Overview
DESCRIPTION Each diphenoxylate hydrochloride and atropine sulfate tablet, USP 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...
Mechanism of Action
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.
Indications
- INDICATIONS AND USAGE Diphenoxylate hydrochloride and atropine sulfate tablets are indicated as adjunctive therapy in the management of diarrhea in patients 13 years of age and older.
Common Doses
- 20 mg
Dosage
DOSAGE AND ADMINISTRATION Management of Diarrhea in Patients 13 Years of Age and Older Diphenoxylate hydrochloride and atropine sulfate tablets are recommended as adjunctive therapy for the management of diarrhea in patients 13 years of age and older. Consider the nutritional status and degree of dehydration in patients prior to initiating therapy with diphenoxylate hydrochloride and atropine sulfate tablets. The use of diphenoxylate hydrochloride and atropine sulfate tablets should be accompanied by appropriate fluid and electrolyte therapy, when indicated.
Contraindications
- CONTRAINDICATIONS Diphenoxylate hydrochloride and atropine sulfate tablets are 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.
Side Effects
- ADVERSE REACTIONS The following serious adverse reactions are described elsewhere in labeling: Respiratory and/or CNS depression (see WARNINGS ) Anticholinergic and opioid-toxicities, including atroponism (see WARNINGS and PRECAUTIONS ) Dehydration and electrolyte imbalance (see WARNINGS ) GI Complications in patients with infectious diarrhea (see WARNINGS ) Toxic megacolon in patients with acute ulcerative colitis (see WARNINGS ) At therapeutic doses of diphenoxylate hydrochloride and atropine sulfate tablets, the following other adverse reactions have been reported; they are listed in...
Interactions
- Drug Interactions Alcohol Alcohol may increase the CNS depressant effects of diphenoxylate hydrochloride and atropine sulfate tablets and may cause drowsiness (see WARNINGS ). Avoid concomitant use of diphenoxylate hydrochloride and atropine sulfate tablets with alcohol. Other Drugs that Cause CNS Depression The concurrent use of diphenoxylate hydrochloride and atropine sulfate tablets with other drugs that cause CNS depression (e.g.