MOTOFEN- difenoxin and atropine sulfate tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

ATROPINE SULFATE (UNII: 03J5ZE7KA5) (ATROPINE - UNII:7C0697DR9I), DIFENOXIN HYDROCHLORIDE (UNII: VQZ63K01IW) (DIFENOXIN - UNII:3ZZ5BJ9F2Q)

Available from:

Sebela Pharmaceuticals Inc.

INN (International Name):

ATROPINE SULFATE

Composition:

ATROPINE SULFATE 0.025 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

MOTOFEN® is indicated as adjunctive therapy in the management of acute nonspecific diarrhea and acute exacerbations of chronic functional diarrhea. MOTOFEN® is contraindicated in patients with diarrhea associated with organisms that penetrate the intestinal mucosa (toxigenic E. coli, Salmonella species, Shigella ) and pseudomembranous colitis associated with broad spectrum antibiotics. Antiperistaltic agents should not be used in the conditions because they may prolong and/or worsen diarrhea. MOTOFEN® is contraindicated in children under 2 years of age because of the decreased margin of safety of drugs in this class in younger age groups. MOTOFEN® is contraindicated in patients with a known hypersensitivity to difenoxin, atropine, or any of the inactive ingredients, and in patients who are jaundiced. MOTOFEN® tablets are a Schedule IV controlled substance. Addiction to (dependence on) difenoxin hydrochloride is theoretically possible at high dosage. Therefore, the recommended dosage should not be e

Product summary:

MOTOFEN® is available as a white, dye-free, five-sided, scored tablet with “0200” on the scored side and "M" on the other side. Each tablet contains 1 mg difenoxin and 0.025 mg atropine sulfate. Supplied in bottles of 100 tablets (NDC 54766-200-10). Store at 20°-25°C (68°-77°F) [See USP Controlled Room Temperature].

Authorization status:

New Drug Application

Summary of Product characteristics

MOTOFEN- DIFENOXIN AND ATROPINE SULFATE TABLET
SEBELA PHARMACEUTICALS INC.
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MOTOFEN® (DIFENOXIN AND ATROPINE SULFATE TABLETS) CIV
RX ONLY
DESCRIPTION
Each five-sided dye free MOTOFEN® tablet contains: 1 mg of difenoxin
(equivalent to 1.09 mg of
difenoxin hydrochloride) and 0.025 mg of atropine sulfate (equivalent
to 0.01 mg of atropine).
Difenoxin hydrochloride,
1-(3-cyano-3,3-diphenylpropyl)-4-phenyl-4-piperidinecarboxylic acid
monohydrochloride, is an orally administered antidiarrheal agent which
is chemically related to the
narcotic meperidine.
The structural formula is:
Atropine sulfate is present to discourage deliberate overdose.
Atropine sulfate, an anticholinergic, is benzeneacetic acid,
α-(hydroxymethyl)-, 8-methyl-8-
azabicyclo[3.2.1]oct-3-yl ester, endo-(±)-, (2:1) (salt), monohydrate
and has the following structural
formula:
Inactive Ingredients: calcium stearate, cellulose, lactose, corn
starch.
CLINICAL PHARMACOLOGY
Animal studies have shown that difenoxin hydrochloride manifests its
antidiarrheal effect by slowing
intestinal motility. The mechanism of action is by a local effect on
the gastrointestinal wall.
Difenoxin is the principal active metabolite of diphenoxylate.
Following oral administration of MOTOFEN®, difenoxin is rapidly and
extensively absorbed. Mean
peak plasma levels of approximately 160 ng/mL occurred within 40 to 60
minutes in most patients
following an oral dose of 2 mg. Plasma levels decline to less than 10%
of their peak values within 24
hours and to less than 1% of their peak values within 72 hours. This
decline parallels the appearance of
difenoxin and its metabolites in the urine. Difenoxin is metabolized
to an inactive hydroxylated
metabolite. Both the drug and its metabolites are excreted, mainly as
conjugates, in urine and feces.
INDICATIONS AND USAGE
MOTOFEN® is indicated as adjunctive therapy in the management of
acute nonspecific diarrhea and
acute exacerbations of chronic functional diarrhea.
CONTRAINDICATIONS
MOTOFEN® is contraindicated in patients wi