section name header

Pronunciation

benazepril: ben-AYE-ze-pril

captopril: KAP-toe-pril

enalapril/enalaprilat: e-NAL-a-pril/e-NAL-a-pril-at

fosinopril: foe-SIN-oh-pril

lisinopril: lyse-IN-oh-pril

moexipril: moe-EKS-i-pril

perindopril: pe-RIN-do-pril

quinapril: KWIN-a-pril

ramipril: ra-MI-pril

trandolapril: tran-DOE-la-pril

Classifications

Therapeutic Classification: antihypertensives

Pharmacologic Classification: ace inhibitors

Indications

REMS


Captopril, enalapril, fosinopril, lisinopril, quinapril, ramipril, trandolaprilCaptopril, lisinopril, ramipril, trandolaprilEnalaprilRamiprilCaptoprilPerindopril

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 (selected agents only).
  • development of overt heart failure (enalapril only).
  • Improved survival and development of overt HF after MI (selected agents only).
  • risk of death from cardiovascular causes or MI in patients with stable CAD (perindopril only).
  • risk of MI, stroke, or death from cardiovascular causes in high-risk patients (ramipril only).
  • progression of diabetic nephropathy (captopril only).

Pharmacokinetics

Absorption: Benazepril: 37% absorbed after oral administration. Captopril: 60–75% absorbed after oral administration ( by food). Enalapril: 55–75% absorbed after oral administration. Enalaprilat: IV administration results in complete bioavailability. Fosinopril: 36% absorbed after oral administration. Lisinopril: 25% absorbed after oral administration (much variability). Moexipril: 13% bioavailability as moexiprilat after oral administration ( by food). Perindopril: 25% bioavailability as perindoprilat after oral administration. Quinapril: 60% absorbed after oral administration (high-fat meal may absorption). Ramipril: 50–60% absorbed after oral administration. Trandolapril: 70% bioavailability as trandolapril at after oral administration.

Distribution: All well distributed to tissues

Protein Binding: Benazepril: 95%, Fosinopril: 99.4%, Moexipril: 90%, Quinapril: 97%.

Metabolism/Excretion: Benazepril: Converted by the liver to benazeprilat, the active metabolite. 20% excreted by kidneys; 11–12% nonrenal (biliary elimination). Captopril: 50% metabolized by the liver to inactive compounds, 50% excreted unchanged by the kidneys. Enalapril, enalaprilat: Enalapril is converted by the liver to enalaprilat, the active metabolite; primarily eliminated by the kidneys. Fosinopril: Converted by the liver and GI mucosa to fosinoprilat, the active metabolite; 50% excreted in urine; 50% in feces. Lisinopril: 100% eliminated by the kidneys. Moexipril: Converted by liver and GI mucosa to moexiprilat, the active metabolite; 13% excreted in urine, 53% in feces. Perindopril: Converted by the liver to perindoprilat, the active metabolite; primarily excreted in urine. Quinapril: Converted by the liver, GI mucosa, and tissue to quinaprilat, the active metabolite: 96% eliminated by the kidneys. Ramipril: Converted by the liver to ramiprilat, the active metabolite; 60% excreted in urine, 40% in feces. Trandolapril: Converted by the liver to trandolaprilat, the active metabolite; 33% excreted in urine, 66% in feces.

Half-Life: Benazeprilat: 10–11 hr. Captopril: 2 hr ( in renal impairment). Enalapril: 2 hr ( in renal impairment). Enalaprilat: 35–38 hr ( in renal impairment). Fosinoprilat: 12 hr. Lisinopril: 12 hr ( in renal impairment). Moexiprilat: 2–9 hr ( in renal impairment). Perindoprilat: 3–10 hr ( in renal impairment). Quinaprilat: 3 hr ( in renal impairment). Ramiprilat: 13–17 hr ( in renal impairment). Trandolaprilat: 22.5 hr ( in renal impairment).

Time/Action Profile

( effect on BP: single dose)
ROUTEONSETPEAKDURATION
Benazeprilwithin 1 hr2–4 hr24 hr
Captopril15–60 min60–90 min6–12 hr
Enalapril PO1 hr4–8 hr12–24 hr
Enalapril IV15 min1–4 hr4–6 hr
Fosinoprilwithin 1 hr2–6 hr24 hr
Lisinopril1 hr6 hr24 hr
Moexiprilwithin 1 hr3–6 hrup to 24 hr
Perindoprilatwithin 1–2 hr3–7 hrup to 24 hr
Quinaprilwithin 1 hr2–4 hrup to 24 hr
Ramiprilwithin 1–2 hr3–6 hr24 hr
Trandolaprilwithin 1–2 hr4–10 hrup to 24 hr

Full effects may not be noted for several weeks.



Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Exercise Extreme Caution in:

Adv. Reactions/Side Effects

CV: hypotension, chest pain, edema, tachycardia

Derm: flushing, pruritus, rashes

F and E: hyperkalemia

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

GU: erectile dysfunction, proteinuria, renal impairment

Hemat: AGRANULOCYTOSIS, neutropenia(captopril only)

Metab: hyperuricemia

MS: back pain, muscle cramps, myalgia

Neuro: dysgeusia, dizziness, drowsiness, fatigue, headache, insomnia, vertigo, weakness

Resp: cough, dyspnea

Misc: ANGIOEDEMA, fever

Interactions

Drug-drug:

Drug-Food:

Route/Dosage

Benazepril

Renal Impairment

Renal Impairment

Captopril

Renal Impairment

Enalapril/Enalaprilat

Renal Impairment

Renal Impairment

Fosinopril

Lisinopril

Renal Impairment

Renal Impairment

Moexipril

Renal Impairment

Perindopril

Renal Impairment

Quinapril

Renal Impairment

Ramipril

Renal Impairment

Trandolapril

Renal Impairment

Hepatic Impairment

Availability

Benazepril

(Generic available)

Captopril

(Generic available)

Enalapril

(Generic available)

Enalaprilat

(Generic available)

Fosinopril

(Generic available)

Lisinopril

(Generic available)

Moexipril

(Generic available)

Perindopril

(Generic available)

Quinapril

(Generic available)

Ramipril

(Generic available)

Trandolapril

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Benazepril

Captopril

Enalapril

Enalaprilat

IV Administration:

Lisinopril

Moexipril

Ramipril

Trandolapril

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

benazepril: Lotensin,

captopril: Capoten,

enalapril/enalaprilat: Epaned, Vasotec,

fosinopril: Monopril,

lisinopril: Prinivil, Qbrelis, Zestril,

moexipril: Univasc,

perindopril: Aceon,

quinapril: , Accupril,

ramipril: Altace,

Canadian Brand Names

enalapril/enalaprilat: Vasotec IV,

perindopril: Coversyl,

trandolapril: Mavik