USMLE pharm Flashcards

1
Q

MoA of hydralazine

A

­ cGMP ® SM relax
vasodilates ARTERIOLES > veins
¯ AFTERLOAD

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2
Q

Use of hydralazine

A

Severe HTN, CHF

1st line tx for HTN in pregnancy

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3
Q

Tox of hydralazine

A

Compensatory tachy (co-admin w/β-blocker)

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4
Q

non-DHPR Ca-channel blockers

A

Verapamil

Diltiazem

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5
Q

DHPR Ca-channel blockers

A

Nifedipine

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6
Q

MoA of non-DHPR Ca-channel blockers (class IV antiarrhythmics)

A
Block cardiac voltage-dependent L-type Ca-channels
¯ conduction velocity
­ PR interval
­ ERP
(effects similar to β-blockers)
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7
Q

MoA of DHPR Ca-channel blockers

A

Block voltage-dependent L-type Ca-channels of SM
¯ contractility
(effects similar to nitrates)

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8
Q

Use of non-DHPR Ca-channel blockers

A

Prevention of nodal arrhythmias

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9
Q

Use of DHPR Ca-channel blockers

A

HTN
Angina
Prinzmetals’s angina
Raynaud’s

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10
Q

Tox of non-DHPR Ca-channel blockers

A

Edema, flushing

CHF, AV block, sinus node depression

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11
Q

Tox of DHPR Ca-channel blockers

A

Edema, flushing

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12
Q

Nitrates

A

Nitroglcerin

Isosorbide dinitrate

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13
Q

MoA of nitrates

A

­ cGMP & releases NO ® SM relax
venodilates VEINS&raquo_space; arteries
¯ PRELOAD

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14
Q

Use of nitrates

A

Angina
Pulmonary edema
(Aphrodesiac & erection enhancer)

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15
Q

Tox of nitrates

A

Reflex tachy, hypotension, flushing
Tolerance (‘skip’ dose 1x daily to prevent)
Do NOT use w/sildenafil/vardenafil (accumlation of cGMP)

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16
Q

MoA of nitroprusside

A

­ cGMP via direct release of NO

Short-acting

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17
Q

Use of nitroprusside

A

Malignant HTN

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18
Q

Tox of nitroprusside

A

Cyanide (CN) toxicity ® tx w/sulfates

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19
Q

MoA of fenoldopam

A

Dopamine D1 receptor agonist

Relaxes RENAL vascular SM (­ renal perfusion & diuresis while ¯ HTN)

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20
Q

MoA of diazoxide

A

K-channel OPENer

Hyperpolarizes & relaxes vascular SM

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21
Q

Tox of diazoxide

A

Hyperglycemia (due to insulin release)

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22
Q

MoA of statins

A

HMG-CoA reductase inhibitors
¯¯¯ LDL
(cause ­ LDL endocytosis into liver)

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23
Q

Tox of statins

A

Rhabdomyolysis

Hepatotoxicity

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24
Q

MoA of niacin

A

Inhibits lipolysis in adipose, ¯ VLDL secretion by liver

­­ HDL, ¯¯ LDL

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25
Tox of niacin
Flushing (prevent w/aspirin or long-term use) Hyperglycemia ® acanthosis nigricans Hyperuricemia ® gout exacerbation
26
Bile acid resins
Cholestyramine Colestipol Colesevelam
27
MoA of bile acid resins
Prevent intestinal Reabsorption of bile acids | ¯¯ LDL
28
Tox of bile acid resins
Cholesterol gallstones | ¯ absorption of fat-soluble vit's
29
MoA of ezetimibe
Prevent cholesterol Reabsorption @ intestine brush border | ¯¯ LDL
30
Fibrates
Gemfibrozil | -fibrate
31
MoA of fibrates
Upregulate LPL ® ­ TG clearance | ¯¯¯ TG
32
Tox of fibrates
Cholesterol gallstones Myostitis Hepatotoxicity
33
MoA of digoxin
Inhibit Na/K-ATPase ® indirect inhibition of Na/Ca-exchanger ® ­ [Ca]in ® (+) inotropy (­ contractility) Stimulates vagus nerve ® ­ parasympathetic stim of nodes
34
Use of digoxin
``` CHF (­ contractility) Atrial fibrillation (¯ conduction @ AV node & depression of SA node) ```
35
Tox of digoxin
Blurry yellow vision, nausea vomiting (cholinergic) ­ PR, ¯ QT, T-wave inversion Arrhythmia Hyperkalemia (worsened by renal fail., hypokalemia, quinidine) Antidote: normalize K, lidocaine (if tachy), atropine (if brady), anti-dig Fab fragments, Mg
36
MoA of Class I antiarrhythmics
Na-channel blockers Slow/block conduction ¯ slope of pase 0 depolarization (Na+ in) ­ firing threshold State-dependent (selectively depress frequently depolarized tissue, as in fast tachy)
37
Class IA antiarrhythmics
Quinidine Procainamide Disopyramide
38
Effects of IA antiarrhythmics
­ AP duration, ­ ERP, ­ QT interval
39
Use of IA antiarrhythmics
Reentrant & ectopic SVTs | Ventricular tachy
40
Class IB antiarrhythmics
Lidocaine Mexiletine Tocainide
41
Effects of IB antiarrhythmics
¯ AP duration | Preferentially effect ischemic Purkinje & ventricular tissue
42
Use of IB antiarrhythmics
Acute vertricular arrhythmias (post-MI) | Digitalis-induced arrhythmias
43
Class IC antiarrhythmics
Flecainide Encainide Propafenone
44
Effects of IC antiarrhythmics
No effect on AP duration
45
Use of IC antiarrhythmics
V-tachs that progress to VF Intractable SVT Last resort Contraindicated post-MI
46
Class II antiarrhythmics (Beta-blockers)
``` Propranolol Esmolol Metoprolol Atenolol Timolol ```
47
MoA of β-blockers (Class II antiarrhythmics)
¯ cAMP, ¯ Ca2+ currents ¯ slope of phase 4 (suppress abnormal pacemakers) ­ PR interval (AV node particularly sensitive) Esmolol very short acting
48
Use of β-blockers (Class II antiarrhythmics)
V-tach SVT Slowing ventricular rate during A-fib/flutter
49
Tox of β-blockers (Class II antiarrhythmics)
Contraindicated in asthma & acute exacerbations of CHF Metoprolol: dyslipidemia Tx OD w/glucagon
50
Class III antiarrhythmics (K-channel blockers)
``` Sotalol Ibutilide Dofetilide Bretylium Amiodarone ```
51
MoA of K-channel blockers (Class III)
­ AP duration ­ ERP ­ QT interval Used when other arrhythmics fail
52
Tox of amiodarone
``` Pulmonary fibrosis Hepatotoxicity Hypo/hyper-thyroidism Blue/grey skin ® photodermatitis (has class I, II, III, & IV effects because it alters the lipid membrane) ```
53
Distinguish btw the primary sites of axn of the anti-arrhythmics)
Class I & III primarily act on ventricular cells | Class II & IV primarily act on the nodes
54
MoA of adenosine
­ K out of cells ® hyperpolarization ¯ Ca currents Very short acting
55
Use of adenosine
Drug of choice in diagnosing/abolishing SUPERVENTRICULAR TACHYCARDIA Effects blocked by theophylline
56
Use of K & Mg
K: depress ectopic pacemakers in hypokalemia (e.g. digoxin tox) Mg: torsades de pointes & digoxin tox
57
Use of indomethacin
Close patent ductus arteriosis (inhibits PGE2)
58
Anti-HTN drugs of choice in diabetes
ACEi | ARB
59
Anti-HTN drugs of choice in CHF
ACEi β-blockers Diuretics (thiazides) ARB
60
Anti-HTN drugs of choice in systolic HTN
DHPR Ca-channel blocker (verapamil) | Thiazide diuretic
61
Anti-HTN drugs of choice in MI
β-blocker | ACEi
62
Contraindications for β-blockers
Asthma COPD Depression Non-selective β-blockers: hyperkalemia
63
Contraindications for diuretics
Gout | K-sparing diuretics: renal insufficiency, hyperkalemia
64
Contraindications for ACEi's & ARBs
Pregnancy Renovascular dysfxn Hyperkalemia
65
Tx for hyperthyroidism
Propylthiouracil, methimazole | MoA: inhbits organification of iodide & coupling of thyroid hormone synthesis; PPT also ¯ T4 ® T3 conversion
66
Tx for hypothyroidism
Levothyroixine, triiodothyronine
67
Use for GH
GH deficiency | Turner syndrome
68
Octreotide (somatostatin analog)
Acromegaly Carcinoid Gastrinoma Glucagonoma
69
Oxytocin
``` Stimulate labor (uterine contractions) Milk let-down Ctrls uterine hemorrhage ```
70
ADH (desmopressin)
``` Pituitary DI (central, not nephrogenic) Stimulate vWF release from endothelial cells (von Willebrand's) ```
71
Tx for SIADH
Demeclocycline (a tetracycline) MoA: ADH antagonist Tox: nephrogenic DI, photosensitivity, abnl's of bone/teeth
72
Tx for pheochromocytoma
Phenoxybenzanine (to shrink tumor prior to surgical removal) | MoA: non-selective α-antagonist
73
Tx for prolactinoma
Bromocriptine, cabergolin | MoA: dopamine agonists
74
Bugs assoc'd w/endocarditis
Acute: S. aureus Subacute: viridans streptococci Assoc'd w/colon cancer: S. bovis Assoc'd w/prosthetic valves: S. epidermidis
75
Tx for diabetes insipidus
Adequate fluid intake Central: intranasal desmopressin Nephrogenic: thiazide diuretic, indomethacin, amiloride
76
1st generation H1 blockers
Diphenhydramine Dimenhydrinate Chlorpheniramine (reversible inhibitors of H1 histamine receptors)
77
2nd generation of H1 blockers
``` Loratadine Fexofenadine Desloratadine Cetirizine (reversible inhibitors of H1 histamine receptors; less sedating) ```
78
Asthma drugs that target inflammatory processes
Cromolyn Corticosteroids Antileukotrienes
79
Asthma drugs that target sympathetic tone
Beta agonists Theophylline (methylxanthines) Ipratropium
80
Uses of β-agonists
Isoproterenol (non-specific): relaxes SM (β2); tox = tachycardia (β1) Albuterol (β2): acute exacerbation Salmeterol (β2): prophylaxis; tox = tremor/arrhythmia
81
MoA of theophylline
Inhibits phosphodiesterase ® ¯ cAMP hydrolysis ® bronchodilation
82
Tox of theophylline
Use limited by narrow therapeutic index Cardiotox, neurotox Metabolized by P450 Blocks axns of adenosine
83
MoA & use of Ipratropium
Competitive block of mAChR's ® prevents bronchoconstriction | Use: Asthma prophylaxis, COPD
84
MoA & use of cromolyn
Prevents release of mediators from mast cells | Use: asthma prophylaxis only (not useful for acute attacks)
85
MoA & use of corticosteroids
Beclomethasone, prednisone MoA: inactivates NF-kB ® inhibits synthesis of of all cytokines, incl. TNF-α Use: 1st-line tx for chronic asthma
86
Antileukotrienes
Zileuton Zafirlukast Montelukast
87
MoA & use of zileuton
Inhibits 5-lipoxygenase path: blocks arachidonic acid ® leukotrienes Asthma prophylaxis
88
MoA & use of zafirlukast & motelukast
Block leukotrience receptors | Use: aspirin-induced asthma
89
Expectorants
Guaifenesin | N-acetylcysteine
90
MoA & uses of N-acetylcysteine
Mucolytic | Use: loosen mucous plugs in CF pts; antidote for acetaminophen OD
91
Tx of pulmonary hypertension
Bosentan | competitively antagonizes endothelin-1 receptors, decreasing pulmonary vascular resistance
92
MoA of mannitol
Osmotic diuretic
93
MoA & use & tox of acetazolamide
MoA: Carbonic anydrase inhibitor ® self-limited bicarb diuresis Use: Urinary alkalinization, metabolic alkalosis, altitude sickness Tox: hyperchloremic metabolic acidosis, sulfa allergy
94
MoA & use & tox of furosemide
MoA: sulfonamide LOOP diuretic; inhibits Na/K/2Cl cotransporter (thick ascending LoH) Use: edema, HTN, hypercalCEMIA Tox: Ototoxicity, hypokalemia, allergy (sulfa), nephritis (interstitial), gout
95
MoA & use & tox of ethacrynic acid
MoA: NON-sulfonamide LOOP diuretic; inhibits Na/K/2Cl cotransporter (thick ascending LoH) Use: diuresis in pts allergic to sulfa drugs Tox: similar to furosemide but does not cause gout
96
MoA & use & tox of thiazide diuretics
MoA: inhibits NaCl reabsorption in early DCT Use: HTN, CHF, hypercalciURIA, nephrogenic DI Tox: Hypokalemic metabolic alkalosis, hyperglycemia, hyperlipidemia, hyperuricemia, hypercalcemia; sulfa allergy
97
K-sparing diuretics
Spironolactone Triamterene Amiloride
98
MoA of spironolactone
Competitive aldosterone receptor antagonist (NOT an ARB) in CCT
99
MoA of triamterene & amiloride
Block Na-channels in the CCT
100
Use & tox of K-sparing diuretics
Hyperaldosteronism, hypokalemia, CHF | Tox: hyperkalemia; spironolactone -- endo effects (gynecomastia, anti-androgen effects)
101
Diuretics that can cause acidemia
Acetazolamide | K-sparing diuretics
102
Diuretics that can cause alkalemia
Loop diuretics | Thiazides
103
ACE inhibitors
Captopril Enalapril Lisinopril
104
MoA of ACEi
Inhibit angiotensin-converting enzyme (ACE) ® ¯ angiotensin II ® ¯ inactivation of bradykinin (potent vasodilator)
105
Use of ACEi
HTN CHF DIABETIC renal dz
106
Tox of ACEi
``` COUGH ANGIOEDEMA Proteinuria Hyperkalemia Fetal renal damage (contraindicated) (contraindicated in bilateral renal artery stenosis) ```
107
MoA of losartan
ARB (angiotensin II receptor blocker)
108
MoA of leuprolide
GnRH analog Pulsatile: agonist Continuous: antagonist
109
Use of leuprolide
Pulsatile: infertility Continuous: prostate cancer (use w/flutamide), uterine fibroids
110
Antiandrogens
Finasteride (propecia) Flutamide Ketoconazole Spironolactone
111
MoA & use of finesteride
MoA: 5α-reductase inhibitor (¯ testosterone ® DHT conversion) Use: BPH, male-pattern baldness
112
MoA & use of flutamide
MoA: nonsteroidal competitive testosterone receptor antagonist Use: prostate cancer (w/leuprolide)
113
MoA & use of ketoconazole
MoA: inhibits desmolase (¯ steroid synthesis) Use: prevent hirsutism in tx of PCOS Tox: gynecomastia & amenorrhea
114
MoA & use of spironolactone
MoA: inhibits steroid binding Use: prevent hirsutism in tx of PCOS Tox: gynecomastia & amenorrhea
115
Estrogens
Ethinyl estradiol DES Mestranol
116
Tox of estrogens
­ risk of endometrial cancer Bleeding in postmenopausal women ­ risk of thrombi DES: clear cell adenocarcinoma of vagina in females exposed in utero
117
Selective estrogen receptor modulators (SERMs)
Estrogen partial agonists Clomiphene Tamoxifen Raloxifene
118
MoA of clomiphene
Partial agonist @ estrogen receptors in hypothalamus | Prevents normal feedback inhibition & ­ release of LH & FSH from pituitary ® stimulates ovulation
119
Use & tox of clomiphene
Use: Tx infertility & PCOS Tox: hot flashes, ovarian enlargement, multiple simultaneous pregnancies
120
MoA & use of tamoxifen
MoA: estrogen receptor antagonist on breast tissue Use: tx & prevent recurrence of ER-(+) breast cancer
121
MoA & use of raloxifene
MoA: estrogen receptor agonist on bone ® reduce resoprtion of bone Use: tx osteoporosis
122
MoA of oral contraceptives
Prevent estrogen surge ® no LH surge ® no ovulation
123
Contraindications of oral contraceptives
Smokers > 35y Hx of thromboembolism Hx of stroke Hx of estrogen-dependent tumor
124
MoA & use of dinoprostone
MoA: PGE2 analog causing cervical dilation & uterine contraction Use: Labor induction
125
MoA & use of ritodrine/terbutaline
MoA: β2-agonsits that relax the uterus Use: reduce premature uterine contractions (prevent early delivery)
126
MoA & use of tamsulosin
MoA: α1-antagonist ® inhibit SM contraction; selective for α1A,D receptors (prostate) vs α1B receptors (vascular) Use: BPH
127
MoA of sildenafil & vardenafil
Inhibit cGMP phosphodiesterase ® ­ cGMP ® SM relaxation in corpus cavernosum ® ­ blood flow ­ erection
128
Tox of sildenafil & vardenafil
Headache, flushing, dyspepsia Impaired blue-green color vision Risk of life-threatening hypotension in pts taking nitrates