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:

Taro Pharmaceuticals U.S.A., Inc.

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, Heart Failure, Mortality Trials 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, Heart Failure, Mortality Trials for details and limitations of survival trials

Product summary:

Enalapril Maleate Tablets USP, 2.5 mg are yellow colored, round, biconvex tablets. One side scored and engraved with "T" above the score and "2" below. The other side plain. They are supplied as follows: Enalapril Maleate Tablets USP, 5 mg are yellow colored, round, biconvex tablets. One side scored and engraved with "T" above the score and "5" below. The other side plain. They are supplied as follows: Enalapril Maleate Tablets USP, 10 mg are white colored, round, biconvex tablets. One side scored and engraved with "T" above the score and with "10" under the score. The other side plain. They are supplied as follows: Enalapril Maleate Tablets USP, 20 mg are peach colored, round, biconvex, slightly speckled tablets. One side scored and engraved with "T" above the score and with "20" under the score. The other side plain. They are supplied as follows: Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Keep container tightly closed. Protect from moisture. Dispense in a tight container as per USP, if product package is subdivided.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ENALAPRIL MALEATE- ENALAPRIL MALEATE TABLET
TARO PHARMACEUTICALS U.S.A., INC.
----------
ENALAPRIL MALEATE TABLETS, USP
RX ONLY
WARNING: FETAL TOXICITY
_SEE FULL PRESCRIBING INFORMATION FOR COMPLETE BOXED WARNING._
WHEN PREGNANCY IS DETECTED, DISCONTINUE ENALAPRIL MALEATE AS SOON AS
POSSIBLE.
DRUGS THAT ACT DIRECTLY ON THE RENIN-ANGIOTENSIN SYSTEM CAN CAUSE
INJURY AND DEATH TO THE DEVELOPING FETUS. (SEE WARNINGS: FETAL
TOXICITY.)
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
(S)-1-[_N_-[1-(ethoxycarbonyl)-3-phenylpropyl]-L-alanyl]-L-proline,
_(Z)_-2-
butenedioate salt (1:1). Its empirical 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 to the active ingredient enalapril
maleate, each tablet contains
the following inactive ingredients: lactose monohydrate, magnesium
stearate,
pregelatinized starch and sodium bicarbonate.
The 2.5 mg, 5 mg and 20 mg tablets also contain iron oxide yellow, and
the 20 mg
tablets also contain iron oxide red.
20
28
2
5
4
4
4
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 adrenal cortex. The beneficial
effects of enalapril
in hypertension and heart failure appear