What is lisinopril (Angiotensin-Converting Enzyme (ACE) inhibitor)?

From the Guidelines

Lisinopril is a medication that belongs to a class of drugs called angiotensin-converting enzyme (ACE) inhibitors, primarily used to treat high blood pressure, heart failure, and to improve survival after heart attacks. It works by relaxing blood vessels, allowing blood to flow more easily and reducing the workload on the heart.

Key Points

• Typical dosing ranges from 5 to 40 mg once daily, with treatment usually starting at a lower dose and gradually increasing as needed, as seen in the study 1.
• Lisinopril helps prevent kidney damage in people with diabetes and high blood pressure, as supported by the evidence 1.
• Common side effects include dry cough, dizziness, headache, and rarely angioedema (swelling of face, lips, tongue).
• It should not be taken during pregnancy as it can harm the developing fetus.
• Patients should take lisinopril at the same time each day, and it can be taken with or without food.
• Blood pressure monitoring is essential while using this medication to ensure it's working effectively, with a goal of keeping blood pressure below 130/80 mm Hg, as indicated in the study 1.

Dosage

• The starting dose of lisinopril is typically 10 mg daily, with a goal dose of 20-40 mg daily, as recommended in the study 1.
• The dosage may need to be adjusted based on the patient's response to the medication and their kidney function.

Benefits

• Lisinopril has been shown to reduce the risk of cardiovascular events, such as heart attacks and strokes, in patients with high blood pressure and diabetes, as supported by the evidence 1.
• It also helps to slow the progression of kidney disease in patients with diabetes and high blood pressure.

From the FDA Drug Label

Lisinopril is an oral long-acting angiotensin converting enzyme inhibitor. Lisinopril, a synthetic peptide derivative, is chemically described as (S)-1-[N2-(1-carboxy-3-phenylpropyl)-L-lysyl]-L-proline dihydrate. Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor.

• It is used to treat hypertension and heart failure.
• The mechanism of action is through the inhibition of ACE, which leads to a decrease in plasma angiotensin II and aldosterone secretion.
• The empirical formula of lisinopril is C21H31N3O5 • 2H2O, and it has a molecular weight of 441.53 2.

From the Research

Definition and Mechanism of Action

• Lisinopril is an orally active angiotensin-converting enzyme (ACE) inhibitor 3, 4, 5, 6, 7.
• It works by inhibiting ACE activity, reducing plasma angiotensin II and aldosterone, and increasing plasma renin activity 5.
• Lisinopril is not metabolized or bound to protein, and its bioavailability is approximately 25% 5, 6, 7.

Therapeutic Uses

• Lisinopril is effective in lowering blood pressure in all grades of essential hypertension 3, 6, 7.
• It is also used in the treatment of congestive heart failure, where it improves indices of cardiac function and reduces the risk of major clinical events 3, 4.
• Lisinopril can be used as monotherapy or in combination with other antihypertensive agents, such as diuretics or beta blockers 3, 6, 7.

Pharmacokinetics and Dosage

• Lisinopril is absorbed in its active form, with peak serum concentrations occurring 6-8 hours after oral dosing 5, 6, 7.
• The elimination half-life of lisinopril is approximately 12.6 hours, and it is primarily excreted through renal excretion 5, 6, 7.
• The usual dosage of lisinopril is 20-80 mg once daily, although higher doses may be used in certain cases 3, 4, 6, 7.

Safety and Tolerability

• Lisinopril is generally well tolerated, with few serious adverse effects reported 3, 4, 5, 6, 7.
• Common side effects include dizziness, cough, hypotension, and diarrhea 4, 6, 7.
• Lisinopril may interact with other medications, such as diuretics, potassium supplements, and nonsteroidal anti-inflammatory agents 6, 7.