Yes

Antidiarrheal

Treatment of diarrhea

C-V

C

Hypersensitivity to diphenoxylate, atropine or any component; severe liver disease, jaundice, dehydrated patient, and narrow-angle glaucoma; it should not be used for children <2 years of age

High doses may cause physical and psychological dependence with prolonged use; use with caution in patients with ulcerative colitis, dehydration, and hepatic dysfunction; reduction of intestinal motility may be deleterious in diarrhea resulting from Shigella, Salmonella, toxigenic strains of E. coli, and from pseudomembranous enterocolitis associated with broad spectrum antibiotics; children may develop signs of atropinism (dryness of skin and mucous membranes, thirst, hyperthermia, tachycardia, urinary retention, flushing) even at the recommended dosages; if there is no response with 48 hours, the drug is unlikely to be effective and should be discontinued; if chronic diarrhea is not improved symptomatically within 10 days at maximum dosage of 20 mg/day, control is unlikely with further use.

1% to 10%:

Central nervous system: Nervousness, restlessness, dizziness, drowsiness, headache, mental depression

Gastrointestinal: Paralytic ileus, xerostomia

Genitourinary: Urinary retention and dysuria

Ocular: Blurred vision

Respiratory: Respiratory depression

<1%: Tachycardia, sedation, euphoria, hyperthermia, pruritus, urticaria, nausea, vomiting, abdominal discomfort, pancreatitis, stomach cramps, muscle cramps, weakness, diaphoresis (increased)

Symptoms of overdose include drowsiness, hypotension, blurred vision, flushing, dry mouth, miosis

Administration of activated charcoal will reduce bioavailability of diphenoxylate; naloxone 2 mg I.V. (0.01 mg/kg for children) with repeat administration as necessary up to a total of 10 mg; for anticholinergic overdose with severe life-threatening symptoms, physostigmine 1-2 mg (0.5 mg or 0.02 mg/kg for children) S.C. or I.V., slowly may be given to reverse these effects

Increased toxicity: MAO inhibitors (hypertensive crisis), CNS depressants, antimuscarinics (paralytic ileus); may prolong half-life of drugs metabolized in liver

Protect from light

Diphenoxylate inhibits excessive GI motility and GI propulsion; commercial preparations contain a subtherapeutic amount of atropine to discourage abuse

Onset of action: Within 45-60 minutes

Peak effect: Within 2 hours

Duration: 3-4 hours

Absorption: Oral: Well absorbed

Metabolism: Extensively in the liver to diphenoxylic acid (active)

Half-life: Diphenoxylate: 2.5 hours

Time to peak serum concentration: 2 hours

Elimination: Primarily in feces (via bile); ~14% excreted in urine; <1% excreted unchanged in urine

Oral:

<2 years: Not recommended

2-5 years: 2 mg of diphenoxylate 3 times/day

5-8 years: 2 mg of diphenoxylate 4 times/day

8-12 years: 2 mg of diphenoxylate 5 times/day

Adults: 15-20 mg/day of diphenoxylate in 3-4 divided doses; maintenance: 5-15 mg/day in 2-3 divided doses

Alcohol: Additive CNS effects, avoid use

Watch for signs of atropinism (dryness of skin and mucous membranes, tachycardia, thirst, flushing); monitor number and consistency of stools; observe for signs of toxicity, fluid and electrolyte loss, hypotension, and respiratory depression

May cause nervousness, restlessness, drowsiness, or insomnia; rarely may produce euphoria

Concurrent use with MAOIs may result in hypertensive crisis; additive sedation and dry mouth with psychotropics; use with benztropine or other anticholinergic agents may result in ileus

No information available to require special precautions

Up to 10% of patients will complain of significant dry mouth and drowsiness. This will disappear with cessation of drug therapy.

Take as directed; do not exceed recommended dosage. If no response within 48 hours, notify prescriber. Avoid alcohol or other prescriptive or OTC sedatives or depressants. You may experience drowsiness, blurred vision, impaired coordination; use caution when driving or engaging in tasks that require alertness until response to drug is known. Sucking on lozenges or chewing gum may reduce dry mouth. Report difficulty urinating, persistent diarrhea, respiratory difficulties, fever, or palpitations. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.

Raise bed rails, institute safety measures

Solution, oral: Diphenoxylate hydrochloride 2.5 mg and atropine sulfate 0.025 mg per 5 mL (4 mL, 10 mL, 60 mL)

Tablet: Diphenoxylate hydrochloride 2.5 mg and atropine sulfate 0.025 mg

Cutler EA, Barrett GA, Craven PW, et al, "Delayed Cardiopulmonary Arrest After Lomotil® Ingestion," Pediatrics, 1980, 65(1):157-8.

Ginsburg GM, "Lomotil® (Diphenoxylate and Atropine) Intoxication," Am J Dis Child, 1973, 125(2):241-2.

Karim A, Ranney RE, Evernsen KL, et al, "Pharmacokinetics and Metabolism of Diphenoxylate in Man," Clin Pharmacol Ther, 1972, 13(3):407-19.

McCarron MM, Challoner KR, and Thompson GA, "Diphenoxylate-Atropine (Lomotil®) Overdose in Children: An Update (Report of Eight Cases and Review of the Literature)," Pediatrics, 1991, 87(5):694-700.