats poisoning
Ethinyl Estradiol
Class: EstrogensMOA: growth/development of vagina, uterus, uterine tubes. breast enlargement. pubic/axillary hair. pigmentation of areola and genitalia. mildly anabolic. inhibits PTH-induced bone resorptionUse: primary hypogonadism. postmenopausal HRT. oral contraception. osteoporosis prophylaxisPK/PD: contraindicated in breast/endometrial cancer, liver disease, thromboembolic diseases, smoking, pregnancyAdverse Effects: increased risk of breast/endometrial cancer. nausea, bloating, HTN
Quinidine
Class: Class 1A anti-arrhythmeticsMOA: moderate Na channel block –> elevating depolarization threshold, decreasing phase 4 for depolarization. Block K channel –> prolonging AP duration. Ganglion blockage –> increase AV node conductionUse: arrhythmiaPK/PD: contraindicated in CHFAdverse Effects: Cardiotoxic (torsades de pointes), block alpha adrenergic and muscarinic, GI toxicity, cinchonism, thrombocytopenia, wide QRS*elevated digoxin levels
Metoprolol
Class: Beta Adrenoceptor Antagonists - β1 selectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid), inhibit conversion of T3 to T4Use: hyperthyroidismPK/PD: oral, well absorbedAdverse Effects: due to specificity, no pulmonary effects
Progesterone
Class: ProgestinsMOA: proliferation of mammary acini. thermogenic. moderately anabolic. growth of endometrium. progestational (esp. norgestrel). estrogenic activity (esp. norethynodrel, ethynodiol diacetate). anti-estrogenic activity. androgenic activity (exc. norgestrel, desogestrel)Use: Oral contraception (combo or alone [not at effective])PK/PD: high first pass metabolism. admin oral (norethindrone, norgesterel), implant (norgesterel), IM (medroxy)Adverse Effects: Increase appetite, fatigue
Sarin
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleUse: war gasDistributes to CNSPralidoxime (2-PAM) treats poisoning
Cabergoline
Class: Dopamine receptor agonistsUse: GH excess, tumors secreting GH and PRL
Budesonide
Class: GlucocorticoidsMOA: inhibits cytokines –> decrease airway reactivity –> bronchodilation, decrease edema. Increase lipocortin, which inhibits PLA2Use: Asthma and RAPK/PD: admin oral, IV, or aerosolAdverse Effects: Typical steroid effects (especially w/ oral admin), oral candidiasis, and hoarseness
Dibasic Calcium Phosphate
Use: hypocalcemia and osteoporosis prophylaxis
Diltiazem
Class: Ca channel blockers - non-dihydropyridinesMOA: block L-type Ca channel –> reduced SA/AV conductionUse: Angina prophylaxis, mild/moderate HTN (esp. in AA and elderly), tocolysis, class IV anti-arrhythmic Contraindicated in CHFAdverse Effects: cardiac arrest, AV block, constipation, CHF*blocks binding site 1B, mostly in myocardium NO REFLEX TACHYCARDIA
Muscarine
Class: Direct Muscarinic Agonists - AlkaloidsMOA: Contracts iris sphincter, increases aqueous humor drainageUse: Acute glaucoma
Nesiritide
Class: BNP analogMOA: increases cGMP –> arteriolar and venous dilation –> reduced afterload and preload. Causes natuiresisUse: actue tx of HF
Aspart
Class: Rapid acting insulinUse: DM I
Calcitriol
MOA: 1, 25 dihydroxy vitamin DUse: nutritional rickets, metabolic rickets, hypoparathyroidism, osteoporosis
Estriol
Class: EstrogensMOA: growth/development of vagina, uterus, uterine tubes. breast enlargement. pubic/axillary hair. pigmentation of areola and genitalia. mildly anabolic. inhibits PTH-induced bone resorptionUse: primary hypogonadism. postmenopausal HRT. oral contraception. osteoporosis prophylaxisPK/PD: contraindicated in breast/endometrial cancer, liver disease, thromboembolic diseases, smoking, pregnancyAdverse Effects: increased risk of breast/endometrial cancer. nausea, bloating, HTN
Desogestrel
Class: ProgestinsMOA: proliferation of mammary acini. thermogenic. moderately anabolic. growth of endometrium. progestational (esp. norgestrel). estrogenic activity (esp. norethynodrel, ethynodiol diacetate). anti-estrogenic activity. androgenic activity (exc. norgestrel, desogestrel)Use: Oral contraception (combo or alone [not at effective])PK/PD: high first pass metabolism. admin oral (norethindrone, norgesterel), implant (norgesterel), IM (medroxy)Adverse Effects: Increase appetite, fatigue
Eprosartan
Class: ARBsMOA: selectively inhibit AT1 receptors –> vasodilationUse: HTNPK/PD: more effective at blocking angiotensin than ACE inhibitors b/c more specific*no effect on bradykinin, thus no cough or edema
Quinethazone
Class: Thiazide-like diureticsMOA: inhibit Na/Cl in DCT –> decreased Na/Cl reabsorption –> osmotic diuresis. Increased Ca reapsorptionUse: HTN (especially in AA and elderly), mild CHF, nephrolithiasis, nephrogenic DIPK/PD: oral admin, decrease Ca excretion, secretion = same as uric acid, anti-HTN as low doses, diuresis at high dosesAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, hyperlipidemia, contraction alkalosis*ineffective when GFR is low*more effective for HTN than loop diuretics
Sitagliptin
MOA: inhibits DDP4 –> preventing incretin degradationUse: DM II (combo w/ other tx)
Amyl Nitrate
Class: Nitrates - short actingMOA: sitmulates NO production –> stimulates guanylyl cyclase –> increase cGMP –> decrease phosphorylation of myosin light chain –> vasodilation –> decreased preloadUse: acute anginaAdmin: inhaled or sublingualAdverse Effects: Reflex tachycardia and inotropy (increased O2 demand and reduced perfusion), headacheContraindications: HOCM and patients taking PDE inhibitors (“-fil” ex. sildenafil)*chronic use leads to tolerance (must have nitrate free intervals*toxicity = hypotension, headache, dizziness*veins dilated more than arteries*preferentially dilates epicardial arteries, which is where most ischemia occurs
MDMA
Class: Indirect SympathomimeticsAdverse Effects: Insomnia, anorexia, weight loss
Tolvaptan
Class: Vasopressin receptor antagonistMOA: decrease aquaporins –> water retention in collecting tubuleUse: SIADH, CHF, hyponatremia*admin oralAdverse Effects: Hypernatremia, nephrogenic DI
Prenalterol
Class: Direct Adrenoceptor Agonists - β1 selectiveMOA: increase heart rate*partial agonist
Fludrocortisone
Class: mineralocorticoidMOA: mineralocorticoid actionUse: salt-losing syndrome
Vytorin
Ezetimibe + simvastatin
Anastrazole
Class: Atomatase inhibitorsMOA: Inhibit aromatase –> reduce estrogen synthesisUse: tamoxifen resistant breast cancerPK/PD: non-steroidal and reversible (except exemestane)
Mannitol
Class: osmotic diuretic
Ramipril
Class: ACE inhibitors*pro-drugMOA: prevents formation of angiotensin II, decreases aldosterone, increases bradykinin, cumulatively, these have the effect of decreasing afterload and preloadUse: HTN, CHF, diabetic neuropathyAdverse Effects: dry, hacking cough (due to bradykinin), hyperkalemia
Salicylic Acid
Class: NSAID - salicylatesMOA: inhibits COX enzymes, inhibits renal secretion of uric acid (low dose), inhibits renal reabsorption of uric acid (high dose)Use: analgesic, anti-pyretic, anti-inflammatory (high dose only), inhibit platelet aggregationPK/PD: aspirin (irreversible) is metabolized to salicylic acid (reversible), highly bound to plasma protein (may kick other drugs off), contraindicated in hemophilia, children with viral infections, severe CV diseaseAdverse Effects: same as other NSAIDs, hypersensitivity (due to overutilization of LOX pathway)toxicity: salicycism, hyperthermia, hyperpnea, respiratory alkalosis* treat toxicity with gastric lavage and supportive care.* NSAIDS inhibit renal prostaglandins PGE2 and PGI2, resulting in vasoconstriction and exacerbation of CV disease
Senna
Class: AnthraquinonesMOA: stimulant laxativesUse: constipation
Hydroxyzysine
Class: H1 antagonists - first generationMOA: anti-cholinergic. blocks Na channel (anesthesia)Use: allergic rhinitis or urticaria, motion sickness, local anesthesia, nausea, vomiting, insomnia PK/PD: well-absorbed, inhibit CYP450, cross BBBAdverse Effects: sedation (anti-cholinergic), urinary retention (anti-muscarinic)*cyclizine, meclizine have least sedative effect
Yohimbine
Class: Alpha Adrenoceptor Antagonists - α2 selectiveUse: nothing (purported to treat ED)Adverse Effects: orthostatic hypotension and reflex tachycardia
Sermorelin Acetate
MOA: recombinant GHUse: GH deficiency (ex. growth failure in children, wasting in HIV pts, short bowel syndrome)PK/PD: induce microsomal enzymes, contraindicated in malignancyAdverse Effects: Primarily in adults, peripheral edema, myalgias, arthralgias, carpal tunnel
Oxaprozin
Class: NSAIDMOA: block PGE2 in CNS –> resets temp control –> anti-pyretic Use: analgesic, anti-pyretic, anti-inflammatory (high dose only), inhibit platelet aggregation, gout (indo), ankylosing spondylitis (indo), OA (indo), patent ductus arteriosus (indo)PK/PD: admin oral or parenteral (ketorolac). COX-1 inhibition –> no thromboxane –> anti-platelet activityover-activation of LOX pathway –> hypersensitivityAdverse Effects: GI (esp. ulcers), hepatotoxicity, nephrotoxicity, prolonged bleeding time, hypersensitivity, hematologic toxicity (indo), sore throat (indo)*when used chronically, give misoprostol or PPI to prevent ulcers
Terazosin
Class: Alpha Adrenoceptor Antagonists - α1 selectiveUse: hypertension and PTSDPK/PD: long half lifeAdverse Effects: orthostatic hypotension (lowest risk with tamsulosin), reflex tachycardia
Carboprost
Class: PGF2MOA: relax smooth muscleUse: post-partum hemorrhage Adverse Effects: GI upset
(Methyl)ergonovine
Class: 5-HT agonists - nonselective - ergot alkaloidsMOA: agonists or partial agonists at various receptors, vasoconstrictionUse: migraine (ergotamine or dihydroergotamine), post-partum hemorrhage (ergonovine, if oxytocin fails)PK/PD: caffeine – increases absorption, contraindicated in coronary artery diseaseAdverse Effects: GI upset (most common), prolonged vasospasm (most serious)*for hemorrhage, only use after placenta is delivered
Tolterodine
Class: Muscarinic Antagonists - Tertiary AminesMOA: decrease Ach –> inhibits bronchoconstriction and mucus secretionUse: used to relieve bladder spasm after urologic surgery*M3 selective*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
Omalizumab
Class: Anti-IgE AbMOA: inhibits IgE binding to mast cells –> decrease mast cell activation –> bronchodilationUse: asthma
Amiodarone
Class: Class 3 anti-arrhythmeticsMOA: blocks K channel, prolonging AP, blocking inactivated Na channels, decreasing pacemaker potential, block beta adrenergic and Ca receptorsUse: life threatening ventricular arrhythmia (first choice), supraventricular arrhythmia, wide-complex tachycardiaPK/PD: admin oral and IV, metabolized by CYP450 (3A4), inhibits microsomal enzymes, contraindicated in lung diseaseAdverse Effects: torsades, bradycardia, pulmonary fibrosis, blue/grey color of skin and cornea, respiratory difficulty, neurotoxicity, thyroid dysfunction
Nateglinide
Class: D-phenylalanine derivative (like sulfonylureas)MOA: bind SUR1Use: DM IIPK/PD: rapid onset and short durationAdverse Effects: hypoglycemia*Use if pt has sulfa allergy
Doserelin
Class: GnRH analoguesMOA: chronic use desensitizes GnRH receptor –> suppresses gonadotropin releaseUse: controlled ovarian hyperstimulation, endometriosis, uterine fibroids, prostate cancer, central precocious puberty*initially these stimulate gonadotropin release
Testosterone Enanthate
Class: Androgens*more androgenicUse: Hypogonadism and anemiaAdverse Effects: feminizing effects in post-pubertal males (due to conversion to estrogen)
Nitroglycerin
Class: Nitrates - short actingMOA: sitmulates NO production –> stimulates guanylyl cyclase –> increase cGMP –> decrease phosphorylation of myosin light chain –> vasodilation –> decreased preloadUse: acute angina Admin: inhaled or sublingualAdverse Effects: Reflex tachycardia and inotropy (increased O2 demand and reduced perfusion), headacheContraindications: HOCM and patients taking PDE inhibitors (“-fil” ex. sildenafil)*chronic use leads to tolerance (must have nitrate free intervals*toxicity = hypotension, headache, dizziness*veins dilated more than arteries*preferentially dilates epicardial arteries, which is where most ischemia occurs
Hyoscyamine
Class: anticholinergicsMOA: anti-spasmodic activityUse: IBS
Ergotamine
Class: 5-HT agonists - nonselective - ergot alkaloidsMOA: agonists or partial agonists at various receptors, vasoconstrictionUse: migraine (ergotamine or dihydroergotamine), post-partum hemorrhage (ergonovine, if oxytocin fails)PK/PD: caffeine – increases absorption, contraindicated in coronary artery diseaseAdverse Effects: GI upset (most common), prolonged vasospasm (most serious)*for hemorrhage, only use after placenta is delivered
Mometasone
Class: GlucocorticoidsMOA: inhibits cytokines –> decrease airway reactivity –> bronchodilation, decrease edema. Increase lipocortin, which inhibits PLA2Use: Asthma and RAPK/PD: admin oral or IVAdverse Effects: Typical steroid effects (especially w/ oral admin)
Dolasetron
Class: 5-HT3 antagonists Use: chemo-induced vomiting
Omeprazole
Class: proton pump inhibitorsMOA: irreversibly bind H/K-ATPase of parietal cell –> reduced acid secretionUse: peptic ulcer (treatment and prevention), GERD, h. pylori (+ clarithromycin + amoxicillin)PK/PD: activated/degraded in acidic environment: coated to survive stomach –> absorbed in intestine –> enter circulation –> activated in parietal cell canaliculiAdverse Effects: GI upset, rash, CNS effects, diarrhea (chronic use only: low acidity allows bacterial overgrowth)
Latanoprost
Class: PGF2MOA: relax smooth muscleUse: open angle glaucomaAdverse Effects: GI upset
Cimetidine
Class: H2 antagonistsMOA: inhibit gastric acid secretion (esp. nocturnal secretion)Use: peptic ulcer and h. pylori (+ bismuth + antibiotics)PK/PD: doesn’t impact normal intestinal secretions, contraindicated in pregnant and nursing women. metabolized by CYP450Adverse Effects: GI upset, endocrine effects (cimetidine): gynecomastia, galactorrhea, muscle pain, inhibits microsomal enzymes*nocturnal acid secretion is primarily driven by histamine
Prednisone
Class: Glucocorticoids - short actingUse: adrenal insufficiency, asthmaPK/PD: admin oral aerosol, or topical. inactivated by placenta –> use to treat motherContraindications: gastric ulcer, anaphylaxis, CML, endotoxic shock, sclerodermaAdverse Effects: abdominal striae, osteoporosis, hyperglycemia, moon facies, typical glucocorticoid effects*sudden withdrawal –> adrenal insufficiency. This is due to suppression of endogenous HPA axis
Metformin
Class: biguanidesMOA: activates AMPK –> reduced hepatic gluconeogenesis. Increase peripheral insulin sensitivityUse: DM II (first choice), reduce triglyceridesPK/PD: admin oral, not metabolized, renal excretionAdverse Effects: GI toxicity (anorexia, diarrhea, nausea, vomiting), lactic acidosis (due to impaired hepatic metabolism of lactic acid)
Trimethaphan
Class: Nicotinic Antagonists - Quaternary Ganglion BlockersMOA: competitive blockage of autonomic nicotinic receptors –> decrease in arteriolar and vasomotor tone.
Clemastine
Class: H1 antagonists - first generationMOA: anti-cholinergic. blocks Na channel (anesthesia)Use: allergic rhinitis or urticaria, motion sickness, local anesthesia, nausea, vomiting, insomnia PK/PD: well-absorbed, inhibit CYP450, cross BBBAdverse Effects: sedation (anti-cholinergic), urinary retention (anti-muscarinic)*cyclizine, meclizine have least sedative effect
Timolol
Class: Beta Adrenoceptor Antagonists - nonselectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid)Use: open angle glaucoma, HTN, ischemia, angina prophylaxis, migraine prevention (first choice)PK/PD: oral. well absorbed. Adverse Effects: asthma exacerbation, supersensitivity (with chronic use and abrupt discontinuation), delayed recovery of normoglycemia*toxicity = rash and sedation
Alosetron
Class: 5-HT3 antagonists Use: chemo-induced vomiting and IBS w/ diarrhea predominance
Nafarelin
Class: GnRH analoguesMOA: chronic use desensitizes GnRH receptor –> suppresses gonadotropin releaseUse: controlled ovarian hyperstimulation, endometriosis, uterine fibroids, prostate cancer, central precocious puberty*initially these stimulate gonadotropin release
Indomethacin
Class: NSAIDMOA: block PGE2 in CNS –> resets temp control –> anti-pyretic Use: analgesic, anti-pyretic, anti-inflammatory (high dose only), inhibit platelet aggregation, gout (indo), ankylosing spondylitis (indo), OA (indo), patent ductus arteriosus (indo)PK/PD: admin oral or parenteral (ketorolac). COX-1 inhibition –> no thromboxane –> anti-platelet activityover-activation of LOX pathway –> hypersensitivityAdverse Effects: GI (esp. ulcers), hepatotoxicity, nephrotoxicity, prolonged bleeding time, hypersensitivity, hematologic toxicity (indo), sore throat (indo)*when used chronically, give misoprostol or PPI to prevent ulcers
Glulisine
Class: Rapid acting insulinUse: DM I
Mg Citrate
Class: saline laxativesMOA: non-absorbable salt –> increase osmotic activity in lumenUse: constipationContraindications: renal insufficiency, heart disease, diuretic treatment
Betaxolol
Class: Beta Adrenoceptor Antagonists - β1 selectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid), inhibit conversion of T3 to T4Use: hyperthyroidismPK/PD: oral, well absorbed Adverse Effects: due to specificity, no pulmonary effects
Bicalutamide
Class: anti-androgens MOA: competitively inhibit androgen receptorUse: metastatic prostate cancer (in combo w/ GnRH agonist)*combo tx = maximal androgen blockade (desensitizes pituitary + prevents nadrogen binding)
Dinopristone
Class: PGE2MOA: induce cervical ripeningUse: induce labor and NSAID induced ulcerAdverse Effects: GI upset
Zoledronate
Class: bisphophonatesMOA: pyrophosphate analogs –> inhibit osteoclasts, thereby inhibiting bone resorptionUse: hypercalcemia (in malignancy), osteoporosis, ectopic calcification, Paget’s diseasePK/PD: poorly absorbedAdverse Effects: gastric/esophageal irritation, osteonecrosis of the jaw –> fractures*bone remodeling occurs in jaw more than other bones, which requires osteoclast activity
Ketoconazole
MOA: inhibits CYP17, preventing steroidogenesisUse: Cushing’sAdverse Effects: hepatic dysfunction
Glargine
Class: long acting insulinUse: DM I (used to maintain basal insulin levels)
Mestranol
Class: EstrogensMOA: growth/development of vagina, uterus, uterine tubes. breast enlargement. pubic/axillary hair. pigmentation of areola and genitalia. mildly anabolic. inhibits PTH-induced bone resorptionUse: primary hypogonadism. postmenopausal HRT. oral contraception. osteoporosis prophylaxisPK/PD: contraindicated in breast/endometrial cancer, liver disease, thromboembolic diseases, smoking, pregnancyAdverse Effects: increased risk of breast/endometrial cancer. nausea, bloating, HTN
Methyldopa
Class: Direct Adrenoceptor Agonists - α2 selectiveMOA: increase reuptake of catecholamines –> decreased sympathetic stimulationUse: hypertensionAdverse effects: hypertensive crisis with abrupt withdrawal, autohemolytic anemia, drug induced lupus*preferred in pregnancy *can uncouple autoantigens on RBCs
Chlorthaladone
Class: Thiazide-like diureticsMOA: inhibit Na/Cl in DCT –> decreased Na/Cl reabsorption –> osmotic diuresis. Increased Ca reapsorptionUse: HTN (especially in AA and elderly), mild CHF, nephrolithiasis, nephrogenic DIPK/PD: oral admin, decrease Ca excretion, secretion = same as uric acid, anti-HTN as low doses, diuresis at high dosesAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, hyperlipidemia, contraction alkalosis*ineffective when GFR is low*more effective for HTN than loop diuretics
Olmesartan
Class: ARBsMOA: selectively inhibit AT1 receptors –> vasodilationUse: HTNPK/PD: more effective at blocking angiotensin than ACE inhibitors b/c more specific*no effect on bradykinin, thus no cough or edema
Ethacrynic Acid
Class: Loop diureticsMOA: inhibit NKCC –> decreased Na/Cl/K reabsorption –> osmotic diuresis. Change in potential –> Mg and Ca excretionUse: Pulmonary edema, CHF, HTN, acute hypercalcemia, hyperkalemnia, acute renal failurePK/PD: admin oral, IV, or IM. rapidly absorbed. Elimination = tubular secretion and absorptionAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, ototoxicity, dehydration, hyonatremia, metabolic alkalosis (contraction alkalosis)*hypomagnesemia –> increased PG production and renal blood flow aiding anti-hypertensive effect*Effective when GFR is low*more effective diuretic than thiazide*use ethacrynic acid of pt has sulfa allergy
Almotriptan
Class: 5-HT agonists - selective - 5-HT1B/1DMOA: counteract CGRP –> cerebral vasoconstrictionUse: acute migraines (better choice than ergots)PK/PD: contraindicated in CADAdverse Effects: tingling, warm sensation, may mimic angina
Fadrazole
Class: Atomatase inhibitorsMOA: Inhibit aromatase –> reduce estrogen synthesisUse: tamoxifen resistant breast cancerPK/PD: non-steroidal and reversible (except exemestane)
Atorvastatin
Class: HMG-CoA reductase inhibitorsMOA: reduce hepatic formation of cholesterol. Increase LDL receptors on hepatocytes –> lower plasma LDLUse: lower plasma LDLPK/PD: good GI absorption, hepatic metabolism by CYPs, high first pass metabolism, bile excretion, contraindicated in pregnancy, admin at night when most cholesterol synthesis occursAdverse Effects: hepatotoxicity, rhabdomyolysis (increase CK)*reduces mortality from CVD and MI
Fulvestrant
Class: ER antagonist MOA: pure ER antagonistUse: breast cancer (if SERM and aromatase inhibitor tx fails)
Simcor
Niacin + simvastatin
Piroxicam
Class: NSAIDMOA: block PGE2 in CNS –> resets temp control –> anti-pyretic Use: analgesic, anti-pyretic, anti-inflammatory (high dose only), inhibit platelet aggregation, gout (indo), ankylosing spondylitis (indo), OA (indo), patent ductus arteriosus (indo)PK/PD: admin oral or parenteral (ketorolac). COX-1 inhibition –> no thromboxane –> anti-platelet activityover-activation of LOX pathway –> hypersensitivityAdverse Effects: GI (esp. ulcers), hepatotoxicity, nephrotoxicity, prolonged bleeding time, hypersensitivity, hematologic toxicity (indo), sore throat (indo)*when used chronically, give misoprostol or PPI to prevent ulcers
Ezetimibe
Class: Cholesterol absorption inhibitorMOA: inhibits intestinal absorption of cholesterol and phylosterolsUse: lower plasma LDL, primary hypercholesterolemiaAdverse Effects: steatorrhea, hepatotoxicity
Flutamide
Class: anti-androgens MOA: competitively inhibit androgen receptorUse: metastatic prostate cancer (in combo w/ GnRH agonist)*combo tx = maximal androgen blockade (desensitizes pituitary + prevents nadrogen binding)
Pramlintide
Class: amylin analogMOA: amylin analog –> increased gastric emptying time, decreased glucagon secretion, reduce appetiteUse: DM I and II (especially in obese pts.)PK/PD: admin IM, renal metabolism and excretionAdverse Effects: hypoglycemia
Nadolol
Class: Beta Adrenoceptor Antagonists - nonselectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid)Use: open angle glaucoma, HTN, ischemia, angina prophylaxis, migraine prevention (first choice) PK/PD: oral. well absorbed.Adverse Effects: asthma exacerbation, supersensitivity (with chronic use and abrupt discontinuation), delayed recovery of normoglycemia*toxicity = rash and sedation
Naratriptan
Class: 5-HT agonists - selective - 5-HT1B/1DMOA: counteract CGRP –> cerebral vasoconstrictionUse: acute migraines (better choice than ergots)PK/PD: contraindicated in CADAdverse Effects: tingling, warm sensation, may mimic angina
Donepezil
Class: Cholinesterase InhibitorsUse: Dementia and Alzheimer’sAdverse Effects: Muscle cramps, GI upset
Bosentan
Class: Endothelin receptor antagonistMOA: arterial dilationUse: pulmonary HTNAdverse Effects: hypotension, hepatotoxicity, tachycardia, flushing
Clonidine
Class: Direct Adrenoceptor Agonists - α2 selectiveMOA: increase reuptake of catecholamines –> decreased sympathetic stimulationUse: hypertensionAdverse Effects: hypertensive crisis with abrupt withdrawal and dry mouth
Misoprostol
Class: PGE1MOA: relax smooth muscle, bind prostaglandin receptors on gastric epitheliumUse: Abortion, NSAID-induced ulcerPK/PD: admin injection*contraindicated in pregnancyAdverse Effects: GI upset
Estradiol
Class: EstrogensMOA: growth/development of vagina, uterus, uterine tubes. breast enlargement. pubic/axillary hair. pigmentation of areola and genitalia. mildly anabolic. inhibits PTH-induced bone resorptionUse: primary hypogonadism. postmenopausal HRT. oral contraception. osteoporosis prophylaxisPK/PD: contraindicated in breast/endometrial cancer, liver disease, thromboembolic diseases, smoking, pregnancyAdverse Effects: increased risk of breast/endometrial cancer. nausea, bloating, HTN
Montelukast
Class: Leukotriene AntagonistMOA: LTD4 receptor antagonist –> bronchodilationUse: asthmaPK/PD: admin is oral (good for kids)
Phentolamine
Class: Alpha Adrenoceptor Antagonists - nonselectiveMOA: reduces TPR and MAPUse: PheochromocytomaAdverse Effects: Orthostatic hypotension and reflex tachycardia*reversible
Cascara Sagrada
Class: AnthraquinonesMOA: stimulant laxativesUse: constipation
Pravastatin
Class: HMG-CoA reductase inhibitorsMOA: reduce hepatic formation of cholesterol. Increase LDL receptors on hepatocytes –> lower plasma LDLUse: lower plasma LDLPK/PD: good GI absorption, NOT METABOLIZED BY CYPs, high first pass metabolism, bile excretion, contraindicated in pregnancy, admin at night when most cholesterol synthesis occursAdverse Effects: hepatotoxicity, rhabdomyolysis (increase CK)*reduces mortality from CVD and MI
NPH humulin N
Class: intermediate acting insulinUse: DM I
Pseudoephedrine
Class: Indirect SympathomimeticsPK/PD: CNS stimulationAdverse Effects: Insomnia, anorexia, weight loss
Hydralazine
Class: direct vasodilatorsMOA: arterial dilationUse: pre-eclampsia Admin IVAdverse Effects: lupus-like syndrome, reflex tachycardia, fluid retention, HA, palpitation
Reserpine
Class: Adrenergic Neuron AntagonistsMOA: inhibits VMAT –> prevents NE packaging into vesicles. NE is either chewed up by MAO or spills over into synaptic cleft –> eventually, this will lead to depletion of NEUse: HTN*also blocks packaging of serotonin
Dranabinol
MOA: unknown mechanismUse: vomiting
Alprazolam
Class: benzodiazepines Use: vomiting
Telmisartan
Class: ARBsMOA: selectively inhibit AT1 receptors –> vasodilationUse: HTNPK/PD: more effective at blocking angiotensin than ACE inhibitors b/c more specific*no effect on bradykinin, thus no cough or edema
Pindolol
Class: Beta Adrenoceptor Antagonists - nonselectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid)Use: HTN, ischemia, angina prophylaxis, migraine prevention (first choice)PK/PD: oral. well absorbed. Adverse Effects: asthma exacerbation, supersensitivity (with chronic use and abrupt discontinuation), delayed recovery of normoglycemia*toxicity = rash and sedation*has intrinsic sympathomimetic activity and can protect against asthma, bradycardia, and altered lipid profile
Mexiletine
Class: Class 1B anti-arrhythmeticsMOA: mild Na channel block, shorten AP durationUse: diabetic neuropathy, ventricular arrhythmiaPK/PD: admin oral, resistant to first pass metabolismAdverse Effects: neurotoxicity
Cyproheptadine
Class: 5-HT2 antagonists Use: serotonin syndrome *serotonin syndrome = HTN, hyperreflexia, tremor, clonus, hyperthermia, mydriasis, agitation, coma
Nizatidine
Class: H2 antagonistsMOA: inhibit gastric acid secretion (esp. nocturnal secretion)Use: peptic ulcer and h. pylori (+ bismuth + antibiotics)PK/PD: doesn’t impact normal intestinal secretions, contraindicated in pregnant and nursing women. metabolized by CYP450Adverse Effects: GI upset, endocrine effects (cimetidine): gynecomastia, galactorrhea, muscle pain, inhibits microsomal enzymes*nocturnal acid secretion is primarily driven by histamine
Nifedipine
Class: Ca channel blockers - dihydropyridinesMOA: block L-type Ca channel –> smooth muscle relaxation (esp. arteries). Coronary and systemic vasodilation. Uterine smooth muscle relaxationUse: Prinzemetal’s angina prophylaxis, mild/moderate HTN (esp. in AA and elderly), tocolysisAdverse Effects: reflex tachycardia, peripheral edema*blocks binding site 1A, mostly in vasculature
Desmopressin
Class: Vasopressin agonistMOA: predominantly V2 agonist, anti-diuresis, vasoconstrictionUse: HTN, neurogenic diabetes insipidus*desmopressin is more potent and longer lasting than vasopressin
Potassium Iodide
MOA: thyroglobulin proteolysis and hormone releaseUse: pre-op prepAdverse Effects: depression, insomnia, impotence
Raloxifene
Class: SERMMOA: partial ER agonists –> antagonistic activity in presence of normal hormone levelsUse: ER + breast cancerPK/PD: in premenopausal women, SERM is antagonist in all tissues. in postmenopausal women, SERM is agonist in all except mammary tissueAdverse Effects: in postmenopausal women, increased risk of endometrial cancer*in postmenopausal women, hormone levels remain high in mammary tissue
Disopyramide
Class: Class 1A anti-arrhythmeticsMOA: moderate Na channel block –> elevating depolarization threshold, decreasing phase 4 for depolarization. Block K channel –> prolonging AP duration. Ganglion blockage –> increase AV node conductionUse: ventricular arrhythmiaPK/PD: contraindicated in prostatismAdverse Effects: anti-muscarinic activity, negative inotropic action –> CHF*not really used anymore
Dopamine
Class: CatecholaminesMOA: D1 agonistUse: Shock, heart failure, anaphylaxis, fundoscopic eye exams*Metyrosine inhibits tyrosine hydroxylase, preventing formation of catecholamines*Reserpine inhibits NE uptake into vesicles (VMAT)
Oxybutynin
Class: Muscarinic Antagonists - Tertiary AminesMOA: decrease Ach –> inhibits bronchoconstriction and mucus secretionUse: urinary urgency/frequency*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
Oxymetazoline
Class: Direct Adrenoceptor Agonists - α1 selectiveUse: mydriasis (eye exams) and nasal decongestion*topical administration
Flulnarizine
MOA: Ca channel blockerUse: preventative tx for migraine
Humulin R
Class: short acting insulinUse: DM I and DKAAdmin IV for DKA
Ephedrine
Class: Indirect SympathomimeticsPK/PD: CNS stimulationAdverse Effects: Insomnia, anorexia, weight loss*direct sympathomimetic activity
Histrelin
Class: GnRH analoguesMOA: chronic use desensitizes GnRH receptor –> suppresses gonadotropin releaseUse: controlled ovarian hyperstimulation, endometriosis, uterine fibroids, prostate cancer, central precocious puberty*initially these stimulate gonadotropin release
Homatropine
Class: Muscarinic Antagonists - Tertiary AminesMOA: decrease Ach –> inhibits bronchoconstriction and mucus secretion*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
Enalapril
Class: ACE inhibitors*pro-drugMOA: prevents formation of angiotensin II, decreases aldosterone, increases bradykinin, cumulatively, these have the effect of decreasing afterload and preloadUse: HTN, CHF, diabetic neuropathyAdverse Effects: dry, hacking cough (due to bradykinin), hyperkalemia
Fenofibrate
Class: fibratesMOA: activates PPAR-α –> decreased plasma TG, VLDL, LDL, increases HDLUse: hypertriglyceridemia and dysbetalipoproteinemiaPK/PD: may increase concentration of statinsAdverse Effects: skin rashes, lymphocytopenia, myopathy (increased risk with stain combo), gall bladder disease
Octreotide
Class: Somatostatin analogMOA: inhibits pituitary release of GHUse: GH excess, insulinoma, VIPomaAdverse Effects: GI toxicity, vitamin B12 deficiency
Frovatriptan
Class: 5-HT agonists - selective - 5-HT1B/1DMOA: counteract CGRP –> cerebral vasoconstrictionUse: acute migraines (better choice than ergots)PK/PD: contraindicated in CADAdverse Effects: tingling, warm sensation, may mimic angina
Katanserin
Class: 5-HT2 antagonists *also an alpha 1 antagonistUse: HTN *serotonin syndrome = HTN, hyperreflexia, tremor, clonus, hyperthermia, mydriasis, agitation, coma
Methoxamine
Class: Direct Adrenoceptor Agonists - α1 selectiveUse: mydriasis (eye exams) and nasal decongestion
Nicotine
Class: Direct Nicotinic AgonistsPK/PD: Excess agonist activity results in depolarizing blockade of autonomic ganglia –> flaccid paralysis Distributes to CNS- Tertiary
Exemestane
Class: Atomatase inhibitorsMOA: Inhibit aromatase –> reduce estrogen synthesisUse: tamoxifen resistant breast cancerPK/PD: non-steroidal and reversible (except exemestane)
Xylometazoline
Class: Direct Adrenoceptor Agonists - α1 selectiveUse: mydriasis (eye exams) and nasal decongestion*topical administration
Simvastatin
*prodrugClass: HMG-CoA reductase inhibitorsMOA: reduce hepatic formation of cholesterol. Increase LDL receptors on hepatocytes –> lower plasma LDLUse: lower plasma LDLPK/PD: good GI absorption, hepatic metabolism by CYPs, high first pass metabolism, bile excretion, contraindicated in pregnancy, admin at night when most cholesterol synthesis occursAdverse Effects: hepatotoxicity, rhabdomyolysis (increase CK)*reduces mortality from CVD and MI
Metoclopramide
Class: D2 antagonistsMOA: dopamine receptor antagonistsUse: acute migraine attacks, vomiting (cancer chemo, pot-op)Adverse Effects: extrapyramidal like adverse effects, drowsiness, torsades, neuroleptic malignant syndrome, increased prolactin secretion
Fluprednisolone
Class: Glucocorticoids - intermediate actingUse: adrenal insufficiency, asthmaContraindications: gastric ulcer, anaphylaxis, CML, endotoxic shock, sclerodermaAdverse Effects: abdominal striae, osteoporosis, hyperglycemia, moon facies, typical glucocorticoid effects*sudden withdrawal –> adrenal insufficiency. This is due to suppression of endogenous HPA axis
LSD
Class: 5-HT agonists - nonselective - ergot alkaloidsMOA: agonists or partial agonists at various receptors, vasoconstrictionUse: migraine (ergotamine or dihydroergotamine), post-partum hemorrhage (ergonovine, if oxytocin fails)PK/PD: caffeine – increases absorption, contraindicated in coronary artery diseaseAdverse Effects: GI upset (most common), prolonged vasospasm (most serious)*for hemorrhage, only use after placenta is delivered
Kaolin
MOA: absorb/bind intestinal toxinsUse: diarrhea
Etidronate
Class: bisphophonatesMOA: pyrophosphate analogs –> inhibit osteoclasts, thereby inhibiting bone resorptionUse: hypercalcemia (in malignancy), osteoporosis, ectopic calcification, Paget’s diseasePK/PD: poorly absorbedAdverse Effects: gastric/esophageal irritation, osteonecrosis of the jaw –> fractures*bone remodeling occurs in jaw more than other bones, which requires osteoclast activity
Glucagon
MOA: promotes glucose release from tissues and gluconeogenesis, increase cAMP in cardiac tissueUse: sever hypoglycemia and cardiac stimulant (as in beta blocker OD)
Metolazone
Class: Thiazide-like diureticsMOA: inhibit Na/Cl in DCT –> decreased Na/Cl reabsorption –> osmotic diuresis. Increased Ca reapsorptionUse: HTN (especially in AA and elderly), mild CHF, nephrolithiasis, nephrogenic DIPK/PD: oral admin, decrease Ca excretion, secretion = same as uric acid, anti-HTN as low doses, diuresis at high dosesAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, hyperlipidemia, contraction alkalosis*ineffective when GFR is low*more effective for HTN than loop diuretics
Degarelix
Class: GnRH antagonistsMOA: suppress gonadotropin releaseUse: prostate cancer
Cisapride
Class: 5-HT agonists - selective - 5-HT4Use: GERD *for compassionate use only
Mifepristone
Class: anti-progestinsMOA: inhibits progesterone binding to receptor. inhibits glucocorticoid receptor (high-doses)Use: termination of early pregnancy (in combo w/ misoprostol). postcoital contraceptive. hypercortisolism (if other tx fail)
Benazepril
Class: ACE inhibitors*pro-drugMOA: prevents formation of angiotensin II, decreases aldosterone, increases bradykinin, cumulatively, these have the effect of decreasing afterload and preloadUse: HTN, CHF, diabetic neuropathyAdverse Effects: dry, hacking cough (due to bradykinin), hyperkalemia
Methyltestosterone
Class: Androgens*more androgenicUse: Hypogonadism and anemiaAdverse Effects: feminizing effects in post-pubertal males (due to conversion to estrogen)
Bisoprolol
Class: Beta Adrenoceptor Antagonists - β1 selectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid), inhibit conversion of T3 to T4Use: hyperthyroidismPK/PD: oral, well absorbed Adverse Effects: due to specificity, no pulmonary effects
Brinzolamide
Class: carbonic anhydrase inhibitorsMOA: decrease aqueous humor productionUse: glaucomaPK/PD: admin ophthalmic
Pimdronate
Class: bisphophonatesMOA: pyrophosphate analogs –> inhibit osteoclasts, thereby inhibiting bone resorptionUse: hypercalcemia (in malignancy), osteoporosis, ectopic calcification, Paget’s diseasePK/PD: poorly absorbedAdverse Effects: gastric/esophageal irritation, osteonecrosis of the jaw –> fractures*bone remodeling occurs in jaw more than other bones, which requires osteoclast activity
Irbesartan
Class: ARBsMOA: selectively inhibit AT1 receptors –> vasodilationUse: HTNPK/PD: more effective at blocking angiotensin than ACE inhibitors b/c more specific*no effect on bradykinin, thus no cough or edema
Esomeprazole
Class: proton pump inhibitorsMOA: irreversibly bind H/K-ATPase of parietal cell –> reduced acid secretionUse: peptic ulcer (treatment and prevention), GERD, h. pylori (+ clarithromycin + amoxicillin)PK/PD: activated/degraded in acidic environment: coated to survive stomach –> absorbed in intestine –> enter circulation –> activated in parietal cell canaliculiAdverse Effects: GI upset, rash, CNS effects, diarrhea (chronic use only: low acidity allows bacterial overgrowth)
Dichlorophenamide
Class: carbonic anhydrase inhibitorsMOA: inhibit CA preventing breakdown of carbonic acid and absorption of bicarbonate –> osmotic diuresisUse: promotes urinary alkalinization and prevents acute altitude sicknessPK/PD: admin oral or topical. decreases NH4 secretion*contraindicated in hepatic cirrhosis (b/c alkaline urine traps NH4 as ammonia –> reabsorbed –> hepatic encephalopathy)Adverse Effects: Type II RTA
Iloprost
Class: PGI2MOA: relax smooth muscle Use: pulmonary HTNAdverse Effects: GI upset
Loperamide
Class: opioid analogues MOA: inhibit Ach release onto intestinal opioid receptors –> decreased motilityUse: diarrhea
Rosiglitazone
Class: Thiazolidinediones (TZD)MOA: activated PPAR-γ –> promote adipogenesis, decrease hepatic gluconeogenesis, reduce triglyceridesUse: DM II, reduce triglyceridesPK/PD: hepatic metabolismAdverse Effects: weight gain, hepatotoxicity, peripheral edema
Amiloride
Class: ENaC channel blockersMOA: inhibit ENaC (Na reabsorption) –> loss of potential (driving force for K section) –> decreased K/H secretionUse: primary mineralocorticoid hypersecretion, secondary aldosteronism (ex. CHF, hepatic cirrhosis)
Triptorelin
Class: GnRH analoguesMOA: chronic use desensitizes GnRH receptor –> suppresses gonadotropin releaseUse: controlled ovarian hyperstimulation, endometriosis, uterine fibroids, prostate cancer, central precocious puberty*initially these stimulate gonadotropin release
Ricinoleic Acid (Castor Oil)
MOA: stimulant laxativesUse: constipation
Lisdexmethamphetamine
Class: Indirect SympathomimeticsUse: ADHDAdverse Effects: Insomnia, anorexia, weight loss
Dexamethasone
Class: Glucocorticoids - long-actingMOA: inhibits cytokines –> decrease airway reactivity –> bronchodilation, decrease edema. Increase lipocortin, which inhibits PLA2Use: Asthma and RAPK/PD: admin oral or IVAdverse Effects: Typical steroid effects (especially w/ oral admin)
Losartan
Class: ARBsMOA: selectively inhibit AT1 receptors –> vasodilationUse: HTNPK/PD: more effective at blocking angiotensin than ACE inhibitors b/c more specific*no effect on bradykinin, thus no cough or edema
Parathion
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleUse: InsecticideDistributes to CNSPralidoxime (2-PAM) treats poisoning
Aminoglutethimide
MOA: inhibits CYP11A1, preventing steroidogenesisUse: Cushing’sAdverse Effects: adrenal insufficiency
Atropine methyl nitrate
Class: Muscarinic Antagonists - Quaternary Amines*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
Captopril
Class: ACE inhibitors*active drugMOA: prevents formation of angiotensin II, decreases aldosterone, increases bradykinin, cumulatively, these have the effect of decreasing afterload and preloadUse: HTN, CHF, diabetic neuropathyAdverse Effects: dry, hacking cough (due to bradykinin), hyperkalemia
Chlorpromazine
Class: D2 antagonistsMOA: dopamine receptor antagonistsUse: acute migraine attacks, vomiting (cancer chemo, pot-op)Adverse Effects: extrapyramidal like adverse effects, drowsiness, torsades, neuroleptic malignant syndrome, increased prolactin secretion
Eplerenone
Class: Aldosterone antagonistsMOA: increase Na secretion and K/H reabsorptionUse: Hypokalemia (in combo w/ thiazide or loop)Adverse Effects: Hyperkalemia, hyperchloremic metabolic acidosis
Moexipril
Class: ACE inhibitors*pro-drugMOA: prevents formation of angiotensin II, decreases aldosterone, increases bradykinin, cumulatively, these have the effect of decreasing afterload and preloadUse: HTN, CHF, diabetic neuropathyAdverse Effects: dry, hacking cough (due to bradykinin), hyperkalemia
Potassium
Class: Class 5 (misc.) anti-arrhythmeticsMOA: hyperpolarization –> decrease phase 4 slopeAdmin IV
Methylprednisone
Class: Glucocorticoids - short actingUse: adrenal insufficiency, asthmaPK/PD: admin oral aerosol, or topical. inactivated by placenta –> use to treat motherContraindications: gastric ulcer, anaphylaxis, CML, endotoxic shock, sclerodermaAdverse Effects: abdominal striae, osteoporosis, hyperglycemia, moon facies, typical glucocorticoid effects*sudden withdrawal –> adrenal insufficiency. This is due to suppression of endogenous HPA axis
Dostinex
Class: Dopamine receptor agonistsUse: GH excess, tumors secreting GH and PRL
Stanozol
Class: Androgens*more anabolicUse: Hypogonadism and anemiaAdverse Effects: feminizing effects in post-pubertal males (due to conversion to estrogen)
Bismuth Subsalicylate
Class: mucosal protective agentsMOA: coats ulcer tissue, antibacterial actionUse: h. pylori and diarrheaAdverse Effects: turn tongue black
Aspirin
Class: NSAID - salicylatesMOA: inhibits COX enzymes, inhibits renal secretion of uric acid (low dose), inhibits renal reabsorption of uric acid (high dose)Use: analgesic, anti-pyretic, anti-inflammatory (high dose only), inhibit platelet aggregationPK/PD: aspirin (irreversible) is metabolized to salicylic acid (reversible), highly bound to plasma protein (may kick other drugs off), contraindicated in hemophilia, children with viral infections, severe CV diseaseAdverse Effects: same as other NSAIDs, hypersensitivity (due to overutilization of LOX pathway)toxicity: salicycism, hyperthermia, hyperpnea, respiratory alkalosis* treat toxicity with gastric lavage and supportive care.* NSAIDS inhibit renal prostaglandins PGE2 and PGI2, resulting in vasoconstriction and exacerbation of CV disease
Aloe
Class: AnthraquinonesMOA: stimulant laxativesUse: constipation
Bisacodyl
Class: diphenylmethane derivativesMOA: induce low grade inflammation –> water/electrolyte accumulationUse: constipationPK/PD: admin suppository
Amlodipine
Class: Ca channel blockers - dihydropyridinesMOA: block L-type Ca channel –> smooth muscle relaxation (esp. arteries). Coronary and systemic vasodilation. Uterine smooth muscle relaxationUse: Prinzemetal’s angina prophylaxis, mild/moderate HTN (esp. in AA and elderly), tocolysisAdverse Effects: reflex tachycardia, peripheral edema*blocks binding site 1A, mostly in vasculature
Norethinodrone
Class: ProgestinsMOA: proliferation of mammary acini. thermogenic. moderately anabolic. growth of endometrium. progestational (esp. norgestrel). estrogenic activity (esp. norethynodrel, ethynodiol diacetate). anti-estrogenic activity. androgenic activity (exc. norgestrel, desogestrel)Use: Oral contraception (combo or alone [not at effective])PK/PD: high first pass metabolism. admin oral (norethindrone, norgesterel), implant (norgesterel), IM (medroxy)Adverse Effects: Increase appetite, fatigue
Colesevelam
Class: Bile acid binding resinsMOA: bind bile acids –> increase lipid excretion –> lower LDL. Increase bile acid synthesis. Increase LDL receptorsUse: primary hypercholesterolemia, digoxin toxicityAdverse Effects: bloating, constipation may impair absorption of other drugs/fat soluble vitamins. increased triglycerides
Dihydroergotamine
Class: 5-HT agonists - nonselective - ergot alkaloidsMOA: agonists or partial agonists at various receptors, vasoconstrictionUse: migraine (ergotamine or dihydroergotamine), post-partum hemorrhage (ergonovine, if oxytocin fails)PK/PD: caffeine – increases absorption, contraindicated in coronary artery diseaseAdverse Effects: GI upset (most common), prolonged vasospasm (most serious)*for hemorrhage, only use after placenta is delivered
Increlex
MOA: IGF binding protein 3Use: mutated GH receptorPK/PD: induce microsomal enzymes, contraindicated in malignancyAdverse Effects: Primarily in adults, peripheral edema, myalgias, arthralgias, carpal tunnel
Tolzamide
Class: first generation sulfonylureasMOA: bind SUR1, which is complexed to K channel, inhibiting it –> depolarization –> Ca influx –> insulin secretionUse: DM IIPK/PD: admin oral. hepatic metabolism, renal excretion,Contraindications: DMI, pregnancy, lactationAdverse Effects: Hypoglycemia, weight gain, disulfiram-like reaction, sulfonamide hypersensitivity*2nd gen binds SUR1 with higher affinity
Neostigmine
Class: Cholinesterase Inhibitors - CarbamatesMOA: substrates for AChE –> bind serine hydroxyl and are hydrolyzedUse: Treat MG, reverse neuromuscular blocking agents, post-op urinary retention Reversible Quaternary
Formeterol
Class: Direct Adrenoceptor Agonists - β2 selectiveMOA: increase cAMP –> bronchodilation and smooth muscle relaxationUse: asthmaAdverse effects: tremors*long acting
Betamethasone
Class: Glucocorticoids - long actingUse: adrenal insufficiency, asthma, stimulate surfactant production in prematurityPK/PD: admin oral aerosol, or topical. not inactivated by placenta –> use to treat fetusContraindications: gastric ulcer, anaphylaxis, CML, endotoxic shock, sclerodermaAdverse Effects: abdominal striae, osteoporosis, hyperglycemia, moon facies, typical glucocorticoid effects*sudden withdrawal –> adrenal insufficiency. This is due to suppression of endogenous HPA axis
Magnesium
Class: Class 5 (misc.) anti-arrhythmeticsMOA: unknownUse: Torsades de pointesAdmin IV
Macermin
MOA: IGF binding protein 3Use: mutated GH receptorPK/PD: induce microsomal enzymes, contraindicated in malignancyAdverse Effects: Primarily in adults, peripheral edema, myalgias, arthralgias, carpal tunnel
Desipramine
Class: tricyclic antidepressants Use: IBS associated abdominal pain
Doxazosin
Class: Alpha Adrenoceptor Antagonists - α1 selectiveUse: BPH and HTNPK/PD: long half lifeAdverse Effects: orthostatic hypotension (lowest risk with tamsulosin), reflex tachycardia
Digoxin
Class: cardiac glycosideMOA: inhibits Na/K ATPase –> increased Ca –> increased contractility. Increased K conductance –> shorten AP. Parasympathetic stimulation –> decreased AV conduction and HRUse: CHFPK/PD: high dose elicits sympathetic effects, exaggerating toxicity. multiple drug interactionsAdverse Effects: very toxic. GI toxicity, cadiotoxicity, CNS toxicity. Hypokalemia predisposes to toxicity*treat toxicity w/ K, digitoxin antibodies, lidocaine*thyroxine increases renal clearance of digoxin*cholestyramine decreases GI absorption of digoxin
Trandolapril
Class: ACE inhibitors*pro-drugMOA: prevents formation of angiotensin II, decreases aldosterone, increases bradykinin, cumulatively, these have the effect of decreasing afterload and preloadUse: HTN, CHF, diabetic neuropathyAdverse Effects: dry, hacking cough (due to bradykinin), hyperkalemia
Ritodrine
Class: Direct Adrenoceptor Agonists - β2 selectiveMOA: increase cAMP –> bronchodilation and smooth muscle relaxationUse: asthma and uterine relaxation in premature laborAdverse effects: tremors
Methamphetamine
Class: Indirect SympathomimeticsPK/PD: CNS stimulationAdverse Effects: Insomnia, anorexia, weight loss
Dorzolamide
Class: carbonic anhydrase inhibitorsMOA: decrease aqueous humor productionUse: glaucomaPK/PD: admin ophthalmic
Niacin
Class: NiacinMOA: decreased lipase activity –> decreased FA, decreased hepatic synthesis of TG and VLDL, lower plasma LDL and TGUse: lower plasma LDL and raise plasma HDLAdverse Effects: flushing (due to increased PGs), hyperuricemia, hyperglycemia, hepatotoxicity*take aspirin before use to prevent flushing
Tetrahydrocannabinol
MOA: unknown mechanismUse: vomiting
Esmolol
Class: Beta Adrenoceptor Antagonists - β1 selectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid), inhibit conversion of T3 to T4Use: hyperthyroidismPK/PD: oral, well absorbed, very short half lifeAdverse Effects: due to specificity, no pulmonary effects
Ketoprofen
Class: NSAIDMOA: block PGE2 in CNS –> resets temp control –> anti-pyretic Use: analgesic, anti-pyretic, anti-inflammatory (high dose only), inhibit platelet aggregation, gout (indo), ankylosing spondylitis (indo), OA (indo), patent ductus arteriosus (indo)PK/PD: admin oral or parenteral (ketorolac). COX-1 inhibition –> no thromboxane –> anti-platelet activityover-activation of LOX pathway –> hypersensitivityAdverse Effects: GI (esp. ulcers), hepatotoxicity, nephrotoxicity, prolonged bleeding time, hypersensitivity, hematologic toxicity (indo), sore throat (indo)*when used chronically, give misoprostol or PPI to prevent ulcers
Teriparatide
MOA: recombinant PTHUse: osteoporosis treatment
Lidocaine
Class: Class 1B anti-arrhythmeticsMOA: mild Na channel block, shorten AP durationUse: depolarization arrhythmia (ischemia, digoxin toxicity), post-MI arrhythmia, ventricular tachycardiaPK/PD: admin IV, high first pass metabolismAdverse Effects: Least cardiotoxic, neurotoxicity
Methyclothiazide
Class: Thiazide diureticsMOA: inhibit Na/Cl in DCT –> decreased Na/Cl reabsorption –> osmotic diuresis. Increased Ca reapsorptionUse: HTN (especially in AA and elderly), mild CHF, nephrolithiasis, nephrogenic DIPK/PD: oral admin, decrease Ca excretion, secretion = same as uric acid, anti-HTN as low doses, diuresis at high dosesAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, hyperlipidemia, contraction alkalosis*ineffective when GFR is low*more effective for HTN than loop diuretics
Iohexol
Class: iodinated contract materialMOA: inhibits 5`-deiodinaseUse: hyperthyroidismPK/PD: admin oral or IV, acts in liver, kidney, pituitary and brain
Isoproterenol
Class: CatecholaminesMOA: β1, β2 agonistUse: Shock, heart failure, fundoscopic eye exams*Metyrosine inhibits tyrosine hydroxylase, preventing formation of catecholamines*Reserpine inhibits NE uptake into vesicles (VMAT)
Dofetilide
Class: Class 3 anti-arrhythmeticsMOA: block rectifier K channelUse: Afib or flutterAdmin is oralAdverse Effects: prolonged QT and torsades
Pantoprazole
Class: proton pump inhibitorsMOA: irreversibly bind H/K-ATPase of parietal cell –> reduced acid secretionUse: peptic ulcer (treatment and prevention), GERD, h. pylori (+ clarithromycin + amoxicillin)PK/PD: activated/degraded in acidic environment: coated to survive stomach –> absorbed in intestine –> enter circulation –> activated in parietal cell canaliculiAdverse Effects: GI upset, rash, CNS effects, diarrhea (chronic use only: low acidity allows bacterial overgrowth)
Tyramine
Class: Indirect SympathomimeticsMOA: outcompetes NE for uptake into vesicles via VMATAdverse Effects: hypertensive crisis especially in those taking MAOIs, insomnia, anorexia, weight loss
Docusate
Class: stool softenerMOA: softens stool, promoting expulsionUse: constipation (especially in hospitalized pts.)Adverse Effects: decreased absorption of fat soluble vitamins
Mineral Oil
Class: stool softenerMOA: softens stool, promoting expulsionUse: constipation (especially in hospitalized pts.)Adverse Effects: decreased absorption of fat soluble vitamins
Demecarium
Class: Cholinesterase Inhibitors - CarbamatesMOA: substrates for AChE –> bind serine hydroxyl and are hydrolyzedReversible
Letrozole
Class: Atomatase inhibitorsMOA: Inhibit aromatase –> reduce estrogen synthesisUse: tamoxifen resistant breast cancerPK/PD: non-steroidal and reversible (except exemestane)
Cromolyn Sodium
Class: Mast cell stabilizerUse: asthma prophylaxisPK/PD: admin aerosol (give before exercise or cold/allergen exposure) Adverse Effects: mild throat irritation and cough
Finasteride
Class: anti-androgens MOA: inhibits 5α-reductase, preventing synthesis of DHTUse: BPH and male pattern baldness
Diphenoxylate
Class: opioid analogues MOA: inhibit Ach release onto intestinal opioid receptors –> decreased motilityUse: diarrheaAdverse Effects: sedation*avoid abuse w/ atropine
Isosorbide DInitrate
Class: Nitrates - short actingMOA: sitmulates NO production –> stimulates guanylyl cyclase –> increase cGMP –> decrease phosphorylation of myosin light chain –> vasodilation –> decreased preloadUse: acute anginaAdmin: inhaled or sublingualAdverse Effects: Reflex tachycardia and inotropy (increased O2 demand and reduced perfusion), headacheContraindications: HOCM and patients taking PDE inhibitors (“-fil” ex. sildenafil)*chronic use leads to tolerance (must have nitrate free intervals*toxicity = hypotension, headache, dizziness*veins dilated more than arteries*preferentially dilates epicardial arteries, which is where most ischemia occurs
Quinapril
Class: ACE inhibitors*pro-drugMOA: prevents formation of angiotensin II, decreases aldosterone, increases bradykinin, cumulatively, these have the effect of decreasing afterload and preloadUse: HTN, CHF, diabetic neuropathyAdverse Effects: dry, hacking cough (due to bradykinin), hyperkalemia
Mg Hydroxide
Class: AntacidsMOA: weak base neutralizes gastric acidUse: GERD pain relief, inactive peptic ulcer diseasePK/PD: Mg toxicity: CNS depression, sodium bicarb is systemicAdverse Effects: diarrhea (Mg), constipation (Ca, Al), hypophosphatemia (Al), renal stones (Na)
Acetylcholine
Class: Direct Muscarinic Agonists - Choline EstersUse: Stimulate GI/GU smooth muscle (ex. post-op)PK/PD: poor CNS distribution
Lactulose
Class: non-digestible sugars/alcoholsMOA: water retentionUse: acidify lumen, drawing water inPK/PD: contraindicated in CHF, pulmonary edema (because these will expand ECF by drawing fluid out of tissue)Adverse Effects: dehydration, hypernatremia, metabolic acidosis
Ergocryptine
Class: 5-HT agonists - nonselective - ergot alkaloidsMOA: agonists or partial agonists at various receptors, vasoconstrictionUse: migraine (ergotamine or dihydroergotamine), post-partum hemorrhage (ergonovine, if oxytocin fails)PK/PD: caffeine – increases absorption, contraindicated in coronary artery diseaseAdverse Effects: GI upset (most common), prolonged vasospasm (most serious)*for hemorrhage, only use after placenta is delivered
Candesartan
Class: ARBsMOA: selectively inhibit AT1 receptors –> vasodilationUse: HTNPK/PD: more effective at blocking angiotensin than ACE inhibitors b/c more specific*no effect on bradykinin, thus no cough or edema
Propantheline
Class: Muscarinic Antagonists - Quaternary Amines*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
Gemfibrozil
Class: fibratesMOA: activates PPAR-α –> decreased plasma TG, VLDL, LDL, increases HDLUse: hypertriglyceridemia and dysbetalipoproteinemiaPK/PD: may increase concentration of statinsAdverse Effects: skin rashes, lymphocytopenia, myopathy (increased risk with stain combo), gall bladder disease
Promethazine
Class: D2 antagonistsMOA: dopamine receptor antagonistsUse: acute migraine attacks, vomiting (cancer chemo, pot-op)Adverse Effects: extrapyramidal like adverse effects, drowsiness, torsades, neuroleptic malignant syndrome, increased prolactin secretion
Tolbutamide
Class: first generation sulfonylureasMOA: bind SUR1, which is complexed to K channel, inhibiting it –> depolarization –> Ca influx –> insulin secretionUse: DM IIPK/PD: admin oral. hepatic metabolism, renal excretion,Contraindications: DMI, pregnancy, lactationAdverse Effects: Hypoglycemia, weight gain, disulfiram-like reaction, sulfonamide hypersensitivity*2nd gen binds SUR1 with higher affinity
Amphetamine
Class: Indirect SympathomimeticsMOA: promotes Ca-dependent vesicle fusionPK/PD: CNS stimulation. Not catabolized by MAOAdverse Effects: Insomnia, anorexia, weight loss, psychosis
Aminophylline
Class: MethylxanthinesMOA: inhibits PDE4 –> prevents breakdown of cAMP –> bronchodilation, decreased cytokines, improved contractility of skeletal muscle (diaphragm). Adenosine antagonist –> inhibits bronchoconstrictionUse: asthma (if other tx failed)PK/PD: metabolized in liver by CYP450, monitor plasma levels to prevent toxicityAdverse Effects: GI upset
(Dex)chlorpheniramine
Class: H1 antagonists - first generationMOA: anti-cholinergic. blocks Na channel (anesthesia)Use: allergic rhinitis or urticaria, motion sickness, local anesthesia, nausea, vomiting, insomnia PK/PD: well-absorbed, inhibit CYP450, cross BBBAdverse Effects: sedation (anti-cholinergic), urinary retention (anti-muscarinic)*cyclizine, meclizine have least sedative effect
Prochlorpromazine
Class: D2 antagonistsMOA: dopamine receptor antagonistsUse: acute migraine attacks, vomiting (cancer chemo, pot-op)Adverse Effects: extrapyramidal like adverse effects, drowsiness, torsades, neuroleptic malignant syndrome, increased prolactin secretion
Chlorpropamide
Class: first generation sulfonylureasMOA: bind SUR1, which is complexed to K channel, inhibiting it –> depolarization –> Ca influx –> insulin secretionUse: DM IIPK/PD: admin oral. hepatic metabolism, renal excretion,Contraindications: DMI, pregnancy, lactationAdverse Effects: Hypoglycemia, weight gain, disulfiram-like reaction, sulfonamide hypersensitivity*2nd gen binds SUR1 with higher affinity
Hydrochlorothiazide
Class: Thiazide diureticsMOA: inhibit Na/Cl in DCT –> decreased Na/Cl reabsorption –> osmotic diuresis. Increased Ca reapsorptionUse: HTN (especially in AA and elderly), mild CHF, nephrolithiasis, nephrogenic DIPK/PD: oral admin, decrease Ca excretion, secretion = same as uric acid, anti-HTN as low doses, diuresis at high dosesAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, hyperlipidemia, contraction alkalosis*ineffective when GFR is low*more effective for HTN than loop diuretics
Fenoldopam
Class: direct vasodilatorsMOA: D1 agonist –> arterial dilation –> reduced afterloadUse: HTN Admin IVAdverse Effects: reflex tachycardia, fluid retention, HA, palpitation
Topiramate
Class: anti-convulsants Use: preventative tx for migraine
Lispro
Class: Rapid acting insulinUse: DM I
Estrone
Class: EstrogensMOA: growth/development of vagina, uterus, uterine tubes. breast enlargement. pubic/axillary hair. pigmentation of areola and genitalia. mildly anabolic. inhibits PTH-induced bone resorptionUse: primary hypogonadism. postmenopausal HRT. oral contraception. osteoporosis prophylaxisPK/PD: contraindicated in breast/endometrial cancer, liver disease, thromboembolic diseases, smoking, pregnancyAdverse Effects: increased risk of breast/endometrial cancer. nausea, bloating, HTN
Na Carbonate
Class: AntacidsMOA: weak base neutralizes gastric acidUse: GERD pain relief, inactive peptic ulcer diseasePK/PD: Mg toxicity: CNS depression, sodium bicarb is systemicAdverse Effects: diarrhea (Mg), constipation (Ca, Al), hypophosphatemia (Al), renal stones (Na)
Buspirone
Class: 5-HT agonists - selective - 5HT1A partial agonistUse: anxiolytic PK/PD: slow onset Adverse Effects: dysphoria (high dose)
Rimonabant
MOA: reduces appetiteUse: obesity
Cortisone
Class: Glucocorticoids - short actingUse: adrenal insufficiency, asthmaPK/PD: admin oral aerosol, or topical. inactivated by placenta –> use to treat motherContraindications: gastric ulcer, anaphylaxis, CML, endotoxic shock, sclerodermaAdverse Effects: abdominal striae, osteoporosis, hyperglycemia, moon facies, typical glucocorticoid effects*sudden withdrawal –> adrenal insufficiency. This is due to suppression of endogenous HPA axis
Risendronate
Class: bisphophonatesMOA: pyrophosphate analogs –> inhibit osteoclasts, thereby inhibiting bone resorptionUse: hypercalcemia (in malignancy), osteoporosis, ectopic calcification, Paget’s diseasePK/PD: poorly absorbedAdverse Effects: gastric/esophageal irritation, osteonecrosis of the jaw –> fractures*bone remodeling occurs in jaw more than other bones, which requires osteoclast activity
Liothyronine
MOA: isomer of T3Use: hypothyroidism and myxedema comaPK/PD: acts faster than T4,l but shorter half lifeAdverse Effects: cardiotoxicity
Loratidine
Labetalol
Class: Beta and Alpha Adrenoceptor Antagonists - nonselectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid)Use: HTN, ischemia, angina prophylaxis, migraine prevention (first choice)PK/PD: oral. well absorbed. Adverse Effects: asthma exacerbation, supersensitivity (with chronic use and abrupt discontinuation), delayed recovery of normoglycemia*toxicity = rash and sedation*preferred in pregnancy
Bendroflumethiazide
Class: Thiazide diureticsMOA: inhibit Na/Cl in DCT –> decreased Na/Cl reabsorption –> osmotic diuresis. Increased Ca reapsorptionUse: HTN (especially in AA and elderly), mild CHF, nephrolithiasis, nephrogenic DIPK/PD: oral admin, decrease Ca excretion, secretion = same as uric acid, anti-HTN as low doses, diuresis at high dosesAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, hyperlipidemia, contraction alkalosis*ineffective when GFR is low*more effective for HTN than loop diuretics
Meclizine
Class: H1 antagonists - first generationMOA: anti-cholinergic. blocks Na channel (anesthesia)Use: allergic rhinitis or urticaria, motion sickness, local anesthesia, nausea, vomiting, insomnia PK/PD: well-absorbed, inhibit CYP450, cross BBBAdverse Effects: sedation (anti-cholinergic), urinary retention (anti-muscarinic)*cyclizine, meclizine have least sedative effect
Lovastatin
*prodrugClass: HMG-CoA reductase inhibitorsMOA: reduce hepatic formation of cholesterol. Increase LDL receptors on hepatocytes –> lower plasma LDLUse: lower plasma LDLPK/PD: good GI absorption, hepatic metabolism by CYPs, high first pass metabolism, bile excretion, contraindicated in pregnancy, admin at night when most cholesterol synthesis occursAdverse Effects: hepatotoxicity, rhabdomyolysis (increase CK)*reduces mortality from CVD and MI
Alprostadil
Class: PGE1MOA: relax smooth muscle, bind prostaglandin receptors on gastric epitheliumUse: ED*contraindicated in pregnancyAdverse Effects: GI upset
Indapamide
Class: Thiazide-like diureticsMOA: inhibit Na/Cl in DCT –> decreased Na/Cl reabsorption –> osmotic diuresis. Increased Ca reapsorptionUse: HTN (especially in AA and elderly), mild CHF, nephrolithiasis, nephrogenic DIPK/PD: oral admin, decrease Ca excretion, secretion = same as uric acid, anti-HTN as low doses, diuresis at high dosesAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, hyperlipidemia, contraction alkalosis*ineffective when GFR is low*more effective for HTN than loop diuretics
Isosorbide Mononitrate
Class: Nitrates - long actingMOA: sitmulates NO production –> stimulates guanylyl cyclase –> increase cGMP –> decrease phosphorylation of myosin light chain –> vasodilation –> decreased preloadUse: acute anginaAdmin: oral, ointment, buccal (slow-release), chewable or transdermalAdverse Effects: Reflex tachycardia and inotropy (increased O2 demand and reduced perfusion), headacheContraindications: HOCM and patients taking PDE inhibitors (“-fil” ex. sildenafil)*chronic use leads to tolerance (must have nitrate free intervals*toxicity = hypotension, headache, dizziness*veins dilated more than arteries*preferentially dilates epicardial arteries, which is where most ischemia occurs
Ibandronate
Class: bisphophonatesMOA: pyrophosphate analogs –> inhibit osteoclasts, thereby inhibiting bone resorptionUse: hypercalcemia (in malignancy), osteoporosis, ectopic calcification, Paget’s diseasePK/PD: poorly absorbedAdverse Effects: gastric/esophageal irritation, osteonecrosis of the jaw –> fractures*bone remodeling occurs in jaw more than other bones, which requires osteoclast activity
Nebivolol
Class: Beta BlockerMOA: Cardioselective and vasodilatory (NO production)
Diatriozate
Class: iodinated contract materialMOA: inhibits 5`-deiodinaseUse: hyperthyroidismPK/PD: admin oral or IV, acts in liver, kidney, pituitary and brain
Azelastine
Class: H1 antagonists - second generationMOA: no anti-cholinergic activityUse: allergic rhinitis PK/PD: don’t cross blood-brain barrier (thus, can’t treat motion sickness)Adverse Effects: fewer than first gen
Dycyclomine
Class: anticholinergicsMOA: anti-spasmodic activityUse: IBS
Tolazoline
Class: Alpha Adrenoceptor Antagonists - nonselectiveMOA: reduces TPR and MAPUse: PheochromocytomaAdverse Effects: Orthostatic hypotension and reflex tachycardia
Nedocromil Sodium
Class: Mast cell stabilizerUse: asthma prophylaxisPK/PD: admin aerosol (give before exercise or cold/allergen exposure)Adverse Effects: mild throat irritation and cough
Cyclizine
Class: H1 antagonists - first generationMOA: anti-cholinergic. blocks Na channel (anesthesia)Use: allergic rhinitis or urticaria, motion sickness, local anesthesia, nausea, vomiting, insomnia PK/PD: well-absorbed, inhibit CYP450, cross BBBAdverse Effects: sedation (anti-cholinergic), urinary retention (anti-muscarinic)*cyclizine, meclizine have least sedative effect
Ranitidine
Class: H2 antagonistsMOA: inhibit gastric acid secretion (esp. nocturnal secretion)Use: peptic ulcer and h. pylori (+ bismuth + antibiotics)PK/PD: doesn’t impact normal intestinal secretions, contraindicated in pregnant and nursing women. metabolized by CYP450Adverse Effects: GI upset, endocrine effects (cimetidine): gynecomastia, galactorrhea, muscle pain, inhibits microsomal enzymes*nocturnal acid secretion is primarily driven by histamine
Adenosine
Class: Class 5 (misc.) anti-arrhythmeticsMOA: A1 receptor –> decrease inotropy A2 receptor –> coronary vasodilationUse: paroxysmal supraventricular tachyarrhythmia (PSVT) Admin IVAdverse Effects: flushing, SOA, HA*use verapamil or esmolol if this fails*carotid massage can also treat this
Pegvisomant
MOA: GH receptor antagonistUse: GH excessAdverse Effects: hepatotoxicity*may assist tumor growth
Cetirizine
Class: H1 antagonists - second generationMOA: no anti-cholinergic activityUse: allergic rhinitis PK/PD: don’t cross blood-brain barrier (thus, can’t treat motion sickness)Adverse Effects: fewer than first gen
Carteolol
Class: Beta Adrenoceptor Antagonists - nonselectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid)Use: HTN, ischemia, angina prophylaxis, migraine prevention (first choice)PK/PD: oral. well absorbed. Adverse Effects: asthma exacerbation, supersensitivity (with chronic use and abrupt discontinuation), delayed recovery of normoglycemia*toxicity = rash and sedation*has intrinsic sympathomimetic activity and can protect against asthma, bradycardia, and altered lipid profile
Vasopressin
Class: Vasopressin agonistMOA: predominantly V2 agonist, anti-diuresis, vasoconstrictionUse: HTN, neurogenic diabetes insipidus*desmopressin is more potent and longer lasting than vasopressin
Guanabenz
Class: Direct Adrenoceptor Agonists - α2 selectiveMOA: increase reuptake of catecholamines –> decreased sympathetic stimulationUse: hypertensionAdverse effects: hypertensive crisis with abrupt withdrawal
Glipizide
Class: second generation sulfonylureasMOA: bind SUR1, which is complexed to K channel, inhibiting it –> depolarization –> Ca influx –> insulin secretionUse: DM IIPK/PD: admin oral. hepatic metabolism, renal excretion,Contraindications: DMI, pregnancy, lactationAdverse Effects: Hypoglycemia, weight gain, disulfiram-like reaction, sulfonamide hypersensitivity*2nd gen binds SUR1 with higher affinity
Acarbose
Class: alpha glucosidase inhibitorsMOA: inhibit pancreatic alpha amylase and intestinal alpha glucosidase –> slow glucose absorption and spread it over a larger surface area –> decrease glucose peakUse: DM IIAdverse Effects: flatulence, bloating, diarrhea
Trimazosin
Class: Alpha Adrenoceptor Antagonists - α1 selectiveUse: hypertensionPK/PD: long half lifeAdverse Effects: orthostatic hypotension (lowest risk with tamsulosin), reflex tachycardia
Amrinone
Class: PDE inhibitorsMOA: increase cAMP and Ca –> increased contractility and vasodilation (arteriolar). Increased contractilityUse: acute tx of HF
Testosterone
Class: Androgens*more androgenicUse: Hypogonadism and anemiaAdverse Effects: feminizing effects in post-pubertal males (due to conversion to estrogen)
Ibuprofen
Class: NSAIDMOA: block PGE2 in CNS –> resets temp control –> anti-pyretic Use: analgesic, anti-pyretic, anti-inflammatory (high dose only), inhibit platelet aggregation, gout (indo), ankylosing spondylitis (indo), OA (indo), patent ductus arteriosus (indo)PK/PD: admin oral or parenteral (ketorolac). COX-1 inhibition –> no thromboxane –> anti-platelet activityover-activation of LOX pathway –> hypersensitivityAdverse Effects: GI (esp. ulcers), hepatotoxicity, nephrotoxicity, prolonged bleeding time, hypersensitivity, hematologic toxicity (indo), sore throat (indo)*when used chronically, give misoprostol or PPI to prevent ulcers
Norgestimate
Class: ProgestinsMOA: proliferation of mammary acini. thermogenic. moderately anabolic. growth of endometrium. progestational (esp. norgestrel). estrogenic activity (esp. norethynodrel, ethynodiol diacetate). anti-estrogenic activity. androgenic activity (exc. norgestrel, desogestrel)Use: Oral contraception (combo or alone [not at effective])PK/PD: high first pass metabolism. admin oral (norethindrone, norgesterel), implant (norgesterel), IM (medroxy)Adverse Effects: Increase appetite, fatigue
Salmeterol
Class: Direct Adrenoceptor Agonists - β2 selectiveMOA: increase cAMP –> bronchodilation and smooth muscle relaxationUse: asthmaAdverse effects: tremors*long acting
Atropine
Class: Muscarinic Antagonists - Tertiary AminesMOA: decrease Ach –> inhibits bronchoconstriction and mucus secretionUse: Asthma, muscarinic poisoning, vagal syncopePK/PD: given IV.*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
Lanreotide
Class: Somatostatin analogMOA: inhibits pituitary release of GHUse: GH excess, insulinoma, VIPomaAdverse Effects: GI toxicity, vitamin B12 deficiency*long-acting
Meprednisone
Class: Glucocorticoids - short actingUse: adrenal insufficiency, asthmaPK/PD: admin oral aerosol, or topical. inactivated by placenta –> use to treat motherContraindications: gastric ulcer, anaphylaxis, CML, endotoxic shock, sclerodermaAdverse Effects: abdominal striae, osteoporosis, hyperglycemia, moon facies, typical glucocorticoid effects*sudden withdrawal –> adrenal insufficiency. This is due to suppression of endogenous HPA axis
Rizatriptan
Class: 5-HT agonists - selective - 5-HT1B/1DMOA: counteract CGRP –> cerebral vasoconstrictionUse: acute migraines (better choice than ergots)PK/PD: contraindicated in CADAdverse Effects: tingling, warm sensation, may mimic angina
Milrinone
Class: PDE inhibitorsMOA: increase cAMP and Ca –> increased contractility and vasodilation (arteriolar). Increased contractilityUse: acute tx of HF
Levothyroxine
MOA: isomer of T4Use: hypothyroidism (first line)Adverse Effects: headache and nervousness
NPH novolin N
Class: intermediate acting insulinUse: DM I
Cibacalcin
MOA: synthetic calcitoninUse: osteoporosis treatment and hypercalcemiaPK/PD: admin IM*high Ca due to vitamin D excess, bone cancer, hyper PTH, etc.
Famotidine
Class: H2 antagonistsMOA: inhibit gastric acid secretion (esp. nocturnal secretion)Use: peptic ulcer and h. pylori (+ bismuth + antibiotics)PK/PD: doesn’t impact normal intestinal secretions, contraindicated in pregnant and nursing women. metabolized by CYP450Adverse Effects: GI upset, endocrine effects (cimetidine): gynecomastia, galactorrhea, muscle pain, inhibits microsomal enzymes*nocturnal acid secretion is primarily driven by histamine
Lansoprazole
Class: proton pump inhibitorsMOA: irreversibly bind H/K-ATPase of parietal cell –> reduced acid secretionUse: peptic ulcer (treatment and prevention), GERD, h. pylori (+ clarithromycin + amoxicillin)PK/PD: activated/degraded in acidic environment: coated to survive stomach –> absorbed in intestine –> enter circulation –> activated in parietal cell canaliculiAdverse Effects: GI upset, rash, CNS effects, diarrhea (chronic use only: low acidity allows bacterial overgrowth)
Theophylline
Class: MethylxanthinesMOA: inhibits PDE4 –> prevents breakdown of cAMP –> bronchodilation, decreased cytokines, improved contractility of skeletal muscle (diaphragm). Adenosine antagonist –> inhibits bronchoconstrictionUse: asthma (if other tx failed)PK/PD: metabolized in liver by CYP450, monitor plasma levels to prevent toxicityAdverse Effects: GI upset
Rocuronium
Class: Nicotinic Antagonists - Quaternary ParalyticsMOA: competitive blockage of autonomic nicotinic receptors –> decrease in arteriolar and vasomotor tone.
Fexofenadine
Class: H1 antagonists - second generationMOA: no anti-cholinergic activityUse: allergic rhinitis PK/PD: don’t cross blood-brain barrier (thus, can’t treat motion sickness)Adverse Effects: fewer than first gen
Sodium Nitroprusside
Class: direct vasodilatorsMOA: increase NO –> venous = arterial dilation –> reduced preload and afterloadUse: HTN, CHF Admin IVAdverse Effects: metabolic acidosis, reflex tachycardia, fluid retention, HA, palpitation
Dexmethylphenidate
Class: Indirect SympathomimeticsUse: ADHDAdverse Effects: Insomnia, anorexia, weight loss
Hydroflumethiazide
Class: Thiazide diureticsMOA: inhibit Na/Cl in DCT –> decreased Na/Cl reabsorption –> osmotic diuresis. Increased Ca reapsorptionUse: HTN (especially in AA and elderly), mild CHF, nephrolithiasis, nephrogenic DIPK/PD: oral admin, decrease Ca excretion, secretion = same as uric acid, anti-HTN as low doses, diuresis at high dosesAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, hyperlipidemia, contraction alkalosis*ineffective when GFR is low*more effective for HTN than loop diuretics
Divalproex
Class: anti-convulsants Use: preventative tx for migraine
Propafenone
Class: Class 1C anti-arrhythmeticsMOA: strong Na channel block. blocks K channels. no change to AP.Use: supraventricular arrhythmia Admin is oralAdverse Effects: metallic taste and constipation*must use on structurally healthy hearts
Cocaine
Class: Indirect SympathomimeticsMOA: Inhibits NET (reuptake 1)Adverse Effects: Insomnia, anorexia, weight loss
Zafirlukast
Class: Leukotriene AntagonistMOA: LTD4 receptor antagonist –> bronchodilationUse: asthmaPK/PD: admin is oral (good for kids)
Hexamethonium
Class: Nicotinic Antagonists - Quaternary Ganglion BlockersMOA: competitive blockage of autonomic nicotinic receptors –> decrease in arteriolar and vasomotor tone.
Detemir
Class: long acting insulinUse: DM I (used to maintain basal insulin levels)
Promethazine
Class: H1 antagonists - first generationMOA: anti-cholinergic. blocks Na channel (anesthesia)Use: allergic rhinitis or urticaria, motion sickness, local anesthesia, nausea, vomiting, insomnia PK/PD: well-absorbed, inhibit CYP450, cross BBBAdverse Effects: sedation (anti-cholinergic), urinary retention (anti-muscarinic)*cyclizine, meclizine have least sedative effect
Isoflurophate
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleDistributes to CNSPralidoxime (2-PAM) treats poisoning
Celecoxib
Class: COX-2 inhibitorMOA: inhibit COX-2, especially decrease PGI2 synthesis in endotheliumUse: RA and OA PK/PD: contraindicated in sulfa allergyAdverse Effects: no anti-platelet activity
Guanfacine
Class: Direct Adrenoceptor Agonists - α2 selectiveMOA: increase reuptake of catecholamines –> decreased sympathetic stimulationUse: hypertensionAdverse effects: hypertensive crisis with abrupt withdrawal
Medroxyprogesterone
Class: ProgestinsMOA: proliferation of mammary acini. thermogenic. moderately anabolic. growth of endometrium. progestational (esp. norgestrel). estrogenic activity (esp. norethynodrel, ethynodiol diacetate). anti-estrogenic activity. androgenic activity (exc. norgestrel, desogestrel)Use: Oral contraception (combo or alone [not at effective])PK/PD: high first pass metabolism. admin oral (norethindrone, norgesterel), implant (norgesterel), IM (medroxy)Adverse Effects: Increase appetite, fatigue
Edrophonium
Class: Cholinesterase Inhibitors - Alcohol EsterMOA: Binds anionic site of AChEUse: MG diagnosis (Tinsilon test)ReversibleVery short acting
Oxymethalone
Class: Androgens*more anabolicUse: Hypogonadism and anemiaAdverse Effects: feminizing effects in post-pubertal males (due to conversion to estrogen)
Na Phosphate
Class: saline laxativesMOA: non-absorbable salt –> increase osmotic activity in lumenUse: constipationContraindications: renal insufficiency, heart disease, diuretic treatment
Glycerin
Class: non-digestible sugars/alcoholsMOA: water retentionUse: constipationPK/PD: contraindicated in CHF, pulmonary edema (because these will expand ECF by drawing fluid out of tissue)Adverse Effects: dehydration, hypernatremia, metabolic acidosis
Exenatide
Class: incretin based therapyMOA: incretin analogue (like GLP-1) –> increased insulin secretion and potentiate it’s effectsUse: DM II (when other therapy is suboptimal)PK/PD: admin IMAdverse Effects: GI upset and pancreatitits
Malathion
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleUse: InsecticideDistributes to CNSPralidoxime (2-PAM) treats poisoning
Desloratidine
Class: H1 antagonists - second generationMOA: no anti-cholinergic activityUse: allergic rhinitis PK/PD: don’t cross blood-brain barrier (thus, can’t treat motion sickness)Adverse Effects: fewer than first gen
Somatotropin
MOA: recombinant GHUse: GH deficiency (ex. growth failure in children, wasting in HIV pts, short bowel syndrome)PK/PD: induce microsomal enzymes, contraindicated in malignancyAdverse Effects: Primarily in adults, peripheral edema, myalgias, arthralgias, carpal tunnel*may assist tumor growth
Oxytocin
MOA: stimulates release PG and LT –> uterine contraction. Myoepithelial cell contraction –> milk expression. H2O intoxicationUse: induce labor and post-partum hemorrhagePK/PD: admin IV, short half life, contraindicated in prematurity, fetal distressAdverse Effects: toxicity - fetal distress, uterine rupture, anti-diuresis, vasodilation*only induce labor after cervical ripening
Tiludronate
Class: bisphophonatesMOA: pyrophosphate analogs –> inhibit osteoclasts, thereby inhibiting bone resorptionUse: hypercalcemia (in malignancy), osteoporosis, ectopic calcification, Paget’s diseasePK/PD: poorly absorbedAdverse Effects: gastric/esophageal irritation, osteonecrosis of the jaw –> fractures*bone remodeling occurs in jaw more than other bones, which requires osteoclast activity
Amitryptyline
Class: tricyclic antidepressants Use: preventative tx for migraine
Succinylcholine
Class: Nicotinic Antagonists - Quaternary ParalyticsMOA: Agonist of NMJ nicotinic receptor –> depolarizing blockadeUse: short term paralysisPK/PD: very short duration. Is antagonized by tubocurarineAdverse Effects: fasciculation –> muscle pain
Trichlormethiazide
Class: Thiazide diureticsMOA: inhibit Na/Cl in DCT –> decreased Na/Cl reabsorption –> osmotic diuresis. Increased Ca reapsorptionUse: HTN (especially in AA and elderly), mild CHF, nephrolithiasis, nephrogenic DIPK/PD: oral admin, decrease Ca excretion, secretion = same as uric acid, anti-HTN as low doses, diuresis at high dosesAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, hyperlipidemia, contraction alkalosis*ineffective when GFR is low*more effective for HTN than loop diuretics
Pralidoxime (2-PAM)
Class: Cholinesterase RegeneratorMOA: displaces phosphate bond, regenerating AchEUse: organophosphate poisoning*must be given before organophosphate bond “ages”
Tamsulosin
Class: Alpha Adrenoceptor Antagonists - α1 selectiveUse: very selective for BPHPK/PD: long half lifeAdverse Effects: orthostatic hypotension (lowest risk with tamsulosin), reflex tachycardia
Miglitol
Class: alpha glucosidase inhibitorsMOA: inhibit pancreatic alpha amylase and intestinal alpha glucosidase –> slow glucose absorption and spread it over a larger surface area –> decrease glucose peakUse: DM IIAdverse Effects: flatulence, bloating, diarrhea
Minoxidil
Class: direct vasodilatorsMOA: arterial dilationUse: Chronic HTN and to grow hair Admin oralAdverse Effects: hypertrichosis, reflex tachycardia, fluid retention, HA, palpitation AKA Rogaine
Methacholine
Class: Direct Muscarinic Agonists - Choline EstersUse: Stimulate GI/GU smooth muscle (ex. post-op)PK/PD: poor CNS distribution Hydrolyzed by AchE, so has more transient effects
Pioglitazone
Class: Thiazolidinediones (TZD)MOA: activated PPAR-γ –> promote adipogenesis, decrease hepatic gluconeogenesis, reduce triglycerides, increase peripher insulin sensitivityUse: DM II, reduce triglyceridesPK/PD: hepatic metabolismAdverse Effects: weight gain, hepatotoxicity, peripheral edema
Scopolamine
Class: Muscarinic Antagonists - Tertiary AminesMOA: decrease Ach –> inhibits bronchoconstriction and mucus secretionUse: motion sicknessPK/PD: given transdermally, crosses BBB –> more side effects but can treat motion sickness*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retentionCNS effects: drowsiness, confusion, delerium
Sibutramine
MOA: reduces appetiteUse: obesity
Norepinephrine
Class: CatecholaminesMOA: α1, α2, β1, agonistUse: Shock, heart failure, fundoscopic eye exams*Metyrosine inhibits tyrosine hydroxylase, preventing formation of catecholamines*Reserpine inhibits NE uptake into vesicles (VMAT)
Polycarbaphil
MOA: bulk forming laxativeUse: constipation
Prazosin
Class: Alpha Adrenoceptor Antagonists - α1 selectiveUse: hypertension and PTSDPK/PD: long half lifeAdverse Effects: orthostatic hypotension (lowest risk with tamsulosin), reflex tachycardia
Sucralfate
Class: mucosal protective agentsMOA: selective binding/coating of necrotic ulcer tissueUse: peptic ulcer
Leuprolide
Class: GnRH analoguesMOA: chronic use desensitizes GnRH receptor –> suppresses gonadotropin releaseUse: controlled ovarian hyperstimulation, endometriosis, uterine fibroids, prostate cancer, central precocious puberty*initially these stimulate gonadotropin release
Verapamil
Class: Ca channel blockers - non-dihydropyridinesMOA: block L-type Ca channel –> reduced SA/AV conductionUse: Angina prophylaxis, mild/moderate HTN (esp. in AA and elderly), tocolysis, class IV anti-arrhythmicContraindicated in CHF Adverse Effects: cardiac arrest, AV block, constipation, CHF*blocks binding site 1C, mostly in myocardium NO REFLEX TACHYCARDIA
Carbachol
Class: Direct Muscarinic Agonists - Choline EstersUse: Stimulate GI/GU smooth muscle (ex. post-op)PK/PD: poor CNS distribution Resistant to AchE Has some nicotinic-like activity
Ganirelix
Class: GnRH antagonistsMOA: suppress gonadotropin releaseUse: controlled ovarian hyperstimulation
Granisetron
Class: 5-HT3 antagonists Use: chemo-induced vomiting
Rabeprazole
Class: proton pump inhibitorsMOA: irreversibly bind H/K-ATPase of parietal cell –> reduced acid secretionUse: peptic ulcer (treatment and prevention), GERD, h. pylori (+ clarithromycin + amoxicillin)PK/PD: activated/degraded in acidic environment: coated to survive stomach –> absorbed in intestine –> enter circulation –> activated in parietal cell canaliculiAdverse Effects: GI upset, rash, CNS effects, diarrhea (chronic use only: low acidity allows bacterial overgrowth)
Pilocarpine
Class: Direct Muscarinic Agonists - AlkaloidsMOA: Contracts iris sphincter, increases aqueous humor drainageUse: Acute glaucoma Distributes to CNS because it is tertiary Resistant to AchE
Cabergoline
Class: dopamine agonistMOA: D2 agonistUse: Parkinsonism, hyperprolactinemia, prolactinomaAdverse Effects: NandV, orthostatic hypotension, fluctuation in efficacy of motor control, abnormal involuntary movements, arrhythmia, hypersexuality, hallucinations, paranoia, anxiety, mania, depression
Fluticasone
Class: GlucocorticoidsMOA: inhibits cytokines –> decrease airway reactivity –> bronchodilation, decrease edema. Increase lipocortin, which inhibits PLA2Use: Asthma and RAPK/PD: admin oral, IV, or aerosolAdverse Effects: Typical steroid effects (especially w/ oral admin), oral candidiasis, and hoarseness
Pirenzepine
Class: Muscarinic Antagonists - Tertiary Amines MOA: decrease Ach –> inhibits bronchoconstriction and mucus secretion*M1 selective*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
Sulindac
Class: NSAIDMOA: block PGE2 in CNS –> resets temp control –> anti-pyretic Use: analgesic, anti-pyretic, anti-inflammatory (high dose only), inhibit platelet aggregation, gout (indo), ankylosing spondylitis (indo), OA (indo), patent ductus arteriosus (indo)PK/PD: admin oral or parenteral (ketorolac). COX-1 inhibition –> no thromboxane –> anti-platelet activityover-activation of LOX pathway –> hypersensitivityAdverse Effects: GI (esp. ulcers), hepatotoxicity, nephrotoxicity, prolonged bleeding time, hypersensitivity, hematologic toxicity (indo), sore throat (indo)*when used chronically, give misoprostol or PPI to prevent ulcers
Chlorothiazide
Class: Thiazide diureticsMOA: inhibit Na/Cl in DCT –> decreased Na/Cl reabsorption –> osmotic diuresis. Increased Ca reapsorptionUse: HTN (especially in AA and elderly), mild CHF, nephrolithiasis, nephrogenic DIPK/PD: oral admin, decrease Ca excretion, secretion = same as uric acid, anti-HTN as low doses, diuresis at high dosesAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, hyperlipidemia, contraction alkalosis*ineffective when GFR is low*more effective for HTN than loop diuretics
Albuterol
Class: Direct Adrenoceptor Agonists - β2 selectiveMOA: increase cAMP –> bronchodilation and smooth muscle relaxationUse: asthmaAdverse effects: tremors
Colestipol
Class: Bile acid binding resinsMOA: bind bile acids –> increase lipid excretion –> lower LDL. Increase bile acid synthesis. Increase LDL receptorsUse: primary hypercholesterolemia, digoxin toxicityAdverse Effects: bloating, constipation may impair absorption of other drugs/fat soluble vitamins. increased triglycerides
Tubocurarine
Class: Nicotinic Antagonists - Quaternary ParalyticsMOA: competitive blockage of autonomic nicotinic receptors –> decrease in arteriolar and vasomotor tone and agonist of NMJ nicotinic receptor –> depolarizing blockadeUse: lethal injection and paralysis*antagonizes succinylcholine. increases potency of inhaled anesthetics and antibioticsAdverse Effects: Causes histamine release –> may precipitate asthma
Furosemide
Class: Loop diureticsMOA: inhibit NKCC –> decreased Na/Cl/K reabsorption –> osmotic diuresis. Change in potential –> Mg and Ca excretionUse: Pulmonary edema, CHF, HTN, acute hypercalcemia, hyperkalemnia, acute renal failurePK/PD: admin oral, IV, or IM. rapidly absorbed. Elimination = tubular secretion and absorptionAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, ototoxicity, dehydration, hyonatremia, metabolic alkalosis (contraction alkalosis)*hypomagnesemia –> increased PG production and renal blood flow aiding anti-hypertensive effect*Effective when GFR is low*more effective diuretic than thiazide*use ethacrynic acid of pt has sulfa allergy
Diphenhydramine
Class: H1 antagonists - first generationMOA: anti-cholinergic. blocks Na channel (anesthesia)Use: allergic rhinitis or urticaria, motion sickness, local anesthesia, nausea, vomiting, insomnia PK/PD: well-absorbed, inhibit CYP450, cross BBBAdverse Effects: sedation (anti-cholinergic), urinary retention (anti-muscarinic)*cyclizine, meclizine have least sedative effect
Perindopril
Class: ACE inhibitors*pro-drugMOA: prevents formation of angiotensin II, decreases aldosterone, increases bradykinin, cumulatively, these have the effect of decreasing afterload and preloadUse: HTN, CHF, diabetic neuropathyAdverse Effects: dry, hacking cough (due to bradykinin), hyperkalemia
Ketorolac
Class: NSAIDMOA: block PGE2 in CNS –> resets temp control –> anti-pyretic Use: analgesic, anti-pyretic, anti-inflammatory (high dose only), inhibit platelet aggregation, gout (indo), ankylosing spondylitis (indo), OA (indo), patent ductus arteriosus (indo)PK/PD: admin oral or parenteral (ketorolac). COX-1 inhibition –> no thromboxane –> anti-platelet activityover-activation of LOX pathway –> hypersensitivityAdverse Effects: GI (esp. ulcers), hepatotoxicity, nephrotoxicity, prolonged bleeding time, hypersensitivity, hematologic toxicity (indo), sore throat (indo)*when used chronically, give misoprostol or PPI to prevent ulcers
Lorazepam
Class: benzodiazepines Use: vomiting
Cetrorelix
Class: GnRH antagonistsMOA: suppress gonadotropin releaseUse: controlled ovarian hyperstimulation
Norgestrel
Class: ProgestinsMOA: proliferation of mammary acini. thermogenic. moderately anabolic. growth of endometrium. progestational (esp. norgestrel). estrogenic activity (esp. norethynodrel, ethynodiol diacetate). anti-estrogenic activity. androgenic activity (exc. norgestrel, desogestrel)Use: Oral contraception (combo or alone [not at effective])PK/PD: high first pass metabolism. admin oral (norethindrone, norgesterel), implant (norgesterel), IM (medroxy)Adverse Effects: Increase appetite, fatigue
Ipratoprium
Class: Muscarinic Antagonists - Quaternary AminesMOA: BronchodilationUse: asthma/COPDRoute: aerosol*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
Tiotoprium
Class: Muscarinic Antagonists - Quaternary AminesMOA: BronchodilationUse: asthma/COPD Route: aerosol*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
Pectin
MOA: absorb/bind intestinal toxinsUse: diarrhea
Zolmitriptan
Class: 5-HT agonists - selective - 5-HT1B/1DMOA: counteract CGRP –> cerebral vasoconstrictionUse: acute migraines (better choice than ergots)PK/PD: contraindicated in CADAdverse Effects: tingling, warm sensation, may mimic angina
Tropicamide
Class: Muscarinic Antagonists - Tertiary AminesMOA: decrease Ach –> inhibits bronchoconstriction and mucus secretion*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
Sotalol
Class: Class 3 anti-arrhythmeticsMOA: nonselective beta blockerUse: life threatening ventricular arrhythmia (first choice), supraventricular arrhythmia, wide-complex tachycardia. Can be used in kidsAdmin is oralAdverse Effects: Torsades de pointes
Flecainide
Class: Class 1C anti-arrhythmeticsMOA: strong Na channel block. blocks K channels. no change to AP.Use: supraventricular arrhythmia Admin is oralAdverse Effects: increased mortality with cardiac arrest or MI*must use on structurally healthy hearts
Bumetanide
Class: Loop diureticsMOA: inhibit NKCC –> decreased Na/Cl/K reabsorption –> osmotic diuresis. Change in potential –> Mg and Ca excretionUse: Pulmonary edema, CHF, HTN, acute hypercalcemia, hyperkalemnia, acute renal failurePK/PD: admin oral, IV, or IM. rapidly absorbed. Elimination = tubular secretion and absorptionAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, ototoxicity, dehydration, hyonatremia, metabolic alkalosis (contraction alkalosis)*hypomagnesemia –> increased PG production and renal blood flow aiding anti-hypertensive effect*Effective when GFR is low*more effective diuretic than thiazide*use ethacrynic acid of pt has sulfa allergy
Al Hydroxide
Class: AntacidsMOA: weak base neutralizes gastric acidUse: GERD pain relief, inactive peptic ulcer diseasePK/PD: Mg toxicity: CNS depression, sodium bicarb is systemicAdverse Effects: diarrhea (Mg), constipation (Ca, Al), hypophosphatemia (Al), renal stones (Na)
Carbaryl
Class: Cholinesterase Inhibitors - CarbamatesMOA: substrates for AChE –> bind serine hydroxyl and are hydrolyzedReversible
Butoxamine
Class: Beta Adrenoceptor Antagonists - β2 selective*not used for anything really
Glimepiride
Class: second generation sulfonylureasMOA: bind SUR1, which is complexed to K channel, inhibiting it –> depolarization –> Ca influx –> insulin secretionUse: DM IIPK/PD: admin oral. hepatic metabolism, renal excretion,Contraindications: DMI, pregnancy, lactationAdverse Effects: Hypoglycemia, weight gain, disulfiram-like reaction, sulfonamide hypersensitivity*2nd gen binds SUR1 with higher affinity
Aprepitant
Class: Neurokinin-1 receptor antagonistUse: chemo-induced emesis
Polythiazide
Class: Thiazide diureticsMOA: inhibit Na/Cl in DCT –> decreased Na/Cl reabsorption –> osmotic diuresis. Increased Ca reapsorptionUse: HTN (especially in AA and elderly), mild CHF, nephrolithiasis, nephrogenic DIPK/PD: oral admin, decrease Ca excretion, secretion = same as uric acid, anti-HTN as low doses, diuresis at high dosesAdverse Effects: hypokalemia, hyperuricemia, hyperglycemia, hyperlipidemia, contraction alkalosis*ineffective when GFR is low*more effective for HTN than loop diuretics
DHEA
DihydroepiadrostenedioneUse: Addison’s Dz
Lisinopril
Class: ACE inhibitors*pro-drugMOA: prevents formation of angiotensin II, decreases aldosterone, increases bradykinin, cumulatively, these have the effect of decreasing afterload and preloadUse: HTN, CHF, diabetic neuropathyAdverse Effects: dry, hacking cough (due to bradykinin), hyperkalemia
Diisopropylfluorophosphate
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleDistributes to CNSPralidoxime (2-PAM) treats poisoning
Ipodate
MOA: inhibits 5`-deiodinaseUse: hyperthyroidism
Orlistat
MOA: inhibits lipase –> decreased fat absorptionUse: obesityAdverse Effects: fatty stools
Rivastigmine
Class: Cholinesterase Inhibitors - CarbamatesMOA: substrates for AChE –> bind serine hydroxyl and are hydrolyzedUse: Dementia Reversible
Ca Carbonate
Class: AntacidsMOA: weak base neutralizes gastric acidUse: GERD pain relief, inactive peptic ulcer diseasePK/PD: Mg toxicity: CNS depression, sodium bicarb is systemicAdverse Effects: diarrhea (Mg), constipation (Ca, Al), hypophosphatemia (Al), renal stones (Na)
Acbertoline
Class: dopamine agonistMOA: D2 agonistUse: Parkinsonism, hyperprolactinemia, prolactinomaAdverse Effects: NandV, orthostatic hypotension, fluctuation in efficacy of motor control, abnormal involuntary movements, arrhythmia, hypersexuality, hallucinations, paranoia, anxiety, mania, depression
Nitroglycerin
Class: Nitrates - long actingMOA: sitmulates NO production –> stimulates guanylyl cyclase –> increase cGMP –> decrease phosphorylation of myosin light chain –> vasodilation –> decreased preloadUse: acute anginaAdmin: oral, ointment, buccal (slow-release), chewable or transdermalAdverse Effects: Reflex tachycardia and inotropy (increased O2 demand and reduced perfusion), headacheContraindications: HOCM and patients taking PDE inhibitors (“-fil” ex. sildenafil)*chronic use leads to tolerance (must have nitrate free intervals*toxicity = hypotension, headache, dizziness *veins dilated more than arteries*preferentially dilates epicardial arteries, which is where most ischemia occurs
Metyrapone
MOA: inhibits CYP11B1, preventing cortisol activationUse: hypercortisolismAdverse Effects: hirsutism, nausea, rash*only for compassionate use
Guanadrel
Class: Adrenergic Neuron AntagonistsUse: HTN
Spirinolactone
Class: Aldosterone antagonistsMOA: Increase Na secretion and K/H reabsorption. Also inhibits 17α-hydoxylaseUse: Hypokalemia (in combo w/ thiazide or loop), and PCOSAdverse Effects: Gynecomastia, impotence, hyperkalemia, hyperchloremic metabolic acidosis.
Propranolol
Class: Beta Adrenoceptor Antagonists - nonselectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid)Use: HTN, ischemia, supraventricular and ventricular arrhythmia, prevention of vfib, angina prophylaxis, migraine prevention (first choice), and tremorPK/PD: oral. well absorbed. extensive first pass metabolismAdverse Effects: asthma exacerbation, supersensitivity (with chronic use and abrupt discontinuation), delayed recovery of normoglycemia*toxicity = rash and sedation
Clomiphene
Class: ER agonistMOA: partial ER agonist –> reduce negative feedback by estradiol –> inc FSH/LH –> stimulate ovulationUse: infertility
Acetaminophen
MOA: unknown, does inhibit PG synthesisUse: analgesic and anti-pyreticPK/PD: metabolized by CYP450 and CYP2E1Adverse Effects: no anti-platelet activity, no GI side effects
Aliskiren
Class: Direct renin inhibitorMOA: inhibits reningUse: HTNPK/PD: dose-dependent reduction in renin*don’t use with renal disease
Novolin R
Class: short acting insulinUse: DM I and DKAAdmin IV for DKA
Bromocriptine
Class: dopamine agonistMOA: D2 agonistUse: Parkinsonism, hyperprolactinemia, prolactinomaAdverse Effects: NandV, orthostatic hypotension, fluctuation in efficacy of motor control, abnormal involuntary movements, arrhythmia, hypersexuality, hallucinations, paranoia, anxiety, mania, depression
Alendronate
Class: bisphophonatesMOA: pyrophosphate analogs –> inhibit osteoclasts, thereby inhibiting bone resorptionUse: hypercalcemia (in malignancy), osteoporosis, ectopic calcification, Paget’s diseasePK/PD: poorly absorbedAdverse Effects: gastric/esophageal irritation, osteonecrosis of the jaw –> fractures*bone remodeling occurs in jaw more than other bones, which requires osteoclast activity
Beclomethasone
Class: GlucocorticoidsMOA: inhibits cytokines –> decrease airway reactivity –> bronchodilation, decrease edema. Increase lipocortin, which inhibits PLA2Use: Asthma and RAPK/PD: admin oral, IV, or aerosolAdverse Effects: Typical steroid effects (especially w/ oral admin), oral candidiasis, and hoarseness
Oxandrolone
Class: Androgens*more anabolicUse: Hypogonadism and anemiaAdverse Effects: feminizing effects in post-pubertal males (due to conversion to estrogen)
Rosuvastatin
Class: HMG-CoA reductase inhibitorsMOA: reduce hepatic formation of cholesterol. Increase LDL receptors on hepatocytes –> lower plasma LDLUse: lower plasma LDLPK/PD: good GI absorption, hepatic metabolism by CYPs, high first pass metabolism, bile excretion, contraindicated in pregnancy, admin at night when most cholesterol synthesis occursAdverse Effects: hepatotoxicity, rhabdomyolysis (increase CK)*reduces mortality from CVD and MI
Methylcellulose
MOA: bulk forming laxativeUse: constipation
Penbutolol
Class: Beta Adrenoceptor Antagonists - nonselectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid)Use: HTN, ischemia, angina prophylaxis, migraine prevention (first choice)PK/PD: oral. well absorbed. Adverse Effects: asthma exacerbation, supersensitivity (with chronic use and abrupt discontinuation), delayed recovery of normoglycemia*toxicity = rash and sedation
Ethynodiol Diacetate
Class: ProgestinsMOA: proliferation of mammary acini. thermogenic. moderately anabolic. growth of endometrium. progestational (esp. norgestrel). estrogenic activity (esp. norethynodrel, ethynodiol diacetate). anti-estrogenic activity. androgenic activity (exc. norgestrel, desogestrel)Use: Oral contraception (combo or alone [not at effective])PK/PD: high first pass metabolism. admin oral (norethindrone, norgesterel), implant (norgesterel), IM (medroxy)Adverse Effects: Increase appetite, fatigue
Zileuton
Class: 5-LOX inhibitorUse: Asthma
Mivacurium
Class: Nicotinic Antagonists - Quaternary ParalyticsMOA: competitive blockage of autonomic nicotinic receptors –> decrease in arteriolar and vasomotor tone.
Pyridostigmine
Class: Cholinesterase Inhibitors - CarbamatesMOA: substrates for AChE –> bind serine hydroxyl and are hydrolyzedUse: Treat MG Reversible
Naproxen
Class: NSAIDMOA: block PGE2 in CNS –> resets temp control –> anti-pyretic Use: analgesic, anti-pyretic, anti-inflammatory (high dose only), inhibit platelet aggregation, gout (indo), ankylosing spondylitis (indo), OA (indo), patent ductus arteriosus (indo)PK/PD: admin oral or parenteral (ketorolac). COX-1 inhibition –> no thromboxane –> anti-platelet activityover-activation of LOX pathway –> hypersensitivityAdverse Effects: GI (esp. ulcers), hepatotoxicity, nephrotoxicity, prolonged bleeding time, hypersensitivity, hematologic toxicity (indo), sore throat (indo)*when used chronically, give misoprostol or PPI to prevent ulcers
Tegaserod
Class: 5-HT agonists - selective - 5-HT4Use: IBS w/ constipation*for emergencies only
Conivaptan
Class: Vasopressin receptor antagonistMOA: decrease aquaporins –> water retention in collecting tubuleUse: SIADH, CHF, hyponatremia*admin IVAdverse Effects: Hypernatremia, nephrogenic DI
Glyburide
Class: second generation sulfonylureasMOA: bind SUR1, which is complexed to K channel, inhibiting it –> depolarization –> Ca influx –> insulin secretionUse: DM IIPK/PD: admin oral. hepatic metabolism, renal excretion,Contraindications: DMI, pregnancy, lactationAdverse Effects: Hypoglycemia, weight gain, disulfiram-like reaction, sulfonamide hypersensitivity*2nd gen binds SUR1 with higher affinity
Triamcinolone
Class: Glucocorticoids - intermediate-actingMOA: inhibits cytokines –> decrease airway reactivity –> bronchodilation, decrease edema. Increase lipocortin, which inhibits PLA2Use: Asthma and RA PK/PD: admin oral, IV, or aerosolAdverse Effects: Typical steroid effects (especially w/ oral admin), oral candidiasis, and hoarseness
Ibutilide
Class: Class 3 anti-arrhythmeticsMOA: block rectifier K channelUse: Afib or flutter Admin is oralAdverse Effects: prolonged QT and torsades
Flunosilide
Class: GlucocorticoidsMOA: inhibits cytokines –> decrease airway reactivity –> bronchodilation, decrease edema. Increase lipocortin, which inhibits PLA2Use: Asthma and RAPK/PD: admin oral, IV, or aerosolAdverse Effects: Typical steroid effects (especially w/ oral admin), oral candidiasis, and hoarseness
Trimethobenzamide
Class: D2 antagonistsMOA: dopamine receptor antagonistsUse: acute migraine attacks, vomiting (cancer chemo, pot-op)Adverse Effects: extrapyramidal like adverse effects, drowsiness, torsades, neuroleptic malignant syndrome, increased prolactin secretion
Brompheniramine
Class: H1 antagonists - first generationMOA: anti-cholinergic. blocks Na channel (anesthesia)Use: allergic rhinitis or urticaria, motion sickness, local anesthesia, nausea, vomiting, insomnia PK/PD: well-absorbed, inhibit CYP450, cross BBBAdverse Effects: sedation (anti-cholinergic), urinary retention (anti-muscarinic)*cyclizine, meclizine have least sedative effect
Abarelix
Class: GnRH antagonistsMOA: suppress gonadotropin releaseUse: prostate cancerAdverse Effects: allergy and syndrome of androgen deprivation
Triamterene
Class: ENaC channel blockersMOA: inhibit ENaC (Na reabsorption) –> loss of potential (driving force for K section) –> decreased K/H secretionUse: primary mineralocorticoid hypersecretion, secondary aldosteronism (ex. CHF, hepatic cirrhosis) Adverse Effects: nephrolithiasis
Dobutamine
Class: CatecholaminesMOA: α1, β1 agonistUse: Shock, heart failure, anaphylaxis, fundoscopic eye exams*Metyrosine inhibits tyrosine hydroxylase, preventing formation of catecholamines*Reserpine inhibits NE uptake into vesicles (VMAT)
Ondansetron
Class: 5-HT3 antagonists Use: chemo-induced vomiting
Ambenonium
Class: Cholinesterase Inhibitors - CarbamatesMOA: substrates for AChE –> bind serine hydroxyl and are hydrolyzedReversible
Tamoxifen
Class: SERMMOA: partial ER agonists –> antagonistic activity in presence of normal hormone levelsUse: ER + breast cancerPK/PD: in premenopausal women, SERM is antagonist in all tissues. in postmenopausal women, SERM is agonist in all except mammary tissueAdverse Effects: in postmenopausal women, increased risk of endometrial cancer*in postmenopausal women, hormone levels remain high in mammary tissue
Tacrine
Class: Cholinesterase InhibitorsUse: Dementia and Alzheimer’sAdverse Effects: Hepatotoxicity
Cypropheptadine
Class: H1 antagonists - first generationMOA: anti-cholinergic. blocks Na channel (anesthesia)Use: allergic rhinitis or urticaria, motion sickness, local anesthesia, nausea, vomiting, insomnia PK/PD: well-absorbed, inhibit CYP450, cross BBBAdverse Effects: sedation (anti-cholinergic), urinary retention (anti-muscarinic)*cyclizine, meclizine have least sedative effect
Methylphenidate
Class: Indirect SympathomimeticsUse: ADHDAdverse Effects: Insomnia, anorexia, weight loss
Lobeline
Class: Direct Nicotinic AgonistsPK/PD: Excess agonist activity results in depolarizing blockade of autonomic ganglia –> flaccid paralysis Distributes to CNS- Tertiary
Acebutolol
Class: Beta Adrenoceptor Antagonists - β1 selectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid), inhibit conversion of T3 to T4Use: hyperthyroidismPK/PD: oral, well absorbed Adverse Effects: due to specificity, no pulmonary effects *has intrinsic sympathomimetic activity and can protect against asthma, bradycardia, and altered lipid profile
Diclofenac
Class: NSAIDMOA: block PGE2 in CNS –> resets temp control –> anti-pyretic Use: analgesic, anti-pyretic, anti-inflammatory (high dose only), inhibit platelet aggregation, gout (indo), ankylosing spondylitis (indo), OA (indo), patent ductus arteriosus (indo)PK/PD: admin oral or parenteral (ketorolac). COX-1 inhibition –> no thromboxane –> anti-platelet activityover-activation of LOX pathway –> hypersensitivityAdverse Effects: GI (esp. ulcers), hepatotoxicity, nephrotoxicity, prolonged bleeding time, hypersensitivity, hematologic toxicity (indo), sore throat (indo)*when used chronically, give misoprostol or PPI to prevent ulcers
Megesterol
Class: ProgestinsMOA: proliferation of mammary acini. thermogenic. moderately anabolic. growth of endometrium. progestational (esp. norgestrel). estrogenic activity (esp. norethynodrel, ethynodiol diacetate). anti-estrogenic activity. androgenic activity (exc. norgestrel, desogestrel)Use: Oral contraception (combo or alone [not at effective])PK/PD: high first pass metabolism. admin oral (norethindrone, norgesterel), implant (norgesterel), IM (medroxy)Adverse Effects: Increase appetite, fatigue
Bethanechol
Class: Direct Muscarinic Agonists - Choline EstersUse: Stimulate GI/GU smooth muscle (ex. post-op)PK/PD: poor CNS distribution Resistant to AchE
Atenololol
Class: Beta Adrenoceptor Antagonists - β1 selectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid), inhibit conversion of T3 to T4Use: hyperthyroidismPK/PD: oral, well absorbed, better tolerated in elderlyAdverse Effects: due to specificity, no pulmonary effects
Methoscopolamine
Class: Muscarinic Antagonists - Quaternary Amines*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
Cholestyramine
Class: Bile acid binding resinsMOA: bind bile acids –> increase lipid excretion –> lower LDL. Increase bile acid synthesis. Increase LDL receptorsUse: primary hypercholesterolemia, digoxin toxicityAdverse Effects: bloating, constipation may impair absorption of other drugs/fat soluble vitamins. increased triglycerides
Fluvastatin
Class: HMG-CoA reductase inhibitorsMOA: reduce hepatic formation of cholesterol. Increase LDL receptors on hepatocytes –> lower plasma LDLUse: lower plasma LDL PK/PD: good GI absorption, hepatic metabolism by CYPs, high first pass metabolism, bile excretion, contraindicated in pregnancy, admin at night when most cholesterol synthesis occursAdverse Effects: hepatotoxicity, rhabdomyolysis (increase CK)*reduces mortality from CVD and MI
Phenoxybenzamine
Class: Alpha Adrenoceptor Antagonists - nonselectiveMOA: reduces TPR and MAPUse: PheochromocytomaAdverse Effects: Orthostatic hypotension and reflex tachycardia*irreversible*also a 5-HT2 antagonist
Treprostinil
Class: PGI2MOA: relax smooth muscle Use: pulmonary HTNAdverse Effects: GI upset
Dobutamine
Class: Direct Adrenoceptor Agonists - β1 selectiveMOA: increase heart rate
Epinephrine
Class: CatecholaminesMOA: α1, α2, β1, β2 agonistUse: Shock, heart failure, anaphylaxis, fundoscopic eye exams*Metyrosine inhibits tyrosine hydroxylase, preventing formation of catecholamines*Reserpine inhibits NE uptake into vesicles (VMAT)
Fosinopril
Class: ACE inhibitors*pro-drugMOA: prevents formation of angiotensin II, decreases aldosterone, increases bradykinin, cumulatively, these have the effect of decreasing afterload and preloadUse: HTN, CHF, diabetic neuropathyAdverse Effects: dry, hacking cough (due to bradykinin), hyperkalemia
Droperidol
Class: D2 antagonistsMOA: dopamine receptor antagonistsUse: acute migraine attacks, vomiting (cancer chemo, pot-op)Adverse Effects: extrapyramidal like adverse effects, drowsiness, torsades, neuroleptic malignant syndrome, increased prolactin secretion
Repaglinide
Class: meglitinide (like sulfonylureas)MOA: bind SUR1Use: DM IIPK/PD: rapid onset and short durationAdverse Effects: hypoglycemia*Use if pt has sulfa allergy
Physostigmine
Class: Cholinesterase Inhibitors - CarbamatesMOA: substrates for AChE –> bind serine hydroxyl and are hydrolyzedUse: Glaucoma, anti-cholinergic overdose Reversible Distributes to CNS - TertiaryAdverse Effects: CNS toxicity
Eletriptan
Class: 5-HT agonists - selective - 5-HT1B/1DMOA: counteract CGRP –> cerebral vasoconstrictionUse: acute migraines (better choice than ergots)PK/PD: contraindicated in CADAdverse Effects: tingling, warm sensation, may mimic angina
Carvedilol
Class: Beta and Alpha Adrenoceptor Antagonists - nonselectiveMOA: slowed AV conduction –> decreased chronotropy and inotropy, decreased HR, decreased MAP + decreased BP, bronchoconstriction, decreased aqueous humor production, inhibits lipolysis/glycogenolysis –> increased VLDL and decreased HDL, blocks excess catecholamine production (hyperthyroid)Use: HTN, ischemia, angina prophylaxis, migraine prevention (first choice)PK/PD: oral. well absorbed. Adverse Effects: asthma exacerbation, supersensitivity (with chronic use and abrupt discontinuation), delayed recovery of normoglycemia*toxicity = rash and sedation
Carteolol
Class: Beta BlockerMOA: Intrinsic sympathomimetic activity (NO production)
Difenoxin
Class: opioid analogues MOA: inhibit Ach release onto intestinal opioid receptors –> decreased motilityUse: diarrhea
Sumatriptan
Class: 5-HT agonists - selective - 5-HT1B/1DMOA: counteract CGRP –> cerebral vasoconstrictionUse: acute migraines (better choice than ergots)PK/PD: contraindicated in CADAdverse Effects: tingling, warm sensation, may mimic angina
Acetazolamide
Class: carbonic anhydrase inhibitorsMOA: inhibit CA preventing breakdown of carbonic acid and absorption of bicarbonate –> osmotic diuresisUse: promotes urinary alkalinization and prevents acute altitude sicknessPK/PD: admin oral or topical. decreases NH4 secretion*contraindicated in hepatic cirrhosis (b/c alkaline urine traps NH4 as ammonia –> reabsorbed –> hepatic encephalopathy)Adverse Effects: Type II RTA
