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PHM 521 > Antihypertension Drugs > Flashcards

Antihypertension Drugs Flashcards

1
Q

First line antihypertensives

A

thiazide diuretics, ACEI, ARB, Calcium Channel Blockers

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2
Q

diuretics

A

thiazide diuretics, loop diuretics, mineralocorticoid (aldosterone) receptor antagonists, potassium sparing diuretics

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3
Q

RAAS blockers

A

ACEI, ARB, direct renin inhibitors

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4
Q

direct vasodilators

A

calcium channel blockers, hydralazine, minoxidil

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5
Q

sympatholytic agents

A

beta blockers, clonidine

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6
Q

thiazide diuretics can lower BP up tp ___ mmHg and can be used as _____

A

thiazide diuretics can lower BP up to 10-15 mmHg and can be used as a monotherapy for mild htn, but is often used in combination

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7
Q

chlorthalidone

A

hygroton/thalitone is a first line thiazide diuretic

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8
Q

hydrochlorothiazide;indapamide

A

lozol is a first line thiazide diuretic

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9
Q

metolazone

A

zaroxolyn is a first line thiazide diuretic

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10
Q

thiazide diuretic MOA

A

increases na, water and cl excretion by blocking reabsorption in distal convoluted tubule

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11
Q

thiazide diuretic contraindications

A

hypersensitivity to sulfonamides (low risk of cross reactivity), anuria

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12
Q

thiazide diuretic adr

A

dizziness, hyperuricemia, hyponatremia, hypokalemia, hypomagnesemia, hypercalcemia, pancreatitis

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13
Q

thiazide diuretic key PK/PD parameters

A

secreted by organic acid secretory system in the proximal tubule which completes with secretion of uric acid –> elevates levels of uric acid

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14
Q

thiazide diuretic notes

A

not as effective if CrCl < 30ml/min (chlorthalidone preferred), avoid NSAIDs, avoid in gout, less effective w/ low GFR, take in morning

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15
Q

furosemide

A

lasix is a loop diuretic

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16
Q

loop diuretic moa

A

actively secreted via nonspecific organ acid transport system into the lumen of the thick ascending loop of Henle, decreasing Na absorption

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17
Q

loop diuretic contraindication

A

anuria

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18
Q

loop diuretic adr

A

hyperuricemia, hypokalemia, hypomagnesemia, dizziness, AKI, ototoxicity

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19
Q

loop diuretic DDI

A

increased risk of ototoxicity with aminoglycosides

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20
Q

loop diuretic notes

A

results in most fluid loss, black boxed for profound fluid and electrolyte loss, more potent than thiazides, preferred in patients with HF, consider ethacrynic acid with true sulfa allergy

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21
Q

PK/PD of furosemide

A

loop diuretic, 40-70% bioavailability, lasts 4-8 hrs, 1-2 hr half life, mainly renal elimination

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22
Q

PK/PD of torsemide

A

loop diuretic, 90% bioavailability, lasts 8-12 hrs, 3.5 hr half life, mainly hepatic elimination

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23
Q

PK/PD of bumetanide

A

loop diuretic, 90% oral bioavailability, 3-6 hr duration, ~1 hr half life, half renal and half hepatic elimination

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24
Q

PK/PD of ethacrynic acid

A

loop diuretic with 100% oral bioavailability, 2-4 hr IV, 12 hr duration orally, 2-4 hr half life, renal elimination

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25
Q

spironolactone

A

aldactone/carospir is a mineralocorticoid receptor antagonist (MRA)

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26
Q

eplerenone

A

inspra is a mineralocorticoid receptor antagonist (MRA)

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27
Q

mineralocorticoid receptor antagonist (MRA) moa

A

competes with aldosterone for receptor sites in the distal renal tubules increasing na, cl and water excretion whole conserving k and h ions, may block effect of aldosterone on smooth muscle

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28
Q

mineralocorticoid receptor antagonist (MRA) contraindications

A

anuria, hyperkalemia

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29
Q

mineralocorticoid receptor antagonist (MRA) adr

A

dehydration, hyponatremia, dizziness, cardiac arrhythmias due to electrolyte abnormalities
spironolactone: gynecomastia, breast tenderness, impotence
eplerenone: increased TG

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30
Q

mineralocorticoid receptor antagonist (MRA) key PK/PD

A

spironolactone: binds with high affinity to androgen receptor which causes gynecomastia and decreased libido
eplerenone: much greater selectivity

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31
Q

mineralocorticoid receptor antagonist (MRA) DDi

A

eplerenone: strong CYP3A4 inhibitors will increase concentrations

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32
Q

mineralocorticoid receptor antagonist (MRA) notes

A

minimally efficacious blood pressure control when used as a monotherapy, preferred in aldosteronism and resistant htn, use with thiazide or loop diuretic to combat K loss

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33
Q

triamterene

A

maxzide is a potassium sparing diuretic

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34
Q

amiloride

A

potassium sparing diuretic

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35
Q

potassium sparing diuretic moa

A

competitive inhibition of epithelial na channel in collecting duct of nephron to decrease na reabsorption and increase k reabsorption

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36
Q

potassium sparing diuretic contraindications

A

hypersensitivity to sulfonamides

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37
Q

potassium sparing diuretic adr

A

hyperkalemia, hypotension, dizziness, ha, gout, sjs

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38
Q

potassium sparing diuretic PK/PD

A

amiloride has a longer duration of action that triamterene (24 > 8)

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39
Q

potassium sparing diuretic notes

A

almost always in combination tablet to decrease rates of hyperkalemia with thiazide diuretics, avoid if CrCl <45ml/min, can be used with thiazide or loop diuretic to combat K loss

40
Q

lisinopril

A

prinivil/zestril is an ACEI

41
Q

ACEI moa

A

competitive angiotensin converting enzyme inhibitor that prevents stimulation of angiotensin II receptor which is responsible for vasoconstriction

42
Q

ACEI contraindications

A

history of acei induced, hereditary, or idiopathic angioedema, pregnancy

43
Q

ACEI adr

A

hyperkalemia, aki, dizziness, dry cough, angioedema, liver failure

44
Q

ACEI key PK/PD

A

renally eliminated, inhibits breakdown of bradykinin causing dry cough and angioedema

45
Q

ACEI DDI

A

increased risk of hyperkalemia and/or angioedema in combination with other RAAS inhibitors

46
Q

ACEI notes

A

if side effects- try ARB, combinations available (hydrochlorothiazide, ccb), target organ protection, do not use if K about 5mmol/L, do not use other RAAS

47
Q

valsartan

A

Diovan is an ARB

48
Q

ARB moa

A

selective reversible angiotensin II receptor

49
Q

ARB contraindications

A

pregnancy

50
Q

ARB adr

A

hyperkalemia, AKI, dizziness, angioedema, rhabdomyolysis

51
Q

ARB DDI

A

increased risk of hyperkalemia and/or angioedema in combination with other RAASi

52
Q

ARB notes

A

may use first if trying to prevent side effects like dry cough, combinations available (hydrochlorothiazide, CCB), target organ protection, do not use if K >5mmol/L, no washout period when transitioning, less dry cough /angioedema

53
Q

amlodipine

A

norvasc is a DHP CCB

54
Q

nifedipine

A

procardia is a DHP CCB

55
Q

DHP CCB moa

A

inhibits calcium ions from entering slow channels of vascular smooth muscle- leading to vasodilation

56
Q

DHP CCB adr

A

peripheral and pulmonary edema, hepatotoxicity, thrombocytopenia

57
Q

DHP CCB key PK/PD

A

may cause reflex sympathetic activation –> slight tachycardia and increase in cardiac output
amlodipine may take at least 3 days to 1 week to see full lowering effects

58
Q

DHP CCB ddi

A

major substrate of CYP3A4

59
Q

DHP CCB notes

A

immediate release nifedipine should not be used as it has increased risk for MI and mortality, can take up to one week to see full effect

60
Q

diltiazem

A

cardizem is a NONDHP CCB

61
Q

verapamil

A

calan is a NONDHP CCB

62
Q

NONDHP CCB moa

A

inhibits ca ions from entering smooth muscle and myocardium, causing vasodilation and slowing of AV node

63
Q

NONDHP CCB contraindications

A

2nd or 3rd degree heart block

64
Q

NONDHP CCB adr

A

peripheral edema, pulmonary edema, ha, heart failure, heart block, hepatotoxicity

65
Q

NONDHP CCB key PK/PD

A

verapamil has the greatest depressive effects on SNS

66
Q

NONDHP CCB ddi

A

major substrates of CYP3A4, moderate inhibitors of CYP3A4 - ddi worse with verapamil

67
Q

hydralazine

A

apresoline is a vasodilator

68
Q

hydralazine moa

A

direct vasodilation

69
Q

hydralazine contraindications

A

CAD- causes reflex tachycardia and angina

70
Q

hydralazine adr

A

dizziness, reflex tachycardia, DILE at high doses

71
Q

hydralazine PK/PD

A

variable duration and effect, short half-life that requires frequent dosing

72
Q

hydralazine notes

A

dosing for htn is 4x daily, less reflex tachycardia risk than minoxidil

73
Q

minoxidil moa

A

direct vasodilation

74
Q

minoxidil contraindications

A

CAD- causes reflex tachycardia and angina

75
Q

minoxidil adr

A

dizziness, reflex tachycardia, hypertrichosis, pericarditis

76
Q

minoxidil notes

A

causes fluid and water retention- should be given with a diuretic, should be given with a beta blocker to prevent tachycardia, extremely potent vasodilator, increased risk of reflex tachycardia

77
Q

metoprolol

A

lopressor/toprol is a beta blocker

78
Q

beta blocker moa

A

inhibits beta 1/2 receptors decreasing HR and myocardial contractility- varies based on selectivity

79
Q

beta blocker contraindications

A

severe bradycardia

80
Q

beta blocker adr

A

dizziness, fatigue, reduced exercise tolerance, bronchospasm, insomnia, impotence

81
Q

beta blocker notes

A

avoid abrupt withdrawal, patients may feel fatigued at start- this will abate with time, can mask feelings of low glucose, use with caution in patients with severe bronchospastic disease, can enhance hypoglycemic effects

82
Q

beta blocker ddi

A

additive av nodal blockade with NONDHP CCB

83
Q

beta 1 selective blockers

A

atenolol, betaxolol, bisoprolol, esmolol, metoprolol, nebivolol, acebutolol

84
Q

blockers with beta 1 and 2 activity

A

carvedilol, labetalol, nadolol, pindolol, propranolol, sotalol, timolol

85
Q

beta blockers with alpha 1 blockagte

A

carvedilol, labetalol

86
Q

beta blockers with NO stimulation

A

nebivolol

87
Q

beta blockers with SNS activity

A

acebutolol, pindolol

88
Q

clonidine

A

catapres/kapvay is an alpha 2 agonist

89
Q

alpha 2 agonist moa

A

stimulates alpha 2 receptors resulting in reduced sympathetic outflow from CNS

90
Q

alpha 2 agonist adr

A

dry mouth, somnolence/fatigue/sedation, constipation, clonidine patch may have local irritation as well

91
Q

alpha 2 agonist PK/PD

A

lipid soluble, short half-life- dosed at least 2x daily

92
Q

alpha 2 agonist notes

A

avoid abrupt discontinuation, use patch for 7 days- takes 2-3 days onset- oral dosing needed at that time

93
Q

NON DHP CCB notes

A

cyp3a4 major substrate inhibitor (dose adjustments for lovastatin/simvastatin), avoid in patients w HFrEF, avoid routine use with beta blockers, multiple brands exist, diltiazem is the only brand w capsules that can be sprinkled over food

94
Q

aliskiren

A

tekturna is a direct renin inhibitor
should not be used with other RAAS, long half life, lack of data, expensive

95
Q

doxazosin

A

cardura is an alpha 1 agonist can treat htn and bph in men, increase risk of hf and orthostatic hypotension

PHM 521 (11 decks)

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