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Pharmacology > Unit 4-Antihypertensives > Flashcards

Unit 4-Antihypertensives Flashcards

1
Q

Furosemide

Drug class

A

Loop diuretic

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2
Q

Furosemide

Mechanism

A

Inhibits Cl portion of Na-K-2Cl cotransporter in luminal membrane at medullary and cortical (proximal) talH –> decreased Ca++ and Na+ (and water) reabsorption, resultant K+ loss

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3
Q

Furosemide

Uses

A

Crisis edema (pulmonary, CHF, cirrhosis), hypercalcemia, drug toxicity/OD; severe hypertension in setting of CHF or cirrhosis;

useful in patients with renal insufficiency (GFR < 30-40)

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4
Q

Furosemide

Side effects

A

Hypokalemia/hypomagnesemia, hypercalcinuria, nephrocalcinosis, ototoxicity (esp. w/aminoglycoside)

Hyper -glycemia, -lipidemia, -uricemia; hypo -magnesia, -natremia; gout, photosensitivity, drug interactions; erectile dysfunction

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5
Q

Hydrochlorothiazide

Drug class

A

Thiazide diuretic

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6
Q

Hydrochlorothiazide

Mechanism

A

Inhibits the Cl portion of the Na-Cl cotransporter in the luminal membrane at the early distal tubule –> decreased Na+ (and water) reabsorption, increased Ca++ reabsorption, resultant K+ loss

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7
Q

Hydrochlorothiazide

Uses

A

HTN (intravascular contraction), chronic edema (cardiac insufficiency), idiopathic hypercalciuria (stones), nephrogenic diabetes insipidus

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8
Q

Hydrochlorothiazide

Side effects

A

Hypokalemia/hypomagnesemia, contraction alkalosis, increased BUN & creatinine

Hyper -glycemia, -lipidemia, -uricemia, -calcemia; hypo -magnesia, -natremia; gout, photosensitivity, impotence, drug interactions

avoid NSAIDs, bile sequestrants; ineffective if GFR <30

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9
Q

Chlorthalidone

Drug class

A

Thiazide-like diuretic

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10
Q

Chlorthalidone

Mechanism

A

Inhibits the Cl portion of the Na-Cl cotransporter in the luminal membrane at the early distal tubule –> decreased Na+ (and water) reabsorption, increased Ca++ reabsorption, resultant K+ loss

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11
Q

Chlorthalidone

Uses

A

Reduce stroke risk, CHF events; HTN (intravascular contraction), chronic edema (cardiac insufficiency), idiopathic hypercalciuria (stones), nephrogenic diabetes insipidus

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12
Q

Chlorthalidone

Side effects

A

Hypokalemia/hypomagnesemia, contraction alkalosis, increased BUN & creatinine

Hyper -glycemia, -lipidemia, -uricemia, -calcemia; hypo -magnesia, -natremia; gout, photosensitivity, impotence, drug interactions

avoid NSAIDs, bile sequestrants; ineffective if GFR <30

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13
Q

Metolazone

Drug class

A

Thiazide-like diuretic

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14
Q

Metolazone

Mechanism

A

Inhibits the Cl portion of the Na-Cl cotransporter in the luminal membrane at the early distal tubule –> decreased Na+ (and water) reabsorption, increased Ca++ reabsorption, resultant K+ loss

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15
Q

Metolazone

Uses

A

HTN (intravascular contraction), chronic edema (cardiac insufficiency), idiopathic hypercalciuria (stones), nephrogenic diabetes insipidus

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16
Q

Metolazone

Side effects

A

Hypokalemia/hypomagnesemia, contraction alkalosis, increased BUN & creatinine

Hyper -glycemia, -lipidemia, -uricemia, -calcemia; hypo -magnesia, -natremia; gout, photosensitivity, impotence, drug interactions

avoid NSAIDs, bile sequestrants; ineffective if GFR <30

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17
Q

Amiloride

Drug class

A

Renal ENaC inhibitor

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18
Q

Amiloride

Mechanism

A

Blocks Na channel and Na/H antiporter in lumenal membrane at the late distal tubule and collecting duct –> decreased K+ secretion and distal tubule acid secretion, increased Ca++ absorption

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19
Q

Amiloride

Uses

A

Combination with other diuretics to prevent hypokalemia; edema, idiopathic hypercalciuria (stones); lithium-induced polyuria & toxicity, Liddle syndrome, mucocilliary clearance

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20
Q

Amiloride

Side effects

A

Hyperkalemia in patients with renal failure or on ACE inhibitors

Contraindicated in patients with renal failure (hyperkalemia), ACEi/ARB use; FeNa = 2%

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21
Q

Spironolactone

Drug class

A

Aldosterone receptor antagonist

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22
Q

Spironolactone

Mechanism

A

Competes for aldosterone receptor, inhibiting mRNA transcription and translation –> decreased Na and K channels, decreased number and activity of Na-K-ATPase pumps in the late distal tubule and collecting duct –> decreased K+ secretion, distal tubule acid secretion

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23
Q

Spironolactone

Uses

A

Reduction in CHF mortality (30% in NYHA class III and IV); combination with other diuretics to prevent hypokalemia; edema; primary and secondary aldosteronism; hypertension; anti-testosterone agent

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24
Q

Spironolactone

Side effects

A

Hyperkalemia in patients with renal failure or on ACE inhibitors; male patients may have gynecomastia, erectile dysfunction, and loss of libido; female patients may have amenorrhea, breast soreness, and oligomenorrhea

Contraindicated in patients with renal failure (hyperkalemia); FeNa = 2%; requires a salt-restricted diet; only drug not requiring tubular lumen access

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25
Q

Eplerenone

Drug class

A

Potassium-sparing diuretic

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26
Q

Eplerenone

Mechanism

A

Block alodesterone; inhibits sodium reabsorption in distal tubule

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27
Q

Eplerenone

Uses

A

Reduction in CHF mortality (30% in NYHA class III and IV); combination with other diuretics to prevent hypokalemia; edema; primary and secondary aldosteronism; hypertension; anti-testosterone agent

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28
Q

Eplerenone

Side effects

A

Hyperkalemia; much lower incidence of gynecomastia and mennorhagia

Caution in renal failure, ACEi or ARB use, and in diabetics

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29
Q

Captopril

Drug class

A

short-acting ACE-I (vasodilators)

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30
Q

Captopril

Mechanism

A

Blocks endothelial ACE from converting angiotensin I to angiotensin II (potent vasoconstrictor); as a side effect, also prevents breakdown of bradykinin (potent vasodilator)

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31
Q

Captopril

Uses

A

CHF, left ventricular hypertrophy, post-MI (prevents left ventricular remodeling)

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32
Q

Captopril

Side effects

A

Dry cough, angioedema, inhibits renal autoregulation, hypotension

Short-acting; contraindicated in pregnancy, renal artery stenosis, hyperkalemia, and prior angioedema (no ARB allowed, either); caution in renal failure; reduces incidence of future CAD events, may reduce risk of diabetes

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33
Q

Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)

Drug class

A

long-acting ACE-I (vasodilators)

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34
Q

Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)

Mechanism

A

Blocks endothelial ACE from converting angiotensin I to angiotensin II (potent vasoconstrictor); as a side effect, also prevents breakdown of bradykinin (potent vasodilator)

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35
Q

Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)

Uses

A

CHF, left ventricular hypertrophy, post-MI (prevents left ventricular remodeling)

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36
Q

Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)

Side effects

A

Dry cough, angioedema, decreased renal function, hypotension

Long-acting; contraindicated in pregnancy, renal artery stenosis, hyperkalemia, and prior angioedema (no ARB allowed, either); caution in renal failure; reduces incidence of future CAD events; may reduce risk of diabetes

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37
Q

Enalapril

Drug class

A

ACE-I (vasodilators)

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38
Q

Enalapril

Mechanism

A

Metabolized to active form enalaprat

Blocks endothelial ACE from converting angiotensin I to angiotensin II (potent vasoconstrictor); as a side effect, also prevents breakdown of bradykinin (potent vasodilator)

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39
Q

Enalapril

Uses

A

CHF, left ventricular hypertrophy, post-MI (prevents left ventricular remodeling)

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40
Q

Enalapril

Side effects

A

Dry cough, angioedema, decreased renal function, hypotension

contraindicated in pregnancy, renal artery stenosis, hyperkalemia, and prior angioedema (no ARB allowed, either); caution in renal failure; reduces incidence of future CAD events; may reduce risk of diabetes

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41
Q

Losartan (Cozaar); Valsartan (Diovan); Irbesartan (Avapro)

Drug class

A

Angiotensin II Recepter Blockers

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42
Q

Losartan (Cozaar); Valsartan (Diovan); Irbesartan (Avapro)

Mechanism

A

Competitive inhibition of angiotensin II in vascular endothelium

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43
Q

Losartan (Cozaar); Valsartan (Diovan); Irbesartan (Avapro)

Uses

A

Fall in peripheral vascular resistance, w/little change in HR or CO; same uses as ACE-I

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44
Q

Losartan (Cozaar); Valsartan (Diovan); Irbesartan (Avapro)

Side effects

A

Angioedema, decreased renal function, hypotension; dry cough less frequent than with ACE-I

Contraindicated in pregnancy, renal artery stenosis, hyperkalemia, and prior angioedema (no ARB allowed, either); caution in renal failure

45
Q

Aliskiren

Drug class

A

Renin inhibitor

46
Q

Aliskiren

Uses

A

Not very effective

47
Q

Diltiazem

Drug class

A

Non-dihydropyridine Calcium channel blockers

48
Q

Diltiazem

Mechanism

A

Interact with L-type voltage gated plasma membrane Ca channel –> decreased calcium entry into vascular smooth muscle cell, preventing contraction; causes decreased contractility, firing rate of aberrant pacemaker sites, and conduction velocity; prolongs repolarization in SA node and AV node (–> decreases HR); less vasodilation

49
Q

Diltiazem

Uses

A

Hypertension, anti-anginal (chronotropic effects –> decreased myocardial oxygen demand), SVT (class IV anti-arrhythymic)

50
Q

Diltiazem

Side effects

A

Leg edema, bradycardia, AV nodal blockade, hypotension, worsening heart failure

Constipation (most common), headache, flushing

Contraindicated in overt decompensated heart failure, bradycardia, sinus node dysfunction, high-degree AV block

51
Q

Verapamil

Drug class

A

Non-dihydropyridine Calcium channel blockers

52
Q

Verapamil

Mechanism

A

Interact with L-type voltage gated plasma membrane Ca channel –> decreased calcium entry into vascular smooth muscle cell, preventing contraction; causes decreased contractility, firing rate of aberrant pacemaker sites, and conduction velocity; prolongs repolarization in SA node and AV node (–> decreases HR); less vasodilation

53
Q

Verapamil

Uses

A

Hypertension, anti-anginal (chronotropic effects –> decreased myocardial oxygen demand), SVT (class IV anti-arrhythymic)

54
Q

Verapamil

Side effects

A

Leg edema, bradycardia, AV nodal blockade, hypotension, worsening heart failure

Constipation (most common), headache, flushing

Contraindicated in overt decompensated heart failure, bradycardia, sinus node dysfunction, high-degree AV block

55
Q

Amlodipine

Drug class

A

Dihydropyridine Calcium channel blockers

56
Q

Amlodipine

Mechanism

A

Interact with L-type voltage gated plasma membrane Ca channel –> decreased calcium entry into vascular smooth muscle cell, preventing contraction; causes dilation of epicardial coronary arteries, arteriolar resistance arteries; less heart-specific activity

57
Q

Amlodipine

Uses

A

Hypertension, Raynauds, angina (3rd choice drug)

58
Q

Amlodipine

Side effects

A

Leg edema (less than 1st generation), heart failure, AV nodal blockade, reflex tachycardia (lipophilic agents gain entry to brain and depress vasomotor center, rapidly dropping BP; this causes more reflex sympathetic activation (leading to adverse CV effects); long-acting agents are less lipophilic, and will cause less sympathetic activation and initial fall in BP)

Constipation (most common), headache, flushing

Contraindicated in overt decompensated heart failure, bradycardia, sinus node dysfunction, high-degree AV block

59
Q

Nifedipine

Drug class

A

Dihydropyridine Calcium channel blockers

60
Q

Nifedipine

Mechanism

A

Interact with L-type voltage gated plasma membrane Ca channel –> decreased calcium entry into vascular smooth muscle cell, preventing contraction; causes dilation of epicardial coronary arteries, arteriolar resistance arteries; less heart-specific activity

61
Q

Nifedipine

Uses

A

Hypertension, Raynauds, angina (3rd choice drug)

62
Q

Nifedipine

Side effects

A

Leg edema (less than 1st generation), heart failure, AV nodal blockade, reflex tachycardia (lipophilic agents gain entry to brain and depress vasomotor center, rapidly dropping BP; this causes more reflex sympathetic activation (leading to adverse CV effects); long-acting agents are less lipophilic, and will cause less sympathetic activation and initial fall in BP)

Constipation (most common), headache, flushing

Contraindicated in overt decompensated heart failure, bradycardia, sinus node dysfunction, high-degree AV block

63
Q

Propranolol

Drug class

A

Nonselective β-blocker

64
Q

Propranolol

Mechanism

A

Nonselective β-blocker; primarily reduces cardiac output

65
Q

Propranolol

Side effects

A

Bronchospasm, bradycardia (negative chronotrope), CHF (negative ionotrope), masking of hypoglycemia symptoms

Decreased exercise capacity, depression (crosses BBB), worsening symptoms of peripheral vascular disease

66
Q

Metoprolol

Drug class

A

β1-selective blocker

67
Q

Metroprolol

Mechanism

A

Moderately selective β1 blockade

68
Q

Metoprolol

Side effects

A

Less likely to have bronchospasm, hypoglycemic awareness, and depression

69
Q

Atenolol

Drug class

A

β1-selective blocker

70
Q

Atenolol

Mechanism

A

Moderately selective β1 blockade

71
Q

Atenolol

Side effects

A

Less likely to have bronchospasm, hypoglycemic awareness, and depression

72
Q

Bisoprolol

Drug class

A

β1-selective blocker

73
Q

Bisoprolol

Mechanism

A

Moderately selective β1 blockade

74
Q

Bisoprolol

Side effects

A

Less likely to have bronchospasm, hypoglycemic awareness, and depression

Longer-acting than other beta-blockers

75
Q

Nadolol

Drug class

A

β1-selective blocker

76
Q

Nadolol

Mechanism

A

Moderately selective β1 blockade

77
Q

Nadolol

Side effects

A

Less likely to have bronchospasm, hypoglycemic awareness, and depression

Longer-acting than other beta-blockers

78
Q

Labetolol

Drug class

A

Combined αβ blocker

79
Q

Labetolol

Mechanism

A

β1 blockade with vasodilatory effects

80
Q

Labetolol

Uses

A

Hypertensive urgency

81
Q

Carvedilol

Drug class

A

Combined αβ blocker

82
Q

Carvedilol

Mechanism

A

β1 blockade with vasodilatory effects

83
Q

Carvedilol

Uses

A

Acute coronary syndrome, CHF

84
Q

Esmolol

Drug class

A

β1-selective blocker

85
Q

Esmolol

Uses

A

AV nodal blockade in unstable patients

Short half-life

86
Q

Terazosin (Hytrin); Doxazosin (Cardura)

Drug class

A

α1-adrenergic receptor antagonist

87
Q

Terazosin (Hytrin); Doxazosin (Cardura)

Mechanism

A

Blocks post-synaptic α1-adrenergic receptor antagonist on vascular smooth muscle

88
Q

Terazosin (Hytrin); Doxazosin (Cardura)

Uses

A

BPH; second-tier meds (use when other condition around, not for isolated hypertension)

89
Q

Terazosin (Hytrin); Doxazosin (Cardura)

Side effects

A

Orthostatic hypotension, fluid retention, worsening angina (secondary to reflex tachycardia)

90
Q

Clonidine

Drug class

A

Central α2-agonist

91
Q

Clonidine

Mechanism

A

Stimulation of central α2a adrenergic receptors –> reduction in sympathetic outflow from vasomotor systems in brainstem; inhibition of renin release (secondary to decreased sympathetic tone)

92
Q

Clonidine

Side effects

A

Rebound HTN if abruptly stopped; moderate orthostatic hypotension

Sedation, dry mouth, fatigue, depression

93
Q

α-methyldopa (Aldomet)

Drug class

A

Central α2-agonist

94
Q

α-methyldopa (Aldomet)

Mechanism

A

Stimulation of central α2a adrenergic receptors –> reduction in sympathetic outflow from vasomotor systems in brainstem; inhibition of renin release (secondary to decreased sympathetic tone)

95
Q

α-methyldopa (Aldomet)

Uses

A

Hypertension of pregnancy (only)

96
Q

α-methyldopa (Aldomet)

A

Rebound HTN if abruptly stopped; moderate orthostatic hypotension

Sedation, dry mouth, fatigue, depression

Takes place of dopa, so less NE (also, methyl-NE activates α2)

97
Q

Reserpine

Drug class

A

Ganglion blocking agent (adrenergic neuron blocking agent)

98
Q

Reserpine

Mechanism

A

Blocks transport of NE, DA, and 5HIAA into storage granules in PNS and CNS –> less neurotransmitter available when nerves are stimulated

99
Q

Reserpine

Uses

A

Decrease cardiac output and systemic vascular resistance

100
Q

Reserpine

Side effects

A

Sedation, mental depression, Parkinsonism symptoms

101
Q

Hydralazine

Drug class

A

Direct (vasodilators)

102
Q

Hydralazine

Mechanism

A

Relax smooth muscle of peripheral arterioles

Serves as an antioxidant, preventing oxidation of NO

103
Q

Hydralazine

Uses

A

Hypertensive urgency; patients with BOTH advanced CHF and hypertension

104
Q

Hydralazine

Side effects

A

Drug-induced lupus

reflex tachycardia

105
Q

Minoxidil

Drug class

A

Direct (vasodilators)

106
Q

Minoxidil

Mechanism

A

Relax smooth muscle of peripheral arterioles

Smooth muscle relaxation by opening cardiovascular ATP-sensitive potassium channels

107
Q

Minoxidil

Uses

A

Refractory hypertension; hair loss

108
Q

Minoxidil

Side effects

A

Pericardial effusion; hirsutism

reflex tachycardia

Pharmacology (26 decks)

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