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lisinopril (Prinivil, Zestril)

Tradenames: Prinivil, Zestril. Indications: 1) hypertension 2) heart failure 3) post myocardial infarction (MI) 4) diabetic nephropathy 5) nondiabetic proteinuric nephropathy 6) scleroderma renal crisis 7) migraine prophylaxis [5] Contraindications: - pregnancy: - teratogenic in 1st trimester [7] - fetal or neonatal renal failure in 2nd or 3rd trimester - scleroderma renal crisis is exception [7] - question of safety in lactation (captopril & enalopril are considered safe) [7] Dosage: 1) HTN: Start 10 mg PO QD, max 40 mg/day 2) CHF: Start 2.5-5 mg PO QD/BID, max 20-40 mg/day 3) MI: Start 5 mg within 24 hours if hemodynamically stable 5 mg 24 hours later, then 10 mg QD Tabs: 2.5, 5, 10, 20, 40 mg. Dosage adjustment in renal failure: creatinine clearance dosage 10-50 mL/min 50-75% of normal dose < 10 mL/min 25-50% of normal dose Pharmacokinetics: 1) onset of action: 1 hour 2) peak hypotensive effect within 6 hours after oral dose 3) duration of action 24 hours 4) minimal protein binding 5) elimination 1/2life a) about 12 hours b) prolonged in patients with renal insufficiency 6) 10% of drug is excreted unchanged into the urine Adverse effects: 1) infrequent (1-10%) - dizziness, headache, fatigue, diarrhea, upper respiratory tract symptoms, cough, hypotension, increased BUN & creatinine 2) uncommon (< 1%) - chest discomfort, fever, flushing, malaise, angina pectoris, myocardial infarction, orthostatic hypotension, arrhythmias, tachycardia, peripheral edema, vasculitis, palpitations, pancreatitis, hepatitis, abdominal pain, anorexia, constipation, flatulence, dry mouth, gout, shoulder pain, depression, somnolence, insomnia, bronchitis, sinusitis, pharyngeal pain, urticaria, pruritus, diaphoresis, blurred vision, angioedema, syncope, neutropenia, bone marrow suppression Drug interactions: 1) coadministration of K+ sparing diuretics causes increased hyperkalemic effect 2) coadministration with NSAIDs causes reduced antihypertensive response 3) phenothiazines increase pharmacologic effects of ACE inhibitors 4) allopurinol in combination results in high risk of hyper- sensitivity reactions 5) lisinopril increases plasma lithium & digoxin levels Mechanism of action: 1) dicarocyl-containing ACE inhibitor 2) inhibits conversion of angiotensin I to angiotensin II 3) inhibits degradation of bradykinin Notes: - lisinopril, but not amlodipine seems to protect against cardiac conduction system defects relative to chlorthalidone (RR=0.81) [8]

Interactions

drug interactions drug adverse effects (more general classes) monitor with ACE inhibitors

General

amide amine angiotensin-converting enzyme (ACE) inhibitor carboxylic acid pyrrolidine; tetrahydropyrrole

Properties

INHIBITS: angiotensin converting enzyme MISC-INFO: elimination route KIDNEY pregnancy-category D safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1990. pg 760-1
  2. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Journal Watch 23(4):34, 2003 BMJ 322:19, 2001
  6. Deprecated Reference
  7. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
  8. Dewland TA, Soliman EZ, Davis BR et al Effect of the Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT) on Conduction System Disease. JAMA Intern Med. 2016 Aug 1;176(8):1085-1092. PMID: 27367818 - Narayan SM, Baykaner T, Maron DJ. Can Cardiac Conduction System Disease Be Prevented? JAMA Intern Med. 2016 Aug 1;176(8):1093-1094. PMID: 27367299

Component-of

hydrochlorothiazide/lisinopril; HCTZ/lisinopril (Prinzide, Zestoretic)