ENALAPRILAT injection

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

ENALAPRILAT (UNII: GV0O7ES0R3) (ENALAPRILAT ANHYDROUS - UNII:Q508Q118JM)

Available from:

HF Acquisition Co LLC, DBA HealthFirst

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Enalaprilat injection, USP is indicated for the treatment of hypertension when oral therapy is not practical. Enalaprilat injection, USP has been studied with only one other antihypertensive agent, furosemide, which showed approximately additive effects on blood pressure. Enalapril, the pro-drug of enalaprilat, has been used extensively with a variety of other antihypertensive agents, without apparent difficulty except for occasional hypotension. In using enalaprilat injection, USP, consideration should be given to the fact that another angiotensin converting enzyme inhibitor, captopril, has caused agranulocytosis, particularly in patients with renal impairment or collagen vascular disease, and that available data are insufficient to show that enalaprilat injection, USP does not have a similar risk. (See WARNINGS.) In considering use of enalaprilat injection, USP, it should be noted that in controlled clinical trials ACE inhibitors have an effect on blood pressure that is less in black patients than in non-blacks. In addition, it should be noted that black patients receiving ACE inhibitors have been reported to have a higher incidence of angioedema compared to non-blacks. (See WARNINGS, Angioedema). Enalaprilat injection, USP is contraindicated in patients who are hypersensitive to any component of this product and in patients with a history of angioedema related to previous treatment with an angiotensin converting enzyme inhibitor and in patients with hereditary or idiopathic angioedema.

Product summary:

ENALAPRILAT INJECTION is supplied in the following dosage forms. NDC 51662-1477-1 ENALAPRILAT INJECTION 1.25mg/mL 1mL VIAL HF Acquisition Co LLC, DBA HealthFirst Mukilteo, WA 98275 Also supplied in the following manufacture supplied dosage forms Enalaprilat injection, USP, 1.25 mg per mL, is a clear, colorless solution and is supplied in vials containing 1 mL and 2 mL. NDC 0143-9787-10, 1 mL vials, Carton of 10. NDC 0143-9786-10, 2 mL vials, Carton of 10 Storage Store at 25°C (77 °F); excursions permitted to 15º to 30ºC (59º to 86°F) [see USP Controlled Room Temperature].

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ENALAPRILAT- ENALAPRILAT INJECTION
HF ACQUISITION CO LLC, DBA HEALTHFIRST
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ENALAPRILAT INJECTION 1.25MG/ML 1ML VIAL
BOXED WARNING
DESCRIPTION
Enalaprilat injection, USP is a sterile aqueous solution for
intravenous administration. Enalaprilat is an
angiotensin converting enzyme inhibitor. It is chemically described as
(S)-1-[N-(1-carboxy-3-phenylpropyl)-L-
alanyl]-L-proline dihydrate. Its empirical formula is
C18H24N2O5•2H2O and its structural formula is:
Enalaprilat is a white to off-white, crystalline powder with a
molecular weight of 384.42. It is sparingly soluble
in methanol and slightly soluble in water.
Each milliliter of enalaprilat injection, USP contains 1.25 mg
enalaprilat (anhydrous equivalent); sodium
chloride to adjust tonicity; sodium hydroxide to adjust pH; water for
injection, q.s.; with benzyl alcohol, 9 mg,
added as a preservative.
CLINICAL PHARMACOLOGY
Enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor when
administered intravenously, is the active
metabolite of the orally administered pro-drug, enalapril maleate.
Enalaprilat is poorly absorbed orally.
Mechanism of Action
Intravenous enalaprilat, or oral enalapril, after hydrolysis to
enalaprilat, inhibits ACE in human subjects and
animals. ACE is a peptidyl dipeptidase that catalyzes the conversion
of angiotensin I to the vasoconstrictor
substance, angiotensin II. Angiotensin II also stimulates aldosterone
secretion by the adrenal cortex. Inhibition
of ACE results in decreased plasma angiotensin II, which leads to
decreased vasopressor activity and to
decreased aldosterone secretion. Although the latter decrease is
small, it results in small increases of serum
potassium. In hypertensive patients treated with enalapril alone for
up to 48 weeks, mean increases in serum
potassium of approximately 0.2 mEq/L were observed. In patients
treated with enalapril plus a thiazide
diuretic, there was essentially no change in serum potassium. (See
PRECAUTIONS.) Removal of angiotensin II
negative feedback on renin secretion leads to i