ENALAPRIL MALEATE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

ENALAPRIL MALEATE (UNII: 9O25354EPJ) (ENALAPRIL - UNII:69PN84IO1A)

Available from:

Contract Pharmacy Services-PA

INN (International Name):

ENALAPRIL MALEATE

Composition:

ENALAPRIL 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 trial

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ENALAPRIL MALEATE- ENALAPRIL MALEATE TABLET
CONTRACT PHARMACY SERVICES-PA
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Product Information
ENALAPRIL MALEATE TABLETS, 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, enalapril maleate
should be discontinued as soon as possible. See WARNINGS, _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
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 angiote