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Indications

Canada-Approved Medicine

This monograph describes a medication approved for use in Canada by the Therapeutic Products Directorate, a division of Health Canada’s Health Products and Food Branch. The medication is not approved by the United States Food and Drug Administration; however, a similar formulation carrying a different generic or brand name might be available in the US.

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

  • PO (Adults): CCr >40 mL/min — 1 mg once daily initially, titrate carefully, not to exceed 5 mg once daily; CCr 10–40 mL/min — 0.5 mg once daily initially, titrate carefully, not to exceed 2.5 mg once daily; CCr <10 mL/min — not recommended.

Hepatic Impairment

  • PO (Adults): 0.5 mg once daily or less.

Heart Failure

Renal Impairment

  • PO (Adults): CCr 10–40 mL/min — 0.25–0.5 mg once daily; CCr <10 mL/min — not recommended.

Action

Therapeutic Effects:

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