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Indications

REMS


Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Exercise Extreme Caution in:

Adv. Reactions/Side Effects

CNS: dizziness, drowsiness, fatigue, headache, insomnia, vertigo, weakness

Resp: cough, dyspnea

CV: hypotension, chest pain, edema, tachycardia

Endo: hyperuricemia

GI: taste disturbances, abdominal pain, anorexia, constipation, diarrhea, nausea, vomiting

GU: erectile dysfunction, proteinuria, renal dysfunction, renal failure

Derm: flushing, pruritis, rashes

F and E: hyperkalemia

Hemat: AGRANULOCYTOSIS

MS: back pain, muscle cramps, myalgia

Misc: ANGIOEDEMA, fever

Interactions

Drug-drug:

Availability

Route/Dosage

Hypertension

Renal Impairment

Hepatic Impairment

Heart Failure

Renal Impairment

Action

  • ACE inhibitors block the conversion of angiotensin I to the vasoconstrictor angiotensin II. ACE inhibitors also prevent the degradation of bradykinin and other vasodilatory prostaglandins. ACE inhibitors also plasma renin levels and aldosterone levels. Net result is systemic vasodilation.
Therapeutic effects:
  • Lowering of BP in hypertensive patients.
  • Improved symptoms in patients with HF.

Classifications

Therapeutic Classification: antihypertensives

Pharmacologic Classification: ace inhibitors

Pharmacokinetics

Absorption: Well absorbed following oral administration, rapidly converted to active metabolite, cilazaprilat (57% bioavailability for cilazaprilat).

Distribution: Enters breast milk.

Metabolism/Excretion: Cilazaprilat is eliminated unchanged by the kidneys (91%).

Half-Life: Early elimination phase: 0.9 hr; terminal elimination phase (enzyme-bound cilazaprilat): 36–49 hr.

Canadian Brand Names

Inhibace

Time/Action Profile

(effects on hemodynamics)

ROUTEONSETPEAKDURATION
PO (hypertension)within 1 hr3–7 hr12–24 hr
PO (heart failure)1–2 hr2–4 hr24 hr

Patient/Family Teaching

Pronunciation

sye-LAY-za-pril