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M2 Pharmacology Jen > Antihypertensives > Flashcards

Antihypertensives Flashcards

1
Q

Hydrochlorothiazide: class

A

Thiazide diuretic, reduces Na reabsorption in distal tubule

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2
Q

Hydrocholorthiazide: indication

A

Antihypertensive, diuretic

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3
Q

Lisinopril: class

A

ACE inhibitor

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4
Q

Lisinopril: indication

A

Antihypertensive, CHF

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5
Q

Captopril: class

A

ACE inhibitor

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6
Q

Captopril: indication

A

Antihypertensive, CHF

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7
Q

Enalapril: class

A

ACE Inhibitor

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8
Q

Enalapril: indication

A

Antihypertensive, CHF

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9
Q

Ramipril: class

A

ACE Inhibitor

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10
Q

Ramipril: indication

A

Antihypertensive, CHF

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11
Q

Losartan: class

A

Angiotensin-1 receptor blocker

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12
Q

Losartan: indication

A

Antihypertensive, diuretic

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13
Q

Nitroprusside: class

A

Venous and Arterial Vasodilator

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14
Q

Nitroprusside: indication

A

Antihypertensive, CHF

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15
Q

Hydralazine: class

A

Arterial vasodilator

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16
Q

Hydralazine: indication

A

Antihypertensive, CHF

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17
Q

Verapamil: class

A

Calcium entry blockers

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18
Q

Verapamil: indication

A

Antihypertensive, antianginal, antiarrhythmic Class IV

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19
Q

Nifedipine: class

A

Calcium entry blockers

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20
Q

Nifedipine: indication

A

Antihypertensive, antianginal, antiarrhythmic

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21
Q

Amlodipine: class

A

Calcium entry blockers

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22
Q

Amlodipine: indication

A

Antihypertensive, antianginal, antiarrhythmic

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23
Q

Diltiazem: class

A

Ca entry blocker

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24
Q

Diltiazem: indication

A

Antihypertensive, antianginal, antiarrhythmic

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25
Q

Nicardipine: class

A

Ca entry blocker

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26
Q

Nicardipine: indication

A

Antihypertensive, antianginal, antiarrhythmic

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27
Q

Hydrochlorothiazide: PD

A

block reuptake of Cl and Na from tubular fluid after glomerular filtration; also appears to cause decrease in SVR via unclear mechanism; will lower BP by up to 10-15 mm in many patients; useful as monotherapy or in combinations; HCTZ most commonly used, but perhaps some slight edge to chlorthalidone (duration, efficacy)

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28
Q

Hydrochlorothiazide: PK

A

F ~70%, excreted unchanged in urine; short half-life (hours); HCTZ not available in IV formulation; onset 2 h, peak 5 h, duration 10 h

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29
Q

Hydrochlorothiazide: tox

A

allergy to sulfa antibiotics (?); cause K and Mg depletion; cause Na and Cl depletion, metabolic alkalosis; volume depletion; worsen hyperuricemia

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30
Q

Hydrochlorothiazide: interactions

A

additive effects with most other antihypertensives

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31
Q

Hydrochlorothiazide: special

A

more side effects in geriatric patients; Pregnancy Class D; much less effective in patients with reduced GFR

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32
Q

Hydrochlorothiazide: monitor

A

BP, weight, edema, K, Mg, BUN, creatinine

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33
Q

Lisinopril: PD

A

inhibits conversion of AT I to AT II by ACE; diminishes both vasocontriction and stimulation of aldosterone secretion by AT II

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34
Q

Lisinopril: PK

A

well absorbed; onset 1 h, peak 6 h, duration 24 h; once a day is fine; excreted primarily in urine as unchanged drug

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35
Q

Lisinopril: tox

A

orthostatic hypotension; use with caution in patients with impaired renal function, or renal artery stenosis; be careful in patients on diuretics, or those with aortic stenosis; angioedema, cough; acute renal failure

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36
Q

Lisinopril: interactinos

A

additive effects with most other antihypertensives; NSAIDs may reduce ability to lower BP; hyperkalemia with KCL, others

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37
Q

Lisinopril: special

A

often discontinue diuretics prior to beginning use to reduce hypotension; Category C/D in pregnancy, abnormal cartilage development

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38
Q

Lisinopril: monitor

A

BP, weight, edema, K, BUN, creatinine!!!!!

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39
Q

Why might Lisinopril be best option for preserving renal function?

A

Inhibits ATII, which causes constriction of efferent arterioles. Can damage glomeruli. But if you dilate the efferent, lowers pressure inside glomerulus, preserves fxn longer. Slows progression of renal failure in diabetics.

40
Q

Losartan: PD

A

block stimulation of AT I receptor by angiotensin II, thereby reducing vasoconstriction and production of aldosterone

41
Q

Losartan: PK

A

F ~30%; onset 6 h; extensive first pass effect; active metabolite is 40x more potent, much longer half-life

42
Q

Losartan: tox

A

dizziness; orthostatic hypotension; worsening of renal failure

43
Q

Losartan: interactions

A

additive effects with most other antihypertensives

44
Q

Losartan: special

A

Pregnancy class C/D; use care in patients on diuretics, those with renal artery stenosis, those with mitral or aortic stenosis

45
Q

Losartan: monitor

A

BP, weight, edema, lytes, BUN, creatinine!!!

46
Q

Nitroprusside: PD

A

acts “directly” on vascular smooth muscle to cause dilatation of both veins and arterioles; metabolized to release CN- and NO, which activates guanylate cyclase, leads to production of cGMP from GTP, which then leads to vasodilation; cGMP then hydrolyzed to GMP by PDE

47
Q

Nitroprusside: PK

A

only route is iv; rapid onset (minutes) and cessation (minutes), thereby allowing minute-by-minute titration; CN- metabolite is converted to SCN in liver, then excreted in urine; must be given by continuous infusion

48
Q

Nitroprusside: tox

A

excessive hypotension; accumulation of CN- and thiocyanate; headache; decreased blood flow to brain

49
Q

Nitroprusside: interactions

A

additive effects with most other antihypertensives

50
Q

Nitroprusside: special

A

monitor patient VERYclosely—must be in ICU with arterial line; avoid high infusion rates or prolonged infusions, to prevent accumulation of CN-; use with caution in patients with increased intracranial pressure

51
Q

Nitroprusside: monitor

A

BP, HR, metabolic acidosis; most often requires arterial line

52
Q

Hydralazine: PD

A

“direct” acting vasodilator; seems to act by inducing endothelium to produce NO, which then passes to SM cells and induces production of cGMP, minimal venodilating effect

53
Q

Hydralazine: PK

A

given po, im, iv; metabolized extensively in GI mucosa and in liver, eventually excreted as metabolites in urine; F ~40%; onset 30 after po dose, 10 min after iv dose; persist for 2-6 hours

54
Q

Hydralazine: tox

A

more dangerous in patients with renal disease, prior stroke, angina; watch for hypotension, edema, occasionally drug-induced lupus

55
Q

Hydralazine: interactions

A

additive effects with most other antihypertensives

56
Q

Hydralazine: special

A

never use as chronic oral monotherapy for treatment of hypertension, since edema and reflex tachycardia will result; concern giving to patients with CAD

57
Q

Hydralazine: monitor

A

BP, weight, edema, BUN, creatinine, symptoms of lupus or angina

58
Q

Hydralazine: use in pregnancy

A

Lowers BP in 3rd tri. Used for short period of time, won’t cause lupus.

59
Q

Verapamil: PD

A

reduces BP by inhibiting influx of calcium through “slow channels”, thereby dilating peripheral arterioles; produces negative inotropic effect as well; for angina, reduces afterload, thus decreasing oxygen consumption; also, inhibits spasm of coronary arteries in vasospastic angina; blocks reentry paths through AV nodes in paroxysmal SVT

60
Q

Verapamil: PK

A

absorbed rapidly, but F ~30%; also available in SR tablets; cleared by kidney and liver (produces active metabolites); onset 2 h po, 1-5 min iv; half-life 6-12 h; may be given po or iv

61
Q

Verapamil: tox

A

hypotension, AV block, worsening of CHF, bradycardia

62
Q

Verapamil: interactions

A

additive effects with most other antihypertensives; additive toxic effects on heart when given with beta-blockers

63
Q

Verapamil: special

A

use reduced doses in patients with both renal and hepatic disease; short-acting nifedipine (and similar CEBs) can increase risk of MI (unclear why); Pregnancy C

64
Q

Verapamil: monitor

A

BP, weight, edema

65
Q

Nifedipine: same class as ?

A

same as Verapamil

66
Q

Clonidine: PD

A

stimulates alpha-2 adrenoceptors in brainstem, thereby leading to down-regulation of sympathetic output

67
Q

Clonidine: PK

A

Onset 1 h, duration 8 h, F~85%, also available as cutaneous patch

68
Q

Clonidine: tox

A

withdraw gradually because of risk of rebound HTN; risk of bradycardia in sinus node disease; lethargy, fatigue, depression

69
Q

Clonodine: interaction

A

additive effects with most other antihypertensives; additive sedation with other CNS drugs

70
Q

Clonidine: special

A

Pregnancy class C; avoid in patients with renal insufficiency

71
Q

Clonidine: monitor

A

follow BP and HR, fatigue

72
Q

Methyldopa: class

A

a2 agonist (central action)

73
Q

Methyldopa: indication

A

antihypertensive

74
Q

Clonidine: class

A

a2 agonist (central action)

75
Q

Clonidine: indication

A

antihypertensive

76
Q

Trimethaphan: class

A

NN (ganglionic) blocker

77
Q

Trimethaphan: indication

A

Antihypertensive

78
Q

Reserpine: class

A

Blocks NE uptake into vesicles

79
Q

Reserpine: indication

A

Antihypertensive

80
Q

Reserpine: PD

A

binds to vesicles that contain NE or serotonin, preventing their uptake, and ultimately depleting the neuron of NE (or serotonin); this effect takes 2-3 weeks to develop, and including neurons and also the adrenal medulla

81
Q

Reserpine: PK

A

good oral bioavailability, but biologic effects take 2-3 weeks to develop (via slow depletion of NE from vesicles)

82
Q

Reserpine: tox

A

dizziness; orthostatic hypotension; depression

83
Q

Reserpine: interaction

A

additive effects with most other antihypertensives

84
Q

Reserpine: special

A

approved by the FDA in 1953!!! First antihypertensive drug approved, and first sympatholytic drug approved by the FDA (remember that in 1960’s, drugs included only reserpine, HCTZ, and hydralazine)

85
Q

Reserpine: monitor

A

BP, sympathetic tone, depression!!!!

86
Q

Reserpine: note

A

I include this drug to show that this mechanism does work, and for historical interest!! This drug is not used in the long-term management of HTN today in the US, but it is of great historical importance!!

87
Q

Atenolol: class

A

B1 blocker

88
Q

Atenolol: indication

A

Antihypertensive, antianginal, antiarrhythmic, anti-MI

89
Q

Prazosin: class

A

A1 blocker

90
Q

Prazosin: indication

A

Antihypertensive, Rx for BHP

91
Q

Terazosin: class

A

A1 blocker

92
Q

Terazosin: indication

A

Antihypertensive, Rx for BHP

93
Q

Doxazosin: class

A

A1 blocker

94
Q

Doxazosin: indication

A

Antihypertensive, Rx for BHP

95
Q

Labetalol: class

A

A1 and B blocker

96
Q

Labetalol: indication

A

Antihypertensive, pheochromocytoma, Hypertensive crisis, pre-eclampsia

M2 Pharmacology Jen (11 decks)

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