Lisinopril

Summary

Lisinopril is a long-acting, orally active ACE inhibitor used to treat hypertension, heart failure, and to improve survival post-myocardial infarction. It is also used in diabetic nephropathy. Unlike most ACE inhibitors, it is not a prodrug and does not require hepatic activation.

Mechanism of Action

Competitively inhibits angiotensin-converting enzyme (ACE), preventing conversion of angiotensin I to angiotensin II, thereby reducing vasoconstriction and aldosterone secretion, leading to decreased blood pressure and reduced cardiac preload and afterload.

Routes of Administration

Goals & Uses

• Hypertension managementCardiovascularHigh
• Stroke preventionNeurologicalModerate
• Diabetic nephropathy prevention/slowingRenalHigh
• Post-myocardial infarction cardioprotectionCardiovascularHigh
• Heart failure with reduced ejection fractionCardiovascularHigh

Contraindications

• Severe renal artery stenosis (bilateral)RenalHigh
• Hereditary or idiopathic angioedemaImmunologic/AllergicHigh
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• Concurrent aliskiren use in diabetesDrug InteractionHigh
• History of ACE inhibitor-induced angioedemaImmunologic/AllergicHigh

Adverse Effects

• Acute kidney injuryRenalUncommonSudden decline in kidney function
• Hypotension (first-dose)CardiovascularUncommon
• HyperkalemiaElectrolyte ImbalanceUncommon
• Dry coughRespiratoryCommon
• AngioedemaImmunologicRare
• Dizziness/headacheNeurologicalCommon

Drug Interactions

• Potassium-sparing diuretics (e.g., spironolactone)Moderate
• Diuretics (loop/thiazide)Moderate
• AliskirenHigh
• NSAIDs (e.g., ibuprofen)Moderate
• LithiumHigh

Population Constraints

• Pediatric patients (<6 years or GFR <30)PediatricRelative
• African-American patientsEthnic/GeneticRelative
• Patients with renal impairmentOrgan ImpairmentRelative
• Elderly patientsAgeRelative
• Pregnant womenReproductiveAbsolute

Regulatory Status

• European UnionApprovedApproved: Hypertension, Heart failure, Short-term treatment of acute myocardial infarction, Renal complications of diabetes mellitusApproved by EMA member states; widely available as generic across EU.
• United StatesApprovedApproved: Hypertension (adults and pediatric patients ≥6 years), Heart failure, Acute myocardial infarction (within 24 hours, hemodynamically stable)Approved by FDA 1987; Black Box Warning for fetal toxicity. Available as generic.
• 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

No sources recorded yet.