II. Indications
III. Contraindications
- Clostridioides difficile
- Dysentery (toxigenic Diarrhea)
- Child under age 6 years
- Risk of respiratory depression (anoxic brain injury and death has occurred)
- Down Syndrome (risk of Atropine toxicity, even at low dose)
- Elderly (relative contraindication, risk of Atropine toxicity)
IV. Mechanism
- Diphenoxylate is typically combined with Atropine (Lomotil) for use as an antidiarrheal
- Diphenoxylate is a peripherally acting Opioid acting at gastrointestinal Opioid receptors
- Piperidine derivative similar in structure to Meperidine
- No significant central activity or Analgesic effect (retained in Gastrointestinal Tract due to insolubility)
V. Preparations
VI. Dosing: Acute Diarrhea
- Adult
- Take 2 tabs (or 10 ml) orally up to 4 times daily as needed
- Child
- Give 0.3 to 0.4 mg Diphenoxylate per kg per day in 4 divided doses
- Age 9 to 12 years (weight 23 to 55 kg): 3.5 to 5 ml orally 4 times daily
- Age 6 to 8 years (weight 17 to 32 kg): 2.5 to 5 ml orally 4 times daily
- Maximum 20 mg Diphenoxylate per day
- Give 0.3 to 0.4 mg Diphenoxylate per kg per day in 4 divided doses
VII. Safety
- Pregnancy Category C
- Safe in Lactation
VIII. Drug Interactions
-
CNS Depressants
- Diphenoxylate with Atropine may potentiate CNS Depressant effect
-
MAO Inhibitors
- Hypertension risk
-
Anticholinergic Medications
- Increased ileus risk
IX. Resources
- Diphenoxylate and Atropine, Lomotil (DailyMed)
X. References
- Hamilton (2020) Tarascon Pocket Pharmacopoeia
- Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 96
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Related Studies
diphenoxylate (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
DIPHENOXYLATE-ATROPINE 2.5-0.025 MG TABLET | Generic | $0.18 each |
Ontology: Diphenoxylate (C0012525)
Definition (NCI) | A piperidine derivate, chemically related to narcotic meperidine with antidiarrheal activity and devoid of central nervous system (CNS) activity. Diphenoxylate acts on opioid receptors in the gastrointestinal tract, thereby decreasing gastrointestinal motility and causing constipation or preventing diarrhea. |
Definition (MSH) | A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity. |
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | D004157 |
SnomedCT | 440585000, 317360000, 15052009 |
LNC | LP18090-8, MTHU003372 |
English | Diphenoxylate, 4-Piperidinecarboxylic acid, 1-(3-cyano-3,3-diphenylpropyl)-4-phenyl-, ethyl ester, Diphenoxylate (product), Diphenoxylate [Chemical/Ingredient], DIPHENOXYLATE, diphenoxylate, Diphenoxylate (substance), Diphenoxylate [dup] (substance) |
Swedish | Difenoxylat |
Czech | difenoxylát |
Finnish | Difenoksylaatti |
Russian | DIFENOKSILAT, ДИФЕНОКСИЛАТ |
Japanese | ジフェノキシラート |
Spanish | difenoxilato (producto), difenoxilato (sustancia), difenoxilato, Difenoxilato |
Polish | Difenoksylat |
French | Diphénoxylate |
German | Diphenoxylat |
Italian | Difenossilato |
Portuguese | Difenoxilato |
Ontology: Lomotil (C0065164)
Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
MSH | C002534 |
English | Lomotil, lomotil |