DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- diphenoxylate hydrochloride and atropine sulfate tablet

Land: USA

Sprog: engelsk

Kilde: NLM (National Library of Medicine)

Aktiv bestanddel:

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

Tilgængelig fra:

Lake Erie Medical DBA Quality Care Products LLC

INN (International Name):

DIPHENOXYLATE HYDROCHLORIDE

Sammensætning:

DIPHENOXYLATE HYDROCHLORIDE 2.5 mg

Indgivelsesvej:

ORAL

Recept type:

PRESCRIPTION DRUG

Terapeutiske indikationer:

Diphenoxylate hydrochloride is indicated as adjunctive therapy in the management of diarrhea in patients 13 years of age and older. Diphenoxylate hydrochloride is contraindicated in: - Pediatric patients less than 6 years of age due to the risks of respiratory and central nervous system (CNS) depression (see WARNINGS ). - Patients with diarrhea associated with pseudomembranous enterocolitis (Clostridium difficile ) or other enterotoxin-producing bacteria due to the risk of gastrointestinal (GI) complications, including sepsis (see WARNINGS ). - Patients with known hypersensitivity to diphenoxylate or atropine. - Patients with obstructive jaundice. Diphenoxylate hydrochloride is 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

Produkt oversigt:

Tablets — round, white, with SEARLE debossed on one side and 61 on the other side and containing 2.5 mg of diphenoxylate hydrochloride and 0.025 mg of atropine sulfate, supplied as: 55700-255-20 Store below 25°C (77°F).

Autorisation status:

New Drug Application Authorized Generic

Produktets egenskaber

DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE SULFATE TABLET
LAKE ERIE MEDICAL DBA QUALITY CARE PRODUCTS LLC
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DIPHENOXYLATE HYDROCHLORIDE
AND ATROPINE SULFATE TABLETS, USP CV
DESCRIPTION
Each diphenoxylate hydrochloride and atropine sulfate tablet contains:
diphenoxylate
hydrochloride
2.5 mg
atropine sulfate
0.025 mg
Diphenoxylate hydrochloride, an antidiarrheal, is ethyl
1-(3-cyano-3,3-diphenylpropyl)-4-
phenylisonipecotate monohydrochloride and has the following structural
formula:
Atropine sulfate, an anticholinergic, is endo-(±)-α-(hydroxymethyl)
benzeneacetic acid 8-methyl-8-
azabicyclo[3.2.1] oct-3-yl ester sulfate (2:1) (salt) monohydrate and
has the following structural
formula:
A subtherapeutic amount of atropine sulfate is present to discourage
deliberate overdosage.
Inactive ingredients of diphenoxylate hydrochloride tablets include
acacia, corn starch, magnesium
stearate, sorbitol, sucrose, and talc.
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
16-subject crossover 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 hydrochloride liquid)
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 o