ENALAPRIL MALEATE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

ENALAPRIL MALEATE (UNII: 9O25354EPJ) (ENALAPRILAT ANHYDROUS - UNII:Q508Q118JM)

Available from:

Unit Dose Services

INN (International Name):

ENALAPRIL MALEATE

Composition:

ENALAPRIL MALEATE 2.5 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Enalapril maleate is indicated for the treatment of hypertension. Enalapril maleate is effective alone or in combination with other antihypertensive agents, especially thiazide-type diuretics. The blood pressure lowering effects of enalapril maleate and thiazides are approximately additive. Enalapril maleate is indicated for the treatment of symptomatic congestive heart failure, usually in combination with diuretics and digitalis. In these patients enalapril maleate improves symptoms, increases survival, and decreases the frequency of hospitalization (see CLINICAL PHARMACOLOGY, for details and limitations of survival trials). In clinically stable asymptomatic patients with left ventricular dysfunction (ejection fraction ≤35 percent), enalapril maleate decreases the rate of development of overt heart failure and decreases the incidence of hospitalization for heart failure. (See CLINICAL PHARMACOLOGY, for details and limitations of survival trials.) In using enalapril maleate, consideration should be given to t

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ENALAPRIL MALEATE - ENALAPRIL MALEATE TABLET
UNIT DOSE SERVICES
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Product Information Rx only
ENALAPRIL MALEATE TABLETS, USP
When pregnancy is detected, enalapril maleate should be discontinued
as soon as possible. See
WARNINGS, 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.
_Fetal / Neonatal Morbidity and Mortality._
DESCRIPTION
Enalapril maleate is the maleate salt of enalapril, the ethyl ester of
a long-acting angiotensin converting
enzyme inhibitor, enalaprilat. Enalapril maleate is chemically
described as L-Proline,1-[N-[1-
(ethoxycarbonyl)-3-phenylpropyl]-L-alanyl]- , (S)-, (Z)-2-butenedioate
(1:1). Its molecular formula is, C
H N O ·C H O , and its structural formula is: Enalapril maleate is a
white to off-white, crystalline
powder with a molecular weight of 492.53. It is sparingly soluble in
water, soluble in ethanol, and
freely soluble in methanol. Enalapril is a pro-drug; following oral
administration, it is bioactivated by
hydrolysis of the ethyl ester to enalaprilat, which is the active
angiotensin converting enzyme inhibitor.
Enalapril maleate is supplied as 2.5 mg, 5 mg,10 mg and 20 mg tablets
for oral administration. In
addition, each tablet contains the following inactive ingredients:
hypromellose, anhydrous lactose, corn
starch, stearic acid and talc. The 10 mg and 20 mg tablets also
contain iron oxides.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
Enalapril, after hydrolysis to enalaprilat, inhibits
angiotensin-converting enzyme (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
202825444
adrenal cortex. The beneficial effects of enalapril in hypertension
and heart failure appear to result
primarily from suppression of the renin -angiotensin-aldosterone
system. Inhibition of ACE results in
decreased plasma angiotens