Difenoxin

Identification

Name
Difenoxin
Accession Number
DB01501
Type
Small Molecule
Groups
Approved, Illicit
Description

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.

Structure
Thumb
Synonyms
  • 1-(3-Cyano-3,3-diphenylpropyl)-4-phenylisonipecotic acid
  • Difenoxin
  • Difenoxina
  • Difenoxinum
  • Diphenoxilic acid
  • Diphenoxin
  • Diphenoxylic acid
External IDs
IDS-ND-007 / McN-JR 15403-11 / MCN-JR-15,403-11 / R 15,403 / R-15403
Product Ingredients
IngredientUNIICASInChI Key
Difenoxin hydrochlorideVQZ63K01IW35607-36-4VMIZTXDGZPTKIK-UHFFFAOYSA-N
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
MotofenDifenoxin hydrochloride (1 mg/1) + Atropine Sulfate (.025 mg/1)TabletOralSebela Pharmaceuticals Inc.2017-04-11Not applicableUs
International/Other Brands
Lyspafen (Janssen)
Categories
UNII
3ZZ5BJ9F2Q
CAS number
28782-42-5
Weight
Average: 424.5341
Monoisotopic: 424.21507815
Chemical Formula
C28H28N2O2
InChI Key
UFIVBRCCIRTJTN-UHFFFAOYSA-N
InChI
InChI=1S/C28H28N2O2/c29-22-28(24-12-6-2-7-13-24,25-14-8-3-9-15-25)18-21-30-19-16-27(17-20-30,26(31)32)23-10-4-1-5-11-23/h1-15H,16-21H2,(H,31,32)
IUPAC Name
1-(3-cyano-3,3-diphenylpropyl)-4-phenylpiperidine-4-carboxylic acid
SMILES
OC(=O)C1(CCN(CCC(C#N)(C2=CC=CC=C2)C2=CC=CC=C2)CC1)C1=CC=CC=C1

Pharmacology

Indication

Motofen(R) is a combination of atropine, an anticholinergic drug, and difenoxin, an antidiarrheal drug. It has been used in many countries for many years as a second line opioid-agonist antidiarrheal, which exists an intermediate between loperamide and paragoric. [2]

Diarrhea which is a result of cyclic or diarrhea predominant Inflammatory Bowel Syndrome may not be treated effectively with difenoxin, diphenoxylate, or loperamide. As such, diarrhea and cramping which does not respond to non-centrally acting derivatives or belladonna derivatives such as atropine are often treated with conservative doses of codeine. In patients with acute ulcerative colitis, as induction of toxic megacolon is possible, and thus use of Motofen(R) is cautioned.

Motofen(R) has been assigned pregnancy category C by the FDA, and is to be used only when the potential benefits outweigh the potential risk to the fetus. The safety of use during lactation is unknown and thus not recommended.

Associated Conditions
Pharmacodynamics

Difenoxin acts as a potent antidiarrheal by slowing the movement of the intestines. It also crosses the blood brain barrier to a slight degree to exert weak sedative and analgesic effects.

Adverse reactions thus include dizziness, drowsiness, lightheadedness and headache, in addition to gastrointestal side effects such as nausea, vomiting, dry mouth and epigastric distress. [Lexicomp, 2013]

Mechanism of action

Difenoxin acts as an antidiarrheal by activating peripheral opioid receptors in the small intestine and thereby inhibiting peristalsis. However, research has suggested that non-opioid receptor pathways exist. This would explain the potent antidiarrheal effects of difenoxin despite only limited opioid action [1].

Absorption

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

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

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

Route of elimination

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

Half life

The elimination half life was calculated to be 7.24 hours. The appearance half life was calculated to be 0.82h. [3]

Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
7-NitroindazoleThe risk or severity of adverse effects can be increased when Difenoxin is combined with 7-Nitroindazole.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Aceprometazine.Approved
AdipiplonThe risk or severity of adverse effects can be increased when Difenoxin is combined with Adipiplon.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Agomelatine.Approved, Investigational
AlaproclateThe risk or severity of adverse effects can be increased when Difenoxin is combined with Alaproclate.Experimental
AlfaxaloneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Difenoxin.Approved, Illicit
AllopregnanoloneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Allopregnanolone.Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Difenoxin is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Alphaprodine.Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Difenoxin.Approved, Illicit, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Difenoxin.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Difenoxin.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Difenoxin.Approved
AmperozideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Amperozide.Experimental
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Difenoxin.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Difenoxin.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Azaperone.Investigational, Vet Approved
AzelastineDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Difenoxin.Approved
BarbitalThe risk or severity of adverse effects can be increased when Difenoxin is combined with Barbital.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Difenoxin is combined with Benperidol.Approved, Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Benzocaine.Approved, Investigational
Benzyl alcoholThe risk or severity of adverse effects can be increased when Difenoxin is combined with Benzyl alcohol.Approved
BrexpiprazoleThe risk or severity of adverse effects can be increased when Difenoxin is combined with Brexpiprazole.Approved, Investigational
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.Approved
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Difenoxin.Approved, Illicit, Investigational
BromisovalThe risk or severity of adverse effects can be increased when Difenoxin is combined with Bromisoval.Experimental
BromperidolThe risk or severity of adverse effects can be increased when Difenoxin is combined with Bromperidol.Approved, Investigational
BrompheniramineThe risk or severity of adverse effects can be increased when Brompheniramine is combined with Difenoxin.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Brotizolam.Approved, Investigational, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Bupivacaine.Approved, Investigational
BuprenorphineDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Difenoxin.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Difenoxin.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Butalbital is combined with Difenoxin.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Difenoxin is combined with Butamben.Approved, Withdrawn
ButethalThe risk or severity of adverse effects can be increased when Difenoxin is combined with Butethal.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Difenoxin.Approved, Illicit, Vet Approved
CanertinibThe risk or severity of adverse effects can be increased when Difenoxin is combined with Canertinib.Investigational
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Difenoxin.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Carbinoxamine is combined with Difenoxin.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Difenoxin is combined with Carfentanil.Illicit, Investigational, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Carisoprodol is combined with Difenoxin.Approved
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with Difenoxin.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Difenoxin is combined with Chloral hydrate.Approved, Illicit, Investigational, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Difenoxin.Approved, Illicit, Investigational
ChlormezanoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Chlormezanone.Approved, Investigational, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Chloroprocaine.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Chlorphenamine is combined with Difenoxin.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Difenoxin.Approved, Investigational, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Chlorprothixene.Approved, Investigational, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Chlorzoxazone is combined with Difenoxin.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Cinchocaine.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Difenoxin is combined with Citalopram.Approved
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with Difenoxin.Approved, Investigational
ClidiniumThe risk or severity of adverse effects can be increased when Clidinium is combined with Difenoxin.Approved
ClobazamThe risk or severity of adverse effects can be increased when Clobazam is combined with Difenoxin.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when Difenoxin is combined with clomethiazole.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Difenoxin.Approved, Investigational, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Clonazepam is combined with Difenoxin.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Difenoxin.Approved
ClopenthixolThe risk or severity of adverse effects can be increased when Difenoxin is combined with Clopenthixol.Experimental
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Difenoxin.Approved, Illicit
ClothiapineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Clothiapine.Experimental
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Difenoxin.Approved
CocaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Cocaine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Difenoxin.Approved, Illicit
CyclizineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Difenoxin.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Difenoxin.Approved
CyclopropaneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Cyclopropane.Experimental
CyproheptadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Difenoxin.Approved
DantroleneThe risk or severity of adverse effects can be increased when Dantrolene is combined with Difenoxin.Approved, Investigational
DapiprazoleThe risk or severity of adverse effects can be increased when Difenoxin is combined with Dapiprazole.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Dapoxetine.Investigational
DeramciclaneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Difenoxin.Approved
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Difenoxin.Approved, Investigational
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Difenoxin.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Desvenlafaxine.Approved, Investigational
DetomidineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Detomidine.Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with Difenoxin.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Dexmedetomidine.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Dezocine.Approved, Investigational
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Difenoxin.Approved, Illicit, Investigational, Vet Approved
Diethyl etherThe risk or severity of adverse effects can be increased when Difenoxin is combined with Diethyl ether.Experimental
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Difenoxin.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Dihydromorphine.Experimental, Illicit
DimenhydrinateThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Difenoxin.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Difenoxin.Approved, Investigational
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Difenoxin.Approved, Illicit
DixyrazineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Dixyrazine.Experimental
DoramectinThe risk or severity of adverse effects can be increased when Difenoxin is combined with Doramectin.Vet Approved
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Difenoxin.Approved, Investigational
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Difenoxin is combined with DPDPE.Experimental
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.Approved, Illicit
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Difenoxin is combined with Drotebanol.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Dyclonine.Approved
EcgonineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ecgonine.Experimental, Illicit
EcopipamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Efavirenz is combined with Difenoxin.Approved, Investigational
EltanoloneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Eltanolone.Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Enflurane.Approved, Investigational, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Entacapone is combined with Difenoxin.Approved, Investigational
EscitalopramThe risk or severity of adverse effects can be increased when Difenoxin is combined with Escitalopram.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Difenoxin.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Difenoxin.Approved, Investigational
EthanolDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ethchlorvynol.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Ethosuximide is combined with Difenoxin.Approved
EthotoinThe risk or severity of adverse effects can be increased when Ethotoin is combined with Difenoxin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ethyl carbamate.Withdrawn
Ethyl chlorideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ethyl chloride.Approved, Experimental, Investigational
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ethyl loflazepate.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ethylmorphine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Etifoxine.Investigational, Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Difenoxin is combined with Etomidate.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Etoperidone.Withdrawn
EtorphineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Etorphine.Illicit, Vet Approved
EzogabineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ezogabine.Approved, Investigational
FelbamateThe risk or severity of adverse effects can be increased when Felbamate is combined with Difenoxin.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Difenoxin.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Fexofenadine is combined with Difenoxin.Approved, Investigational
FlibanserinThe risk or severity of adverse effects can be increased when Difenoxin is combined with Flibanserin.Approved, Investigational
FluanisoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Fluanisone.Experimental
FludiazepamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Fludiazepam.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Flunitrazepam.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Difenoxin.Approved, Investigational, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Difenoxin.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Difenoxin.Approved, Illicit, Investigational
FluspirileneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Fluspirilene.Approved, Investigational
Fluticasone propionateThe risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Difenoxin.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Fluvoxamine.Approved, Investigational
FosphenytoinThe risk or severity of adverse effects can be increased when Fosphenytoin is combined with Difenoxin.Approved, Investigational
FospropofolThe risk or severity of adverse effects can be increased when Difenoxin is combined with Fospropofol.Approved, Illicit, Investigational
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Difenoxin.Approved, Investigational
Gabapentin EnacarbilThe risk or severity of adverse effects can be increased when Difenoxin is combined with Gabapentin Enacarbil.Approved, Investigational
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Difenoxin.Approved, Illicit, Investigational
GepironeThe risk or severity of adverse effects can be increased when Difenoxin is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Glutethimide.Approved, Illicit
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Difenoxin.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Halazepam.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Difenoxin.Approved
HalothaneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Halothane.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Difenoxin is combined with Heroin.Approved, Illicit, Investigational
HexobarbitalThe risk or severity of adverse effects can be increased when Difenoxin is combined with Hexobarbital.Approved
HydrocodoneDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Difenoxin.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Iloperidone.Approved
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Difenoxin.Approved
IndalpineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Indalpine.Investigational, Withdrawn
IndiplonThe risk or severity of adverse effects can be increased when Difenoxin is combined with Indiplon.Investigational
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Difenoxin.Approved, Vet Approved
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Difenoxin.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ketazolam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ketobemidone.Approved, Investigational
LamotrigineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with Difenoxin.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Levetiracetam is combined with Difenoxin.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Levobupivacaine.Approved, Investigational
LevocabastineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Levocabastine.Approved, Investigational
LevocetirizineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Levodopa is combined with Difenoxin.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Difenoxin is combined with Levomethadyl Acetate.Approved, Investigational
LevomilnacipranThe risk or severity of adverse effects can be increased when Difenoxin is combined with Levomilnacipran.Approved, Investigational
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Difenoxin.Approved
LidocaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Lidocaine.Approved, Vet Approved
Lithium cationThe risk or severity of adverse effects can be increased when Difenoxin is combined with Lithium.Experimental
LofentanilThe risk or severity of adverse effects can be increased when Difenoxin is combined with Lofentanil.Illicit
LofexidineThe therapeutic efficacy of Difenoxin can be increased when used in combination with Lofexidine.Approved, Investigational
LoprazolamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Loprazolam.Experimental
LoratadineThe risk or severity of adverse effects can be increased when Loratadine is combined with Difenoxin.Approved, Investigational
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Difenoxin.Approved
LormetazepamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Lormetazepam.Approved
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Difenoxin.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Difenoxin.Approved, Investigational
Magnesium sulfateThe therapeutic efficacy of Difenoxin can be increased when used in combination with Magnesium sulfate.Approved, Investigational, Vet Approved
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Difenoxin.Approved, Investigational
MebicarThe risk or severity of adverse effects can be increased when Difenoxin is combined with Mebicar.Experimental
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with Difenoxin.Approved
MedazepamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Medazepam.Experimental
MedetomidineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Medetomidine.Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Difenoxin is combined with Melatonin.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Melperone.Approved, Investigational
MepivacaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Mepivacaine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Difenoxin.Approved, Illicit
MeptazinolThe risk or severity of adverse effects can be increased when Difenoxin is combined with Meptazinol.Experimental
MesoridazineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Mesoridazine.Approved, Investigational
MetaxaloneThe risk or severity of adverse effects can be increased when Metaxalone is combined with Difenoxin.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Difenoxin.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Difenoxin is combined with Methadyl Acetate.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Methaqualone.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Methocarbamol is combined with Difenoxin.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Difenoxin.Approved
MethotrimeprazineDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved, Investigational
MethoxyfluraneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Methoxyflurane.Approved, Investigational, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Methsuximide.Approved
MethylecgonineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Methylecgonine.Experimental
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Difenoxin is combined with Methylphenobarbital.Approved
MetyrosineDifenoxin may increase the sedative activities of Metyrosine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Difenoxin.Approved, Illicit
MilnacipranThe risk or severity of adverse effects can be increased when Difenoxin is combined with Milnacipran.Approved, Investigational
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.Approved, Investigational
MirtazapineDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MolindoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Molindone.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Difenoxin.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Difenoxin.Approved
NefazodoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Nefazodone.Approved, Withdrawn
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Difenoxin.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Difenoxin.Approved, Vet Approved
NordazepamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Nordazepam.Approved
NorfluraneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Norflurane.Approved, Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Normethadone.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Difenoxin.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Difenoxin.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Difenoxin.Approved
OndansetronThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ondansetron.Approved
OpiumThe risk or severity of adverse effects can be increased when Difenoxin is combined with Opium.Approved, Illicit
OrphenadrineDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Difenoxin is combined with Osanetant.Investigational
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Difenoxin.Approved
OxprenololThe risk or severity of adverse effects can be increased when Difenoxin is combined with Oxprenolol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Oxybuprocaine.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Difenoxin.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Difenoxin.Approved, Investigational, Vet Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Difenoxin.Approved
ParaldehydeDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved, Investigational
ParoxetineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Paroxetine.Approved, Investigational
PenfluridolThe risk or severity of adverse effects can be increased when Difenoxin is combined with Penfluridol.Experimental
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Difenoxin.Approved, Vet Approved
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Difenoxin.Approved, Investigational, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.Approved
PerazineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Perazine.Approved, Investigational
PerospironeThe risk or severity of adverse effects can be increased when Difenoxin is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Difenoxin.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Difenoxin.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Phenazocine.Experimental
PhenibutThe risk or severity of adverse effects can be increased when Difenoxin is combined with Phenibut.Experimental
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Difenoxin.Approved, Investigational
PhenoperidineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Phenoperidine.Experimental
PhenoxyethanolThe risk or severity of adverse effects can be increased when Difenoxin is combined with Phenoxyethanol.Approved
PhenytoinThe risk or severity of adverse effects can be increased when Phenytoin is combined with Difenoxin.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Difenoxin.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Pipamperone.Approved, Investigational
PipotiazineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Pipotiazine.Approved, Investigational
PiritramideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Piritramide.Approved, Investigational
PizotifenThe risk or severity of adverse effects can be increased when Difenoxin is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Pomalidomide.Approved
PramipexoleDifenoxin may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Pramocaine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Prazepam.Approved, Illicit
PregabalinThe therapeutic efficacy of Difenoxin can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Prilocaine.Approved
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with Difenoxin.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Procaine.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Difenoxin.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Difenoxin.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Difenoxin.Approved, Investigational
PropanididThe risk or severity of adverse effects can be increased when Difenoxin is combined with Propanidid.Experimental
ProparacaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Proparacaine.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Difenoxin.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Propoxycaine.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Difenoxin.Approved
ProxibarbalThe risk or severity of adverse effects can be increased when Difenoxin is combined with Proxibarbal.Experimental
PSD502The risk or severity of adverse effects can be increased when Difenoxin is combined with PSD502.Investigational
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Difenoxin.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Difenoxin.Approved
QuinisocaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Quinisocaine.Experimental
RacloprideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Ramelteon is combined with Difenoxin.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Difenoxin.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Remoxipride.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Difenoxin.Approved, Investigational
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Difenoxin.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ritanserin.Investigational
RomifidineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Romifidine.Vet Approved
RopiniroleDifenoxin may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ropivacaine.Approved
RotigotineDifenoxin may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Difenoxin.Approved
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Difenoxin.Approved, Investigational
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Difenoxin.Approved, Vet Approved
SepranoloneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Sepranolone.Investigational
SertindoleThe risk or severity of adverse effects can be increased when Difenoxin is combined with Sertindole.Approved, Investigational, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Difenoxin.Approved, Vet Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.Approved
StiripentolThe risk or severity of adverse effects can be increased when Difenoxin is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Difenoxin.Approved, Investigational
SulpirideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Sulpiride.Approved, Investigational
SultoprideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Sultopride.Experimental
SuvorexantDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved, Investigational
TandospironeThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tasimelteon.Approved, Investigational
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Difenoxin.Approved, Investigational
TetrabenazineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tetrabenazine.Approved, Investigational
TetracaineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tetracaine.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tetrahydropalmatine.Investigational
TetrodotoxinThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tetrodotoxin.Investigational
ThalidomideDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe risk or severity of adverse effects can be increased when Difenoxin is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Difenoxin is combined with Thiopental.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Difenoxin.Approved, Withdrawn
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Difenoxin.Approved
TiagabineThe risk or severity of adverse effects can be increased when Tiagabine is combined with Difenoxin.Approved, Investigational
TiaprideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tiapride.Approved, Investigational
TiletamineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tiletamine.Vet Approved
TilidineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tilidine.Experimental
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Difenoxin.Approved, Investigational
TolcaponeThe risk or severity of adverse effects can be increased when Tolcapone is combined with Difenoxin.Approved, Withdrawn
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with Difenoxin.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Difenoxin.Approved, Investigational
TranylcypromineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tranylcypromine.Approved, Investigational
TrazodoneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Trazodone.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Difenoxin.Approved, Investigational
Tricaine methanesulfonateThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tricaine methanesulfonate.Vet Approved
TrichloroethyleneThe risk or severity of adverse effects can be increased when Difenoxin is combined with Trichloroethylene.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Difenoxin.Approved, Investigational
TrifluperidolThe risk or severity of adverse effects can be increased when Difenoxin is combined with Trifluperidol.Experimental
TriflupromazineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Triflupromazine.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Difenoxin.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Triprolidine is combined with Difenoxin.Approved
Valproic AcidThe risk or severity of adverse effects can be increased when Difenoxin is combined with Valproic Acid.Approved, Investigational
VenlafaxineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Venlafaxine.Approved
VeraliprideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Veralipride.Experimental
VigabatrinThe risk or severity of adverse effects can be increased when Vigabatrin is combined with Difenoxin.Approved
Vinyl etherThe risk or severity of adverse effects can be increased when Difenoxin is combined with Vinyl ether.Experimental
VortioxetineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Vortioxetine.Approved, Investigational
XenonThe risk or severity of adverse effects can be increased when Difenoxin is combined with Xenon.Experimental
XylazineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Xylazine.Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Difenoxin.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Difenoxin is combined with Ziconotide.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Zimelidine.Withdrawn
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Difenoxin.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Difenoxin is combined with Zolazepam.Vet Approved
ZolpidemDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Zonisamide is combined with Difenoxin.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Difenoxin.Approved
ZotepineThe risk or severity of adverse effects can be increased when Difenoxin is combined with Zotepine.Approved, Investigational, Withdrawn
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Difenoxin.Approved, Investigational
Food Interactions
  • Ethanol use may increase CNS depression.

References

Synthesis Reference

Soudyn, W. and van Wijngaarden, I.; US. Patent 3,646,207; February 29,1972; assigned to Janssen Pharrnaceutica, N.V. (Belgium).

General References
  1. 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. [PubMed:8386327]
  2. 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. [PubMed:6675727]
  3. 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. [PubMed:3682841]
External Links
KEGG Drug
D03809
KEGG Compound
C07871
PubChem Compound
34328
PubChem Substance
46508854
ChemSpider
31620
ChEBI
4534
ChEMBL
CHEMBL1201321
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Difenoxin
ATC Codes
A07DA04 — Difenoxin

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Amarin Pharmaceuticals
  • Dispensing Solutions
  • Physicians Total Care Inc.
  • Valeant Ltd.
  • West-Ward Pharmaceuticals
Dosage forms
FormRouteStrength
TabletOral
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00208 mg/mLALOGPS
logP4.39ALOGPS
logP2.65ChemAxon
logS-5.3ALOGPS
pKa (Strongest Acidic)3.38ChemAxon
pKa (Strongest Basic)9.41ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area64.33 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity137.24 m3·mol-1ChemAxon
Polarizability47.56 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9182
Blood Brain Barrier+0.8984
Caco-2 permeable+0.507
P-glycoprotein substrateSubstrate0.6311
P-glycoprotein inhibitor INon-inhibitor0.7353
P-glycoprotein inhibitor IIInhibitor0.5519
Renal organic cation transporterInhibitor0.6229
CYP450 2C9 substrateNon-substrate0.8171
CYP450 2D6 substrateNon-substrate0.6612
CYP450 3A4 substrateNon-substrate0.6411
CYP450 1A2 substrateNon-inhibitor0.8832
CYP450 2C9 inhibitorNon-inhibitor0.8628
CYP450 2D6 inhibitorNon-inhibitor0.6599
CYP450 2C19 inhibitorNon-inhibitor0.8411
CYP450 3A4 inhibitorNon-inhibitor0.6724
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9199
Ames testNon AMES toxic0.8242
CarcinogenicityNon-carcinogens0.9211
BiodegradationNot ready biodegradable0.9849
Rat acute toxicity3.4236 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.827
hERG inhibition (predictor II)Non-inhibitor0.6311
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (7.02 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as diphenylacetonitriles. These are cyclic aromatic compounds containing a diphenylacetonitrile moiety, which consists of a diphenylmethane linked to and acetonitrile to form 2,2-diphenylacetonitrile.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylacetonitriles
Direct Parent
Diphenylacetonitriles
Alternative Parents
Diphenylmethanes / Phenylpiperidines / Piperidinecarboxylic acids / Aralkylamines / Trialkylamines / Amino acids / Nitriles / Monocarboxylic acids and derivatives / Carboxylic acids / Azacyclic compounds
show 4 more
Substituents
Diphenylacetonitrile / Diphenylmethane / Phenylpiperidine / Piperidinecarboxylic acid / Aralkylamine / Piperidine / Amino acid or derivatives / Amino acid / Tertiary aliphatic amine / Tertiary amine
show 17 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
tertiary amine, piperidinemonocarboxylic acid, nitrile (CHEBI:4534)

Drug created on July 31, 2007 07:10 / Updated on July 02, 2018 20:31