Trade Names:Accupril- Tablets 5 mg- Tablets 10 mg- Tablets 20 mg- Tablets 40 mg
Competitively inhibits angiotensin I-converting enzyme, resulting in prevention of angiotensin I conversion to angiotensin II, a potent vasoconstrictor that also stimulates aldosterone release. Clinical consequences are decrease in BP, reduced sodium resorption, and potassium retention.
T max is 1 h for the parent drug, quinapril. T max is 2 h for the metabolite, quinaprilat. Food decreases rate 25% and extent of absorption 30% when administered with a high-fat meal.
Protein binding is about 97%.
De-esterified to major active metabolite quinaprilat (about 38% of dose).
Renal (96% of quinaprilat) IV dose. The t ½ accumulation is about 3 h for quinaprilat; t ½ elimination is about 2 h for quinaprilat; and t ½ prolonged terminal phase is about 25 h for quinaprilat.
Within 1 h.
2 to 4 h.
When CrCl decreases, the elimination t ½ increases for quinaprilat.Elderly
Elimination of quinaprilat is decreased.Heart failure
Elimination of quinaprilat is decreased.Alcoholic cirrhosis
Quinaprilat concentrations are decreased because of impaired de-esterification of quinapril.
Treatment of hypertension; adjunctive therapy of CHF.
Hypersensitivity to ACE inhibitors; history of angioedema related to previous treatment with an ACE inhibitor.
PO 5 mg twice daily initially; may increase dose weekly for clinical control, usually 20 to 40 mg in 2 equally divided doses.Renal Function Impairment
Initial dose is 5 mg with CrCl more than 30 mL/min or 2.5 mg with CrCl 10 to 30 mL/min. If well tolerated, it may be given the following day as a twice daily regimen. In the absence of excessive hypotension or significant deterioration of renal function, the dose may be increased at weekly intervals based on clinical and hemodynamic response.HypertensionAdults
PO 10 or 20 mg every day initially; adjust dosage at intervals of at least 2 wk.Adults (maintenance)
PO 20, 40, or 80 mg/day as single dose or 2 equally divided doses.Elderly
PO 10 mg every day followed by titration to the optimal response.Renal Function Impairment
Initial dose varies based on CrCl: more than 60 mL/min is 10 mg; 30 to 60 mL/min is 5 mg; 10 to 30 mL/min is 2.5 mg.
Store tablets at controlled room temperature (59° to 89°F). Protect from light.
Quinapril bioavailability may be decreased. Separate administration times by 1 to 2 h.Capsaicin
Cough may be exacerbated.Digoxin
May cause increased or decreased digoxin levels.Diuretics
Increased risk of hypotension.Food
Food (especially fat) reduces bioavailability of quinapril.Indomethacin, salicylates (eg, aspirin)
May reduce hypotensive effects, especially in low renin or volume-dependent hypertensive patients.Lithium
May cause increased lithium levels and symptoms of lithium toxicity.Loop diuretics
Effects of loop diuretics may be decreased.Phenothiazines
Enhanced hypotensive effect.Potassium supplements and potassium-sparing diuretics
Decreased tetracycline absorption.
False elevation of liver enzymes, serum bilirubin, uric acid, and blood glucose may occur.
Dizziness (8%); headache (6%); fatigue (3%).
Nausea, vomiting, diarrhea (2%).
BUN (11%); serum creatinine (8%).
Chest pain (2%); abdominal pain, back pain (1%); angioedema (0.1%); anaphylactoid reactions.
When used in pregnancy during the second and third trimesters, ACE inhibitors can cause injury and even death to the developing fetus. When pregnancy is detected, discontinue therapy as soon as possible.
Category D (second, third trimester); Category C (first trimester). Avoid use in pregnant patients and discontinue drug as soon as pregnancy is detected; closely observe infants with histories of in utero exposure.
Safety and efficacy not established.
May show higher peak blood levels of metabolite.
May further decrease renal function with elevations in BUN and serum creatinine because of decreased renal perfusion. Furthermore, dosage should be reduced to compensate for reduced drug elimination.
Use drug with caution; dosage reduction may be necessary because of impaired metabolism.
May occur and is potentially fatal if laryngeal edema occurs. Intestinal angioedema has occurred. Use drug with extreme caution in patients with hereditary angioedema.
Chronic cough may occur during treatment; more common in women.
Rarely, ACE inhibitors have been associated with a syndrome that starts with cholestatic jaundice and progresses to fulminant hepatic necrosis and sometimes death.
Significant decreases in BP may occur after first dose, especially in severely salt- or volume-depleted patients (eg, patients on aggressive diuretic therapy) or in those with heart failure.
Have occurred rarely; risk appears greater with renal function impairment, heart failure, or immunosuppression.
Has occurred with similar agents, especially with high doses or prior renal disease.
Copyright © 2009 Wolters Kluwer Health.