DIPHENOXYLATE HCL 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:

Stat Rx USA

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 HCl 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 HCl 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

Product summary:

Diphenoxylate Hydrochloride and Atropine Sulfate Tablets USP are available as white, round tablets, debossed, 3966 containing 2.5 mg diphenoxylate hydrochloride USP and 0.025 mg atropine sulfate USP, packaged in bottles of 100, 1000 and unit-dose boxes of 100 tablets. PHARMACIST: Dispense in a well-closed, light-resistant container as defined in the USP. Use child-resistant closure. Store at controlled room temperature 15°-30°C (59°-86°F) (See USP). MANUFACTURED BY 0172 IVAX PHARMACEUTICALS, INC. 04/02 MIAMI, FL 33137 B9

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

DIPHENOXYLATE HCL AND ATROPINE SULFATE - DIPHENOXYLATE HCL AND
ATROPINE
SULFATE TABLET
STAT RX USA
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DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE (DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE
SULFATE) TABLET
DESCRIPTION
Each tablet, for oral administration, contains:
Diphenoxylate Hydrochloride USP . . . . . . . . . . . 2.5 mg
Atropine Sulfate USP . . . . . . . . . . . . . . . . . . . . . 0.025
mg
In addition, each tablet, contains the following inactive ingredients:
confectioner’s sugar, corn starch,
lactose monohydrate, magnesium stearate and sodium starch glycolate.
Diphenoxylate hydrochloride, an antidiarrheal, is ethyl
1-(3-cyano-3,3-diphenylpropyl)-4-
phenylisonipecotate monohydrochloride and has the following structural
formula:
C
H N O •HCl M.W. 489.06
Atropine sulfate, an anticholinergic, is Benzeneacetic
acid,-(hydroxymethyl)-8-methyl-8-azabicyclol
[3.2.1] oct-3-yl ester, _endo_-±, sulfate(2:1) (salt), monohydrate
and has the following structural formula:
C
H NO ) •H SO •H20 M.W. 694.85
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
30
32
2
2
17
23
3 2
2
4
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 a