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Pharmacokinetics of lisinopril
1Department of Drugs, National Board of Health and Welfare, Uppsala, Sweden.
The American Journal of Medicine
|September 23, 1988
Summary
Lisinopril, an angiotensin-converting enzyme inhibitor, is 25% bioavailable orally, unaffected by food. It is eliminated by the kidneys with a 12.6-hour accumulation half-life, reaching steady state in two days.
Area of Science:
- Pharmacology
- Nephrology
- Cardiovascular Medicine
Background:
- Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor.
- Understanding its pharmacokinetic profile is crucial for effective therapeutic use.
Purpose of the Study:
- To characterize the pharmacokinetics of lisinopril in healthy volunteers.
- To assess the influence of food on lisinopril bioavailability.
- To determine the elimination pathways and half-life of lisinopril.
Main Methods:
- Oral administration of lisinopril.
- Blood sampling for pharmacokinetic analysis.
- Assessment of drug levels in serum and urine.
- Evaluation of drug interactions with furosemide.
Main Results:
- Oral bioavailability of lisinopril is 25% ± 4%, not affected by food.
- Accumulation half-life averages 12.6 hours; terminal half-life is approximately 40 hours.
- Steady-state concentrations achieved within two daily doses.
- Lisinopril is eliminated unchanged by the kidneys via filtration, secretion, and reabsorption.
- No pharmacokinetic interaction observed with furosemide.
Conclusions:
- Lisinopril exhibits predictable oral bioavailability and elimination kinetics.
- Renal excretion is the primary route of lisinopril elimination.
- The drug's pharmacokinetic profile supports a once-daily dosing regimen.