Difenoxin

DB01501

small molecule approved illicit

Deskripsi

Difenoxin is a 4-phenylpiperidine which is closely related to the opioid analgesic meperidine. Difenoxin alone is a USA Schedule I controlled drug, as it may be habit forming. However, it is listed as a Schedule IV controlled drug if combined with atropine, which is added to decrease deliberate misuse. Motofen(R) is a brand mixture which combines atropine sulfate and difenoxin hydrochloride. It is approved by the FDA to treat acute and chronic diarrhea.

Difenoxin is an active metabolite of the anti-diarrheal drug, diphenoxylate, which is also used in combination with atropine in the brand mixture Lomotil(R). It works mostly in the periphery and activates opioid receptors in the intestine rather than the central nervous system (CNS). 3 Difenoxin is also closely related to loperamide, but unlike loperamide it is still capable of crossing the blood brain barrier to produce weak sedative and analgesic effects. However, the antidiarrheal potency of difenoxin is much greater than its CNS effects, which makes it an attractive alternative to other opioids.

Struktur Molekul 2D

Berat 424.5341
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half life was calculated to be 7.24 hours. The appearance half life was calculated to be 0.82h. [3]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

A high percentage of Motofen(R) is absorbed, and absorption occurs rapidly. Peak plasma concentrations are achieved within 40-60 minutes. Lexicomp, 2013

Metabolisme

Metabolism occurs by hydroxylation to form an inactive metabolite. Lexicomp, 2013

Rute Eliminasi

Both the drug and its metabolites are excreted, mainly as conjugates, in urine and feces. Lexicomp, 2012

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Alcohol can enhance the CNS depressant effects of this drug.

Interaksi Obat

662 Data
Buprenorphine Difenoxin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.
Hydrocodone Difenoxin may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.
Magnesium sulfate The therapeutic efficacy of Difenoxin can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Difenoxin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Difenoxin may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.
Mirtazapine Difenoxin may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.
Orphenadrine Difenoxin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Difenoxin may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.
Pramipexole Difenoxin may increase the sedative activities of Pramipexole.
Ropinirole Difenoxin may increase the sedative activities of Ropinirole.
Rotigotine Difenoxin may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Difenoxin.
Sodium oxybate Difenoxin may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Difenoxin may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.
Thalidomide Difenoxin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Difenoxin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Difenoxin.
Ethanol Difenoxin may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Difenoxin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.
Fluvoxamine The risk or severity of adverse effects can be increased when Difenoxin is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Difenoxin is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Difenoxin is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Difenoxin is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Difenoxin is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Difenoxin is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Difenoxin is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Difenoxin is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Difenoxin is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Difenoxin is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Difenoxin is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Difenoxin is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Difenoxin is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Difenoxin is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Difenoxin is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Difenoxin is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Difenoxin is combined with Alaproclate.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Difenoxin.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Difenoxin.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Difenoxin.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Difenoxin.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Difenoxin.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Difenoxin.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Difenoxin.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Difenoxin.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Difenoxin.
Pizotifen The risk or severity of CNS depression can be increased when Difenoxin is combined with Pizotifen.
Dosulepin The risk or severity of CNS depression can be increased when Difenoxin is combined with Dosulepin.
Zopiclone The risk or severity of adverse effects can be increased when Difenoxin is combined with Zopiclone.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Difenoxin.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Difenoxin.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Difenoxin.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Difenoxin.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Difenoxin.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Difenoxin.
Reserpine The risk or severity of CNS depression can be increased when Reserpine is combined with Difenoxin.
Eletriptan The risk or severity of CNS depression can be increased when Eletriptan is combined with Difenoxin.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Difenoxin.
Temazepam The risk or severity of CNS depression can be increased when Temazepam is combined with Difenoxin.
Reboxetine The risk or severity of CNS depression can be increased when Reboxetine is combined with Difenoxin.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Difenoxin.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Difenoxin.
Methysergide The risk or severity of CNS depression can be increased when Methysergide is combined with Difenoxin.
Cabergoline The risk or severity of CNS depression can be increased when Cabergoline is combined with Difenoxin.
Phenytoin The risk or severity of CNS depression can be increased when Phenytoin is combined with Difenoxin.
Topiramate The risk or severity of CNS depression can be increased when Topiramate is combined with Difenoxin.
Clemastine The risk or severity of CNS depression can be increased when Clemastine is combined with Difenoxin.
Venlafaxine The risk or severity of CNS depression can be increased when Venlafaxine is combined with Difenoxin.
Etomidate The risk or severity of CNS depression can be increased when Etomidate is combined with Difenoxin.
Morphine The risk or severity of CNS depression can be increased when Morphine is combined with Difenoxin.
Talbutal The risk or severity of CNS depression can be increased when Talbutal is combined with Difenoxin.
Pentobarbital The risk or severity of CNS depression can be increased when Pentobarbital is combined with Difenoxin.
Valproic acid The risk or severity of CNS depression can be increased when Valproic acid is combined with Difenoxin.
Zolmitriptan The risk or severity of CNS depression can be increased when Zolmitriptan is combined with Difenoxin.
Codeine The risk or severity of CNS depression can be increased when Codeine is combined with Difenoxin.
Dihydroergotamine The risk or severity of CNS depression can be increased when Dihydroergotamine is combined with Difenoxin.
Tolcapone The risk or severity of CNS depression can be increased when Tolcapone is combined with Difenoxin.
Hydromorphone The risk or severity of CNS depression can be increased when Hydromorphone is combined with Difenoxin.
Olanzapine The risk or severity of CNS depression can be increased when Olanzapine is combined with Difenoxin.
Cetirizine The risk or severity of CNS depression can be increased when Cetirizine is combined with Difenoxin.
Protriptyline The risk or severity of CNS depression can be increased when Protriptyline is combined with Difenoxin.
Trimethadione The risk or severity of CNS depression can be increased when Trimethadione is combined with Difenoxin.
Clobazam The risk or severity of sedation, somnolence, and CNS depression can be increased when Clobazam is combined with Difenoxin.
Chlorzoxazone The risk or severity of CNS depression can be increased when Chlorzoxazone is combined with Difenoxin.
Clozapine The risk or severity of CNS depression can be increased when Clozapine is combined with Difenoxin.
Meprobamate The risk or severity of CNS depression can be increased when Meprobamate is combined with Difenoxin.
Thiethylperazine The risk or severity of CNS depression can be increased when Thiethylperazine is combined with Difenoxin.
Palonosetron The risk or severity of CNS depression can be increased when Palonosetron is combined with Difenoxin.
Sulpiride The risk or severity of CNS depression can be increased when Sulpiride is combined with Difenoxin.
Alprazolam The risk or severity of CNS depression can be increased when Alprazolam is combined with Difenoxin.
Dexbrompheniramine The risk or severity of CNS depression can be increased when Dexbrompheniramine is combined with Difenoxin.

Target Protein

Mu-type opioid receptor OPRM1

Referensi & Sumber

Synthesis reference: Soudyn, W. and van Wijngaarden, I.; US. Patent 3,646,207; February 29,1972; assigned to Janssen Pharrnaceutica, N.V. (Belgium).
Artikel (PubMed)
  • PMID: 8386327
    De Luca A, Coupar IM: Difenoxin and loperamide: studies on possible mechanisms of intestinal antisecretory action. Naunyn Schmiedebergs Arch Pharmacol. 1993 Feb;347(2):231-7.
  • PMID: 6675727
    Innocenti P, Rossi L, Bombardieri G: Clinical effectiveness of difenoxine in patients with acute and chronic diarrhea. Boll Chim Farm. 1983 Dec;122(12):64S-68S.
  • PMID: 3682841
    Jackson LS, Stafford JE: The evaluation and application of a radioimmunoassay for the measurement of diphenoxylic acid, the major metabolite of diphenoxylate hydrochloride (Lomotil), in human plasma. J Pharmacol Methods. 1987 Nov;18(3):189-97.

Contoh Produk & Brand

Produk: 3 • International brands: 1
Produk
  • Motofen
    Tablet • - • Oral • US • Approved
  • Motofen
    Tablet • - • Oral • US • Approved
  • Motofen
    Tablet • - • Oral • US • Approved
International Brands
  • Lyspafen — Janssen

Sekuens Gen/Protein (FASTA)

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