Diphenoxylate



Diphenoxylate
Systematic (IUPAC) name
ethyl 1-(3-cyano-3,3-diphenyl-propyl)- 4-phenyl-piperidine-4-carboxylate
Identifiers
CAS number 915-30-0
ATC code A07DA01
PubChem 13505
DrugBank APRD00366
Chemical data
O2 
Mol. mass 452.587 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 74-95%
Metabolism  ?
Half life 12-14 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status

Schedule II(US)

Routes  ?

Diphenoxylate is an Lomotil®).

This pharmaceutical strategy is designed to discourage abuse, because the anticholinergic effect of atropine will produce severe weakness and nausea if standard dosage is exceeded.

This medication is classified as a Schedule V under the Controlled Substances Act by the Food and Drug Administration (FDA) and the DEA in the United States when used in preparations. When diphenoxylate is used alone, it is classified as a Schedule II.

References

  • Merlo M, Brown CH, The effect of diphenoxylate hydrochloride on diarrhea, Am J Gastroenterol. 1960 Dec;34:625-30.
  • Kasic AM, Treatment of diarrhea in irritable colon, including preliminary observations with a new antidiarrheal agent, diphenoxylate hydrochloride (Lomotil), Am J Gastroenterol. 1961 Jan;35:46-9.
 
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