Страна: США
мова: англійська
Джерело: NLM (National Library of Medicine)
ENALAPRILAT DIHYDRATE (UNII: GV0O7ES0R3) (ENALAPRILAT ANHYDROUS - UNII:Q508Q118JM)
Hikma Pharmaceuticals USA Inc.
ENALAPRILAT
ENALAPRILAT 1.25 mg in 1 mL
INTRAVENOUS
PRESCRIPTION DRUG
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.
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].
Abbreviated New Drug Application
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 Прочитайте повний документ