Enalaprilat

From Anvita Health Wiki

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

Introduction

• Enalapril is hepatically hydrolyzed to the active ACE inhibitor enalaprilat. Enalaprilat is available for IV administration.

Indications

• treatment of hypertension &/or congestive heart failure ( CHF) in patients without enteral access

Dosage

• start 1.25 mg IV every 6 hours
• max 5 mg IV every 6 hours
• 0.625 mg IV every 6 hours of enalaprilat is approximately equivalent to 2.5 mg PO QD of enalapril.

• Use lower initial dose when creatinine clearance < 30 mL/min.
• For patients with creatinine > 3 mg/dL or creatinine clearance < 30 mL/min, begin 0.625 mg IV every 6 hours.

Pharmacokinetics

• IV onset is within 15 minutes
• duration of action is dose-dependent, usually lasting 4-6 hours
• < 50% is bound to plasma proteins
• elimination 1/2life is 35 hours
• clearance is decreased in CHF, uremia & the elderly
  

• elimination via liver
• elimination via kidney

Adverse-effects

• not common (1-10%)

• chest pain, palpitations, tachycardia, syncope, insomnia, headache, dizziness, fatigue, malaise, rash, abnormal taste, abdominal pain, nausea/vomiting, diarrhea, anorexia, constipation, paresthesia, weakness, bronchitis, cough, dyspnea

• uncommon (< 1%)

• angina pectoris, flushing, alopecia, erythema multiforme, pruritis, Stevens-Johnson syndrome, urticaria, angioedema, hypoglycemia, hyperkalemia, impotence, agranulocytosis, neutropenia, anemia, myalgia, blurred vision, tinnitus, oliguria, bronchospasm, diaphoresis

• other [2]

• dry, non-productive cough
• rash
• worsening renal failure
• angioedema (rare)
  
• drug adverse effects of ACE inhibitors

Drug-interactions

• see ACE inhibitor
• high risk of hypersensitivity reactions when used in combination with allopurinol
• enalaprilat increases plasma levels of lithium & digoxin
  
• 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

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

Mechanism-of-action

• see ACE inhibitor

More General Terms

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

Internet Database

PubChem: 53504
PubChem: 55286
PubChem: 443379

References

1. Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 120
2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998 - not on National VA formulary
3. Kaiser Permanente Northern California Regional Drug Formulary, 1998

enalaprilat (Vasotec IV)