ace inhibitors-prils

Question 1

Angiotensin-Converting Enzyme (ACE) Inhibitors

Answer 1

■ Mechanism of action and overview of pharmacologic effects
– Reduce levels of angiotensin II
– Increase levels of bradykinin

Therapeutic uses
– Hypertension
– Heart failure
– Myocardial infarction (MI)
– Diabetic and nondiabetic nephropathy
– Prevention of MI, stroke, and death in patients at high cardiovascular risk

Adverse effects
– First-dose hypotension
– Cough
– Angioedema
■ ACE inhibitors can cause angioedema, a potentially life- threatening reaction. If patients report edema of the
tongue, lips, or eyes, emergency care should be sought immediately. The patient must never take ACE inhibitors again

Adverse effects
– Hyperkalemia
– Renal failure – Neutropenia

Drug interactions
– Diuretics
– Antihypertensive agents
– Drugs that raise potassium levels
– Lithium
– Nonsteroidal antiinflammatory drugs

Except for enalaprilat, all ACE inhibitors are
administered orally
– All are available in single-drug formulations
– Except for captopril and moexipril, all oral formulations may be administered without regard to meals

Question 2

Direct Renin Inhibitors

Aliskiren [Tekturna]

Answer 2

– Binds tightly with renin and inhibits the cleavage of angiotensinogen to angiotensin I
– Side effects
■ Angioedema, cough, GI effects, hyperkalemia,
fetal injury, and death

Question 3

Eplerenone [Inspra]

Answer 3

Aldosterone Antagonists

Eplerenone [Inspra]
– Mechanism of action
■ Selective blockade of aldosterone receptors – Therapeutic uses
■ Hypertension
■ Heart failure
– Pharmacokinetics
■ Absorption is not affected by food – Adverse effects
■ Hyperkalemia

– Drug interactions
■ ■ ■
Inhibitors of CYP3A4
Drugs that raise potassium levels
Use with caution when combined with lithium

Question 4

Spironolactone [Aldactone]

Answer 4

Aldosterone Antagonists

■ Spironolactone [Aldactone]
– Mechanism of action
■ Blocks aldosterone receptors
■ Binds with receptors for other steroid hormones
– Therapeutic uses ■ Hypertension
■ Heart failure

– Adverse effects
■ Hyperkalemia
■ Gynecomastia
■ Menstrual irregularities
■ Impotence
■ Hirsutism
■ Deepening of the voice