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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
what are the non-selective alpha antagonists and what are their primary uses?
* block both a1 and a2 * phenoxybenzmine: treats pheochromocytoma * phentolamine: treats hypertensive crisis
26
what are the selective a1 antagonists and what is their primary use
* **- zosins** * prazosin * terazosin * ect. * used to treat **chronic hypertension**
27
what are the a2 receptor antagonists and their primary use?
* methyldopa: * prodrug that is safe during pregnancy * used to treat HTN during pregnancy * clonidine: not a first line HTN drug
28
list the alpha blockers that are used to treat HTN and what type of HTN they treat
* phentolamine (non-selective): for hypertensive crisis * -zosins (a1 blockers): for chronic hypertension * methyldopa (a2 blocker): for hypertension in pregnancy
29
hydralazine * what kind of drug? * MOA * route of administration * pharmokinetics * therapuetic uses
* **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
minoxidil * what kind of drug? * MOA * route of adminsitration * therapuetic uses
* an arterial vasodilator * MOA * opens K+ channels, which _hyperpolarizes_ the arterial cell membrane and directly i**_nhibits_** Ca++ influx * route of adminsitration: oral * therapuetic uses: for **_severe, refractory hypertension_** * **_​_***like hydralazine, combined sympatholytic + a diruetic*
31
what are the arterial vasodilatrors and what adverse effects do they share?
(hyralazine and minoxidil) * excessive vasodilation * fluid retention * hypotension * reflex tachycardia
32
adverse effects of minoxidil
* excessive vasodilation, fluid retension, hypotension, reflex tachycardia * **_stimulates hair growth_**
33
AEs of hydralazine
* excessive vasodilation, fluid retention, hypotention, reflex tachycardia * **_lupus erythematous like syndrome_** * **_​_**especially in patients that are _slow acetylators_
34
what are the top drugs for initial treatment of hypertension?
**"ACT-B"** ACE Inhibitors & Ang-receptor Blockers Ca++ channel blockers Thiazide diuretics B-receptor antagonists
35
36
what are the types of combination therapy that can be done with anti-hypertensives?
* Combination therapy (i.e. drugs with complementary mechanisms). * Thiazide diuretic + most other drugs * ACE inhibitor or ARB + Ca2+ channel blocker
37
what blood pressure constitutes a hypertensive crisis? what cardiovascular emergencies and neurovascular emergencies can can cause a hypertensive crisis?
* 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
what parenteral drugs can be used for hypertensive emergencies?
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
nitroprusside * MOA * effects * pharmokinetics
* 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
adverse effects of nitroprusside
* excessive vasodilation * hypotension * cyanide toxicity
41
contraindications of nitroprusside?
* patients with **leber's optic atroph**y 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
nitrates * list the drugs in this class * MOA * pharmokinetics * clinical uses
* 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
AES of nitrates
nitroglycerin, isorbide, dinitrate * headache * tolerance * **tachycardia**

S2B5 Pharmacology (3 decks)

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