Unit 4-Antihypertensives Flashcards Preview

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Flashcards in Unit 4-Antihypertensives Deck (108):
1

Furosemide

Drug class

Loop diuretic

2

Furosemide

Mechanism

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

3

Furosemide

Uses

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)

4

Furosemide

Side effects

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

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

5

Hydrochlorothiazide

Drug class

Thiazide diuretic

6

Hydrochlorothiazide

Mechanism

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

7

Hydrochlorothiazide

Uses

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

8

Hydrochlorothiazide

Side effects

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

9

Chlorthalidone

Drug class

Thiazide-like diuretic

10

Chlorthalidone

Mechanism

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

11

Chlorthalidone

Uses

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

12

Chlorthalidone

Side effects

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

13

Metolazone

Drug class

Thiazide-like diuretic

14

Metolazone

Mechanism

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

15

Metolazone

Uses

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

16

Metolazone

Side effects

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

17

Amiloride

Drug class

Renal ENaC inhibitor

18

Amiloride

Mechanism

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

19

Amiloride

Uses

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

20

Amiloride

Side effects

Hyperkalemia in patients with renal failure or on ACE inhibitors

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

21

Spironolactone

Drug class

Aldosterone receptor antagonist

22

Spironolactone

Mechanism

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

23

Spironolactone

Uses

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

24

Spironolactone

Side effects

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

25

Eplerenone

Drug class

Potassium-sparing diuretic

26

Eplerenone

Mechanism

Block alodesterone; inhibits sodium reabsorption in distal tubule

27

Eplerenone

Uses

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

28

Eplerenone

Side effects

Hyperkalemia; much lower incidence of gynecomastia and mennorhagia

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

29

Captopril

Drug class

short-acting ACE-I (vasodilators)

30

Captopril

Mechanism

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

31

Captopril

Uses

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

32

Captopril

Side effects

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

33

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

Drug class

long-acting ACE-I (vasodilators)

34

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

Mechanism

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

35

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

Uses

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

36

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

Side effects

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

37

Enalapril

Drug class

ACE-I (vasodilators)

38

Enalapril

Mechanism

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)

39

Enalapril

Uses

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

40

Enalapril

Side effects

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

41

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

Drug class

Angiotensin II Recepter Blockers

42

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

Mechanism

Competitive inhibition of angiotensin II in vascular endothelium

43

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

Uses

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

44

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

Side effects

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

Aliskiren

Drug class

Renin inhibitor

46

Aliskiren

Uses

Not very effective

47

Diltiazem

Drug class

Non-dihydropyridine Calcium channel blockers

48

Diltiazem

Mechanism

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

Diltiazem

Uses

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

50

Diltiazem

Side effects

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

Verapamil

Drug class

Non-dihydropyridine Calcium channel blockers

52

Verapamil

Mechanism

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

Verapamil

Uses

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

54

Verapamil

Side effects

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

Amlodipine

Drug class

Dihydropyridine Calcium channel blockers

56

Amlodipine

Mechanism

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

Amlodipine

Uses

Hypertension, Raynauds, angina (3rd choice drug)

58

Amlodipine

Side effects

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

Nifedipine

Drug class

Dihydropyridine Calcium channel blockers

60

Nifedipine

Mechanism

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

Nifedipine

Uses

Hypertension, Raynauds, angina (3rd choice drug)

62

Nifedipine

Side effects

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

Propranolol

Drug class

Nonselective β-blocker

64

Propranolol

Mechanism

Nonselective β-blocker; primarily reduces cardiac output

 

65

Propranolol

Side effects

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

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

66

Metoprolol

Drug class

β1-selective blocker

67

Metroprolol

Mechanism

Moderately selective β1 blockade

 

68

Metoprolol

Side effects

Less likely to have bronchospasm, hypoglycemic awareness, and depression

69

Atenolol

Drug class

β1-selective blocker

70

Atenolol

Mechanism

Moderately selective β1 blockade

 

71

Atenolol

Side effects

Less likely to have bronchospasm, hypoglycemic awareness, and depression

72

Bisoprolol

Drug class

β1-selective blocker

73

Bisoprolol

Mechanism

Moderately selective β1 blockade

74

Bisoprolol

Side effects

Less likely to have bronchospasm, hypoglycemic awareness, and depression

Longer-acting than other beta-blockers

75

Nadolol

Drug class

β1-selective blocker

76

Nadolol

Mechanism

Moderately selective β1 blockade

77

Nadolol

Side effects

Less likely to have bronchospasm, hypoglycemic awareness, and depression

Longer-acting than other beta-blockers

78

Labetolol

Drug class

Combined αβ blocker

79

Labetolol

Mechanism

β1 blockade with vasodilatory effects

80

Labetolol

Uses

Hypertensive urgency

81

Carvedilol

Drug class

Combined αβ blocker

82

Carvedilol

Mechanism

β1 blockade with vasodilatory effects

83

Carvedilol

Uses

Acute coronary syndrome, CHF

84

Esmolol

Drug class

β1-selective blocker

85

Esmolol

Uses

AV nodal blockade in unstable patients

Short half-life

86

Terazosin (Hytrin); Doxazosin (Cardura)

Drug class

α1-adrenergic receptor antagonist

87

Terazosin (Hytrin); Doxazosin (Cardura)

Mechanism

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

88

Terazosin (Hytrin); Doxazosin (Cardura)

Uses

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

89

Terazosin (Hytrin); Doxazosin (Cardura)

Side effects

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

90

Clonidine

Drug class

Central α2-agonist

91

Clonidine

Mechanism

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

Clonidine

Side effects

Rebound HTN if abruptly stopped; moderate orthostatic hypotension

Sedation, dry mouth, fatigue, depression

93

α-methyldopa (Aldomet)

Drug class

Central α2-agonist

94

α-methyldopa (Aldomet)

Mechanism

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

α-methyldopa (Aldomet)

Uses

Hypertension of pregnancy (only)

96

α-methyldopa (Aldomet)

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

Reserpine

Drug class

Ganglion blocking agent (adrenergic neuron blocking agent)

98

Reserpine

Mechanism

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

99

Reserpine

Uses

Decrease cardiac output and systemic vascular resistance

100

Reserpine

Side effects

Sedation, mental depression, Parkinsonism symptoms

101

Hydralazine

Drug class

Direct (vasodilators)

102

Hydralazine

Mechanism

Relax smooth muscle of peripheral arterioles

Serves as an antioxidant, preventing oxidation of NO

103

Hydralazine

Uses

Hypertensive urgency; patients with BOTH advanced CHF and hypertension

104

Hydralazine

Side effects

Drug-induced lupus

reflex tachycardia

 

105

Minoxidil

Drug class

Direct (vasodilators)

106

Minoxidil

Mechanism

Relax smooth muscle of peripheral arterioles

Smooth muscle relaxation by opening cardiovascular ATP-sensitive potassium channels

107

Minoxidil

Uses

Refractory hypertension; hair loss

108

Minoxidil

Side effects

Pericardial effusion; hirsutism

reflex tachycardia