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CV Pharmacology > Anti-HTN Drugs > Flashcards

Anti-HTN Drugs Flashcards

1
Q

What classes of drugs are used for treating HTN?

A

Alpha1 blockers, beta-blockers, ACEI, ARBs, renin inhibitors, L-type Ca+ channel blockers, centrally acting alpha2 agonists, direct vasodilators

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2
Q

What are the pharmacological effects of alpha1 receptor blockers?

A
  • decrease TPR & reduce BP
  • treat benign prostatic hyperplasia (BPH)
  • increase HDL and lower LDL, improve insulin resistance
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3
Q

How are apha1 receptor blockers used to treat hypertension?

A

Given as an adjunctive therapy. Not recommended as monotherapy by ALLHAT study.

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4
Q

Which patients with hypertension benefit from a beta-blocker?

A

Effective for all grades of HTN. No salt/water retention, can be taken with diuretic for additive effect.

Very useful in patients with high renin HTN, but work with normal-low renin.

Preferred for patients with MI, IHD, CHF, hyperthyroidism, migraines.

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5
Q

What are the pharmacological effects of beta-blockers (with no ISA)?

A
  • Block beta-1 receptors
  • Decrease HR and contractility → decreased CO
  • Inhibit renin release from JGA
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6
Q

What are the adverse effects of beta-blockers?

A
  • cold extremities
  • bradycardia from decreased AV node conduction
  • bronchospasm
  • CNS: bad dreams, depression
  • block glycogenolysis
  • block HSL in adipocytes, increase LDL & TGs, reduce HDL
  • must withdraw slowly to prevent tachycardia
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7
Q

What drug is given for hypertensive emergencies?

A

Labetalol - non-selective beta + alpha1 receptor antagonist

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8
Q

What are the effects of carvedilol?

A
  • Non-selective beta + alpha1 receptor antagonist
  • antioxidant
  • prevents LDL oxidation, decreases LDL uptake into coronary vessels
  • decreased m/m in pts with CHF
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9
Q

What are the effects of Nebivolol?

A
  • highly selective beta1 antagonist
  • NO-mediated vasodilation
  • significantly increases SV
  • antioxidant activity with favorable effects - used for HTN with metabolic syndrome
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10
Q

What is the mechanism of action of ACE inhibitors?

A
  • inhibit conversion of Ang I to Ang II
  • prevent degradation of bradykinin
  • decreased secretion of aldosterone
  • increase renal blood flow
  • (captopril increases the synthesis of renal prostaglandins & delays progression of renal disease in diabetics)
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11
Q

What are the pharmacological effects of ACE inhibitors?

A
  • prevent vasoconstrictive effect of AngII - dilate arteries and veins - reduce BP
  • reduce AngII-mediate thickening of BV and cardiac hypertrophy
  • increases longevity in CHF
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12
Q

What are the side effect of ACE inhibitors?

A
  • hypotension in hypovolemic and/or Na+-depleted pts
  • hyperkalemia
  • dry cough and angioedema
  • fetotoxicity
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13
Q

What is the mechanism of action of ARBs?

A

Block angiotension II type 1 receptors

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14
Q

What are the pharmacological effects of ARBs?

A
  • vasodilation to decrease TPR and BP
  • increase Na+ and water excretion to decrease plasma volume, CO
  • no effect on bradykinin
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15
Q

What are the unique properties of Losartan?

A
  • prodrug
  • competitive antagonist of TXA2 receptor
  • increases uric acid urinary excretion
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16
Q

What is the main side effect of ARBs?

A

fetotoxicity

17
Q

What are the selectivities of the different CCBs?

A
  • Verapamil: myocardium
  • Diltiazem: intermediate between verapamil & dihydropyridines in selectivity for vascular channels
  • Dihydropyridines: blood vessels, used for HTN
18
Q

What is the mechanism of dihydropyridines?

A

Decrease BP and TPR by relaxing arteriolar smooth muscle.

Do not cause reflex tachycardia.

19
Q

Which patients with hypertension benefit from a CCB?

A
  • more effective for pts with low renin - elderly and AA
  • for older pts with systolic HTN
  • added to ACEI/ARB for diabetics if necessary
20
Q

What is the mechanism of action of clonidine, guanfacine, guanabenz?

A
  • agonize postsynaptic alpha2-receptors in CNS
    • decreases SNS activity to heart & BV
      • decrease TPR and HR
21
Q

What are the clinical uses for Clonidine?

A
  • analgesic for neuropathy
  • ADHD
  • tertiary for HTN
22
Q

What are the side effects of alpha2 agonists?

A

Sedation, drowsiness, fatigue

Clonidine withdrawal leads to hypertension.

23
Q

What is the mechanism of action of Hydralazine?

A
  • selective arteriolar smooth muscle relaxer
  • triggers reflex SNS activity and leads to increased catecholamine/renin secretion
24
Q

What are the clinical uses for Hydralazine?

A
  • IV for HTN emergency from eclampsia
  • used with beta-blockers and diuretics for HTN
25
Q

What are the side effects of Hydralazine?

A
  • palpitations, pronounced tachycardia, angina
  • hemolytic anemia
  • drug-induced lupus-like syndrome
26
Q

What is the mechanism of action of Minoxidil?

A
  • opens K+ channels in smooth muscles to cause arteriolar smooth muscle relaxation
  • does not dilate veins
27
Q

What are the adverse effects of Minoxidil?

A
  • increases renin
  • reflex tachycardia
  • hirsutism
  • **rarely prescribed - marked fluid retention **(only for severe refractory HTN)
28
Q

When is Nitroprusside used to treat HTN?

A

Given IV for HTN emergencies in patients with ventricular failure (will increase CO by decreasing afterload and does not worsen preload)

29
Q

What are the best drugs for monotherapy of HTN?

A

Diuretics and ACEIs - fewest side effects

30
Q

In which patients are diuretics indicated for treatment of HTN?

A
  • edema - heart failure, renal insufficiency
  • volume dependent HTN (low renin)
31
Q

In which patients are beta-blockers indicated for treatment of HTN?

A
  • not first line treatment
  • with tachycardia, high CO, and/or high renin
  • hyperthyroidism, migraine, glaucoma
  • less effective in African-Americans and elderly
  • Bisoprolol standard for use with ACEIs and diuretics (with CHF)
32
Q

In which patients are ACEIs/ARBs indicated for treatment of HTN?

A
  • pts with high renin levels (young people, middle-aged whites)
  • with a diuretic in low renin pts, AA, elderly
  • initial drug in diabetics (prevents nephropathy) and CHF pts
  • never in pregnancy
33
Q

In which patients are dihydropyridine CCBs indicated for treatment of HTN?

A
  • can be added to an ACEI/ARB in diabetics
  • very useful in AA and pts with low renin
  • might slightly increase risk of CAD and HF compared to ACEIs, beta-blockers, and diuretics

CV Pharmacology (5 decks)

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