lisinopril (Prinivil, Zestril)
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Introduction
Tradenames: Prinivil, Zestril.
Indications
- hypertension
- heart failure
- post myocardial infarction (MI)
- diabetic nephropathy
- nondiabetic proteinuric nephropathy
- scleroderma renal crisis
- 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
- HTN: Start 10 mg PO QD, max 40 mg/day
- CHF: Start 2.5-5 mg PO QD/BID, max 20-40 mg/day
- 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
Table
| creatinine clearance | dosage |
|---|---|
| 10-50 mL/min | 50-75% of normal dose |
| < 10 mL/min | 25-50% of normal dose |
Pharmacokinetics
- onset of action: 1 hour
- peak hypotensive effect within 6 hours after oral dose
- duration of action 24 hours
- minimal protein binding
- elimination 1/2life
- about 12 hours
- prolonged in patients with renal insufficiency
- 10% of drug is excreted unchanged into the urine
elimination via kidney
Adverse effects
- infrequent (1-10%)
- dizziness, headache, fatigue, diarrhea, upper respiratory tract symptoms, cough, hypotension, increased BUN & creatinine
- 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 adverse effects of renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
- drug adverse effects of ACE inhibitors
- drug adverse effects of antihypertensive agents
Drug interactions
- coadministration of K+ sparing diuretics causes increased hyperkalemic effect
- coadministration with NSAIDs causes reduced antihypertensive response
- phenothiazines increase pharmacologic effects of ACE inhibitors
- allopurinol in combination results in high risk of hyper- sensitivity reactions
- lisinopril increases plasma lithium & digoxin levels
- drug interaction(s) of fluticasone with HIV1 protease inhibitors
- drug interaction(s) of calcineurin inhibitors with ACE inhibitors
- drug interaction(s) of calcium channel blockers with ACE inhibitors
- drug interaction(s) of renin-angiotensin-aldosterone inhibitors with trimethoprim-sulfamethoxazole
- drug interaction(s) of lithium carbonate with ACE inhibitors
- drug interaction(s) of ACE inhibitor with trimethoprim
- drug interaction(s) of ACE inhibitors with potassium-sparing diuretics
- drug interaction(s) of ACE inhibitors with aliskiren
- drug interaction(s) of ACE inhibitors with angiotensin II receptor antagonists
- drug interaction(s) of potassium chloride with ACE inhibitors
- drug interaction(s) of spironolactone with ACE inhibitors
- drug interaction(s) of diuretics with ACE inhibitors
- drug interaction(s) of beta blockers with ACE inhibitors
- drug interaction(s) of NSAIDs, diuretics & ACE inhibitors
- drug interaction(s) of NSAIDs with ACE inhibitors
- drug interaction(s) of NSAIDs & antihypertensives
Mechanism of action
- dicarocyl-containing ACE inhibitor
- inhibits conversion of angiotensin I to angiotensin II
- inhibits degradation of bradykinin
Notes
- lisinopril, but not amlodipine seems to protect against cardiac conduction system defects relative to chlorthalidone (RR=0.81)[8]
More general terms
- pyrrolidine; tetrahydropyrrole
- amide
- amine
- carboxylic acid
- angiotensin-converting enzyme (ACE) inhibitor
Component of
References
- ↑ Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1990. pg 760-1
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 5.0 5.1 Journal Watch 23(4):34, 2003 BMJ 322:19, 2001
- ↑ Deprecated Reference
- ↑ 7.0 7.1 7.2 7.3 Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
- ↑ 8.0 8.1 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: https://www.ncbi.nlm.nih.gov/pubmed/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: https://www.ncbi.nlm.nih.gov/pubmed/27367299