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Pharm exam 5 > Antihypertensives > Flashcards

Antihypertensives Flashcards

1
Q

evidence based tx of systemic arterial HTN

A

Treat with the intent of reducing risk of CV events and thereby reducing CV morbidity and mortality.

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2
Q

BP goal (controversial)

A

< 150/90 mmHg for patients > 60 y.o. (<140/90? controversial)

< 140/90mmHg for most patients < 60 years of age

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3
Q

strategies for antihypertensive therapy

A

Reduce TPR

Reduce CO

Reduce body fluid volume (salt & water)

Adjust homeostatic regulatory reflexes

  • reflex tachycardia (increased SANS)
  • edema (increased renin activity)
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4
Q

MOA of clonidine and role in therapy?

A

increase a2 activity - alter SANS activity

Most commonly prescribed central alpha2-agonist

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5
Q

SE of clonidine

A

Can cause rebound hypertension if stopped abruptly

Optimally used with a diuretic to diminish fluid retention

Overdose can cause paradoxical hypertension

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6
Q

MOA of a-methyldopa

A

Stimulate central alpha2 receptors –> decreased release of NE

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7
Q

role of a methyldopa in therapy

A

gestational hypertension

chronic hypertension in pregnancy

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8
Q

MOA of reserpine

A

blocks transport of NE into storage granules

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9
Q

role of reserpine in therapy

A

the most effective use of reserpine is in combination with a thiazide diuretic, which can mitigate related sodium and water retention.

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10
Q

SE of resserpine

A
  • *strong sympatholytic effect results in increased parasympathetic activity:**
  • nasal stuffiness, increased gastric acid secretion, diarrhea, and bradycardia.
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11
Q

MOA of guanethidine

A

affect vesicle storage:
- Transported across the sympathetic nerve membrane via NET1 –> concentrated in transmitter vesicles & replaces NE –> gradual depletion of NE stores

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12
Q

name the ACE inhibitors

A

Captopril, Lisinopril, Fosinopril

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13
Q

role of ACE inhibitors in therapy (Captopril, Lisinopril, Fosinopril)

A

First-line or add-on therapy for uncomplicated HTN

First-line therapy for compelling indications of:

  • diabetes
  • chronic kidney disease
  • coronary artery disease
  • left ventricular dysfunction
  • previous ischemic stroke
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14
Q

ACE inhibitors are cleared mostly by what?

when would you reduce the dose?

A

Cleared mostly by the kidney –> reduce dose in kidney failure

Elevated plasma renin activity causes hyperresponsive to ACEIs  reduce doses in pts with high plasma renin levels (e.g., heart failure, Na+-depleted patients)

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15
Q

action of ACE?

A

Angiotensin I –> angiotensin II

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16
Q

SE of ACEI

A

coughing

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17
Q

who should avoid use of ACEI

A

pregnancy

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18
Q

what are the angiotensin receptor blockers (ARBs)

receptor = AT1

A

Losartan, Valsartan, Candesartan

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19
Q

effects of ARBs (Losartan, Valsartan, Candesartan)

A
  • *Inhibit Ang II-induced:**
    1) contraction of vascular smooth muscle
    2) thirst
    3) vasopressinrelease
    4) aldosterone secretion
    5) release of adrenal catecholamines
    6) enhancement of noradrenergic neurotransmission
    7) increases in sympathetic tone
    8) changes in renal function
    9) cellular hypertrophy and hyperplasia
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20
Q

role of ARBs (losartan, valsartan, candesartan) in therapy

A

First-line or add-on therapy for uncomplicated hypertension – as effective as ACEIs

First-line therapy for compelling indications of

  • Diabetes
  • Chronic kidney disease
  • Coronary artery disease
  • Left ventricular dysfunction

Commonly used as an alternative for patients with intolerance to ACE inhibitors

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21
Q

when should ARBs not be used

A

pregnancy

22
Q

what is a direct renin inhibitor?

what is it preventing?

A

Aliskiren

Binds directly to the catalytic site of renin –> prevents it from cleaving angiotensinogen to generate angiotensin I

23
Q

role of aliskiren in therapy

A

Approved as monotherapy or in combination therapy for HTN

Demonstrated efficacy in lowering BP when used in combination with a thiazide, ACE inhibitor, ARB, or CCB

24
Q

SE of aliskiren

A

Can cause hyperkalemia in patients with CKD and diabetes or in those receiving a potassium-sparing diuretic, aldosterone antagonist, ACE inhibitor, or ARB

25
Q

when should aliskiren not be used

A

pregnancy

26
Q

what antihypertensive therapies should not be used in pregnancy

A

Angiotensin Receptor Blockers (Losartan, Valsartan, Candesartan)

ACE inhibitors (Captopril, Lisinopril, Fosinopril)

Aliskiren

27
Q

what are the Dihydropyridine Calcium Channel Blockers for HTN

A

Amlodipine, Clevidipine, Nicardipine, Nifedipine, Nimodipine, Felodipine

28
Q

role of Dihydropyridine Calcium Channel Blockers for HTN (“-dipine”) in HTN therapy

A

First-line or add-on therapy for uncomplicated hypertension

Add-on therapy for

  • Diabetes
  • Coronary artery disease
29
Q

when should you avoid use of Dihydropyridine Calcium Channel Blockers for HTN (“-dipine”) in HTN therapy

A

left ventricular dysfunction (all except amlodipine and felodipine)

30
Q

what are the Non-dihydropyridine Calcium Channel Blockers for HTN

A

Verapamil

Diltiazem

31
Q

role of Non-dihydropyridine Calcium Channel Blockers for HTN therapy (verapamil, diltiazem)

A

Alternative to β-blockers in coronary artery disease

32
Q

when should verapamil and diltiazem be avoided

A

left ventricular dysfunction

33
Q

Verapamil, Diltiazem:

situation with potentially favorable effects?

A
  • Migraine headache
  • Arrhythmias
  • High-normal heart rate or tachycardia
34
Q

Verapamil, Diltiazem:

situation with potentially unfavorable effects?

A

Low-normal HR

35
Q

what drug - direct acting vasodilators –> opening K+ channels

decrease IP3-induced Ca2+ release from smooth muscle SR –> decrease contraction

Opens Ca2+-activated K+ channels in smooth muscle –> relaxation

Relaxes arterioles; little/no effect on veins;

A

Hydralazine

36
Q

role of hydralazine for therapy

A
  • often used as ADD ON (often with diuretic) therapy to manage resistant HTN, particularly in patients with severe chronic kidney disease
  • Safe in pregnant women –> used for gestational HTN
37
Q

SE of hydralazine

A

Drug-induced lupus with long-term use

compensatory tachycardia and Na+ retention

38
Q

when using hydralzaine for chronic HTN what should you do to mitigate SE of compensatory tachycardia and Na+ retention

A

used in combination with both a diuretic and β-blocker or NDHP CCB

39
Q

MOA of minoxidil

A

direct-acting vasodilator –> opening K+ channels

relaxes arteriolar VSMCs (no effects on veins)

40
Q

role of minoxidil in therapy

A

Oral use only for severe, refractory hypertension

Use in combination with β-blockers and diuretics

41
Q

SE of minoxidil

A

Reflex increase in myocardial contractility

42
Q

what is minoxiil used in combination with

A

Use in combination with β-blockers and diuretics

43
Q

MOA of sodium nitroprusside

A

direct-acting vasodilator - via NO

donates NO ⇒ cGMP-mediated Ca2+ sequestration
- decreases both afterload and preload (venodilation)

44
Q

how is sodium nitroprusside administered

A

IV

45
Q

use for sodium nitroprusside

A

Intravenous agent used in hypertensive emergencies and the rapid management of CHF

  • very rapid onset of action
46
Q

how can the diuretics - Chlorthalidone, Hydrochlorothiazide, Indapamide - be used for HTN

A

First-line or add-on therapy for uncomplicated HTN

First-line therapy for compelling indications of

  • left ventricular dysfunction
  • previous ischemic stroke
47
Q

how can spironolactone or eplerenone (aldosterone antagonist - diuretic) be used for HTN

A

Add-on therapy for resistant hypertension

Add-on therapy for:

  • coronary artery disease
  • left ventricular dysfunction
48
Q

what drugs can be used for hypertension in pregnancy

A

methyldopa - extensive safety data

labetalol

long-acting nifedipine

hydralazone

metoprolol

49
Q

advantage and disadvantage of hydralazine in tx for HTN in pregnancy

A

Ad. = extensive clinical experience

Disad = increased risk of maternal hypotension

50
Q

why is labetalol preferred over other beta blockers for HTN in pregnancy

A

because of a theoretical beneficial effect of α-blockade on uteroplacental blood flow

51
Q

what drugs should be avoided if pregnant?

what drugs are contraindicated?

A

Avoid:

  • diuretics
  • atenolol
  • nitroprusside

Contraindicated:

  • ACE inhibitors
  • Angiotensin receptor antagonists

Pharm exam 5 (9 decks)

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