DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Apotheca 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, USP 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. Diphenoxylate hydrochloride and atropine sulfate tablets are classified as a Schedule V controlled substance. 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 hydro

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: Bottles of 10 tablets NDC 12634-531-00 Bottles of 50 tablets NDC 12634-531-50 Blister Card of 14 NDC 12634-531-54 Blister Card of 15 NDC 12634-531-55 Blister Card of 30 NDC 12634-531-59 Bottles of 60 NDC 12634-531-60 Blister card of 10 NDC 12634-531-61 Bottles of 25 NDC 12634-531-79 Bottles of 20 NDC 12634-531-80 Bottles of 12 NDC 12634-531-82 Blister card of 1 NDC 12634-531-1 Bottles of 5 NDC 12634-531-95 Bottles of 7 NDC 12634-531-97 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. Manufactured by Mylan Pharmaceuticals Inc. Morgantown, WV 26505 U.S.A. REVISED SEPTEMBER 2015 DPXAS:R13

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE SULFATE TABLET
APOTHECA INC.
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DESCRIPTION
Each tablet for oral administration contains:
diphenoxylate hydrochloride, USP
(Warning – May be habit forming)
2.5 mg
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 (corn) 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
liquid was a