Identification

Name
Orphenadrine
Accession Number
DB01173  (APRD00097)
Type
Small Molecule
Groups
Approved
Description

A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. [PubChem]

Structure
Thumb
Synonyms
  • 2-(phenyl-o-tolylmethoxy)ethyldimethylamine
  • 2-methyldiphenhydramine
  • beta-Dimethylaminoethyl 2-methylbenzhydryl ether
  • Dimethyl-[2-(phenyl-O-tolyl-methoxy)-ethyl]-amine
  • N,N-Dimethyl-2-(alpha-2-tolylbenzoyloxy)ethylamine
  • N,N-Dimethyl-2-(phenyl(O-tolyl)methoxy)ethanamine
  • N,N-Dimethyl-2-[(O-methyl-alpha-phenylbenzyl)oxy]ethylamine
  • o-methyldiphenhydramine
  • o-monomethyldiphenhydramine
  • Orfenadrina
  • ORPHENADRINE
  • Orphenadrinum
  • Phenyl-O-tolylmethyl dimethyaminoethyl ether
  • β-dimethylaminoethyl 2-methylbenzhydryl ether
Product Ingredients
IngredientUNIICASInChI Key
Orphenadrine citrateX0A40N8I4S4682-36-4MMMNTDFSPSQXJP-UHFFFAOYNA-N
Orphenadrine hydrochlorideUBY910DUXH341-69-5UQZKYYIKWZOKKD-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Disipal Tab 50mgTablet50 mgOral3 M Pharmaceuticals, A Division Of 3 M Canada Company1957-12-312002-07-09Canada
NorflexLiquid30 mgIntramuscular; IntravenousValeant Canada Lp Valeant Canada S.E.C.1961-12-312014-07-30Canada
Orphenadrine Citrate Injection, USPLiquid30 mgIntramuscular; IntravenousSterimax Inc1996-12-02Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Orphenadrine CitrateTablet, extended release100 mg/1OralPreferreed Pharmaceuticals Inc.1998-06-19Not applicableUs
Orphenadrine CitrateTablet, extended release100 mg/1OralPd Rx Pharmaceuticals, Inc.1998-06-19Not applicableUs43386 0480 24 nlmimage10 ac085622
Orphenadrine CitrateInjection30 mg/mLIntramuscular; IntravenousWatson Pharmaceuticals2010-07-08Not applicableUs
Orphenadrine CitrateTablet100 mg/1OralMesource Pharmaceuticals2000-02-15Not applicableUs
Orphenadrine CitrateTablet, extended release100 mg/1OralNucare Pharmaceuticals, Inc.1998-06-19Not applicableUs
Orphenadrine CitrateTablet, extended release100 mg/1OralImpax Generics2000-06-23Not applicableUs
Orphenadrine CitrateTablet100 mg/1OralLake Erie Medical Dba Quality Care Produts Llc2000-02-15Not applicableUs
Orphenadrine CitrateInjection30 mg/mLIntramuscular; IntravenousAkorn2006-10-17Not applicableUs
Orphenadrine CitrateTablet, extended release100 mg/1OralPhysicians Total Care, Inc.2000-04-17Not applicableUs
Orphenadrine CitrateTablet, extended release100 mg/1OralRed Pharm Drug, Inc.1998-06-19Not applicableUs
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NorflexTablet, extended release100 mgOralValeant Canada Lp Valeant Canada S.E.C.1993-12-312014-07-30Canada
Orfenace Tablet 100mgTablet100 mgOralSterimax Inc1994-12-31Not applicableCanada
Sandoz OrphenadrineTablet, extended release100 mgOralSandoz Canada Incorporated2001-02-27Not applicableCanada
International/Other Brands
Antiflex / Banflex / Biorphen / Disipal / Flexoject / Mio-Rel / Myolin / OrfenAce / Orfro
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
NorgesicOrphenadrine citrate (25 mg/1) + Acetylsalicylic acid (385 mg/1) + Caffeine (30 mg/1)Tablet, multilayerOral3 M Pharmaceuticals1964-03-042015-12-31Us
Norgesic ForteOrphenadrine citrate (50 mg/1) + Acetylsalicylic acid (770 mg/1) + Caffeine (60 mg/1)Tablet, multilayerOral3 M Pharmaceuticals1964-03-042015-12-31Us
Norgesic Forte TabOrphenadrine citrate (50 mg) + Acetylsalicylic acid (770 mg) + Caffeine (60 mg)TabletOral3 M Pharmaceuticals, A Division Of 3 M Canada Company1976-12-312006-07-24Canada
Norgesic TabOrphenadrine citrate (25 mg) + Acetylsalicylic acid (385 mg) + Caffeine (30 mg)TabletOral3 M Pharmaceuticals, A Division Of 3 M Canada Company1964-12-312006-07-24Canada
Orphenadrine Citrate, Aspirin and CaffeineOrphenadrine citrate (50 mg/1) + Acetylsalicylic acid (770 mg/1) + Caffeine (60 mg/1)Tablet, multilayerOralRebel Distributors1996-12-31Not applicableUs
Categories
UNII
AL805O9OG9
CAS number
83-98-7
Weight
Average: 269.3813
Monoisotopic: 269.177964363
Chemical Formula
C18H23NO
InChI Key
QVYRGXJJSLMXQH-UHFFFAOYSA-N
InChI
InChI=1S/C18H23NO/c1-15-9-7-8-12-17(15)18(20-14-13-19(2)3)16-10-5-4-6-11-16/h4-12,18H,13-14H2,1-3H3
IUPAC Name
dimethyl({2-[(2-methylphenyl)(phenyl)methoxy]ethyl})amine
SMILES
CN(C)CCOC(C1=CC=CC=C1)C1=CC=CC=C1C

Pharmacology

Indication

Indicated for the treatment of Parkinson's disease.

Structured Indications
Pharmacodynamics

Orphenadrine is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculoskeletal conditions. Orphenadrine is an anticholinergic with a predominantly central effect and only a weak peripheral effect. In addition, it has mild antihistaminic and local anaesthetic properties. Parkinson's syndrome is the consequence of a disturbed balance between cholinergic and dopaminergic neurotransmission in the basal ganglia caused by a decrease in dopamine. Orphenadrine restores the physiological equilibrium and has a favourable effect on the rigidity and tremor of Parkinson's disease and Parkinsonian syndromes. The effect is somewhat less on bradykinesia.

Mechanism of action

Orphenadrine binds and inhibits both histamine H1 receptors and NMDA receptors. It restores the motor disturbances induced by neuroleptics, in particular the hyperkinesia. The dopamine deficiency in the striatum increases the stimulating effects of the cholinergic system. This stimulation is counteracted by the anticholinergic effect of orphenadrine. It may have a relaxing effect on skeletal muscle spasms and it has a mood elevating effect.

TargetActionsOrganism
AGlutamate receptor ionotropic, NMDA 2D
antagonist
Human
AGlutamate receptor ionotropic, NMDA 1
antagonist
Human
AGlutamate receptor ionotropic, NMDA 3B
antagonist
Human
AGlutamate receptor ionotropic, NMDA 3A
antagonist
Human
AHistamine H1 receptor
antagonist
Human
ASodium-dependent noradrenaline transporter
inhibitor
Human
USodium channel protein type 10 subunit alpha
inhibitor
Human
Absorption

Orphenadrine is almost completely absorbed in the gastrointestinal tract.

Volume of distribution
Not Available
Protein binding

95%

Metabolism

Biotransformation occurs mainly in the liver. Pharmacologically active metabolites are N-demethyl orphenadrine and N,N-didemethyl orphenadrine.

Route of elimination
Not Available
Half life

13-20 hours

Clearance
Not Available
Toxicity

Oral, mouse LD50 = 100 mg/kg; oral, rat LD50 = 255 mg/kg

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Orphenadrine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with 1,10-Phenanthroline.Experimental
7-Nitroindazole7-Nitroindazole may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
AcepromazineAcepromazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
AceprometazineAceprometazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
AclidiniumAclidinium may increase the anticholinergic activities of Orphenadrine.Approved
AdipiplonAdipiplon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
AgomelatineAgomelatine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
AlaproclateThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Alaproclate.Experimental
AlcuroniumThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Alcuronium.Experimental
AlfaxaloneAlfaxalone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Vet Approved
AlfentanilAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
AllopregnanoloneAllopregnanolone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
AlphacetylmethadolAlphacetylmethadol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental, Illicit
AlphaprodineAlphaprodine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Illicit
AlprazolamAlprazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit, Investigational
AmbenoniumThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Ambenonium.Approved
AmiodaroneThe metabolism of Orphenadrine can be decreased when combined with Amiodarone.Approved, Investigational
AmisulprideAmisulpride may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
AmitriptylineAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
AmobarbitalAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
AmoxapineAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
AmperozideAmperozide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Anisotropine Methylbromide.Approved
AprepitantThe serum concentration of Orphenadrine can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleAripiprazole may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
ArticaineArticaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
AsenapineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
AtazanavirThe metabolism of Orphenadrine can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Orphenadrine can be decreased when combined with Atomoxetine.Approved
AtracuriumThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Atracurium.Experimental
Atracurium besylateThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Atracurium besylate.Approved
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Orphenadrine.Approved, Vet Approved
AzaperoneAzaperone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Vet Approved
AzelastineAzelastine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
BaclofenBaclofen may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
BarbitalBarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Illicit
BenactyzineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Benactyzine.Withdrawn
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Orphenadrine.Approved
BenperidolBenperidol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Orphenadrine.Approved
BenzocaineBenzocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
Benzyl alcoholBenzyl alcohol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
BezitramideThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Bezitramide.Experimental, Illicit, Withdrawn
BiperidenThe risk or severity of adverse effects can be increased when Biperiden is combined with Orphenadrine.Approved
BoceprevirThe metabolism of Orphenadrine can be decreased when combined with Boceprevir.Withdrawn
BornaprineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Bornaprine.Experimental
BortezomibThe metabolism of Orphenadrine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Orphenadrine can be decreased when it is combined with Bosentan.Approved, Investigational
Botulinum Toxin Type AOrphenadrine may increase the anticholinergic activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BOrphenadrine may increase the anticholinergic activities of Botulinum Toxin Type B.Approved
BrexpiprazoleBrexpiprazole may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
BromazepamBromazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
BromisovalBromisoval may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
BromperidolBromperidol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
BrompheniramineBrompheniramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
BrotizolamBrotizolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Withdrawn
BupivacaineBupivacaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
BuspironeBuspirone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
ButabarbitalButabarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
ButacaineButacaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Vet Approved
ButalbitalButalbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
ButambenButamben may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ButethalButethal may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
ButorphanolButorphanol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit, Vet Approved
CanertinibCanertinib may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
CarbamazepineCarbamazepine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
CarbinoxamineCarbinoxamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
CarfentanilCarfentanil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Illicit, Vet Approved
CarisoprodolCarisoprodol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
CeritinibThe serum concentration of Orphenadrine can be increased when it is combined with Ceritinib.Approved
CetirizineCetirizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
Chloral hydrateChloral hydrate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit, Vet Approved
ChlordiazepoxideChlordiazepoxide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
ChlormezanoneChlormezanone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Withdrawn
ChloroprocaineChloroprocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Orphenadrine.Approved, Vet Approved
ChlorphenamineChlorphenamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Chlorphenoxamine.Withdrawn
ChlorpromazineChlorpromazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
ChlorprothixeneChlorprothixene may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Withdrawn
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Orphenadrine.Approved
ChlorzoxazoneChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
CimetropiumOrphenadrine may increase the anticholinergic activities of Cimetropium.Experimental
CinchocaineCinchocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Citalopram.Approved
ClarithromycinThe metabolism of Orphenadrine can be decreased when combined with Clarithromycin.Approved
ClemastineClemastine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ClidiniumClidinium may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ClobazamClobazam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
clomethiazoleclomethiazole may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
ClomipramineClomipramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
ClonazepamClonazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
ClonidineClonidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ClopenthixolClopenthixol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
ClorazepateClorazepate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
ClothiapineClothiapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
ClotrimazoleThe metabolism of Orphenadrine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineClozapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
CobicistatThe metabolism of Orphenadrine can be decreased when combined with Cobicistat.Approved
CocaineCocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
CodeineCodeine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
ConivaptanThe serum concentration of Orphenadrine can be increased when it is combined with Conivaptan.Approved, Investigational
CoumaphosThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Coumaphos.Vet Approved
CrizotinibThe metabolism of Orphenadrine can be decreased when combined with Crizotinib.Approved
CyclizineCyclizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
CyclobenzaprineCyclobenzaprine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
CyclopenthiazideThe serum concentration of Cyclopenthiazide can be increased when it is combined with Orphenadrine.Experimental
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Orphenadrine.Approved
CyclosporineThe metabolism of Orphenadrine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyproheptadineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
DabrafenibThe serum concentration of Orphenadrine can be decreased when it is combined with Dabrafenib.Approved
DantroleneDantrolene may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
DapiprazoleDapiprazole may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Dapoxetine.Investigational
DarifenacinThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Darifenacin.Approved, Investigational
DarunavirThe metabolism of Orphenadrine can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Orphenadrine can be increased when it is combined with Dasatinib.Approved, Investigational
DecamethoniumThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Decamethonium.Approved
DeferasiroxThe serum concentration of Orphenadrine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Orphenadrine can be decreased when combined with Delavirdine.Approved
DemecariumThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Demecarium.Approved
DeramciclaneDeramciclane may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
DesfluraneDesflurane may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
DesipramineDesipramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
DesloratadineDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Desvenlafaxine.Approved
DetomidineDetomidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Vet Approved
DexbrompheniramineDexbrompheniramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
DexetimideThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Dexetimide.Withdrawn
DexmedetomidineDexmedetomidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
DextromoramideDextromoramide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental, Illicit
DextropropoxypheneDextropropoxyphene may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit, Withdrawn
DezocineDezocine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
DiazepamDiazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit, Vet Approved
DichlorvosThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Dichlorvos.Vet Approved
DicyclomineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Dicyclomine.Approved
Diethyl etherDiethyl ether may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
DifenoxinDifenoxin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
DihydrocodeineDihydrocodeine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
DihydroergotamineThe metabolism of Orphenadrine can be decreased when combined with Dihydroergotamine.Approved
DihydroetorphineDihydroetorphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental, Illicit
DihydromorphineDihydromorphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental, Illicit
DiltiazemThe metabolism of Orphenadrine can be decreased when combined with Diltiazem.Approved
DimenhydrinateDimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
DiphenhydramineDiphenhydramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
DiphenoxylateDiphenoxylate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
DistigmineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Distigmine.Experimental
DixyrazineDixyrazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
DonepezilThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Donepezil.Approved
DoramectinDoramectin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Vet Approved
DoxepinDoxepin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
DoxycyclineThe metabolism of Orphenadrine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEDPDPE may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
DronedaroneThe metabolism of Orphenadrine can be decreased when combined with Dronedarone.Approved
DrotebanolDrotebanol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Duloxetine.Approved
DyclonineDyclonine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
EcgonineEcgonine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental, Illicit
EchothiophateThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Echothiophate.Approved
EcopipamEcopipam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
EdrophoniumThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Edrophonium.Approved
EfavirenzEfavirenz may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
EltanoloneEltanolone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
EluxadolineOrphenadrine may increase the constipating activities of Eluxadoline.Approved
EmeproniumThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Emepronium.Experimental
EnfluraneEnflurane may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
EntacaponeEntacapone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
EnzalutamideThe serum concentration of Orphenadrine can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Orphenadrine can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Escitalopram.Approved, Investigational
EstazolamEstazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
EszopicloneEszopiclone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
EtanautineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Etanautine.Experimental
EthanolEthanol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
EthchlorvynolEthchlorvynol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit, Withdrawn
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Orphenadrine.Approved
EthosuximideEthosuximide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
EthotoinEthotoin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
Ethyl carbamateEthyl carbamate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Withdrawn
Ethyl chlorideEthyl chloride may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
Ethyl loflazepateEthyl loflazepate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
EthylmorphineEthylmorphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
EtidocaineEtidocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
EtifoxineEtifoxine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Withdrawn
EtizolamEtizolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
EtomidateEtomidate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Etoperidone.Approved
EtorphineEtorphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Illicit, Vet Approved
EtybenzatropineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Etybenzatropine.Experimental
EzogabineEzogabine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
FelbamateFelbamate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
FencamfamineFencamfamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit, Withdrawn
FentanylFentanyl may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit, Investigational, Vet Approved
FenthionThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Fenthion.Vet Approved
FesoterodineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Fesoterodine.Approved
FexofenadineFexofenadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
FlibanserinFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
FluanisoneFluanisone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
FluconazoleThe metabolism of Orphenadrine can be decreased when combined with Fluconazole.Approved
FludiazepamFludiazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
FlunarizineFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
FlunitrazepamFlunitrazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Fluoxetine.Approved, Vet Approved
FlupentixolFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Withdrawn
FluphenazineFluphenazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
FlurazepamFlurazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
FluspirileneFluspirilene may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
Fluticasone propionateFluticasone propionate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
FluvoxamineFluvoxamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
FosamprenavirThe metabolism of Orphenadrine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Orphenadrine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
FospropofolFospropofol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
Fusidic AcidThe serum concentration of Orphenadrine can be increased when it is combined with Fusidic Acid.Approved
GabapentinGabapentin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
Gabapentin EnacarbilGabapentin Enacarbil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
GalantamineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Galantamine.Approved
GallamineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Gallamine.Experimental
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Gallamine Triethiodide.Approved
Gamma Hydroxybutyric AcidGamma Hydroxybutyric Acid may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
GepironeGepirone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
Ginkgo bilobaThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Ginkgo biloba.Approved, Nutraceutical
Glucagon recombinantThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Glucagon recombinant.Approved
GlutethimideGlutethimide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
GlycopyrroniumOrphenadrine may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
GuanfacineGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
HalazepamHalazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit, Withdrawn
HaloperidolHaloperidol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
HalothaneHalothane may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
HeroinHeroin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
HexamethoniumThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Hexamethonium.Experimental
HexobarbitalHexobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
HomatropineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Homatropine.Approved
Huperzine AThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Huperzine A.Investigational
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Orphenadrine.Approved, Vet Approved
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Orphenadrine.Approved
HydromorphoneHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
HyoscyamineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Hyoscyamine.Approved
IdelalisibThe serum concentration of Orphenadrine can be increased when it is combined with Idelalisib.Approved
IloperidoneIloperidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ImatinibThe metabolism of Orphenadrine can be decreased when combined with Imatinib.Approved
ImipramineImipramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Indalpine.Investigational, Withdrawn
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Orphenadrine.Approved
IndinavirThe metabolism of Orphenadrine can be decreased when combined with Indinavir.Approved
IndiplonIndiplon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
IpidacrineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Ipidacrine.Experimental
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Orphenadrine.Approved
IsavuconazoniumThe metabolism of Orphenadrine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsofluraneIsoflurane may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
IsoflurophateThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Isoflurophate.Approved, Withdrawn
IsradipineThe metabolism of Orphenadrine can be decreased when combined with Isradipine.Approved
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Orphenadrine.Investigational
ItraconazoleThe metabolism of Orphenadrine can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Orphenadrine can be increased when it is combined with Ivacaftor.Approved
KetamineKetamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
KetazolamKetazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
KetobemidoneKetobemidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
KetoconazoleThe metabolism of Orphenadrine can be decreased when combined with Ketoconazole.Approved, Investigational
LamotrigineLamotrigine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
LevetiracetamLevetiracetam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
LevobupivacaineLevobupivacaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
LevocabastineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
LevocetirizineLevocetirizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
LevodopaLevodopa may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
Levomethadyl AcetateLevomethadyl Acetate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Levomilnacipran.Approved
LevorphanolLevorphanol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
LidocaineLidocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
LithiumLithium may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
LofentanilLofentanil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Illicit
LopinavirThe metabolism of Orphenadrine can be decreased when combined with Lopinavir.Approved
LoprazolamLoprazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
LoratadineLoratadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
LorazepamLorazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
LormetazepamLormetazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
LovastatinThe metabolism of Orphenadrine can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineLoxapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
LuliconazoleThe serum concentration of Orphenadrine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Orphenadrine can be increased when combined with Lumacaftor.Approved
LurasidoneLurasidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
MalathionThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Malathion.Approved, Investigational
MaprotilineMaprotiline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
MazaticolThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Mazaticol.Experimental
MebicarMebicar may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
MecamylamineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Mecamylamine.Approved
MeclizineMeclizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
MedazepamMedazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
MedetomidineMedetomidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Vet Approved
MefloquineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Mefloquine.Approved
MelatoninMelatonin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Nutraceutical, Vet Approved
MelperoneMelperone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
MemantineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Memantine.Approved, Investigational
MepivacaineMepivacaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
MeprobamateMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
MeptazinolMeptazinol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
MesoridazineMesoridazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
MetaxaloneMetaxalone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
MethadoneMethadone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
Methadyl AcetateMethadyl Acetate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
Methanesulfonyl FluorideThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Methanesulfonyl Fluoride.Investigational
MethanthelineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Methantheline.Approved
MethapyrileneMethapyrilene may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Withdrawn
MethaqualoneMethaqualone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Illicit, Withdrawn
MethocarbamolMethocarbamol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
MethohexitalMethohexital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
MethoxyfluraneMethoxyflurane may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
MethsuximideMethsuximide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Orphenadrine.Approved
Methyl salicylateThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Methyl salicylate.Approved, Vet Approved
MethylecgonineMethylecgonine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
MethylphenobarbitalMethylphenobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
MetixeneThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Metixene.Approved
MetoclopramideThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Metoclopramide.Approved, Investigational
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Orphenadrine.Approved
MetyrosineOrphenadrine may increase the sedative activities of Metyrosine.Approved
MianserinMianserin may increase the anticholinergic activities of Orphenadrine.Approved
MidazolamMidazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
MifepristoneThe serum concentration of Orphenadrine can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Milnacipran.Approved
MinaprineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Minaprine.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
MirabegronThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Mirabegron.Approved
MitotaneThe serum concentration of Orphenadrine can be decreased when it is combined with Mitotane.Approved
MolindoneMolindone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
MorphineMorphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
NalbuphineNalbuphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
NefazodoneThe metabolism of Orphenadrine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Orphenadrine can be decreased when combined with Nelfinavir.Approved
NeostigmineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Orphenadrine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Orphenadrine can be increased when combined with Nevirapine.Approved
NicomorphineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Nicomorphine.Experimental
NilotinibThe metabolism of Orphenadrine can be decreased when combined with Nilotinib.Approved, Investigational
NitrazepamNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
Nitrous oxideNitrous oxide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
NorfluraneNorflurane may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
NormethadoneNormethadone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
NortriptylineNortriptyline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OlanzapineOlanzapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
OlaparibThe metabolism of Orphenadrine can be decreased when combined with Olaparib.Approved
OlopatadineOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OndansetronOndansetron may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OpiumOpium may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
OsanetantOsanetant may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
OsimertinibThe serum concentration of Orphenadrine can be increased when it is combined with Osimertinib.Approved
OtiloniumThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Otilonium.Experimental
OxazepamOxazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OxethazaineOxethazaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
OxitropiumThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Oxitropium.Investigational
OxprenololOxprenolol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OxybuprocaineOxybuprocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OxybutyninThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Oxybutynin.Approved, Investigational
OxycodoneOxycodone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit, Investigational
OxymorphoneOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Oxyphenonium.Approved
PalbociclibThe serum concentration of Orphenadrine can be increased when it is combined with Palbociclib.Approved
PaliperidonePaliperidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PancuroniumThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Pancuronium.Approved
ParaldehydeParaldehyde may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ParaoxonThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Paraoxon.Experimental
ParoxetineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Paroxetine.Approved, Investigational
PenfluridolPenfluridol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
PentazocinePentazocine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
PentobarbitalPentobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Pentolinium.Approved
PerazinePerazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
PerospironePerospirone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PerphenazinePerphenazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PethidinePethidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PhenazocinePhenazocine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
PhenglutarimideThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Phenglutarimide.Experimental
PhenibutPhenibut may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
PhenobarbitalPhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PhenoperidinePhenoperidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
PhenoxyethanolPhenoxyethanol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PhenytoinPhenytoin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
PhysostigmineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Physostigmine.Approved
PimozidePimozide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PipamperonePipamperone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PipecuroniumThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Pipecuronium.Approved
PipotiazinePipotiazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PirenzepineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Pirenzepine.Approved
PiritramidePiritramide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
PizotifenPizotifen may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Orphenadrine.Approved
PomalidomidePomalidomide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PosaconazoleThe metabolism of Orphenadrine can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
Potassium ChlorideOrphenadrine may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PramipexoleOrphenadrine may increase the sedative activities of Pramipexole.Approved, Investigational
PramlintidePramlintide may increase the anticholinergic activities of Orphenadrine.Approved, Investigational
PramocainePramocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PrazepamPrazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
PregabalinPregabalin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit, Investigational
PrilocainePrilocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PrimidonePrimidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
ProcaineProcaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational, Vet Approved
ProchlorperazineProchlorperazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Orphenadrine.Approved
PromazinePromazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
PromethazinePromethazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
PropanididPropanidid may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
PropanthelineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Propantheline.Approved
ProparacaineProparacaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
PropiverineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Propiverine.Investigational
PropofolPropofol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational, Vet Approved
PropoxycainePropoxycaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ProtriptylineProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ProxibarbalProxibarbal may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
PSD502PSD502 may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
PyridostigmineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Pyridostigmine.Approved
QuazepamQuazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit
QuetiapineQuetiapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Orphenadrine.Approved
QuinidineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Quinidine.Approved
QuinisocaineQuinisocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
RacloprideRaclopride may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
RamelteonRamelteon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
RamosetronOrphenadrine may increase the constipating activities of Ramosetron.Approved
RanolazineThe metabolism of Orphenadrine can be decreased when combined with Ranolazine.Approved, Investigational
RemifentanilRemifentanil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
RemoxiprideRemoxipride may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Withdrawn
ReserpineReserpine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
RifabutinThe metabolism of Orphenadrine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Orphenadrine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Orphenadrine can be increased when combined with Rifapentine.Approved
RisperidoneRisperidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
RitanserinRitanserin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
RitonavirThe metabolism of Orphenadrine can be decreased when combined with Ritonavir.Approved, Investigational
RivastigmineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Rivastigmine.Approved, Investigational
RomifidineRomifidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Vet Approved
RopiniroleOrphenadrine may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineRopivacaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
RotigotineOrphenadrine may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Orphenadrine.Approved
SaquinavirThe metabolism of Orphenadrine can be decreased when combined with Saquinavir.Approved, Investigational
ScopolamineScopolamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Scopolamine butylbromide.Approved, Vet Approved
SecobarbitalSecobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Orphenadrine.Approved, Investigational
SepranoloneSepranolone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
SertindoleSertindole may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Sertraline.Approved
SevofluraneSevoflurane may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
SildenafilThe metabolism of Orphenadrine can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Orphenadrine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Orphenadrine can be increased when it is combined with Simeprevir.Approved
SolifenacinThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Solifenacin.Approved
St. John's WortThe serum concentration of Orphenadrine can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Orphenadrine can be increased when it is combined with Stiripentol.Approved
SufentanilSufentanil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
SulfisoxazoleThe metabolism of Orphenadrine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideSulpiride may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
SultoprideSultopride may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
TacrineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Tacrine.Withdrawn
TandospironeTandospirone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
TasimelteonTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
TelaprevirThe metabolism of Orphenadrine can be decreased when combined with Telaprevir.Withdrawn
TelithromycinThe metabolism of Orphenadrine can be decreased when combined with Telithromycin.Approved
TemazepamTemazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
TetrabenazineTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
TetracaineTetracaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
TetrahydropalmatineTetrahydropalmatine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
TetrodotoxinTetrodotoxin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Investigational
ThalidomideThalidomide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational, Withdrawn
ThiamylalThiamylal may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
ThiopentalThiopental may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
ThioridazineThioridazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Withdrawn
ThiothixeneThiothixene may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
TiagabineTiagabine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
TiaprideTiapride may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
TiclopidineThe metabolism of Orphenadrine can be decreased when combined with Ticlopidine.Approved
TiletamineTiletamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Vet Approved
TilidineTilidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
TiotropiumOrphenadrine may increase the anticholinergic activities of Tiotropium.Approved
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Orphenadrine.Approved
TocilizumabThe serum concentration of Orphenadrine can be decreased when it is combined with Tocilizumab.Approved
TolcaponeTolcapone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Withdrawn
TolterodineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Tolterodine.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Topiramate.Approved
TramadolTramadol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
TranylcypromineTranylcypromine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
TrazodoneTrazodone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
TriazolamTriazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
Tricaine methanesulfonateTricaine methanesulfonate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Vet Approved
TrichlorfonThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Trichlorfon.Vet Approved
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Orphenadrine.Approved, Vet Approved
TrichloroethyleneTrichloroethylene may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
TrifluoperazineTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
TrifluperidolTrifluperidol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
TriflupromazineTriflupromazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Orphenadrine.Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Trimethaphan.Approved
TrimipramineTrimipramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
TriprolidineTriprolidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
TropatepineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Tropatepine.Experimental
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Orphenadrine.Approved
TrospiumThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Trospium.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Tubocurarine.Approved
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Orphenadrine.Approved
Valproic AcidValproic Acid may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
VecuroniumThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Vecuronium.Approved
VenlafaxineThe metabolism of Orphenadrine can be decreased when combined with Venlafaxine.Approved
VeraliprideVeralipride may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
VerapamilThe metabolism of Orphenadrine can be decreased when combined with Verapamil.Approved
VigabatrinVigabatrin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
Vinyl etherVinyl ether may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
VoriconazoleThe metabolism of Orphenadrine can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineVortioxetine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
XenonXenon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Experimental
XylazineXylazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Vet Approved
ZaleplonZaleplon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Illicit, Investigational
ZiconotideZiconotide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Zimelidine.Withdrawn
ZiprasidoneZiprasidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ZolazepamZolazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Vet Approved
ZonisamideZonisamide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
ZopicloneZopiclone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ZotepineZotepine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
ZuclopenthixolZuclopenthixol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved, Investigational
Food Interactions
  • Take without regard to meals. Avoid alcohol.

References

General References
  1. Ji D, Sui ZY, Ma YY, Luo F, Cui CL, Han JS: NMDA receptor in nucleus accumbens is implicated in morphine withdrawal in rats. Neurochem Res. 2004 Nov;29(11):2113-20. [PubMed:15662845]
External Links
Human Metabolome Database
HMDB15304
KEGG Compound
C07935
PubChem Compound
4601
PubChem Substance
46506085
ChemSpider
4440
BindingDB
50062614
ChEBI
7789
ChEMBL
CHEMBL900
Therapeutic Targets Database
DAP000858
PharmGKB
PA450715
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Orphenadrine
ATC Codes
M03BC51 — Orphenadrine, combinationsN04AB02 — Orphenadrine (chloride)M03BC01 — Orphenadrine (citrate)
AHFS Codes
  • 12:20.92 — Miscellaneous Skeletal Muscle Relaxants
FDA label
Download (247 KB)
MSDS
Download (73.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingTreatmentOsteoarthritis of the Hands1
3Not Yet RecruitingTreatmentMechanical Low Back Pain / Postural Low Back Pain1
3RecruitingTreatmentLiver Cirrhosis / Muscle Cramps1
4CompletedTreatmentUnilateral Knee Arthroplasty1
4RecruitingSupportive CareColon Diverticulosis / Colonic Neoplasms / Constipation Drug Induced / Diverticulitis, Colonic / Ileus / Ileus paralytic / Ileus; Mechanical / Malignant Neoplasm of Colon / Occasional Constipation / Postoperative pain / Rectum Cancer / Rectum Neoplasm1
4RecruitingTreatmentLow Back Pain (LBP)1
Not AvailableUnknown StatusTreatmentPain Relief1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
TabletOral50 mg
LiquidIntramuscular; Intravenous30 mg
TabletOral
TabletOral100 mg
InjectionIntramuscular; Intravenous30 mg/mL
Injection, solutionIntramuscular; Intravenous30 mg/mL
TabletOral100 mg/1
Tablet, extended releaseOral100 mg/1
Tablet, multilayerOral
Tablet, extended releaseOral100 mg
Prices
Unit descriptionCostUnit
Norflex 30 mg/ml ampul14.31USD ml
Orphenadrine 30 mg/ml ampule11.25USD ml
Orphenadrine Compound-DS 50-770-60 mg tablet2.94USD tablet
Orphenadrine comp forte tablet2.84USD tablet
Norflex er 100 mg tablet2.67USD tablet
Norflex 100 mg tablet sa2.64USD tablet
Orphenadrine Citrate CR 100 mg 12 Hour tablet2.26USD tablet
Orphenadrine er 100 mg tablet2.17USD tablet
Orphenadrine citrate powder1.6USD g
Orphenadrine comp tablet1.31USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)< 25 °CPhysProp
boiling point (°C)195 °C at 1.20E+01 mm HgPhysProp
water solubilitySparingly soluble in waterNot Available
logP3.77SANGSTER (1993)
pKa8.91SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.03 mg/mLALOGPS
logP3.5ALOGPS
logP4.17ChemAxon
logS-4ALOGPS
pKa (Strongest Basic)8.87ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area12.47 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity84.97 m3·mol-1ChemAxon
Polarizability31.83 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9881
Blood Brain Barrier+0.9134
Caco-2 permeable+0.8654
P-glycoprotein substrateSubstrate0.6196
P-glycoprotein inhibitor IInhibitor0.5825
P-glycoprotein inhibitor IINon-inhibitor0.6378
Renal organic cation transporterInhibitor0.7359
CYP450 2C9 substrateNon-substrate0.7658
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.6958
CYP450 1A2 substrateNon-inhibitor0.6363
CYP450 2C9 inhibitorNon-inhibitor0.9191
CYP450 2D6 inhibitorInhibitor0.8949
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9363
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5979
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.6341
BiodegradationNot ready biodegradable0.9422
Rat acute toxicity2.8405 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5224
hERG inhibition (predictor II)Inhibitor0.7052
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0a4i-9200000000-213fd17f1f5014e79c8b
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
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-001i-0900000000-e233c4258b887b1c4d95
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-001i-0900000000-6eb16a45ba9f222e4a96
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-001i-0900000000-46ad662bd87fac31bf96
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0900000000-1e90246098db8159dcdd
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0900000000-98528e097df59735a4a2
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0900000000-b09cb35d4c4d1563eab0
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0900000000-98fb2ac7e2a7b5389c76
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0900000000-f5b29d73b614d9a50c8c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-02t9-2900000000-5e46822ba471971d2ed4
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00lr-0900000000-02f47ad2686722a25761
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00lr-0900000000-c646cee3a03cb818670b

Taxonomy

Description
This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Benzylethers / Toluenes / Trialkylamines / Dialkyl ethers / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Diphenylmethane / Benzylether / Toluene / Tertiary aliphatic amine / Tertiary amine / Ether / Dialkyl ether / Organic nitrogen compound / Organic oxygen compound / Organopnictogen compound
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
tertiary amino compound, ether (CHEBI:7789)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Nmda glutamate receptor activity
Specific Function
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine.
Gene Name
GRIN2D
Uniprot ID
O15399
Uniprot Name
Glutamate receptor ionotropic, NMDA 2D
Molecular Weight
143750.685 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Kornhuber J, Parsons CG, Hartmann S, Retz W, Kamolz S, Thome J, Riederer P: Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect. 1995;102(3):237-46. [PubMed:8788072]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Voltage-gated cation channel activity
Specific Function
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. This protein plays a key role in synaptic p...
Gene Name
GRIN1
Uniprot ID
Q05586
Uniprot Name
Glutamate receptor ionotropic, NMDA 1
Molecular Weight
105371.945 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Kornhuber J, Parsons CG, Hartmann S, Retz W, Kamolz S, Thome J, Riederer P: Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect. 1995;102(3):237-46. [PubMed:8788072]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Nmda glutamate receptor activity
Specific Function
NMDA receptor subtype of glutamate-gated ion channels with reduced single-channel conductance, low calcium permeability and low voltage-dependent sensitivity to magnesium. Mediated by glycine.
Gene Name
GRIN3B
Uniprot ID
O60391
Uniprot Name
Glutamate receptor ionotropic, NMDA 3B
Molecular Weight
112990.98 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Kornhuber J, Parsons CG, Hartmann S, Retz W, Kamolz S, Thome J, Riederer P: Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect. 1995;102(3):237-46. [PubMed:8788072]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Protein phosphatase 2a binding
Specific Function
NMDA receptor subtype of glutamate-gated ion channels with reduced single-channel conductance, low calcium permeability and low voltage-dependent sensitivity to magnesium. Mediated by glycine. May ...
Gene Name
GRIN3A
Uniprot ID
Q8TCU5
Uniprot Name
Glutamate receptor ionotropic, NMDA 3A
Molecular Weight
125464.07 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Kornhuber J, Parsons CG, Hartmann S, Retz W, Kamolz S, Thome J, Riederer P: Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect. 1995;102(3):237-46. [PubMed:8788072]
Details
5. Histamine H1 receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Rumore MM, Schlichting DA: Analgesic effects of antihistaminics. Life Sci. 1985 Feb 4;36(5):403-16. [PubMed:2578597]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Norepinephrine:sodium symporter activity
Specific Function
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name
SLC6A2
Uniprot ID
P23975
Uniprot Name
Sodium-dependent noradrenaline transporter
Molecular Weight
69331.42 Da
References
  1. Pubill D, Canudas AM, Pallas M, Sureda FX, Escubedo E, Camins A, Camarasa J: Assessment of the adrenergic effects of orphenadrine in rat vas deferens. J Pharm Pharmacol. 1999 Mar;51(3):307-12. [PubMed:10344632]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Voltage-gated sodium channel activity
Specific Function
Tetrodotoxin-resistant channel that mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference acro...
Gene Name
SCN10A
Uniprot ID
Q9Y5Y9
Uniprot Name
Sodium channel protein type 10 subunit alpha
Molecular Weight
220623.605 Da
References
  1. Pubill D, Canudas AM, Pallas M, Sureda FX, Escubedo E, Camins A, Camarasa J: Assessment of the adrenergic effects of orphenadrine in rat vas deferens. J Pharm Pharmacol. 1999 Mar;51(3):307-12. [PubMed:10344632]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Peng FC, Lin Wu SW: Metabolism of territrem a in liver microsomes from male wistar rats: 3. Cytochrome p-450 isoforms catalyzing tra metabolism. J Toxicol Environ Health A. 2002 Dec 27;65(24):2163-75. [PubMed:12515593]
  2. Lin Wu SW, Jean WC, Peng FC, Edwards RJ: Cytochrome P-4503A1 catalyzes the formation of MA1 from territrem a in liver microsomes of 7-week-old female Wistar rats. J Toxicol Environ Health A. 2003 Mar 14;66(5):453-67. [PubMed:12712632]
  3. Chang TK, Weber GF, Crespi CL, Waxman DJ: Differential activation of cyclophosphamide and ifosphamide by cytochromes P-450 2B and 3A in human liver microsomes. Cancer Res. 1993 Dec 1;53(23):5629-37. [PubMed:8242617]
  4. Stresser DM, Dehal SS, Kupfer D: Ring hydroxylation of [o-3H]methoxychlor as a probe for liver microsomal CYP2B activity: potential for in vivo CYP2B assay. Anal Biochem. 1996 Jan 1;233(1):100-7. [PubMed:8789153]
  5. Murray M, Fiala-Beer E, Sutton D: Upregulation of cytochromes P450 2B in rat liver by orphenadrine. Br J Pharmacol. 2003 Jun;139(4):787-96. [PubMed:12813002]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Roos PH, Mahnke A: Metabolite complex formation of orphenadrine with cytochrome P450. Involvement of CYP2C11 and CYP3A isozymes. Biochem Pharmacol. 1996 Jul 12;52(1):73-84. [PubMed:8678911]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Sai Y, Dai R, Yang TJ, Krausz KW, Gonzalez FJ, Gelboin HV, Shou M: Assessment of specificity of eight chemical inhibitors using cDNA-expressed cytochromes P450. Xenobiotica. 2000 Apr;30(4):327-43. [PubMed:10821163]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da

Drug created on June 13, 2005 07:24 / Updated on October 23, 2017 14:13