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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
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

Pharmacology (26 decks)

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