DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE tablet

Država: Sjedinjene Američke Države

Jezik: engleski

Izvor: NLM (National Library of Medicine)

Aktivni sastojci:

DIPHENOXYLATE HYDROCHLORIDE (UNII: W24OD7YW48) (DIPHENOXYLATE - UNII:73312P173G), ATROPINE SULFATE (UNII: 03J5ZE7KA5) (ATROPINE - UNII:7C0697DR9I)

Dostupno od:

Aphena Pharma Solutions - Tennessee, LLC

INN (International ime):

DIPHENOXYLATE HYDROCHLORIDE

Sastav:

DIPHENOXYLATE HYDROCHLORIDE 2.5 mg

Administracija rute:

ORAL

Tip recepta:

PRESCRIPTION DRUG

Terapijske indikacije:

Diphenoxylate hydrochloride is effective as adjunctive therapy in the management of diarrhea. Diphenoxylate hydrochloride is contraindicated in patients with: - Known hypersensitivity to diphenoxylate or atropine. - Obstructive jaundice. - Diarrhea associated with pseudomembranous enterocolitis or enterotoxin-producing bacteria. Diphenoxylate hydrochloride is classified as a Schedule V controlled substance by federal regulation. Diphenoxylate hydrochloride is chemically related to the narcotic analgesic meperidine. In doses used for the treatment of diarrhea, whether acute or chronic, diphenoxylate has not produced addiction. Diphenoxylate hydrochloride is devoid of morphine-like subjective effects at therapeutic doses. At high doses it exhibits codeine-like subjective effects. The dose which produces antidiarrheal action is widely separated from the dose which causes central nervous system effects. The insolubility of diphenoxylate hydrochloride in commonly available aqueous media precludes intravenous self-

Proizvod sažetak:

Tablets — round, white, with SEARLE debossed on one side and 61 on the other side and containing 2.5 mg of diphenoxylate hydrochloride and 0.025 mg of atropine sulfate, supplied as:

Status autorizacije:

New Drug Application Authorized Generic

Svojstava lijeka

DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE SULFATE TABLET
APHENA PHARMA SOLUTIONS - TENNESSEE, LLC
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DIPHENOXYLATE HYDROCHLORIDE
AND ATROPINE SULFATE CV, TABLETS, USP
DESCRIPTION
Each diphenoxylate hydrochloride and atropine sulfate tablet contains:
diphenoxylate hydrochloride
2.5 mg
atropine sulfate
0.025 mg
Diphenoxylate hydrochloride, an antidiarrheal, is ethyl
1-(3-cyano-3,3-diphenylpropyl)-4-
phenylisonipecotate monohydrochloride and has the following structural
formula:
Atropine sulfate, an anticholinergic, is endo-(±)-α-(hydroxymethyl)
benzeneacetic acid 8-methyl-8-
azabicyclo[3.2.1] oct-3-yl ester sulfate (2:1) (salt) monohydrate and
has the following structural
formula:
A subtherapeutic amount of atropine sulfate is present to discourage
deliberate overdosage.
Inactive ingredients of diphenoxylate hydrochloride tablets include
acacia, corn starch, magnesium
stearate, sorbitol, sucrose, and talc.
CLINICAL PHARMACOLOGY
Diphenoxylate is rapidly and extensively metabolized in man by ester
hydrolysis to diphenoxylic acid
(difenoxine), which is biologically active and the major metabolite in
the blood. After a 5-mg oral dose
of carbon-14 labeled diphenoxylate hydrochloride in ethanolic solution
was given to three healthy
volunteers, an average of 14% of the drug plus its metabolites was
excreted in the urine and 49% in the
feces over a four-day period. Urinary excretion of the unmetabolized
drug constituted less than 1% of
the dose, and diphenoxylic acid plus its glucuronide conjugate
constituted about 6% of the dose. In a
16-subject crossover bioavailability study, a linear relationship in
the dose range of 2.5 to 10 mg was
found between the dose of diphenoxylate hydrochloride (given as
diphenoxylate hydrochloride liquid)
and the peak plasma concentration, the area under the plasma
concentration-time curve, and the amount of
diphenoxylic acid excreted in the urine. In the same study the
bioavailability of the tablet compared with
an equal dose of the