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:

Par Pharmaceutical, 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: 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. 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-administration. A dose of 100 to 300 mg/day, which is equivalent to 40 to 120 tabl

Product summary:

Diphenoxylate Hydrochloride and Atropine Sulfate Tablets, USP 2.5 mg/0.025 mg are white, round, biconvex tablets, debossed ‘P’ over ‘771’ on one side and other side plain. NDC 49884-771-01 Bottles of 100 NDC 49884-771-10 Bottles of 1000 Store below 25°C (77°F). Dispense in a well-closed, light-resistant, child-resistant container. Manufactured by: PAR PHARMACEUTICAL, INC. Spring Valley, NY 10977 Revise 07/07 OS771-01-1-06

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE SULFATE TABLET
PAR PHARMACEUTICAL, INC.
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DESCRIPTION
Each diphenoxylate hydrochloride and atropine sulfate tablet for oral
use contains:
Diphenoxylate Hydrochloride
........................................... 2.5 mg
Atropine Sulfate.....................................................
0.025 mg
In addition, each tablet contains the following inactive ingredients:
colloidal silicon dioxide, lactose
monohydrate, microcrystalline cellulose, pregelatinized starch, and
stearic acid.
Diphenoxylate hydrochloride, an antidiarrheal, is ethyl
1-(3-cyano-3,3-diphenyl-propyl)-4-
phenylisonipecotate monohydrochloride and has the following structural
formula:
Molecular formula C
H N O •HCl
M.W. = 489.05
Atropine sulfate, an anticholinergic, is
1αH,5αH-Tropan-3-α-ol(±)-tropate (ester), sulfate (2:1) (salt)
monohydrate and has the following structural formula:
Molecular formula (C
H NO ) •H SO •H O M.W. = 694.83
A subtherapeutic amount of atropine sulfate is present to discourage
deliberate overdosage.
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
sixteen-subject cross-over 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 HCl and Atropine
Sulfate Oral Solution) and the peak plasma concentration, the area
under the plasma concentration