DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE tablet

Ülke: ABD

Dil: İngilizce

Kaynak: NLM (National Library of Medicine)

Aktif bileşen:

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

Mevcut itibaren:

Greenstone LLC

INN (International Adı):

DIPHENOXYLATE HYDROCHLORIDE

Kompozisyon:

DIPHENOXYLATE HYDROCHLORIDE 2.5 mg

Uygulama yolu:

ORAL

Reçete türü:

PRESCRIPTION DRUG

Terapötik endikasyonlar:

Diphenoxylate hydrochloride and atropine sulfate is indicated as adjunctive therapy in the management of diarrhea in patients 13 years of age and older. Diphenoxylate hydrochloride and atropine sulfate is contraindicated in: Diphenoxylate hydrochloride and atropine sulfate 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 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 tablets

Ürün özeti:

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: 59762-1061-1 bottle of 100 59762-1061-2 bottle of 1000 Store below 25°C (77°F).

Yetkilendirme durumu:

New Drug Application Authorized Generic

Ürün özellikleri

DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE SULFATE TABLET
GREENSTONE LLC
----------
DIPHENOXYLATE HYDROCHLORIDE
AND ATROPINE SULFATE TABLETS, FOR ORAL USE C-V
DESCRIPTION
Each diphenoxylate hydrochloride and atropine sulfate tablet contains:
2.5 mg of diphenoxylate hydrochloride USP (equivalent to 2.3 mg of
diphenoxylate) and
0.025 mg of atropine sulfate USP (equivalent to 0.01 mg of atropine)
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 and atropine
sulfate 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 and atropine sulfate liquid) and
the peak plasma
concentration, the area under the plasma concentration-time curve, and
the amount of
diphenoxy