Antihypertensives Flashcards

1
Q

What are the 4 categories of Hypertension?

A

Normal 120/80

Elevated (120-129)/80

Hypertension

Stage 1 (130-139)/(80-89)

Stage 2(140/90)

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2
Q

How does hypertension lead to Heart Failure

A
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3
Q

What is the compensatory response to a decrease in BP

A
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4
Q

what is the main difference in treatment strategies between stage 1 and stage 2 hypertension?

A
  • Stage 1 hypertension - Often controlled with single drug
  • Stage 2 hypertension - Often requires multiple drugs
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5
Q

If the BP is still not controlled after starting therapy for stage 2 hypertension, what is the next drug that should be added?

A
  • Stage 2 Hypertension -Two first-line drugs of different classes are recommended
  • If BP still not controlled a third drug can be added - Usually vasodilator
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6
Q

What are the 1st line agents, second- line agents, and other major agents?

A
  • First-line agents :• ACE-inhibitors, ARBs, calcium channel blockers, thiazide diuretics
  • Second-line agents : • b-blockers, aldosterone antagonists
  • Other agents: • Loop diuretics, a-blockers, direct vasodilators, central a2-agonists, renin inhibitors
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7
Q

What are the Ace inhibitors and their mechanism of actions?

A

Captopril / Enalapril / Lisinopril
• First-line agents (in particular for diabetics and patients with CKD)
• decrease BP by decreasing peripheral vascular resistance

  • INHIBIT ACE (angiotensin converting enzyme) that cleaves angiotensin I to form angiotensin II
  • DECREASE Na+ & H20 retention
  • INCREASE BRADYKININ levels
  • DO NOT reflexively increase cardiac output, rate or contractility
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8
Q

what is the ACE inhibitor mechanism of action?

A
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9
Q

What are the clinical applications of ACE inhibitors ?

A

• Hypertension (most effective in white and/or young patients)

+ diuretic = effectiveness similar in non-black and black patients

  • Preserve renal function in patients with either diabetic or non-diabetic nephropathy
  • Effective in treatment of chronic HF
  • Standard of care for patients following MI (started 24hafter end of infarction)
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10
Q

What are the adverse effects of ACE inhibitors?

A
  • Dry hacking cough
  • Hyperkalemia
  • Hypotension
  • Angioedema (rare but life-threatening)
  • Acute renal failure (patients with bilateral renal artery stenosis)
  • Rash, fever, altered taste
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11
Q

What are the contraindications of ACE inhibitors?

A
  • Pregnancy: During 1st trimester due to risk of congenital malformations and during 2nd and 3rd trimesters because of risk of fetal hypotension, anuria & renal failure
  • Patients with bilateral renal artery stenosis
  • Patients with a history of angioedema related to previous treatment with an ACEI and in patients with hereditary or idiopathic angioedema.
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12
Q

What are the Angiotension receptor blockers ?

A

Losartan / Valsartan

  • Angiotension receptor blockers (ARB’s)
  • First-line agents
  • Alternatives to ACEI’s (in intolerant patients)
  • Block angiotensin-2 type 1 receptors
  • decrease BP by causing arteriolar & venous dilation
  • Block aldosterone secretion which causes a decrease Na+ & H20 retention
  • diabetic nephrotoxicity
  • DO NOT INCREASE BRADYKININ levels
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13
Q

what is the mechanism of action of Angiotension receptor blockers (ARB’s)

A
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14
Q

What are the adverse effects of Angiotension receptor blockers

A
  • Similar to those of ACE inhibitors
  • Dry cough does not occur (due to no effect on bradykinin levels)
  • Angioedema risk is significantly lower than withACEI’s

• Losartan reduces plasma uric acid levels by inhibiting URAT1 transporter – can be useful in patients with gout

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15
Q

What are the contraindications of Angiotension receptor blockers (ARB’s) ?

A
  • Pregnancy
  • Patients with bilateral renal artery stenosis
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16
Q

What is the renin inhibitor and its mechanism of action?

A

• Alternative agent in the treatment of hypertension

MOA
• Inhibits enzyme activity of renin and prevents conversion of angiotensinogen into angiotensin I

End result:
• Inhibits production of both angiotensin II and aldosterone

17
Q

What is the adverse effect of Aliskiren?

A
  • Similar to those of ACE inhibitors
  • Dry cough does not occur (due to no effect on bradykinin levels)
  • Angioedema risk is significantly lower than with ACEI’s
18
Q

What are the Ca2+ Channel blockers?

A

Verapamil / Diltiazem / Nifedipine / Amlodipine
• First-line agents (particularly black and/or elderly patients)

Ca2+ CHANNEL CLASSES
• Non-dihydropyridines: • Verapamil , Diltiazem
• Dihydropyridines: Nifedipine, amlodipine

19
Q

Verapamil

A
  • Least selective of any Ca2+-blocker
  • Significant effects in cardiac & vascular smooth muscle
  • Used to treat angina, supraventricular tachyarrhythmias, hypertension, migraine & cerebral vasospasm
20
Q

Diltiazem

A
  • Effects in both cardiac & vascular smooth muscle (less pronounced effect on heart than verapamil)
  • Good side-effect profile
  • Used to treat angina, hypertension, supraventricular tachyarrhythmias & cerebral vasospasm
21
Q

What are the dihydropyridine?

A

Amlodipine, nifedipine

  • Greater affinity for vascular Ca2+-channels than for cardiac Ca2+-channels
  • Reduce Ca2+ entry into smooth muscles to cause coronary & peripheral vasodilatation & lower BP
  • Primarily used in treating hypertension.
22
Q

What are the clinical applications of Ca2+ Channel blocers?

A
  • Hypertension (particularly black and/or elderly patients)
  • Have intrinsic natriuretic effect (no need for diuretic)
  • Useful in patients with asthma, diabetes, peripheral vascular disease
23
Q

What Ca2+ channel blocker will you not use for cardiac arrhytmias?

A

Dihydropyridines

(amlodipine, nifedipine)

  • High-doses of short-acting dihydropyridine Ca2+- channel blockers can increase risk of MI (excessive vasodilation & reflex cardiac stimulation)
  • Sustained release preparations are preferred
24
Q

What are the adverse effects of Ca2+ Channel Blockers?

A

• Verapamil -Constipation (~7%), negative inotropic effects, gingival
hyperplasia

• Dihydropyridines
Hypotension, peripheral edema (esp. feet & ankles), dizziness, headache, fatigue, gingival hyperplasia, flushing, reflex tachycardia can occur (especially in short-acting preparations)

25
Q

What are the contraindications of Ca2+ channel blockers?

A

• Non-dihydropyridines (verapamil & diltiazem)
Relatively contraindicated in patients taking b-blockers, or who have 2nd or 3rd degree AV block, or severe left ventricular systolic dysfunction

26
Q

What are the diuretics and their mechanism of action?

A

• First-line agents (particularly black and/or elderly patients)

MOA

  • Lower BP by increasing Na+ and H20 excretion which leads to a decrease in extracellular volume and an increase in cardiac output & renal blood flow.
  • Long-term treatment = normal plasma volume but sustained decreased peripheral resistance
27
Q
A