Innovace
enalapril maleate
enalaprilat
Pharmacologic class: Angiotensin-converting enzyme (ACE) inhibitor
Therapeutic class: Antihypertensive
Pregnancy risk category C (first trimester), D (second and third trimesters)
FDA Box Warning
• When used during second or third trimester of pregnancy, drug can cause fetal injury and even death. Discontinue as soon as pregnancy is detected.
Action
Inhibits conversion of angiotensin I to angiotensin II, a potent vasoconstrictor; inactivates bradykinin and prostaglandins. Also increases plasma renin and potassium levels and reduces aldosterone levels, resulting in systemic vasodilation.
Availability
Injection: 1.25 mg/ml
Tablets: 2.5 mg, 5 mg, 10 mg, 20 mg
Indications and dosages
➣ Hypertension
Adults: For patients not taking concomitant diuretics-initially, 5 mg P.O. once daily, increased after 1 to 2 weeks as needed to a maintenance dosage of 10 to 40 mg P.O. daily given as a single dose or in two divided doses; or 1.25 mg I.V. q 6 hours. For patients taking diuretics-initially, 2.5 mg P.O. or 0.625 mg I.V.
Children: 0.08 mg/kg P.O. once daily; may be increased based on blood pressure response up to 5 mg daily. Maximum dosage is 0.58 mg/kg/dose.
➣ Heart failure
Adults: Initially, 2.5 mg P.O. once or twice daily, increased after 1 to 2 weeks as needed to maintenance dosage of 5 to 40 mg P.O. daily given as a single dose or in two divided doses
➣ Asymptomatic left ventricular dysfunction
Adults: Initially, 2.5 mg P.O. once or twice daily, increased after 1 to 2 weeks as needed to a maximum of 20 mg/day in divided doses
Dosage adjustment
• Renal impairment
Off-label uses
• Diabetic nephropathy
• Hypertensive emergency
Contraindications
• Hypersensitivity to drug or other ACE inhibitors
• Angioedema
• Pregnancy
Precautions
Use cautiously in:
• renal or hepatic impairment, hypovolemia, hyponatremia, aortic stenosis, hypertrophic cardiomyopathy, cerebrovascular or cardiac insufficiency
• concurrent diuretic use
• elderly patients
• breastfeeding patients
• children.
Administration
• Give oral doses with food or beverage.
• Discontinue diuretics for 2 to 3 days before starting drug, if possible.
• Know that I.V. administration is usually reserved for patients who cannot take P.O. form.
• Be aware that I.V. administration isn't recommended for pediatric patients.
• Administer I.V. dose either undiluted or diluted in 50 ml of dextrose 5% in water, normal saline solution, dextrose 5% in normal saline solution, or dextrose 5% in lactated Ringer's solution.
• Give single I.V. dose by push or piggyback over 5 minutes. If patient is at risk for hypotension, infusion may be given over 1 hour.
• Be aware that black patients have a higher risk of angioedema.
Adverse reactions
CNS: dizziness, fatigue, headache, insomnia, drowsiness, vertigo, asthenia, paresthesia, ataxia, confusion, depression, nervousness,cerebrovascular accident
CV: orthostatic hypotension, palpitations, angina pectoris, tachycardia, peripheral edema,arrhythmias, cardiac arrest
EENT: sinusitis
GI: nausea, vomiting, constipation, dyspepsia, abdominal pain, dry mouth, pancreatitis
GU: proteinuria, urinary tract infection, erectile dysfunction, decreased libido,oliguria
Hematologic: agranulocytosis, bone marrow depression
Hepatic: hepatitis
Metabolic: hyponatremia,hyperkalemia Respiratory: cough, upper respiratory tract infection, asthma, bronchitis, dyspnea,eosinophilic pneumonitis
Skin: rash, alopecia, photosensitivity, diaphoresis, exfoliative dermatitis, angioedema,erythema multiforme
Other: altered taste, fever, increased appetite, anaphylactoid reactions
Interactions
Drug-drug. Allopurinol: increased risk of hypersensitivity reaction
Antacids: decreased enalapril absorption Cyclosporine, indomethacin, potassiumsparing diuretics, potassium supplements: hyperkalemia
Digoxin, lithium: increased blood levels of these drugs, possible toxicity
Diuretics, nitrates, other antihypertensives, phenothiazines: additive hypotension
Nonsteroidal anti-inflammatory drugs: decreased antihypertensive response
Rifampin: decreased enalapril efficacy
Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, bilirubin, blood urea nitrogen (BUN), creatinine, potassium: increased levels Antinuclear antibodies: positive titer Sodium: decreased level
Drug-food. Salt substitutes containing potassium: hyperkalemia
Drug-herbs. Capsaicin: increased incidence of cough
Drug-behaviors. Acute alcohol ingestion: additive hypotension
Sun exposure: photosensitivity reaction
Patient monitoring
See Assess for rapid blood pressure drop leading to cardiovascular collapse, especially when giving with diuretics.
See In patient with renal insufficiency or renal artery stenosis, monitor for worsening renal function.
• After initial dose, observe patient closely for at least 2 hours until blood pressure has stabilized. Then continue to observe for additional hour.
• Monitor vital signs, fluid intake and output, and daily weight.
• Supervise patient during ambulation until effects of drug are known.
• Monitor liver function tests, BUN, and creatinine and electrolyte levels.
Patient teaching
• Inform patient that drug's full effect may not occur for several weeks.
• Advise patient to report persistent dry cough with nasal congestion.
See Tell patient to immediately report swelling of face, eye area, tongue, lips, hands, or feet; rash, hives, or severe itching; unexplained fever; unusual tiredness; yellowing of skin or eyes; abdominal pain; or easy bruising.
• Instruct patient to move slowly when sitting up or standing, to avoid dizziness or light-headedness from sudden blood pressure decrease.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.