Enalapril

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Contents 1 Introduction 2 Indications 3 Contraindications 4 Dosage 5 Pharmacokinetics 6 Adverse-effects 7 Drug-interactions 8 Test-interactions 9 More General Terms 10 Additional Terms 11 Internet Database 12 References

Introduction

• Tradename: Vasotec. ( enalapril maleate)

Indications

• (Benefits)
• improved survival in patients with mild to severe heart failure
• diminished incidence of heart failure in patients with asymptomatic left ventricular systolic dysfunction

Contraindications

• increases mortality when give in 1st 24 hours after acute myocardial infarction [4]
  

• pregnancy category = d
• safety in lactation = ?

Dosage

• HTN:

• 1.25 mg IV every 6 hours.
• Start 5 mg PO QD, max 40 mg/day.

• CHF: Start 2.5 mg PO QD/ BID, max 40 mg/day.

• Tabs: 2.5, 5, 10, 20 mg.

Pharmacokinetics

• Enalapril is hepatically hydrolyzed to the active ACE inhibitor enalaprilat.
  

• elimination via liver
• elimination via kidney
• 1/2life = 12-24 hours
• 1/2life = 35-38 hours

Adverse-effects

• infrequent (1-10%)

• chest pain, palpitations, tachycardia, syncope, insomnia, headache, dizziness, fatigue, malaise, rash, abnormal taste, abdominal pain, nausea/vomiting, anorexia, constipation, paresthesia, weakness, bronchitis, cough dyspnea
• uncommon (< 1%) agranulocytosis - incidence may be less than for captopril, angina pectoris, flushing, alopecia, erythema multiforme, pruritis, Stevens-Johnson syndrome, urticaria, angioedema, hypoglycemia, hyperkalemia, impotence, anemia, myalgia, blurred vision, tinnitus, oliguria, asthma, bronchospasm, diaphoresis
  
• drug adverse effects of ACE inhibitors

Drug-interactions

• non-steroidal anti-inflammatory agents (NSAIDs) decrease effect of enalapril
• Li+ increases serum levels & toxicity of enalapril
  
• drug interaction(s) of renin-angiotensin inhibitors with trimethoprim-sulfamethoxazole
• drug interaction(s) of lithium carbonate with ACE inhibitors
• 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 with ACE inhibitors
• drug interaction(s) of ACE inhibitors, angiotensin II receptor antagonists & beta-blockers
• drug interaction(s) of NSAIDs, diuretics & ACE inhibitors

Test-interactions

• positive direct antiglubin (Coomb's) test ( DAT)
• may cause false positive urine acetone with sodium nitroprusside reagent

More General Terms

• pyrrolidine; tetrahydropyrrole
• amide
• amine
• carboxylic acid
• ester
• angiotensin-converting enzyme [ACE] inhibitor

Additional Terms

• ACE inhibitors vs angiotensin receptor blockers (ARB)
• enalaprilat (Vasotec IV)

Internet Database

PubChem: 53370
PubChem: 441208
PubChem: 3222

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. Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 117
4. contribution from Paul Goebel, M.D., UCSF Fresno
5. Kaiser Permanente Northern California Regional Drug Formulary, 1998
6. Department of Veterans Affairs, VA National Formulary

enalapril (Vasotec)