04/27/2026
Medication Monday: Lisinopril
Brand Names
Zestril. Prinivil. Qbrelis.
Mechanism
Lisinopril is a competitive angiotensin-converting enzyme (ACE) inhibitor used primarily to manage hypertension and heart failure. ACE normally converts the inactive decapeptide angiotensin I into the potent vasoconstrictor angiotensin II. Lisinopril inhibits this process by competitively binding to the zinc ion within the ACE active site. This decrease in angiotensin II reduces systemic vascular resistance and suppresses aldosterone secretion. This suppression decreases sodium and water reabsorption in the distal tubule and collecting duct, while slightly increasing serum potassium levels. Further, because ACE is also responsible for the degradation of bradykinin (a vasodilator), lisinopril increases circulating bradykinin levels, causing increased vasodilation. However, this accumulation of bradykinin is also associated with the common side effect of a dry cough and an increased risk of angioedema.
Indications
FDA-Approved Indications:
- Hypertension
- Heart failure (adjunctive therapy)
- STEMI (if given within 24 hours)
Off-Label Uses:
- Diabetic nephropathy
- Proteinuria
- Post-transplant erthryocytosis
Contraindications
- Hypersensitivity
- Hyperkalemia
- Hx of angioedema
- Renal failure with prior lisinopril use
- Bilateral renal artery stenosis
- Concomitant use with Aliskiren in patients with diabetes mellitus
- Nephrilysin inhibitor use within the last 36 hours
- Pregnancy
Routes
- Oral
Source
https://www.ncbi.nlm.nih.gov/books/NBK482230/