Lisinopril is a synthetic, nonsulfhydryl,
angiotensin-converting enzyme inhibitor. Its bioavailability is approximately 25% and is not affected by food. Hepatic metabolism is not required for pharmacologic effect, which occurs 1 hour after administration. Peak serum concentration and effect are delayed, occurring 6-8 hours after a single dose and lasting for at least 24 hours. The
drug is eliminated primarily by the kidneys. The elimination half-life is 12.6 hours and is prolonged in renal impairment.
Lisinopril 10-80 mg once a day is effective in lowering blood pressure in all grades of essential and
renovascular hypertension. It is as effective as
hydrochlorothiazide,
atenolol,
metoprolol, and
nifedipine. Combining
lisinopril with
hydrochlorothiazide produces a greater degree of blood pressure reduction. Patients with
congestive heart failure have demonstrated immediate and prolonged beneficial hemodynamic effects and increased exercise tolerance.
Lisinopril is well tolerated. Clinically significant drug interactions have not been reported, but caution should be used when
lisinopril is administered with
diuretics,
nifedipine, or agents that may increase concentrations of
potassium. The usual initial oral dosage of
lisinopril is 10 mg once a day (range 20-40 mg/day). Lower dosages may be necessary in patients with renal impairment or
congestive heart failure, elderly persons, and those receiving
diuretics.