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Pronunciation

diphenoxylate/atropine: dye-fen-OX-i-late/A-troe-peen

difenoxin/atropine : dye-fen-OX-in/A-troe-peen

Classifications

Therapeutic Classification: antidiarrheals

Pharmacologic Classification: anticholinergics

Indications

REMS


Action

  • Inhibits excess GI motility.
  • Structurally related to opioid analgesics but has no analgesic properties.
  • Atropine added to discourage abuse.
Therapeutic effects:
  • Decreased GI motility with subsequent decrease in diarrhea.

Pharmacokinetics

Absorption: Well absorbed from the GI tract.

Distribution: Enters breast milk.

Metabolism/Excretion: Diphenoxylate: mostly metabolized by the liver with some conversion to an active antidiarrheal compound (difenoxin). Difenoxin: metabolized by the liver. Minimal excretion in urine.

Half-Life: Diphenoxylate: 2.5 hr; difenoxin: 4.5 hr.

Time/Action Profile

(antidiarrheal action)

ROUTEONSETPEAKDURATION
Difenoxin–PO45–60 min2 hr3–4 hr
Diphenoxylate–PO45–60 min2 hr3–4 hr



Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: tachycardia

Derm: flushing

EENT: blurred vision, dry eyes

GI: constipation, dry mouth, epigastric distress, ileus, nausea, vomiting

GU: urinary retention

Neuro: dizziness, confusion, drowsiness, headache, insomnia, nervousness

Interactions

Drug-drug:

Drug-Natural Products:

Route/Dosage

Difenoxin/Atropine

Diphenoxylate/Atropine

Availability

Difenoxin/Atropine

Diphenoxylate/Atropine

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

diphenoxylate/atropine: Lomotil,

difenoxin/atropine : Motofen

Contr. Subst. Schedule

Schedule V (C-V)diphenoxylate/atropine
Schedule IV (C-IV)difenoxin/atropine

Code

NDC Code