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
Q

Tox of niacin

A

Flushing (prevent w/aspirin or long-term use)
Hyperglycemia ® acanthosis nigricans
Hyperuricemia ® gout exacerbation

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26
Q

Bile acid resins

A

Cholestyramine
Colestipol
Colesevelam

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27
Q

MoA of bile acid resins

A

Prevent intestinal Reabsorption of bile acids

¯¯ LDL

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28
Q

Tox of bile acid resins

A

Cholesterol gallstones

¯ absorption of fat-soluble vit’s

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29
Q

MoA of ezetimibe

A

Prevent cholesterol Reabsorption @ intestine brush border

¯¯ LDL

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30
Q

Fibrates

A

Gemfibrozil

-fibrate

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31
Q

MoA of fibrates

A

Upregulate LPL ® ­ TG clearance

¯¯¯ TG

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32
Q

Tox of fibrates

A

Cholesterol gallstones
Myostitis
Hepatotoxicity

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33
Q

MoA of digoxin

A

Inhibit Na/K-ATPase ® indirect inhibition of Na/Ca-exchanger ® ­ [Ca]in ® (+) inotropy (­ contractility)
Stimulates vagus nerve ® ­ parasympathetic stim of nodes

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34
Q

Use of digoxin

A
CHF (­ contractility)
Atrial fibrillation (¯ conduction @ AV node & depression of SA node)
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35
Q

Tox of digoxin

A

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

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36
Q

MoA of Class I antiarrhythmics

A

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)

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37
Q

Class IA antiarrhythmics

A

Quinidine
Procainamide
Disopyramide

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38
Q

Effects of IA antiarrhythmics

A

­ AP duration, ­ ERP, ­ QT interval

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39
Q

Use of IA antiarrhythmics

A

Reentrant & ectopic SVTs

Ventricular tachy

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40
Q

Class IB antiarrhythmics

A

Lidocaine
Mexiletine
Tocainide

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41
Q

Effects of IB antiarrhythmics

A

¯ AP duration

Preferentially effect ischemic Purkinje & ventricular tissue

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42
Q

Use of IB antiarrhythmics

A

Acute vertricular arrhythmias (post-MI)

Digitalis-induced arrhythmias

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43
Q

Class IC antiarrhythmics

A

Flecainide
Encainide
Propafenone

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44
Q

Effects of IC antiarrhythmics

A

No effect on AP duration

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45
Q

Use of IC antiarrhythmics

A

V-tachs that progress to VF
Intractable SVT
Last resort
Contraindicated post-MI

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46
Q

Class II antiarrhythmics (Beta-blockers)

A
Propranolol
Esmolol
Metoprolol
Atenolol
Timolol
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47
Q

MoA of β-blockers (Class II antiarrhythmics)

A

¯ cAMP, ¯ Ca2+ currents
¯ slope of phase 4 (suppress abnormal pacemakers)
­ PR interval (AV node particularly sensitive)
Esmolol very short acting

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48
Q

Use of β-blockers (Class II antiarrhythmics)

A

V-tach
SVT
Slowing ventricular rate during A-fib/flutter

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49
Q

Tox of β-blockers (Class II antiarrhythmics)

A

Contraindicated in asthma & acute exacerbations of CHF
Metoprolol: dyslipidemia
Tx OD w/glucagon

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50
Q

Class III antiarrhythmics (K-channel blockers)

A
Sotalol
Ibutilide
Dofetilide
Bretylium
Amiodarone
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51
Q

MoA of K-channel blockers (Class III)

A

­ AP duration
­ ERP
­ QT interval
Used when other arrhythmics fail

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52
Q

Tox of amiodarone

A
Pulmonary fibrosis
Hepatotoxicity
Hypo/hyper-thyroidism
Blue/grey skin ® photodermatitis
(has class I, II, III, & IV effects because it alters the lipid membrane)
53
Q

Distinguish btw the primary sites of axn of the anti-arrhythmics)

A

Class I & III primarily act on ventricular cells

Class II & IV primarily act on the nodes

54
Q

MoA of adenosine

A

­ K out of cells ® hyperpolarization
¯ Ca currents
Very short acting

55
Q

Use of adenosine

A

Drug of choice in diagnosing/abolishing SUPERVENTRICULAR TACHYCARDIA
Effects blocked by theophylline

56
Q

Use of K & Mg

A

K: depress ectopic pacemakers in hypokalemia (e.g. digoxin tox)
Mg: torsades de pointes & digoxin tox

57
Q

Use of indomethacin

A

Close patent ductus arteriosis (inhibits PGE2)

58
Q

Anti-HTN drugs of choice in diabetes

A

ACEi

ARB

59
Q

Anti-HTN drugs of choice in CHF

A

ACEi
β-blockers
Diuretics (thiazides)
ARB

60
Q

Anti-HTN drugs of choice in systolic HTN

A

DHPR Ca-channel blocker (verapamil)

Thiazide diuretic

61
Q

Anti-HTN drugs of choice in MI

A

β-blocker

ACEi

62
Q

Contraindications for β-blockers

A

Asthma
COPD
Depression
Non-selective β-blockers: hyperkalemia

63
Q

Contraindications for diuretics

A

Gout

K-sparing diuretics: renal insufficiency, hyperkalemia

64
Q

Contraindications for ACEi’s & ARBs

A

Pregnancy
Renovascular dysfxn
Hyperkalemia

65
Q

Tx for hyperthyroidism

A

Propylthiouracil, methimazole

MoA: inhbits organification of iodide & coupling of thyroid hormone synthesis; PPT also ¯ T4 ® T3 conversion

66
Q

Tx for hypothyroidism

A

Levothyroixine, triiodothyronine

67
Q

Use for GH

A

GH deficiency

Turner syndrome

68
Q

Octreotide (somatostatin analog)

A

Acromegaly
Carcinoid
Gastrinoma
Glucagonoma

69
Q

Oxytocin

A
Stimulate labor (uterine contractions)
Milk let-down
Ctrls uterine hemorrhage
70
Q

ADH (desmopressin)

A
Pituitary DI (central, not nephrogenic)
Stimulate vWF release from endothelial cells (von Willebrand's)
71
Q

Tx for SIADH

A

Demeclocycline (a tetracycline)
MoA: ADH antagonist
Tox: nephrogenic DI, photosensitivity, abnl’s of bone/teeth

72
Q

Tx for pheochromocytoma

A

Phenoxybenzanine (to shrink tumor prior to surgical removal)

MoA: non-selective α-antagonist

73
Q

Tx for prolactinoma

A

Bromocriptine, cabergolin

MoA: dopamine agonists

74
Q

Bugs assoc’d w/endocarditis

A

Acute: S. aureus
Subacute: viridans streptococci
Assoc’d w/colon cancer: S. bovis
Assoc’d w/prosthetic valves: S. epidermidis

75
Q

Tx for diabetes insipidus

A

Adequate fluid intake
Central: intranasal desmopressin
Nephrogenic: thiazide diuretic, indomethacin, amiloride

76
Q

1st generation H1 blockers

A

Diphenhydramine
Dimenhydrinate
Chlorpheniramine
(reversible inhibitors of H1 histamine receptors)

77
Q

2nd generation of H1 blockers

A
Loratadine
Fexofenadine
Desloratadine
Cetirizine
(reversible inhibitors of H1 histamine receptors; less sedating)
78
Q

Asthma drugs that target inflammatory processes

A

Cromolyn
Corticosteroids
Antileukotrienes

79
Q

Asthma drugs that target sympathetic tone

A

Beta agonists
Theophylline (methylxanthines)
Ipratropium

80
Q

Uses of β-agonists

A

Isoproterenol (non-specific): relaxes SM (β2); tox = tachycardia (β1)
Albuterol (β2): acute exacerbation
Salmeterol (β2): prophylaxis; tox = tremor/arrhythmia

81
Q

MoA of theophylline

A

Inhibits phosphodiesterase ® ¯ cAMP hydrolysis ® bronchodilation

82
Q

Tox of theophylline

A

Use limited by narrow therapeutic index
Cardiotox, neurotox
Metabolized by P450
Blocks axns of adenosine

83
Q

MoA & use of Ipratropium

A

Competitive block of mAChR’s ® prevents bronchoconstriction

Use: Asthma prophylaxis, COPD

84
Q

MoA & use of cromolyn

A

Prevents release of mediators from mast cells

Use: asthma prophylaxis only (not useful for acute attacks)

85
Q

MoA & use of corticosteroids

A

Beclomethasone, prednisone
MoA: inactivates NF-kB ® inhibits synthesis of of all cytokines, incl. TNF-α
Use: 1st-line tx for chronic asthma

86
Q

Antileukotrienes

A

Zileuton
Zafirlukast
Montelukast

87
Q

MoA & use of zileuton

A

Inhibits 5-lipoxygenase path: blocks arachidonic acid ® leukotrienes
Asthma prophylaxis

88
Q

MoA & use of zafirlukast & motelukast

A

Block leukotrience receptors

Use: aspirin-induced asthma

89
Q

Expectorants

A

Guaifenesin

N-acetylcysteine

90
Q

MoA & uses of N-acetylcysteine

A

Mucolytic

Use: loosen mucous plugs in CF pts; antidote for acetaminophen OD

91
Q

Tx of pulmonary hypertension

A

Bosentan

competitively antagonizes endothelin-1 receptors, decreasing pulmonary vascular resistance

92
Q

MoA of mannitol

A

Osmotic diuretic

93
Q

MoA & use & tox of acetazolamide

A

MoA: Carbonic anydrase inhibitor ® self-limited bicarb diuresis
Use: Urinary alkalinization, metabolic alkalosis, altitude sickness
Tox: hyperchloremic metabolic acidosis, sulfa allergy

94
Q

MoA & use & tox of furosemide

A

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
Q

MoA & use & tox of ethacrynic acid

A

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
Q

MoA & use & tox of thiazide diuretics

A

MoA: inhibits NaCl reabsorption in early DCT
Use: HTN, CHF, hypercalciURIA, nephrogenic DI
Tox: Hypokalemic metabolic alkalosis, hyperglycemia, hyperlipidemia, hyperuricemia, hypercalcemia; sulfa allergy

97
Q

K-sparing diuretics

A

Spironolactone
Triamterene
Amiloride

98
Q

MoA of spironolactone

A

Competitive aldosterone receptor antagonist (NOT an ARB) in CCT

99
Q

MoA of triamterene & amiloride

A

Block Na-channels in the CCT

100
Q

Use & tox of K-sparing diuretics

A

Hyperaldosteronism, hypokalemia, CHF

Tox: hyperkalemia; spironolactone – endo effects (gynecomastia, anti-androgen effects)

101
Q

Diuretics that can cause acidemia

A

Acetazolamide

K-sparing diuretics

102
Q

Diuretics that can cause alkalemia

A

Loop diuretics

Thiazides

103
Q

ACE inhibitors

A

Captopril
Enalapril
Lisinopril

104
Q

MoA of ACEi

A

Inhibit angiotensin-converting enzyme (ACE) ® ¯ angiotensin II ® ¯ inactivation of bradykinin (potent vasodilator)

105
Q

Use of ACEi

A

HTN
CHF
DIABETIC renal dz

106
Q

Tox of ACEi

A
COUGH
ANGIOEDEMA
Proteinuria
Hyperkalemia
Fetal renal damage (contraindicated)
(contraindicated in bilateral renal artery stenosis)
107
Q

MoA of losartan

A

ARB (angiotensin II receptor blocker)

108
Q

MoA of leuprolide

A

GnRH analog
Pulsatile: agonist
Continuous: antagonist

109
Q

Use of leuprolide

A

Pulsatile: infertility
Continuous: prostate cancer (use w/flutamide), uterine fibroids

110
Q

Antiandrogens

A

Finasteride (propecia)
Flutamide
Ketoconazole
Spironolactone

111
Q

MoA & use of finesteride

A

MoA: 5α-reductase inhibitor (¯ testosterone ® DHT conversion)
Use: BPH, male-pattern baldness

112
Q

MoA & use of flutamide

A

MoA: nonsteroidal competitive testosterone receptor antagonist
Use: prostate cancer (w/leuprolide)

113
Q

MoA & use of ketoconazole

A

MoA: inhibits desmolase (¯ steroid synthesis)
Use: prevent hirsutism in tx of PCOS
Tox: gynecomastia & amenorrhea

114
Q

MoA & use of spironolactone

A

MoA: inhibits steroid binding
Use: prevent hirsutism in tx of PCOS
Tox: gynecomastia & amenorrhea

115
Q

Estrogens

A

Ethinyl estradiol
DES
Mestranol

116
Q

Tox of estrogens

A

­ risk of endometrial cancer
Bleeding in postmenopausal women
­ risk of thrombi
DES: clear cell adenocarcinoma of vagina in females exposed in utero

117
Q

Selective estrogen receptor modulators (SERMs)

A

Estrogen partial agonists
Clomiphene
Tamoxifen
Raloxifene

118
Q

MoA of clomiphene

A

Partial agonist @ estrogen receptors in hypothalamus

Prevents normal feedback inhibition & ­ release of LH & FSH from pituitary ® stimulates ovulation

119
Q

Use & tox of clomiphene

A

Use: Tx infertility & PCOS
Tox: hot flashes, ovarian enlargement, multiple simultaneous pregnancies

120
Q

MoA & use of tamoxifen

A

MoA: estrogen receptor antagonist on breast tissue
Use: tx & prevent recurrence of ER-(+) breast cancer

121
Q

MoA & use of raloxifene

A

MoA: estrogen receptor agonist on bone ® reduce resoprtion of bone
Use: tx osteoporosis

122
Q

MoA of oral contraceptives

A

Prevent estrogen surge ® no LH surge ® no ovulation

123
Q

Contraindications of oral contraceptives

A

Smokers > 35y
Hx of thromboembolism
Hx of stroke
Hx of estrogen-dependent tumor

124
Q

MoA & use of dinoprostone

A

MoA: PGE2 analog causing cervical dilation & uterine contraction
Use: Labor induction

125
Q

MoA & use of ritodrine/terbutaline

A

MoA: β2-agonsits that relax the uterus
Use: reduce premature uterine contractions (prevent early delivery)

126
Q

MoA & use of tamsulosin

A

MoA: α1-antagonist ® inhibit SM contraction; selective for α1A,D receptors (prostate) vs α1B receptors (vascular)
Use: BPH

127
Q

MoA of sildenafil & vardenafil

A

Inhibit cGMP phosphodiesterase ® ­ cGMP ® SM relaxation in corpus cavernosum ® ­ blood flow ­ erection

128
Q

Tox of sildenafil & vardenafil

A

Headache, flushing, dyspepsia
Impaired blue-green color vision
Risk of life-threatening hypotension in pts taking nitrates