Based on urinary recovery, the mean extent of absorption of lisinopril is approximately 25%, with large interpatient variability (6 to 60%) at all doses tested (5 to 80 mg). Lisinopril absorption is not affected by the presence of food in the gastrointestinal tract.Studies in rats indicate that lisinopril crosses the blood-brain barrier poorly. Multiple doses of lisinopril in rats do not result in accumulation in any tissues. Usual  bioavailability of ~25% (reduced to 16% in people with New York Heart Association Functional Classification (NYHA) Class II–IV heart failure). Its time to peak concentration is 7 hours. The peak effect of lisinopril is about 4 to 8 hours after administration. Food does not affect its absorption. Distribution
Lisinopril does not bind to proteins in the blood. It does not distribute as well in people with NYHA Class II–IV heart failure. Metabolism
Lisinopril is the only water-soluble member of the ACE inhibitor class, with no metabolism by the liver. Elimination
Lisinopril leaves the body completely unchanged in the urine. The half-life of lisinopril is 12 hours, and is increased in people with kidney problems. While the plasma half-life of lisinopril has been estimated between 12 and 13 hours, the elimination half-life is much longer, at around 30 hours. The full duration of action is between 24 and 30 hours. Chemistry
Pure lisinopril powder is white to off white in color. Lisinopril is soluble in water (approximately 13 mg/L at room temperature), less soluble in methanol, and virtually insoluble in ethanol.
Lisinopril is a medication of the angiotensin-converting enzyme (ACE) inhibitor and is used to treat high blood pressure, heart failure, and after heart attacks. For high blood pressure it is usually a first-line treatment. It is also used to prevent kidney problems in people with diabetes mellitus. Lisinopril is taken by mouth. Full effect may take up to four weeks to occur.Common side effects include headache, dizziness, feeling tired, cough, nausea, and rash. Serious side effects may include low blood pressure, liver problems, high blood potassium, and angioedema. Use is not recommended during the entire duration of pregnancy as it may harm the baby. Lisinopril works by inhibiting the renin–angiotensin–aldosterone system.Lisinopril was patented in 1978 and approved for medical use in the United States in 1987. It is available as a generic medication. In 2020, it was the fourth most commonly prescribed medication in the United States, with more than 88 million prescriptions. In July 2016, an oral solution formulation of lisinopril was approved for use in the United States. Structure–activity relationships
Lisinopril has a proline group that is responsible for the availability of the drug in oral formulation. The carboxylate group interacts with zinc ions to inhibit the ACE enzyme found in the kidneys and lungs. The other substituents participate in binding the same enzyme. Unlike Captopril, another ACE Inhibitor, Lisinopril lacks a thiol group. Medical uses
Lisinopril is typically used for the treatment of high blood pressure, congestive heart failure, and diabetic nephropathy and after acute myocardial infarction (heart attack).