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S2B5 Pharmacology > Antihypertensives > Flashcards

Antihypertensives Flashcards

1
Q

discuss the role of diuretics in management of hypertension

  • what effects do they have?
A
  • initial effect: volume depletion
  • long term effects: decrease PVR of by reducing sodium content/and decreasing senstivity of smooth muscle cells
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2
Q

what are the thiazides and and how can they be used to treat HTN

A

hydrochlorothiazide, chlorthoalidone, polythiazide, metolzode, indapamide

  • monotherapy:
    • thiazed can used as an initial therapy for patients with mild/moderate HTN and normal renal function
      • ​(if renal function is impaired or the patient has heart failure, loop diuretics are better)
  • in combination with other drugs:
    • for counteracting fluid retention
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3
Q

what are the loop durietcs and how are they used to treat HTN?

A

= furosemide

  • used hypertensive patients with for patients with renal dysfunction or CHF
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4
Q

K+ sparing diruetics

what are they and what is their role in the management of hypertension?

A

= spironlactone, eplerenone

  • these are weaker diuretics that can can be used to counter the hypokalemic effects of other diuretics.
    • (they block aldosterone and limit K+ secretion)
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5
Q

AES of thiazide and loop diuretics

A
  • hyponatremia
  • hypokalemia
  • hypomagnesia

may increase plasma lipid, uric acid and gucose levels

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6
Q

what are the ACE inhibitors and ARBs

what is their role in management of hypertension?

what are their limitations?

A

ACE inhibitors: - prils

ARBs (AT1 receptor blockers): - sartans

  • benefitial in patients with:
    • ​diabetes
    • chronic renal disease
    • HF
    • patients with hyperuricemia due to diuretics
  • less effective in African American patients
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7
Q

AEs of ACE inhibitors/ARBs

A
  • both
    • hypotension
    • hypoglycemia
    • hyperkalemia
    • impaired renal function
    • angioedema (mostly ACE inhibitors)
  • just ACE inhibitors: persistent dry cough
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8
Q

contraindications of ACE inhibitors/ARBs

A
  • pregnancy
  • bilateral renal artery stenosis
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9
Q

major drug drug interactions of ACE/inhibitors & ARBS

A
  • NSAIDS: counter their anti-hypertensive effects
  • potassium sparing diuretics: together, there drugs put the patient at high risk of hyperkalemia
  • lithium
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10
Q

MOA of calcium channel blockers

A
  • block smooth muscle contraction
    • block Ca++ influx –> no ca++-calmodulin formation –> no myoskin light chain kinase phosphorylation –> inactivate myosin light chain
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11
Q

what are the two classes of calcium channel blockers used to treat HTN?

A
  • non-dihydropyridines
  • dihydropyridines
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12
Q

non-dydropyramids

  • MOA
  • list the drugs
A
  • MOA: block contraction of cardiac muscle
    • ​reduce SA influx into cardiac muscle, SA nodes, AV nodes
    • lower CO –> lower blood pressure
  • drugs:
    • verapamil
    • diltiazem
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13
Q

dihydropyridines (DHPs)

  • MOA
  • drugs in this class
A
  • MOA: reduce vascular smooth muscle contraction
    • reduce Ca++ influx into vascular smooth muscle cells –> lower peripheal resistance –> lower BP
  • drugs: - dipines
    • ​long acting:
      • more commonly used
      • ex: amlodipine
    • short acting:
      • no commonly used for HTN (too many AEs)
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14
Q

indication (s) for DHPs

A

hypertension in pregnant women (they are safe during pregnancy)

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15
Q

AES of both long and short acting DHPs

A
  • flushing
  • dizziness
  • headache
  • periphal edema in lower legs/hands
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16
Q

AEs specific to short acting DHPs

A

tachycardia - hence, short acting DHP rarely used to treat HTN

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17
Q

drug drug interactions of DHPS

A
  • CYP - 3A4 inhibitors
  • these will increase plasma concentration of DHPs – > can cause hypotension
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18
Q

MAO of B1 receptor blockers in treatment of HTN

A
  • in the heart: reduce HR and contracility
  • in the kidney: inhibit renin release
19
Q

what drugs are non selective B1, B2 blockers?

A

propanolol

20
Q

what are the cardioselective (B1) blockers

A
  • metoprolol
  • atenolol
21
Q

what drugs are a1 and non- selective beta blockers

A
  • labetalol
  • carvedilol
22
Q

when are beta-blockers a top choice for hypertension?

A
  • in patients with other indications:
    • MI
    • angina
    • migraine
    • arythmias
    • HF
23
Q

caution when giving beta blockers for HTN

A

Abrupt discontinuation of beta blockers can lead to withdrawal hypertension and ischemia

  • must taper the dose
24
Q

drug drug interactions of beta blockers

A

NSAIDS (reduce B blocker anti-hypertensive effects)

25
Q

what are the non-selective alpha antagonists and what are their primary uses?

A
  • block both a1 and a2
    • phenoxybenzmine: treats pheochromocytoma
    • phentolamine: treats hypertensive crisis
26
Q

what are the selective a1 antagonists and what is their primary use

A
  • - zosins
    • prazosin
    • terazosin
    • ect.
  • used to treat chronic hypertension
27
Q

what are the a2 receptor antagonists and their primary use?

A
  • methyldopa:
    • prodrug that is safe during pregnancy
    • used to treat HTN during pregnancy
  • clonidine: not a first line HTN drug
28
Q

list the alpha blockers that are used to treat HTN and what type of HTN they treat

A
  • phentolamine (non-selective): for hypertensive crisis
  • -zosins (a1 blockers): for chronic hypertension
  • methyldopa (a2 blocker): for hypertension in pregnancy
29
Q

hydralazine

  • what kind of drug?
  • MOA
  • route of administration
  • pharmokinetics
  • therapuetic uses
A
  • an arterial vasodilator
    • (MOA not understood)
  • administration: oral or parentral
  • pharmokinetics
    • metabolized via acetylation
  • therapuetic uses:
    • moderate to severe hypertension
      • given with a diuretic and a sympatholytic
      • safe during pregnancy
    • chronic heart failure:
      • when combined with a nitrate
30
Q

minoxidil

  • what kind of drug?
  • MOA
  • route of adminsitration
  • therapuetic uses
A
  • an arterial vasodilator
    • MOA
      • opens K+ channels, which hyperpolarizes the arterial cell membrane and directly inhibits Ca++ influx
  • route of adminsitration: oral
  • therapuetic uses: for severe, refractory hypertension
    • ​like hydralazine, combined sympatholytic + a diruetic
31
Q

what are the arterial vasodilatrors and what adverse effects do they share?

A

(hyralazine and minoxidil)

  • excessive vasodilation
  • fluid retention
  • hypotension
  • reflex tachycardia
32
Q

adverse effects of minoxidil

A
  • excessive vasodilation, fluid retension, hypotension, reflex tachycardia
  • stimulates hair growth
33
Q

AEs of hydralazine

A
  • excessive vasodilation, fluid retention, hypotention, reflex tachycardia
  • lupus erythematous like syndrome
    • ​especially in patients that are slow acetylators
34
Q

what are the top drugs for initial treatment of hypertension?

A

“ACT-B”

ACE Inhibitors & Ang-receptor Blockers

Ca++ channel blockers

Thiazide diuretics

B-receptor antagonists

35
Q
A
36
Q

what are the types of combination therapy that can be done with anti-hypertensives?

A
  • Combination therapy (i.e. drugs with complementary mechanisms).
    • Thiazide diuretic + most other drugs
    • ACE inhibitor or ARB + Ca2+ channel blocker
37
Q

what blood pressure constitutes a hypertensive crisis?

what cardiovascular emergencies and neurovascular emergencies can can cause a hypertensive crisis?

A
  • Sudden, life-threatening elevation of BP accompanied by acute end-organ damage (systolic >180 mmHg and diastolic BP usually > 120 mm Hg).
    • cardiovascular emergencies: aortic dissection, acute coronary syndrome, and acute heart failure.
    • neurologic emergencies: hypertensive encephalopathy, acute ischemic stroke, acute intracerebral hemorrhage, and subarachnoid hemorrhage.
38
Q

what parenteral drugs can be used for hypertensive emergencies?

A

D1 dopamine receptor agonist: fenoldopam

β-blocker: Esmolol

α1- and β-blocker: Labetalol

Calcium channel blockers: nicardipine, clevidipine

α-blocker: Phentolamine

ACE inhibitor: Enalaprilat

39
Q

nitroprusside

  • MOA
  • effects
  • pharmokinetics
A
  • nitroprusside is an NO donor
  • pharmokinetics:
    • administered IV
    • rapid onset of action (< 1 min) and short duration of action (<10 min)
  • MOA:
    • relaxes veins an arteries
    • reduces preload and afterload
    • immediate onset and allows rapid BP control
40
Q

adverse effects of nitroprusside

A
  • excessive vasodilation
  • hypotension
  • cyanide toxicity
41
Q

contraindications of nitroprusside?

A
  • patients with leber’s optic atrophy and tobacco ambyopia:
    • these patients are rhonadese deficient
  • impaired renal function
  • patients treated with other NO donotrs
  • hypertension caused by:
    • aortic coarctation
    • ateriovenous shunting
  • acute HF with systemic vascular resistance
    • septic shock
42
Q

nitrates

  • list the drugs in this class
  • MOA
  • pharmokinetics
  • clinical uses
A
  • nitrates
    • nitroglycerin
    • isorbide
    • dinitrate
  • pharmokinetics: like nitroprusside, administered IV, rapid onset of action
  • clinical uses: like nitroprusside, these drugs are used in hypertensive crisis
  • MOA:
    • similar to nitroprusside
    • cause both arterial and venous dilation, but venodilation > arteriol dilation
  • clinical uses:
    • beneficial to treating hypertensive crisis due to coronary heart disease and coronary bypass
43
Q

AES of nitrates

A

nitroglycerin, isorbide, dinitrate

  • headache
  • tolerance
  • tachycardia

S2B5 Pharmacology (3 decks)

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