Trade Names:Vasotec- Tablets 2.5 mg- Tablets 5 mg- Tablets 10 mg- Tablets 20 mg
Trade Names:Vasotec IV- Injection 1.25 mg enalaprilat/mLVasotec IV (Canada)
Competitively inhibits angiotensin I-converting enzyme, preventing conversion of angiotensin I to angiotensin II, a potent vasoconstrictor that also stimulates release of aldosterone. Results in decrease in BP, reduced sodium absorption, and potassium retention.
Bioavailability is approximately 60%. T max is within 1 h (enalapril); 3 to 4 h (enalaprilat).
Enalapril crosses the blood-brain barrier poorly, if at all. Enalaprilat does not cross the blood-brain barrier.
Enalapril is a prodrug and is hydrolyzed to enalaprilat (more potent than enalapril).
Intact enalapril and approximately 40% of the dose as enalaprilat is excreted in the urine. Approximately 94% is recovered in the urine and feces. The t ½ is 1.3 h (enalapril). Enalaprilat is dialyzable.
4 to 6 h.
At least 24 h.
In those with glomerular filtration rate 30 mL/min or less, the peak and trough enalaprilat levels increase, T max increases, and time to steady state may be delayed. Dosage adjustment recommended.
Treatment of hypertension and symptomatic CHF in combination with diuretics and digitalis and asymptomatic left ventricular dysfunction.
Treatment of diabetic nephropathy, childhood hypertension, hypertension related to scleroderma, and renal crisis scleroderma.
History of angioedema related to previous treatment with an ACE inhibitor and in patients with hereditary or idiopathic angioedema; hypersensitivity to ACE inhibitors.
PO Initial dose: 2.5 mg twice daily. Usual dose: 2.5 to 20 mg/day in 2 divided doses (max, 40 mg/day). Titrate doses upward as tolerated over a period of a few days or weeks. The max daily dose is 40 mg in divided doses.High-Risk PatientsAdults
IV Hypertensive patients at risk (eg, those with heart failure, hyponatremia, high-dose diuretic therapy, recent intensive diureses or increase in diuretic dose, renal dialysis, or severe volume or salt depletion of any etiology) have potential for extremely hypotensive response. Initiate therapy under very close medical supervision. The starting dose should be 0.625 mg or less administered IV over a period of 5 min or more and preferably longer (up to 1 h).HypertensionAdults
PO Initial dose: 2.5 to 5 mg/day. Titrate to desired BP control. Usual maintenance dose: 10 to 40 mg/day in single or twice daily doses. IV 1.25 mg over a 5-min period every 6 h. For patients with Ccr of 30 mL/min or less, the dose is 0.625 mg. Dose may be repeated if after 1 h the clinical response is inadequate. Additional doses of 1.25 mg may be administered at 6-h intervals. For dialysis patients, the initial dose is 0.625 mg or less given over 5 min or preferably longer (up to 1 h).Children
PO Initial dose: 0.08 mg/kg (up to 5 mg) every day. Adjust dose according to BP response. Doses above 0.58 mg/kg (or in excess of 40 mg) have not been studied in pediatric patients.Left Ventricular DysfunctionAdults
PO Initial dose: 2.5 mg twice daily. Titrate to targeted daily dose of 20 mg in divided doses.Renal Function ImpairmentAdults
PO Titrate dosage upward until BP is controlled or until a max dosage of 40 mg/day is reached. Use an initial dosage of 5 mg/day in normal renal function and mild impairment (Ccr more than 30 mL/min); 2.5 mg/day in moderate to severe renal function impairment (Ccr 30 mL/min or less); and 2.5 mg on the day of dialysis in dialysis patients (adjust dosage on nondialysis days based on BP response).
Greater risk of hypersensitivity possible with coadministration.Antacids
Enalapril bioavailability may be decreased. Separate administration times by 1 to 2 h.Capsaicin
Cough may be exacerbated.Digoxin
May increase or decrease plasma levels of digoxin.Indomethacin, salicylates (eg, aspirin)
Hypotensive effects may be reduced, especially in low-renin or volume-dependent hypertensive patients.Lithium
Increased lithium levels and symptoms of lithium toxicity may occur.Phenothiazines
May increase pharmacologic effect of enalapril.Potassium preparations, potassium-sparing diuretics
May increase serum potassium levels.Rifampin
Pharmacologic effects of enalapril may be decreased.
False elevation of liver enzymes or serum bilirubin may occur.
Hypotension (7%); angina, chest pain, orthostatic hypotension, syncope (2%); myocardial infarction (1%); tachycardia (less than 1%).
Headache (5%); dizziness (4%); fatigue (3%); vertigo (2%); asthenia (1%).
Rash (1%); photosensitivity (less than 1%).
Abdominal pain, diarrhea (2%); nausea, vomiting (1%).
Decreased hemoglobin and hematocrit, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, eosinophilia.
Bronchitis, cough, dyspnea (1%).
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.
MonitorWorsening heart failure
Assess heart failure patient for evidence of worsening failure (eg, daily weights, evaluation of peripheral edema, shortness of breath). Inform health care provider if rapid weight gain (eg, 2 pounds in 1 day or 5 pounds in 1 wk) is noted or if patient is experiencing worsening edema or other symptoms of heart failure (eg, worsening shortness of breath).
Category D (second, third trimester); Category C (first trimester).
Excreted in breast milk.
Safety and efficacy not established in pediatric patients younger than 1 mo of age, neonates, or pediatric patients with glomerular filtration rate less than 30 mL/min/1.73 m 2 (oral). Safety and efficacy not established (IV).
Reduce dose and give less frequently. In renal function impairment, stable elevations in BUN and serum creatinine may occur because of inadequate renal perfusion; monitor renal function during first few weeks of therapy and adjust dosage.
May occur. Use drug with extreme caution in patients with hereditary angioedema.
As with other vasodilators, enalapril should be used with caution in patients with obstruction in the outflow tract of the left ventricle.
Chronic dry cough may occur during treatment; higher incidence 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 or in those with heart failure; monitor closely for 2 h or more after initial dose and during first 2 wk of therapy. Minimize risk by discontinuing diuretics, decreasing dose, or increasing salt intake approximately 1 wk prior to initiating enalapril.
Have occurred; risk appears greater with renal dysfunction, heart failure, or immunosuppression; monitor WBC counts frequently.
Copyright © 2009 Wolters Kluwer Health.