Lisinopril pharmacokinetics
Pro Research Analysisby 
Searched over 200M research papers for "lisinopril pharmacokinetics"
Lisinopril Pharmacokinetics: Absorption, Distribution, Metabolism, and Elimination
Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor with unique pharmacokinetic properties. Its oral bioavailability is about 25%, and this is generally unaffected by food intake, although some studies in specific populations have shown a reduction in systemic exposure when taken with food, with a loss of about 20–25% in healthy Chinese subjects under postprandial conditions compared to fasting states 17. In patients with congestive heart failure, absorption is further reduced, with bioavailability dropping to around 16% .
After oral administration, the maximum concentration (C_max) of lisinopril is typically reached 5–6 hours post-dose. The drug is not metabolized and is eliminated unchanged by the kidneys, primarily through glomerular filtration, tubular secretion, and reabsorption 12. The terminal serum half-life is approximately 40 hours, but the effective half-life for drug accumulation is shorter, averaging about 12.6 hours. Steady-state concentrations are usually achieved after two daily doses 12.
Lisinopril Pharmacokinetics in Special Populations
Renal Impairment and Elderly Patients
Lisinopril clearance is significantly influenced by renal function. In patients with chronic renal failure, there is a strong inverse correlation between creatinine clearance and both the area under the curve (AUC) and plateau lisinopril concentrations, indicating that reduced kidney function leads to higher drug exposure . Population studies confirm that clearance is also affected by age, weight, and the presence of cardiac failure, but not by other clinical features . In patients with congestive heart failure, both absorption and disposition of lisinopril are altered, likely due to the disease state and age .
Pediatric Patients
In children, lisinopril pharmacokinetics vary by age and body weight. After dosing, younger children (6–23 months) have lower C_max and AUC values compared to older children (6–15 years), who show higher systemic exposure . Physiologically based pharmacokinetic (PBPK) models have been developed to better predict appropriate pediatric dosing, as traditional weight- or surface area-based calculations tend to overestimate the required dose. PBPK models account for age- and gender-related physiological differences, providing more accurate dosing recommendations for children 810.
Drug Interactions and Formulation Considerations
Lisinopril does not undergo significant drug-drug interactions with furosemide, and its pharmacokinetics are not affected by co-administration with this diuretic . Studies comparing generic and reference formulations of lisinopril/hydrochlorothiazide tablets have shown bioequivalence and similar safety profiles under both fasting and fed conditions .
Conclusion
Lisinopril displays predictable pharmacokinetics in healthy adults, with renal function being the primary determinant of drug clearance. Special populations, such as those with renal impairment, heart failure, the elderly, and children, require careful consideration of dosing due to altered absorption and elimination. PBPK modeling offers a promising approach for optimizing pediatric dosing. Overall, lisinopril is not metabolized, is eliminated unchanged by the kidneys, and reaches steady-state quickly, making it a reliable option for hypertension and heart failure management across diverse patient groups 1234+5 MORE.
Sources and full results
Most relevant research papers on this topic
Lisinopril population pharmacokinetics in elderly and renal disease patients with hypertension.
Lisinopril clearance is significantly influenced by creatinine concentration, age, weight, and cardiac failure, while volume of distribution is unaffected by these factors.
A multicenter study of the pharmacokinetics of lisinopril in pediatric patients with hypertension
Lisinopril's pharmacokinetics in children with hypertension are similar to adults, with doses varying based on body weight and no serious adverse events reported.
Pharmacokinetic evaluation of lisinopril-tryptophan, a novel C-domain ACE inhibitor.
Lisinopril-tryptophan (LisW-S) is a novel C-domain ACE inhibitor with a 5.4% oral bioavailability and potential for improved clinical application.
DOI