Lisinopril
Also known as: C07AB03, L-lysyl-L-proline, Lisodur, MK-521, Prinivil, Qbrelis, Zestril
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Summary
Lisinopril is an orally administered, prescription‑only angiotensin‑converting‑enzyme (ACE) inhibitor approved for the treatment of hypertension, chronic heart failure, and post‑myocardial‑infarction care. By blocking ACE, it diminishes angiotensin II production, leading to vasodilation and reduced blood‑volume retention. It is a widely used member of the RAAS‑acting peptide family and is taken once daily.
Mechanism of Action
Lisinopril binds to and inhibits the active site of angiotensin‑converting‑enzyme, preventing conversion of angiotensin I to the potent vasoconstrictor angiotensin II. This lowers circulating angiotensin II and aldosterone, raises plasma renin activity, promotes vasodilation, natriuresis, and reduces preload and afterload, collectively lowering arterial pressure.
What the Research Shows
A systematic review of 135 RCTs (45,420 participants) found ACE inhibitors, including lisinopril, double the risk of dry cough versus placebo (RR 2.21) and rank lisinopril mid‑range for cough incidence. In chronic heart failure, the ATLAS trial showed high‑dose lisinopril reduced death or hospitalization (12% relative reduction) but increased dizziness and renal insufficiency. The ALLHAT trial (9,054 participants on lisinopril) demonstrated similar primary cardiovascular outcomes to a thiazide diuretic but higher rates of combined CVD, stroke, and heart‑failure events. A crossover trial highlighted substantial individual variability in blood‑pressure response to lisinopril. Post‑partum hypertension data are limited, with lisinopril/thiazide combinations requiring more additional antihypertensives than nifedipine. Overall, lisinopril reliably lowers blood pressure but its comparative advantage varies across populations.
Reported Benefits
Clinical data confirm that lisinopril produces a smooth, gradual reduction in systolic and diastolic blood pressure (≈11‑15% systolic, 13‑17% diastolic) and improves heart‑failure outcomes, reducing hospitalizations and mortality trends. It is effective as monotherapy and synergistic with thiazides, and does not cause hypokalemia, hyperglycaemia, or hyperuricaemia.
Limitations of the Evidence
Cough is a common adverse effect, occurring roughly twice as often as with placebo. High‑dose therapy can cause dizziness and renal insufficiency. In the large ALLHAT trial, lisinopril was less effective than thiazide diuretics for preventing major cardiovascular events. Evidence for postpartum hypertension and pregnancy use is limited, and individual blood‑pressure responses vary widely.
Safety Considerations
The most frequent safety concerns are dry cough (RR 2.21 vs placebo), dizziness, and renal insufficiency, especially at higher doses or in patients with creatinine clearance ≤30 mL/min, where drug accumulation occurs. Lisinopril is generally well tolerated, does not affect potassium, glucose, uric acid, or cholesterol, but renal function should be monitored.
How It Is Administered
Lisinopril is taken orally, usually once daily. Peak plasma levels appear 6‑8 hours after dosing; antihypertensive effect begins within 2 hours and lasts at least 24 hours. Bioavailability is about 25% and is unchanged by food. The drug is excreted unchanged in urine, with dose adjustment needed in severe renal impairment.
Routes of Administration
Goals & Uses
- Heart failureCardiovascularHigh
- Hypertension managementCardiovascularHigh
- HypertensionCardiovascularHigh
- Stroke preventionNeurologicalModerate
- Diabetic nephropathy prevention/slowingRenalHigh
- Post-myocardial infarction cardioprotectionCardiovascularHigh
- Post‑myocardial InfarctionCardiovascularHigh
- Heart failure with reduced ejection fractionCardiovascularHigh
Contraindications
- Severe renal artery stenosis (bilateral)RenalHigh
- Hereditary or idiopathic angioedemaImmunologic/AllergicHigh
- Severe renal impairmentOrganModerateKidney function concerns
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Concurrent aliskiren use in diabetesDrug InteractionHigh
- Hereditary AngioedemaGeneticHigh
- History of ACE inhibitor-induced angioedemaImmunologic/AllergicHigh
Adverse Effects
- CoughRespiratoryCommonPersistent or episodic cough
- Acute kidney injuryRenalUncommonSudden decline in kidney function
- HypotensionCardiovascularCommonLow blood pressure
- Hypotension (first-dose)CardiovascularUncommon
- HyperkalemiaElectrolyte ImbalanceUncommon
- Dry coughRespiratoryCommon
- AngioedemaImmunologicRare
- Dizziness/headacheNeurologicalCommon
Drug Interactions
- Potassium-sparing diuretics (e.g., spironolactone)Moderate
- Diuretics (loop/thiazide)Moderate
- Potassium‑sparing diuretics (e.g., spironolactone)Moderate
- AliskirenHigh
- NSAIDsLowMay increase renal risk in susceptible patients
- NSAIDs (e.g., ibuprofen)Moderate
- LithiumModerate
Population Constraints
- Pediatric patients (<6 years or GFR <30)PediatricRelative
- ElderlyAgeRelative
- African-American patientsEthnic/GeneticRelative
- Patients with renal impairmentOrgan ImpairmentRelative
- Children < 6 monthsPediatricAbsolute
- Elderly patientsAgeRelative
- Pregnant womenReproductiveAbsolute
Regulatory Status
- European UnionApprovedApproved: Hypertension, Heart FailureEMA approval; same indications as US with minor variations
- United StatesApprovedApproved: Hypertension, Heart Failure, Post‑myocardial InfarctionFDA approved since 1995
- United KingdomApprovedApproved: Hypertension, Congestive heart failure, Short-term treatment following acute myocardial infarction, Renal complications in hypertensive diabetic patientsApproved by MHRA; available as generic. Included in NHS formulary.
Approved by the FDA in 1987. Available as generic and under brand names Prinivil and Zestril. Black box warning for fetal toxicity when used during pregnancy.
Evidence & Sources
- Journal ArticleHighHu Y, et al.2023-01-01T00:00:00.000000Z
- Journal ArticleHighTol ID, et al.2026-01-01T00:00:00.000000Z
- Journal ArticleModeratePacker M, et al.1999-01-01T00:00:00.000000Z
- Journal ArticleModerateSundström J, et al.2023-01-01T00:00:00.000000Z
- Journal ArticleModerateGomez HJ, Cirillo VJ, Moncloa F1987-01-01T00:00:00.000000Z
- Journal ArticleModerateALLHAT Officers and Coordinators for the ALLHAT Collaborative Research Group. The Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial2002-01-01T00:00:00.000000Z
Frequently Asked Questions
What medical conditions is lisinopril prescribed for?
Lisinopril is approved for treating high blood pressure, chronic heart failure, and for reducing cardiovascular risk after a heart attack. It may be used alone or together with other antihypertensives such as thiazide diuretics.
How does lisinopril lower blood pressure?
By inhibiting angiotensin‑converting‑enzyme, lisinopril blocks formation of angiotensin II, a powerful vasoconstrictor, and reduces aldosterone‑driven sodium retention. The resulting vasodilation and natriuresis lower arterial pressure and lessen cardiac workload.
Why can lisinopril cause a persistent dry cough?
ACE inhibition leads to accumulation of bradykinin and substance P in the respiratory tract, which can irritate airway nerves and trigger a dry cough. The systematic review showed ACE inhibitors double the cough risk compared with placebo.
How should dosing be adjusted in people with kidney disease?
Lisinopril is excreted unchanged in urine; in patients with severe renal impairment (creatinine clearance ≤30 mL/min) drug accumulation occurs. Dose reduction or careful monitoring of renal function and serum potassium is recommended in this population.
What is Lisinopril?
Lisinopril is an orally administered, prescription‑only angiotensin‑converting‑enzyme (ACE) inhibitor approved for the treatment of hypertension, chronic heart failure, and post‑myocardial‑infarction care. By blocking ACE, it diminishes angiotensin II production, leading to vasodilation and reduced blood‑volume retention. It is a widely used member of the RAAS‑acting peptide family and is taken once daily.
What is Lisinopril used for?
Lisinopril is educationally associated with: Heart failure, Hypertension management, Hypertension, Stroke prevention, Diabetic nephropathy prevention/slowing, Post-myocardial infarction cardioprotection, Post‑myocardial Infarction, Heart failure with reduced ejection fraction. Educational only — not medical advice.
How is Lisinopril administered?
Recorded routes of administration: Oral.
What are the potential side effects of Lisinopril?
Reported adverse effects include: Cough, Acute kidney injury, Hypotension, Hypotension (first-dose), Hyperkalemia, Dry cough, Angioedema, Dizziness/headache. This list is not exhaustive — consult a qualified clinician.
Who should avoid Lisinopril?
Recorded contraindications: Severe renal artery stenosis (bilateral), Hereditary or idiopathic angioedema, Severe renal impairment, Pregnancy, Concurrent aliskiren use in diabetes, Hereditary Angioedema, History of ACE inhibitor-induced angioedema. Consult a qualified clinician before use.