DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE tablet

Ország: Egyesült Államok

Nyelv: angol

Forrás: NLM (National Library of Medicine)

Aktív összetevők:

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

Beszerezhető a:

RPK Pharmaceuticals, Inc.

Az alkalmazás módja:

ORAL

Recept típusa:

PRESCRIPTION DRUG

Terápiás javallatok:

Diphenoxylate hydrochloride and atropine sulfate tablets are indicated as adjunctive therapy in the management of diarrhea in patients 13 years of age and older. Diphenoxylate hydrochloride and atropine sulfate tablets are contraindicated in: - Pediatric patients less than 6 years of age due to the risks of respiratory and central nervous system (CNS) depression (see WARNINGS ). - Patients with diarrhea associated with pseudomembranous enterocolitis (Clostridium difficile) or other enterotoxin-producing bacteria due to the risk of gastrointestinal (GI) complications, including sepsis (see WARNINGS ). - Patients with known hypersensitivity to diphenoxylate or atropine. - Patients with obstructive jaundice. Controlled Substance: Diphenoxylate hydrochloride and atropine sulfate tablets are classified as a Schedule V controlled substance by federal regulation. Diphenoxylate hydrochloride is chemically related to the narcotic analgesic meperidine. Drug Abuse and Dependence: In doses used for the treatment of dia

Termék összefoglaló:

Product: 53002-3401 NDC: 53002-3401-1 10 TABLET in a BOTTLE NDC: 53002-3401-2 20 TABLET in a BOTTLE NDC: 53002-3401-3 30 TABLET in a BOTTLE

Engedélyezési státusz:

Abbreviated New Drug Application

Termékjellemzők

DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE SULFATE TABLET
RPK PHARMACEUTICALS, INC.
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DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE TABLETS, FOR ORAL
USE, C-V
DESCRIPTION
Each diphenoxylate hydrochloride and atropine sulfate tablet, USP
contains:
2.5 mg of diphenoxylate hydrochloride, USP (equivalent to 2.3 mg of
diphenoxylate) and
0.025 mg of atropine sulfate, USP (equivalent to 0.01 mg of atropine)
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-(±)-alpha-(hydroxymethyl) benzeneacetic
acid 8-methyl-8- azabicylo[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 and atropine
sulfate tablets include
colloidal silicon dioxide, lactose monohydrate, microcrystalline
cellulose, pregelatinized
starch and stearic acid.
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 and atropine sulfate liquid) and
the peak plasma
concentration, the area u