Master drugs Flashcards
1
Q
Epoprostenol
A
Class: PGI2MOA: relax smooth muscle Use: pulmonary HTNAdverse Effects: GI upset
2
Q
Methazolamide
A
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
3
Q
Mecamylamine
A
Class: Nicotinic Antagonists - Tertiary Ganglion BlockersMOA: competitive blockage of autonomic nicotinic receptors –> decrease in arteriolar and vasomotor tone.PK/PD: can distribute to CNS
4
Q
Sorbitol
A
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
5
Q
Glycopyrolate
A
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
6
Q
Dimenhydrinate
A
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
7
Q
Terbutaline
A
Class: Direct Adrenoceptor Agonists - β2 selectiveMOA: increase cAMP –> bronchodilation and smooth muscle relaxationUse: asthma, status asthmaticus, and uterine relaxation in premature laborAdverse effects: tremors
8
Q
Procainamide
A
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
9
Q
Hydrocortisone
A
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
10
Q
Echothiophate
A
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleDistributes to CNSPralidoxime (2-PAM) treats poisoning
11
Q
Diazoxide
A
Class: direct vasodilatorsMOA: K channel activation –> hyperpolarization. Arterial dilationUse: HTN Admin IVAdverse Effects: reflex tachycardia, fluid retention, HA, palpitation
12
Q
Fosaprepitant
A
Class: Neurokinin-1 receptor antagonistUse: chemo-induced emesis
13
Q
Norethynodrel
A
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
14
Q
Cabergoline
A
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
15
Q
Phenylephrine
A
Class: Direct Adrenoceptor Agonists - α1 selectiveUse: mydriasis (eye exams) and nasal decongestion
16
Q
Valsartan
A
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
17
Q
Torsemide
A
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
18
Q
Soman
A
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleUse: war gasDistributes to CNSPralidoxime (2-PAM) treats poisoning
19
Q
Ethinyl Estradiol
A
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
20
Q
Quinidine
A
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
21
Q
Metoprolol
A
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
22
Q
Progesterone
A
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
23
Q
Sarin
A
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleUse: war gasDistributes to CNSPralidoxime (2-PAM) treats poisoning
24
Q
Cabergoline
A
Class: Dopamine receptor agonistsUse: GH excess, tumors secreting GH and PRL
25
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
26
Dibasic Calcium Phosphate
Use: hypocalcemia and osteoporosis prophylaxis
27
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
28
Muscarine
Class: Direct Muscarinic Agonists - AlkaloidsMOA: Contracts iris sphincter, increases aqueous humor drainageUse: Acute glaucoma
29
Nesiritide
Class: BNP analogMOA: increases cGMP --\> arteriolar and venous dilation --\> reduced afterload and preload. Causes natuiresisUse: actue tx of HF
30
Aspart
Class: Rapid acting insulinUse: DM I
31
Calcitriol
MOA: 1, 25 dihydroxy vitamin DUse: nutritional rickets, metabolic rickets, hypoparathyroidism, osteoporosis
32
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
33
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
34
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
35
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
36
Sitagliptin
MOA: inhibits DDP4 --\> preventing incretin degradationUse: DM II (combo w/ other tx)
37
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
38
MDMA
Class: Indirect SympathomimeticsAdverse Effects: Insomnia, anorexia, weight loss
39
Tolvaptan
Class: Vasopressin receptor antagonistMOA: decrease aquaporins --\> water retention in collecting tubuleUse: SIADH, CHF, hyponatremia\*admin oralAdverse Effects: Hypernatremia, nephrogenic DI
40
Prenalterol
Class: Direct Adrenoceptor Agonists - β1 selectiveMOA: increase heart rate\*partial agonist
41
Fludrocortisone
Class: mineralocorticoidMOA: mineralocorticoid actionUse: salt-losing syndrome
42
Vytorin
Ezetimibe + simvastatin
43
Anastrazole
Class: Atomatase inhibitorsMOA: Inhibit aromatase --\> reduce estrogen synthesisUse: tamoxifen resistant breast cancerPK/PD: non-steroidal and reversible (except exemestane)
44
Mannitol
Class: osmotic diuretic
45
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
46
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
47
Senna
Class: AnthraquinonesMOA: stimulant laxativesUse: constipation
48
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
49
Yohimbine
Class: Alpha Adrenoceptor Antagonists - α2 selectiveUse: nothing (purported to treat ED)Adverse Effects: orthostatic hypotension and reflex tachycardia
50
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
51
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
52
Terazosin
Class: Alpha Adrenoceptor Antagonists - α1 selectiveUse: hypertension and PTSDPK/PD: long half lifeAdverse Effects: orthostatic hypotension (lowest risk with tamsulosin), reflex tachycardia
53
Carboprost
Class: PGF2MOA: relax smooth muscleUse: post-partum hemorrhage Adverse Effects: GI upset
54
(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
55
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
56
Omalizumab
Class: Anti-IgE AbMOA: inhibits IgE binding to mast cells --\> decrease mast cell activation --\> bronchodilationUse: asthma
57
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
58
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
59
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
60
Testosterone Enanthate
Class: Androgens\*more androgenicUse: Hypogonadism and anemiaAdverse Effects: feminizing effects in post-pubertal males (due to conversion to estrogen)
61
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
62
Hyoscyamine
Class: anticholinergicsMOA: anti-spasmodic activityUse: IBS
63
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
64
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)
65
Dolasetron
Class: 5-HT3 antagonists Use: chemo-induced vomiting
66
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)
67
Latanoprost
Class: PGF2MOA: relax smooth muscleUse: open angle glaucomaAdverse Effects: GI upset
68
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
69
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
70
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)
71
Trimethaphan
Class: Nicotinic Antagonists - Quaternary Ganglion BlockersMOA: competitive blockage of autonomic nicotinic receptors --\> decrease in arteriolar and vasomotor tone.
72
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
73
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
74
Alosetron
Class: 5-HT3 antagonists Use: chemo-induced vomiting and IBS w/ diarrhea predominance
75
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
76
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
77
Glulisine
Class: Rapid acting insulinUse: DM I
78
Mg Citrate
Class: saline laxativesMOA: non-absorbable salt --\> increase osmotic activity in lumenUse: constipationContraindications: renal insufficiency, heart disease, diuretic treatment
79
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
80
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)
81
Dinopristone
Class: PGE2MOA: induce cervical ripeningUse: induce labor and NSAID induced ulcerAdverse Effects: GI upset
82
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
83
Ketoconazole
MOA: inhibits CYP17, preventing steroidogenesisUse: Cushing'sAdverse Effects: hepatic dysfunction
84
Glargine
Class: long acting insulinUse: DM I (used to maintain basal insulin levels)
85
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
86
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
87
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
88
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
89
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
90
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
91
Fadrazole
Class: Atomatase inhibitorsMOA: Inhibit aromatase --\> reduce estrogen synthesisUse: tamoxifen resistant breast cancerPK/PD: non-steroidal and reversible (except exemestane)
92
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
93
Fulvestrant
Class: ER antagonist MOA: pure ER antagonistUse: breast cancer (if SERM and aromatase inhibitor tx fails)
94
Simcor
Niacin + simvastatin
95
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
96
Ezetimibe
Class: Cholesterol absorption inhibitorMOA: inhibits intestinal absorption of cholesterol and phylosterolsUse: lower plasma LDL, primary hypercholesterolemiaAdverse Effects: steatorrhea, hepatotoxicity
97
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)
98
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
99
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
100
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
101
Donepezil
Class: Cholinesterase InhibitorsUse: Dementia and Alzheimer'sAdverse Effects: Muscle cramps, GI upset
102
Bosentan
Class: Endothelin receptor antagonistMOA: arterial dilationUse: pulmonary HTNAdverse Effects: hypotension, hepatotoxicity, tachycardia, flushing
103
Clonidine
Class: Direct Adrenoceptor Agonists - α2 selectiveMOA: increase reuptake of catecholamines --\> decreased sympathetic stimulationUse: hypertensionAdverse Effects: hypertensive crisis with abrupt withdrawal and dry mouth
104
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
105
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
106
Montelukast
Class: Leukotriene AntagonistMOA: LTD4 receptor antagonist --\> bronchodilationUse: asthmaPK/PD: admin is oral (good for kids)
107
Phentolamine
Class: Alpha Adrenoceptor Antagonists - nonselectiveMOA: reduces TPR and MAPUse: PheochromocytomaAdverse Effects: Orthostatic hypotension and reflex tachycardia\*reversible
108
Cascara Sagrada
Class: AnthraquinonesMOA: stimulant laxativesUse: constipation
109
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
110
NPH humulin N
Class: intermediate acting insulinUse: DM I
111
Pseudoephedrine
Class: Indirect SympathomimeticsPK/PD: CNS stimulationAdverse Effects: Insomnia, anorexia, weight loss
112
Hydralazine
Class: direct vasodilatorsMOA: arterial dilationUse: pre-eclampsia Admin IVAdverse Effects: lupus-like syndrome, reflex tachycardia, fluid retention, HA, palpitation
113
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
114
Dranabinol
MOA: unknown mechanismUse: vomiting
115
Alprazolam
Class: benzodiazepines Use: vomiting
116
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
117
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
118
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
119
Cyproheptadine
Class: 5-HT2 antagonists Use: serotonin syndrome \*serotonin syndrome = HTN, hyperreflexia, tremor, clonus, hyperthermia, mydriasis, agitation, coma
120
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
121
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
122
Desmopressin
Class: Vasopressin agonistMOA: predominantly V2 agonist, anti-diuresis, vasoconstrictionUse: HTN, neurogenic diabetes insipidus\*desmopressin is more potent and longer lasting than vasopressin
123
Potassium Iodide
MOA: thyroglobulin proteolysis and hormone releaseUse: pre-op prepAdverse Effects: depression, insomnia, impotence
124
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
125
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
126
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)
127
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
128
Oxymetazoline
Class: Direct Adrenoceptor Agonists - α1 selectiveUse: mydriasis (eye exams) and nasal decongestion\*topical administration
129
Flulnarizine
MOA: Ca channel blockerUse: preventative tx for migraine
130
Humulin R
Class: short acting insulinUse: DM I and DKAAdmin IV for DKA
131
Ephedrine
Class: Indirect SympathomimeticsPK/PD: CNS stimulationAdverse Effects: Insomnia, anorexia, weight loss\*direct sympathomimetic activity
132
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
133
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
134
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
135
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
136
Octreotide
Class: Somatostatin analogMOA: inhibits pituitary release of GHUse: GH excess, insulinoma, VIPomaAdverse Effects: GI toxicity, vitamin B12 deficiency
137
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
138
Katanserin
Class: 5-HT2 antagonists \*also an alpha 1 antagonistUse: HTN \*serotonin syndrome = HTN, hyperreflexia, tremor, clonus, hyperthermia, mydriasis, agitation, coma
139
Methoxamine
Class: Direct Adrenoceptor Agonists - α1 selectiveUse: mydriasis (eye exams) and nasal decongestion
140
Nicotine
Class: Direct Nicotinic AgonistsPK/PD: Excess agonist activity results in depolarizing blockade of autonomic ganglia --\> flaccid paralysis Distributes to CNS- Tertiary
141
Exemestane
Class: Atomatase inhibitorsMOA: Inhibit aromatase --\> reduce estrogen synthesisUse: tamoxifen resistant breast cancerPK/PD: non-steroidal and reversible (except exemestane)
142
Xylometazoline
Class: Direct Adrenoceptor Agonists - α1 selectiveUse: mydriasis (eye exams) and nasal decongestion\*topical administration
143
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
144
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
145
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
146
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
147
Kaolin
MOA: absorb/bind intestinal toxinsUse: diarrhea
148
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
149
Glucagon
MOA: promotes glucose release from tissues and gluconeogenesis, increase cAMP in cardiac tissueUse: sever hypoglycemia and cardiac stimulant (as in beta blocker OD)
150
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
151
Degarelix
Class: GnRH antagonistsMOA: suppress gonadotropin releaseUse: prostate cancer
152
Cisapride
Class: 5-HT agonists - selective - 5-HT4Use: GERD \*for compassionate use only
153
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)
154
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
155
Methyltestosterone
Class: Androgens\*more androgenicUse: Hypogonadism and anemiaAdverse Effects: feminizing effects in post-pubertal males (due to conversion to estrogen)
156
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
157
Brinzolamide
Class: carbonic anhydrase inhibitorsMOA: decrease aqueous humor productionUse: glaucomaPK/PD: admin ophthalmic
158
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
159
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
160
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)
161
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
162
Iloprost
Class: PGI2MOA: relax smooth muscle Use: pulmonary HTNAdverse Effects: GI upset
163
Loperamide
Class: opioid analogues MOA: inhibit Ach release onto intestinal opioid receptors --\> decreased motilityUse: diarrhea
164
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
165
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)
166
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
167
Ricinoleic Acid (Castor Oil)
MOA: stimulant laxativesUse: constipation
168
Lisdexmethamphetamine
Class: Indirect SympathomimeticsUse: ADHDAdverse Effects: Insomnia, anorexia, weight loss
169
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)
170
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
171
Parathion
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleUse: InsecticideDistributes to CNSPralidoxime (2-PAM) treats poisoning
172
Aminoglutethimide
MOA: inhibits CYP11A1, preventing steroidogenesisUse: Cushing'sAdverse Effects: adrenal insufficiency
173
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
174
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
175
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
176
Eplerenone
Class: Aldosterone antagonistsMOA: increase Na secretion and K/H reabsorptionUse: Hypokalemia (in combo w/ thiazide or loop)Adverse Effects: Hyperkalemia, hyperchloremic metabolic acidosis
177
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
178
Potassium
Class: Class 5 (misc.) anti-arrhythmeticsMOA: hyperpolarization --\> decrease phase 4 slopeAdmin IV
179
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
180
Dostinex
Class: Dopamine receptor agonistsUse: GH excess, tumors secreting GH and PRL
181
Stanozol
Class: Androgens\*more anabolicUse: Hypogonadism and anemiaAdverse Effects: feminizing effects in post-pubertal males (due to conversion to estrogen)
182
Bismuth Subsalicylate
Class: mucosal protective agentsMOA: coats ulcer tissue, antibacterial actionUse: h. pylori and diarrheaAdverse Effects: turn tongue black
183
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
184
Aloe
Class: AnthraquinonesMOA: stimulant laxativesUse: constipation
185
Bisacodyl
Class: diphenylmethane derivativesMOA: induce low grade inflammation --\> water/electrolyte accumulationUse: constipationPK/PD: admin suppository
186
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
187
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
188
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
189
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
190
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
191
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
192
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
193
Formeterol
Class: Direct Adrenoceptor Agonists - β2 selectiveMOA: increase cAMP --\> bronchodilation and smooth muscle relaxationUse: asthmaAdverse effects: tremors\*long acting
194
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
195
Magnesium
Class: Class 5 (misc.) anti-arrhythmeticsMOA: unknownUse: Torsades de pointesAdmin IV
196
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
197
Desipramine
Class: tricyclic antidepressants Use: IBS associated abdominal pain
198
Doxazosin
Class: Alpha Adrenoceptor Antagonists - α1 selectiveUse: BPH and HTNPK/PD: long half lifeAdverse Effects: orthostatic hypotension (lowest risk with tamsulosin), reflex tachycardia
199
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
200
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
201
Ritodrine
Class: Direct Adrenoceptor Agonists - β2 selectiveMOA: increase cAMP --\> bronchodilation and smooth muscle relaxationUse: asthma and uterine relaxation in premature laborAdverse effects: tremors
202
Methamphetamine
Class: Indirect SympathomimeticsPK/PD: CNS stimulationAdverse Effects: Insomnia, anorexia, weight loss
203
Dorzolamide
Class: carbonic anhydrase inhibitorsMOA: decrease aqueous humor productionUse: glaucomaPK/PD: admin ophthalmic
204
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
205
Tetrahydrocannabinol
MOA: unknown mechanismUse: vomiting
206
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
207
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
208
Teriparatide
MOA: recombinant PTHUse: osteoporosis treatment
209
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
210
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
211
Iohexol
Class: iodinated contract materialMOA: inhibits 5`-deiodinaseUse: hyperthyroidismPK/PD: admin oral or IV, acts in liver, kidney, pituitary and brain
212
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)
213
Dofetilide
Class: Class 3 anti-arrhythmeticsMOA: block rectifier K channelUse: Afib or flutterAdmin is oralAdverse Effects: prolonged QT and torsades
214
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)
215
Tyramine
Class: Indirect SympathomimeticsMOA: outcompetes NE for uptake into vesicles via VMATAdverse Effects: hypertensive crisis especially in those taking MAOIs, insomnia, anorexia, weight loss
216
Docusate
Class: stool softenerMOA: softens stool, promoting expulsionUse: constipation (especially in hospitalized pts.)Adverse Effects: decreased absorption of fat soluble vitamins
217
Mineral Oil
Class: stool softenerMOA: softens stool, promoting expulsionUse: constipation (especially in hospitalized pts.)Adverse Effects: decreased absorption of fat soluble vitamins
218
Demecarium
Class: Cholinesterase Inhibitors - CarbamatesMOA: substrates for AChE --\> bind serine hydroxyl and are hydrolyzedReversible
219
Letrozole
Class: Atomatase inhibitorsMOA: Inhibit aromatase --\> reduce estrogen synthesisUse: tamoxifen resistant breast cancerPK/PD: non-steroidal and reversible (except exemestane)
220
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
221
Finasteride
Class: anti-androgens MOA: inhibits 5α-reductase, preventing synthesis of DHTUse: BPH and male pattern baldness
222
Diphenoxylate
Class: opioid analogues MOA: inhibit Ach release onto intestinal opioid receptors --\> decreased motilityUse: diarrheaAdverse Effects: sedation\*avoid abuse w/ atropine
223
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
224
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
225
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)
226
Acetylcholine
Class: Direct Muscarinic Agonists - Choline EstersUse: Stimulate GI/GU smooth muscle (ex. post-op)PK/PD: poor CNS distribution
227
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
228
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
229
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
230
Propantheline
Class: Muscarinic Antagonists - Quaternary Amines\*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
231
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
232
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
233
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
234
Amphetamine
Class: Indirect SympathomimeticsMOA: promotes Ca-dependent vesicle fusionPK/PD: CNS stimulation. Not catabolized by MAOAdverse Effects: Insomnia, anorexia, weight loss, psychosis
235
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
236
(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
237
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
238
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
239
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
240
Fenoldopam
Class: direct vasodilatorsMOA: D1 agonist --\> arterial dilation --\> reduced afterloadUse: HTN Admin IVAdverse Effects: reflex tachycardia, fluid retention, HA, palpitation
241
Topiramate
Class: anti-convulsants Use: preventative tx for migraine
242
Lispro
Class: Rapid acting insulinUse: DM I
243
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
244
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)
245
Buspirone
Class: 5-HT agonists - selective - 5HT1A partial agonistUse: anxiolytic PK/PD: slow onset Adverse Effects: dysphoria (high dose)
246
Rimonabant
MOA: reduces appetiteUse: obesity
247
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
248
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
249
Liothyronine
MOA: isomer of T3Use: hypothyroidism and myxedema comaPK/PD: acts faster than T4,l but shorter half lifeAdverse Effects: cardiotoxicity
250
Loratidine
251
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
252
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
253
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
254
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
255
Alprostadil
Class: PGE1MOA: relax smooth muscle, bind prostaglandin receptors on gastric epitheliumUse: ED\*contraindicated in pregnancyAdverse Effects: GI upset
256
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
257
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
258
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
259
Nebivolol
Class: Beta BlockerMOA: Cardioselective and vasodilatory (NO production)
260
Diatriozate
Class: iodinated contract materialMOA: inhibits 5`-deiodinaseUse: hyperthyroidismPK/PD: admin oral or IV, acts in liver, kidney, pituitary and brain
261
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
262
Dycyclomine
Class: anticholinergicsMOA: anti-spasmodic activityUse: IBS
263
Tolazoline
Class: Alpha Adrenoceptor Antagonists - nonselectiveMOA: reduces TPR and MAPUse: PheochromocytomaAdverse Effects: Orthostatic hypotension and reflex tachycardia
264
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
265
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
266
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
267
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
268
Pegvisomant
MOA: GH receptor antagonistUse: GH excessAdverse Effects: hepatotoxicity\*may assist tumor growth
269
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
270
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
271
Vasopressin
Class: Vasopressin agonistMOA: predominantly V2 agonist, anti-diuresis, vasoconstrictionUse: HTN, neurogenic diabetes insipidus\*desmopressin is more potent and longer lasting than vasopressin
272
Guanabenz
Class: Direct Adrenoceptor Agonists - α2 selectiveMOA: increase reuptake of catecholamines --\> decreased sympathetic stimulationUse: hypertensionAdverse effects: hypertensive crisis with abrupt withdrawal
273
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
274
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
275
Trimazosin
Class: Alpha Adrenoceptor Antagonists - α1 selectiveUse: hypertensionPK/PD: long half lifeAdverse Effects: orthostatic hypotension (lowest risk with tamsulosin), reflex tachycardia
276
Amrinone
Class: PDE inhibitorsMOA: increase cAMP and Ca --\> increased contractility and vasodilation (arteriolar). Increased contractilityUse: acute tx of HF
277
Testosterone
Class: Androgens\*more androgenicUse: Hypogonadism and anemiaAdverse Effects: feminizing effects in post-pubertal males (due to conversion to estrogen)
278
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
279
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
280
Salmeterol
Class: Direct Adrenoceptor Agonists - β2 selectiveMOA: increase cAMP --\> bronchodilation and smooth muscle relaxationUse: asthmaAdverse effects: tremors\*long acting
281
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
282
Lanreotide
Class: Somatostatin analogMOA: inhibits pituitary release of GHUse: GH excess, insulinoma, VIPomaAdverse Effects: GI toxicity, vitamin B12 deficiency\*long-acting
283
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
284
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
285
Milrinone
Class: PDE inhibitorsMOA: increase cAMP and Ca --\> increased contractility and vasodilation (arteriolar). Increased contractilityUse: acute tx of HF
286
Levothyroxine
MOA: isomer of T4Use: hypothyroidism (first line)Adverse Effects: headache and nervousness
287
NPH novolin N
Class: intermediate acting insulinUse: DM I
288
Cibacalcin
MOA: synthetic calcitoninUse: osteoporosis treatment and hypercalcemiaPK/PD: admin IM\*high Ca due to vitamin D excess, bone cancer, hyper PTH, etc.
289
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
290
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)
291
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
292
Rocuronium
Class: Nicotinic Antagonists - Quaternary ParalyticsMOA: competitive blockage of autonomic nicotinic receptors --\> decrease in arteriolar and vasomotor tone.
293
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
294
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
295
Dexmethylphenidate
Class: Indirect SympathomimeticsUse: ADHDAdverse Effects: Insomnia, anorexia, weight loss
296
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
297
Divalproex
Class: anti-convulsants Use: preventative tx for migraine
298
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
299
Cocaine
Class: Indirect SympathomimeticsMOA: Inhibits NET (reuptake 1)Adverse Effects: Insomnia, anorexia, weight loss
300
Zafirlukast
Class: Leukotriene AntagonistMOA: LTD4 receptor antagonist --\> bronchodilationUse: asthmaPK/PD: admin is oral (good for kids)
301
Hexamethonium
Class: Nicotinic Antagonists - Quaternary Ganglion BlockersMOA: competitive blockage of autonomic nicotinic receptors --\> decrease in arteriolar and vasomotor tone.
302
Detemir
Class: long acting insulinUse: DM I (used to maintain basal insulin levels)
303
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
304
Isoflurophate
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleDistributes to CNSPralidoxime (2-PAM) treats poisoning
305
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
306
Guanfacine
Class: Direct Adrenoceptor Agonists - α2 selectiveMOA: increase reuptake of catecholamines --\> decreased sympathetic stimulationUse: hypertensionAdverse effects: hypertensive crisis with abrupt withdrawal
307
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
308
Edrophonium
Class: Cholinesterase Inhibitors - Alcohol EsterMOA: Binds anionic site of AChEUse: MG diagnosis (Tinsilon test)ReversibleVery short acting
309
Oxymethalone
Class: Androgens\*more anabolicUse: Hypogonadism and anemiaAdverse Effects: feminizing effects in post-pubertal males (due to conversion to estrogen)
310
Na Phosphate
Class: saline laxativesMOA: non-absorbable salt --\> increase osmotic activity in lumenUse: constipationContraindications: renal insufficiency, heart disease, diuretic treatment
311
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
312
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
313
Malathion
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleUse: InsecticideDistributes to CNSPralidoxime (2-PAM) treats poisoning
314
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
315
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
316
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
317
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
318
Amitryptyline
Class: tricyclic antidepressants Use: preventative tx for migraine
319
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
320
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
321
Pralidoxime (2-PAM)
Class: Cholinesterase RegeneratorMOA: displaces phosphate bond, regenerating AchEUse: organophosphate poisoning\*must be given before organophosphate bond "ages"
322
Tamsulosin
Class: Alpha Adrenoceptor Antagonists - α1 selectiveUse: very selective for BPHPK/PD: long half lifeAdverse Effects: orthostatic hypotension (lowest risk with tamsulosin), reflex tachycardia
323
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
324
Minoxidil
Class: direct vasodilatorsMOA: arterial dilationUse: Chronic HTN and to grow hair Admin oralAdverse Effects: hypertrichosis, reflex tachycardia, fluid retention, HA, palpitation AKA Rogaine
325
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
326
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
327
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
328
Sibutramine
MOA: reduces appetiteUse: obesity
329
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)
330
Polycarbaphil
MOA: bulk forming laxativeUse: constipation
331
Prazosin
Class: Alpha Adrenoceptor Antagonists - α1 selectiveUse: hypertension and PTSDPK/PD: long half lifeAdverse Effects: orthostatic hypotension (lowest risk with tamsulosin), reflex tachycardia
332
Sucralfate
Class: mucosal protective agentsMOA: selective binding/coating of necrotic ulcer tissueUse: peptic ulcer
333
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
334
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
335
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
336
Ganirelix
Class: GnRH antagonistsMOA: suppress gonadotropin releaseUse: controlled ovarian hyperstimulation
337
Granisetron
Class: 5-HT3 antagonists Use: chemo-induced vomiting
338
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)
339
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
340
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
341
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
342
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
343
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
344
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
345
Albuterol
Class: Direct Adrenoceptor Agonists - β2 selectiveMOA: increase cAMP --\> bronchodilation and smooth muscle relaxationUse: asthmaAdverse effects: tremors
346
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
347
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
348
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
349
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
350
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
351
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
352
Lorazepam
Class: benzodiazepines Use: vomiting
353
Cetrorelix
Class: GnRH antagonistsMOA: suppress gonadotropin releaseUse: controlled ovarian hyperstimulation
354
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
355
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
356
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
357
Pectin
MOA: absorb/bind intestinal toxinsUse: diarrhea
358
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
359
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
360
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
361
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
362
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
363
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)
364
Carbaryl
Class: Cholinesterase Inhibitors - CarbamatesMOA: substrates for AChE --\> bind serine hydroxyl and are hydrolyzedReversible
365
Butoxamine
Class: Beta Adrenoceptor Antagonists - β2 selective\*not used for anything really
366
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
367
Aprepitant
Class: Neurokinin-1 receptor antagonistUse: chemo-induced emesis
368
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
369
DHEA
DihydroepiadrostenedioneUse: Addison's Dz
370
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
371
Diisopropylfluorophosphate
Class: Cholinesterase Inhibitors - Organophosphates IrreversibleDistributes to CNSPralidoxime (2-PAM) treats poisoning
372
Ipodate
MOA: inhibits 5`-deiodinaseUse: hyperthyroidism
373
Orlistat
MOA: inhibits lipase --\> decreased fat absorptionUse: obesityAdverse Effects: fatty stools
374
Rivastigmine
Class: Cholinesterase Inhibitors - CarbamatesMOA: substrates for AChE --\> bind serine hydroxyl and are hydrolyzedUse: Dementia Reversible
375
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)
376
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
377
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
378
Metyrapone
MOA: inhibits CYP11B1, preventing cortisol activationUse: hypercortisolismAdverse Effects: hirsutism, nausea, rash\*only for compassionate use
379
Guanadrel
Class: Adrenergic Neuron AntagonistsUse: HTN
380
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.
381
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
382
Clomiphene
Class: ER agonistMOA: partial ER agonist --\> reduce negative feedback by estradiol --\> inc FSH/LH --\> stimulate ovulationUse: infertility
383
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
384
Aliskiren
Class: Direct renin inhibitorMOA: inhibits reningUse: HTNPK/PD: dose-dependent reduction in renin\*don't use with renal disease
385
Novolin R
Class: short acting insulinUse: DM I and DKAAdmin IV for DKA
386
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
387
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
388
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
389
Oxandrolone
Class: Androgens\*more anabolicUse: Hypogonadism and anemiaAdverse Effects: feminizing effects in post-pubertal males (due to conversion to estrogen)
390
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
391
Methylcellulose
MOA: bulk forming laxativeUse: constipation
392
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
393
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
394
Zileuton
Class: 5-LOX inhibitorUse: Asthma
395
Mivacurium
Class: Nicotinic Antagonists - Quaternary ParalyticsMOA: competitive blockage of autonomic nicotinic receptors --\> decrease in arteriolar and vasomotor tone.
396
Pyridostigmine
Class: Cholinesterase Inhibitors - CarbamatesMOA: substrates for AChE --\> bind serine hydroxyl and are hydrolyzedUse: Treat MG Reversible
397
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
398
Tegaserod
Class: 5-HT agonists - selective - 5-HT4Use: IBS w/ constipation\*for emergencies only
399
Conivaptan
Class: Vasopressin receptor antagonistMOA: decrease aquaporins --\> water retention in collecting tubuleUse: SIADH, CHF, hyponatremia\*admin IVAdverse Effects: Hypernatremia, nephrogenic DI
400
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
401
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
402
Ibutilide
Class: Class 3 anti-arrhythmeticsMOA: block rectifier K channelUse: Afib or flutter Admin is oralAdverse Effects: prolonged QT and torsades
403
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
404
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
405
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
406
Abarelix
Class: GnRH antagonistsMOA: suppress gonadotropin releaseUse: prostate cancerAdverse Effects: allergy and syndrome of androgen deprivation
407
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
408
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)
409
Ondansetron
Class: 5-HT3 antagonists Use: chemo-induced vomiting
410
Ambenonium
Class: Cholinesterase Inhibitors - CarbamatesMOA: substrates for AChE --\> bind serine hydroxyl and are hydrolyzedReversible
411
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
412
Tacrine
Class: Cholinesterase InhibitorsUse: Dementia and Alzheimer'sAdverse Effects: Hepatotoxicity
413
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
414
Methylphenidate
Class: Indirect SympathomimeticsUse: ADHDAdverse Effects: Insomnia, anorexia, weight loss
415
Lobeline
Class: Direct Nicotinic AgonistsPK/PD: Excess agonist activity results in depolarizing blockade of autonomic ganglia --\> flaccid paralysis Distributes to CNS- Tertiary
416
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
417
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
418
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
419
Bethanechol
Class: Direct Muscarinic Agonists - Choline EstersUse: Stimulate GI/GU smooth muscle (ex. post-op)PK/PD: poor CNS distribution Resistant to AchE
420
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
421
Methoscopolamine
Class: Muscarinic Antagonists - Quaternary Amines\*Contraindicated in glaucoma, BPH, and gastric ulcersAdverse Effects: tachycardia, dry mouth, mydriasis, blurred vision, constipation, urinary retention
422
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
423
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
424
Phenoxybenzamine
Class: Alpha Adrenoceptor Antagonists - nonselectiveMOA: reduces TPR and MAPUse: PheochromocytomaAdverse Effects: Orthostatic hypotension and reflex tachycardia\*irreversible\*also a 5-HT2 antagonist
425
Treprostinil
Class: PGI2MOA: relax smooth muscle Use: pulmonary HTNAdverse Effects: GI upset
426
Dobutamine
Class: Direct Adrenoceptor Agonists - β1 selectiveMOA: increase heart rate
427
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)
428
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
429
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
430
Repaglinide
Class: meglitinide (like sulfonylureas)MOA: bind SUR1Use: DM IIPK/PD: rapid onset and short durationAdverse Effects: hypoglycemia\*Use if pt has sulfa allergy
431
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
432
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
433
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
434
Carteolol
Class: Beta BlockerMOA: Intrinsic sympathomimetic activity (NO production)
435
Difenoxin
Class: opioid analogues MOA: inhibit Ach release onto intestinal opioid receptors --\> decreased motilityUse: diarrhea
436
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
437
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
