Diphenoxylate
in LOMOTIL
Pronunciation: dye-fen-OX-i-layt
“Dippin’ (Dots) Lower motility”
Opioid that stays in the gut → slows motility
Paired with atropine to deter misuse
What it isMu agonist slowing gut transit, combined with subtherapeutic atropine; diarrhea.
Why this oneEffective antidiarrheal where loperamide has failed.
What limits itIt crosses into the CNS at higher doses, so unlike loperamide it can cause euphoria and dependence — the atropine is added to deter that. Avoid in invasive colitis and in young children.
FDA-approved for
- diarrhea (~1960)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Adjunctive management of diarrhea | ≥13 yr | 2 tablets QID | reduce after control; maintenance as low as 2 tablets QD | 20 mg/day diphenoxylate (8 tablets/day) |
Renal Undefined
Hepatic Undefined
Instructions
- Reduce dose to individual requirements after initial control of diarrhea
- Discontinue if no improvement of chronic diarrhea within 10 days at maximum dose
- Accompany with appropriate fluid and electrolyte therapy
Available strengths
- tab 0.025/2.5 mg
- sol 0.025/2.5 mg/5 mL
Contraindications
- Children <6 years (risk of respiratory and CNS depression)
- Diarrhea from pseudomembranous enterocolitis (C. difficile) or enterotoxin-producing bacteria
- Obstructive jaundice
Cautions
- Respiratory and/or CNS depression, especially in children
- Anticholinergic and opioid toxicity, including atropinism
- Dehydration and electrolyte imbalance
- GI complications in infectious diarrhea
- Toxic megacolon in acute ulcerative colitis
Adverse reactions
- Numbness of extremities, euphoria, sedation/drowsiness, dizziness, headache
- Anticholinergic: dry skin/mucous membranes, tachycardia, urinary retention, flushing, hyperthermia
- GI: nausea, vomiting, abdominal discomfort, anorexia
- Anaphylaxis, angioedema, urticaria, pruritus
Pregnancy No adequate studies; use only if benefit justifies risk; animal fertility and litter-size effects at high doses.
Lactation Undefined
Cost
| Strength | #/mo | generic $/mo | CostPlus | |
|---|---|---|---|---|
| 0.025/2.5 mg | tab | 120 QID | $16.66 | not offered |
⚠ BOXED WARNING
- Not for children under 6; overdose causes severe respiratory depression
Classes and tags
Clinical profile
Defining liabilityOpioid CNS depression, dependence and severe intestinal complications
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