Diphenoxylate

Indications
 Oral
Acute diarrhoea
Adult: Initial dose: 10 mg, followed by 5 mg every 6 hr.
Child: >12 yr: 5 mg tid; 9-12 yr: 2.5 mg 4 times daily; 4-8 yr: 2.5 mg tid.
Oral
Chronic diarrhoea
Adult: Initial dose: 10 mg followed by 5 mg every 6 hr. Discontinue use if no clinical improvement is noted after 10 days of continuous usage at 20 mg/day. Max: 20 mg/day.
Contraindications
 Infants and children <4 yr. Jaundice, intestinal obstruction. Diarrhoea associated with pseudomembranous colitis or enterotoxin-producing bacteria.
Warnings / Precautions
 Hepatic dysfunction, inflammatory bowel disease. Pregnancy, lactation; young children.
Adverse Reactions
 GI effects; headache, drowsiness, dizziness, restlessness, euphoria, depression, numbness of the extremities; hypersensitivity reactions, swelling of the gums.
Overdose Reactions
 Symptoms: Atropinism may persist for 2-3 hr (e.g. high fever, generalised flushing, and tachypnoea). Drowsiness, miosis, hypotonia, loss of tendon reflexes, nystagmus, and seizures followed by respiratory depression and total apnoea may manifest 12-30 hr after drug ingestion. Treatment: empty stomach by emesis or by gastric lavage. Gastric lavage may be effective even after several hr due to decreased GI motility and pylorospasm. Treatment is supportive and symptomatic and monitor closely for 48 hr. Naloxone may be useful in the treatment of severe respiratory depression.
Drug Interactions
 Potentiates effects of other CNS depressants (alcohol, barbiturates) and some anxiolytics.
Potentially Fatal: Theoretical hypertensive crisis with MAOIs.
See Below for More diphenoxylate Drug Interactions
Mechanism of Actions
 Diphenoxylate is a synthetic derivative of pethidine with little or no analgesic activity. It reduces intestinal motility and excessive GI propulsion by acting on the smooth muscle of the intestinal tract.
Onset: 45 min to 1 hr.
Duration: 3-4 hr.
Absorption: Well absorbed from the GI tract.
Distribution: May distribute into breast milk.
Metabolism: Rapidly and extensively metabolised in the liver.
Excretion: Excreted mainly as metabolites and their conjugates in the faeces.
Administration
 May be taken with or without food.
ATC Classification
 A07DA01 - diphenoxylate ; Belongs to the class of antipropulsives. Used in the treatment of diarrhea.
Available As
  • Diphenoxylate 2.5 mg

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