ENALAPRILAT injection

Ország: Egyesült Államok

Nyelv: angol

Forrás: NLM (National Library of Medicine)

Aktív összetevők:

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

Beszerezhető a:

Cardinal Health

INN (nemzetközi neve):

ENALAPRILAT

Összetétel:

ENALAPRILAT ANHYDROUS 1.25 mg in 1 mL

Recept típusa:

PRESCRIPTION DRUG

Engedélyezési státusz:

Abbreviated New Drug Application

Termékjellemzők

ENALAPRILAT- ENALAPRILAT INJECTION
CARDINAL HEALTH
----------
ENALAPRILAT INJECTION
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
should be discontinued as soon as possible. See WARNINGS,
Fetal/Neonatal Morbidity and
Mortality .
DESCRIPTION
Enalaprilat injection is a sterile aqueous solution for intravenous
administration. Enalaprilat is an
angiotensin converting enzyme inhibitor. It is chemically described as
1-[_N_-[(_S_)-1-Carboxy-3-
phenylpropyl]-
-alanyl]-
-proline dihydrate. Its molecular formula is C
H N 0 •2H O and its
structural formula is:
Enalaprilat is a white to off-white, crystalline powder with a
molecular weight of 384.43. It is sparingly
soluble in methanol and slightly soluble in water.
Each milliliter of enalaprilat injection 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