enalaprilat (redirected from Vasotec IV)

enalaprilat /enal·a·pril·at/ (-pril-at″) an angiotensin-converting enzyme inhibitor, the active metabolite of enalapril, used to treat hypertensive crisis and as an intravenous substitute for oral enalapril maleate.

---

enalaprilat

the pharmacologically active product of hepatic hydrolysis of enalapril.

---

enalaprilat

Vasotec IV

Pharmacologic class: Angiotensin-converting enzyme (ACE) inhibitor

Therapeutic class: Antihypertensive

Pregnancy risk category C (first trimester), D (second and third trimesters)

FDA Boxed 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
• black patients with hypertension
• 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's at risk for hypotension, infusion may be given over 1 hour.

Route	Onset	Peak	Duration
P.O.	1 hr	4-6 hr	24 hr
I.V.	15 min	3-4 hr	6 hr

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, potassium-sparing 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

☞ Assess for rapid blood pressure drop leading to cardiovascular collapse, especially when giving with diuretics.
☞ 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.
☞ 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.