ENALAPRILAT injection

Kraj: Stany Zjednoczone

Język: angielski

Źródło: NLM (National Library of Medicine)

Składnik aktywny:

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

Dostępny od:

Hikma Pharmaceuticals USA Inc.

INN (International Nazwa):

ENALAPRILAT

Skład:

ENALAPRILAT 1.25 mg in 1 mL

Droga podania:

INTRAVENOUS

Typ recepty:

PRESCRIPTION DRUG

Wskazania:

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.

Podsumowanie produktu:

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 Store at 25°C (77 °F); excursions permitted to 15º to 30ºC (59º to 86°F) [see USP Controlled Room Temperature].

Status autoryzacji:

Abbreviated New Drug Application

Charakterystyka produktu

ENALAPRILAT- ENALAPRILAT INJECTION
HIKMA PHARMACEUTICALS USA INC.
----------
ENALAPRILAT INJECTION, USP
RX ONLY
USE IN PREGNANCY
WHEN USED IN PREGNANCY DURING THE SECOND AND THIRD TRIMESTERS, ACE
INHIBITORS CAN CAUSE INJURY AND EVEN DEATH TO THE DEVELOPING FETUS.
When
pregnancy is detected, enalaprilat injection, USP should be
discontinued as soon as
possible. See WARNINGS, _FETAL/NEONATAL MORBIDITY AND MORTALITY_.
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
C
H
N O •2H O 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
18
24
2
5
2
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