FOSINOPRIL SODIUM tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

FOSINOPRIL SODIUM (UNII: NW2RTH6T2N) (FOSINOPRILAT - UNII:S312EY6ZT8)

Available from:

Unit Dose Services

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Fosinopril sodium tablets are indicated for the treatment of hypertension. It may be used alone or in combination with thiazide diuretics. Fosinopril sodium tablets are indicated in the management of heart failure as adjunctive therapy when added to conventional therapy including diuretics with or without digitalis (see ). DOSAGE AND ADMINISTRATION In using fosinopril sodium, 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. Available data are insufficient to show that fosinopril sodium does not have a similar risk (see ). WARNINGS In considering use of fosinopril sodium, it should be noted that in controlled trials ACE inhibitors have an effect on blood pressure that is less in black patients than in non- blacks. In addition, ACE inhibitors (for which adequate data are available) cause a higher

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

FOSINOPRIL SODIUM - FOSINOPRIL SODIUM TABLET
UNIT DOSE SERVICES
----------
FOSINOPRIL SODIUM TABLETS 10 MG, 20 MG AND 40 MG RX ONLY
USE IN PREGNANCY
When pregnancy is detected, Fosinopril Sodium Tablet should be
discontinued as soon as possible.
WHEN USED IN PREGNANCY DURING THE SECOND AND THIRD TRIMESTERS, ACE
INHIBITORS CAN CAUSE INJURY
AND EVEN DEATH TO THE DEVELOPING FETUS.SEEWARNINGS:FETAL/NEONATAL
MORBIDITY AND MORTALITY.
DESCRIPTION
Fosinopril sodium tablet is the sodium salt of fosinopril, the ester
prodrug of an angiotensin coverting
enzyme (ACE) inhibitor, fosinoprilat. It contains a phosphinate group
capable of specific binding to the
active site of angiotensin converting enzyme.
Fosinopril sodium is designated chemically
as:L-proline,4-cyclohexyl-1-[[[2-methyl-1-(1-oxopro-
poxy)propoxy](4- phenylbutyl)phosphinyl]acetyl]-, sodium salt, trans-.
Fosinopril sodium is a white to
off-white crystalline powder. It is soluble in water (100 mg/mL),
methanol, and ethanol and slightly
soluble in hexane.
Its structural formula is:
Its empirical formula is C30H45NNaO7P, and its molecular weight is
585.65.
Fosinopril Sodium is available for oral administrations as 10 mg, 20
mg, and 40 mg tablets. Inactive
ingredients include: crospovidone, lactose, microcrystalline
cellulose, magnesium stearate, and
povidone.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
In animals and humans, fosinopril sodium is hydrolyzed by esterases to
the pharmacologically active
form, fosinoprilat, a specific competitive inhibitor of
angiotensin-converting enzyme (ACE).
ACE is a peptidyl dipeptidase that catalyzes the conversion of
angiotensin l 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. The latter decrease
may result in a small increase of
serum potassium.
In 647 hypertensive patients treated with fosinopril alone for