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ALIMENTARY TRACT AND METABOLISM › ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS › ANTIPROPULSIVES › Antipropulsives
diphenoxylate
A07DA01
Forms & Strengths
- Tablet: 2.5 mg diphenoxylate hydrochloride with 0.025 mg atropine sulfate
- Oral liquid: 2.5 mg diphenoxylate hydrochloride with 0.025 mg atropine sulfate per 5 mL
Adult Dosing
- Acute diarrhea: Initial 5 mg (two 2.5 mg tablets or 10 mL liquid) four times daily (max 20 mg/day)
- Maintenance: Reduce dosage as soon as initial control is achieved; titrate to minimum effective dose
Pediatric Dosing
- Children < 2 years: Contraindicated
- Children 2 to 12 years: 0.3 to 0.4 mg/kg/day divided in 4 doses (use liquid formulation only)
- Not recommended for chronic diarrhea in pediatric patients
Indications
- Adjunctive therapy in the management of acute diarrhea
Mechanism of Action
- Synthetic opioid analog structurally related to meperidine; acts on smooth muscle of the intestinal tract through opioid receptors to inhibit GI motility and peristalsis
- Combined with a subtherapeutic dose of atropine to discourage deliberate overdosage
Contraindications
- Hypersensitivity to diphenoxylate or atropine
- Diarrhea associated with organisms that penetrate the intestinal mucosa (e.g., toxigenic E. coli, Salmonella, Shigella) or pseudomembranous colitis
- Obstructive jaundice
- Children under 2 years of age due to risk of severe respiratory depression
Adverse Reactions
- Drowsiness, dizziness, headache, euphoria
- Dry mouth, nausea, vomiting, abdominal discomfort, paralytic ileus
- Tachycardia, blurring of vision, urinary retention (due to atropine component)
- Respiratory depression in high doses or pediatric patients
Drug Interactions
- Monoamine oxidase inhibitors (MAOIs): Risk of hypertensive crisis
- Central nervous system (CNS) depressants (alcohol, barbiturates, opioids, tranquilizers): Additive CNS depression
- Anticholinergic drugs: Potentiation of atropine-like side effects
Curated Content: Needs Vetting Before Put to Clinical Use