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enalaprilat (Vasotec IV)
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:
1) start 1.25 mg IV every 6 hours
2) max 5 mg IV every 6 hours
3) 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:
1) IV onset is within 15 minutes
2) duration of action is dose-dependent, usually lasting 4-6 hours
3) < 50% is bound to plasma proteins
4) elimination 1/2life is 35 hours
5) clearance is decreased in CHF, uremia & the elderly
Adverse effects:
1) 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
3) other [2]
- dry, non-productive cough
- rash
- worsening renal failure
- angioedema (rare)
Drug interactions:
1) see ACE inhibitor
2) high risk of hypersensitivity reactions when used in combination with allopurinol
3) enalaprilat increases plasma levels of lithium & digoxin
Test interactions:
1) may cause positive direct antiglobulin (Coomb's) test
2) may cause false positive urine acetone determinations with sodium nitroprusside reagent
Mechanism of action: see ACE inhibitor
Interactions
drug interactions
drug adverse effects (more general classes)
monitor with ACE inhibitors
General
amide
amine
angiotensin-converting enzyme (ACE) inhibitor
carboxylic acid
ester
pyrrolidine; tetrahydropyrrole
Properties
INHIBITS: angiotensin converting enzyme
MISC-INFO: elimination route LIVER
KIDNEY
pregnancy-category D
Database Correlations
PUBCHEM correlations
References
- Manual of Medical Therapeutics, 28th ed, Ewald &
McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 120
- 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