DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE tablet
Country: United States
Language: English
Source: NLM (National Library of Medicine)
Summary of Product characteristics
(SPC)
17-02-2012
Send request.
Active ingredient:
DIPHENOXYLATE HYDROCHLORIDE (UNII: W24OD7YW48) (DIPHENOXYLATE - UNII:73312P173G), ATROPINE SULFATE (UNII: 03J5ZE7KA5) (ATROPINE - UNII:7C0697DR9I)
Available from:
Dispensing Solutions, Inc.
INN (International Name):
DIPHENOXYLATE HYDROCHLORIDE
Composition:
DIPHENOXYLATE HYDROCHLORIDE 2.5 mg
Administration route:
ORAL
Prescription type:
PRESCRIPTION DRUG
Therapeutic indications:
Diphenoxylate hydrochloride and atropine sulfate tablets are effective as adjunctive therapy in the management of diarrhea. Diphenoxylate hydrochloride and atropine sulfate tablets are contraindicated in patients with - Known hypersensitivity to diphenoxylate or atropine, - Obstructive jaundice, - Diarrhea associated with pseudomembranous enterocolitis or enterotoxin-producing bacteria.
Product summary:
Diphenoxylate Hydrochloride and Atropine Sulfate Tablets, USP are available containing 2.5 mg of diphenoxylate hydrochloride, USP (Warning: May be habit forming) and 0.025 mg of atropine sulfate, USP. The tablets are white round, unscored tablets debossed with M over 15 on one side of the tablet and blank on the other side. They are available as follows: NDC 66336-0437-15 bottles of 15 tablets NDC 66336-0437-20 bottles of 20 tablets Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Protect from light. Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure. Pharmacist: Dispense with a child-resistant closure only. Manufacture: Mylan Pharmaceuticals Inc. Morgantown, WV 26505 REVISED NOVEMBER 2009 DPXAS:R12
Authorization status:
Abbreviated New Drug Application
Summary of Product characteristics
DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE - DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE SULFATE TABLET
DISPENSING SOLUTIONS, INC.
----------
DESCRIPTION
Each tablet for oral administration contains:
diphenoxylate
hydrochloride, USP 2.5 mg
(Warning – May be habit forming)
atropine
sulfate, USP 0.025 mg
Diphenoxylate hydrochloride, an antidiarrheal, is ethyl 1-(3-cyano-3,
3-diphenylpropyl)-4-phenyl-
isonipecotate monohydrochloride and has the following structure:
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 structure:
A subtherapeutic amount of atropine sulfate is present to discourage
deliberate overdosage.
Each tablet for oral administration contains the following inactive
ingredients: colloidal silicon dioxide,
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 4-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 cross-over bioavailability study, a linear relationship in the
dose range of 2.5 mg to 10 mg was
found between the dose of diphenoxylate hydrochloride (given as
Diphenoxylate Hydrochloride and
Atropine Sulfate Oral Solution) 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
liqui
Read the complete document
