enalaprilat (Vasotec IV)
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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 B2) uncommon (< 1%)
- angina pectoris, flushing, alopecia, erythema multiforme, pruritus, 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 renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
- drug adverse effects of ACE inhibitors
- drug adverse effects of antihypertensive agents
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 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
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
References
- ↑ Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 120
- ↑ 2.0 2.1 Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998 - not on National VA formulary
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998