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Identification
NameOrphenadrine
Accession NumberDB01173  (APRD00097)
TypeSmall Molecule
GroupsApproved
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
External Identifiers Not Available
Approved 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
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Orphenadrine Citratetablet, extended release100 mg/1oralPreferred Pharmaceuticals, Inc.1998-06-19Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralGAVIS Pharmaceuticals, LLC1998-06-19Not applicableUs
Orphenadrine Citratetablet100 mg/1oralPreferred Pharmaceuticals, Inc.2000-02-15Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-02-07Not applicableUs
Orphenadrine Citratetablet100 mg/1oralEon Labs, Inc.2000-02-15Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralClinical Solutions Wholesale1998-06-19Not applicableUs
Orphenadrine Citrateinjection, solution30 mg/mLintramuscular; intravenousSagent Pharmaceuticals2011-10-01Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralPd Rx Pharmaceuticals, Inc.1998-06-19Not applicableUs
Orphenadrine Citratetablet100 mg/1oralCarilion Materials Management2000-02-15Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralPd Rx Pharmaceuticals, Inc.1998-06-19Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralRebel Distributors Corp1998-06-19Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralSTAT Rx USA LLC2000-06-23Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralAmerican Health Packaging2014-09-15Not applicableUs
Orphenadrine Citrateinjection30 mg/mLintramuscular; intravenousAkorn, Inc.2006-10-17Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralPhysicians Total Care, Inc.2000-04-17Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralAv Kare, Inc.2015-11-022016-03-18Us
Orphenadrine Citratetablet, extended release100 mg/1oralDispensing Solutions, Inc.1998-06-19Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralSTAT Rx USA LLC2000-06-23Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralA S Medication Solutions Llc1998-06-19Not applicableUs
Orphenadrine Citratetablet100 mg/1oralLake Erie Medical DBA Quality Care Products LLC2000-02-15Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralbryant ranch prepack1998-06-19Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralBlenheim Pharmacal, Inc.2011-08-10Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralImpax Generics2000-06-23Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralH.J. Harkins Company, Inc.2000-06-23Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralProficient Rx LP1998-06-19Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralRx Change Co.2014-11-15Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralPreferred Pharmaceuticals, Inc1998-06-19Not applicableUs
Orphenadrine Citratetablet100 mg/1oralMedsource Pharmaceuticals2000-02-15Not applicableUs
Orphenadrine Citratetablet100 mg/1oralProficient Rx LP2000-02-15Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralUnit Dose Services1998-06-19Not applicableUs
Orphenadrine Citrateinjection30 mg/mLintramuscular; intravenousWatson Laboratories, Inc.2010-07-08Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralDIRECT RX2014-01-01Not applicableUs
Orphenadrine Citratetablet, extended release100 mg/1oralAidarex Pharmaceuticals LLC1998-06-19Not applicableUs
Approved Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Norflextablet (extended-release)100 mgoralValeant Canada Lp Valeant Canada S.E.C.1993-12-312014-07-30Canada
Orfenace Tablet 100mgtablet100 mgoralSterimax Inc1994-12-31Not applicableCanada
Sandoz Orphenadrinetablet (extended-release)100 mgoralSandoz Canada Incorporated2001-02-27Not applicableCanada
Unapproved/Other Products Not Available
International Brands
NameCompany
AntiflexNot Available
BanflexNot Available
BiorphenNot Available
DisipalNot Available
FlexojectNot Available
Mio-RelNot Available
MyolinNot Available
OrfenAceNot Available
OrfroNot Available
Brand mixtures
NameLabellerIngredients
Norgesic3 M Pharmaceuticals
Norgesic Forte3 M Pharmaceuticals
Norgesic Forte Tab3 M Pharmaceuticals, A Division Of 3 M Canada Company
Norgesic Tab3 M Pharmaceuticals, A Division Of 3 M Canada Company
Orphenadrine Citrate, Aspirin and CaffeineRebel Distributors Corp
Salts
Name/CASStructureProperties
Orphenadrine citrate
4682-36-4
Thumb
  • InChI Key: MMMNTDFSPSQXJP-UHFFFAOYNA-N
  • Monoisotopic Mass: 461.204966973
  • Average Mass: 461.5048
DBSALT000400
Orphenadrine hydrochloride
ThumbNot applicableDBSALT001021
Categories
UNIIAL805O9OG9
CAS number83-98-7
WeightAverage: 269.3813
Monoisotopic: 269.177964363
Chemical FormulaC18H23NO
InChI KeyInChIKey=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
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassDiphenylmethanes
Direct ParentDiphenylmethanes
Alternative Parents
Substituents
  • Diphenylmethane
  • Benzylether
  • Toluene
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ether
  • Dialkyl ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationIndicated for the treatment of Parkinson's disease.
PharmacodynamicsOrphenadrine 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 actionOrphenadrine 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.
Related Articles
AbsorptionOrphenadrine is almost completely absorbed in the gastrointestinal tract.
Volume of distributionNot Available
Protein binding95%
Metabolism

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

SubstrateEnzymesProduct
Orphenadrine
Not Available
N-demethyl orphenadrineDetails
Orphenadrine
Not Available
N,N-didemethyl orphenadrineDetails
Route of eliminationNot Available
Half life13-20 hours
ClearanceNot Available
ToxicityOral, mouse LD50 = 100 mg/kg; oral, rat LD50 = 255 mg/kg
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot 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-release)oral100 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.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point< 25 °CPhysProp
boiling point195 °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 RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
MSMass Spectrum (Electron Ionization)splash10-0a4i-9200000000-213fd17f1f5014e79c8bView in MoNA
References
Synthesis ReferenceNot Available
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
ATC CodesM03BC51N04AB02M03BC01
AHFS Codes
  • 12:20.00
PDB EntriesNot Available
FDA labelDownload (247 KB)
MSDSDownload (73.6 KB)
Interactions
Drug Interactions
Drug
AclidiniumAclidinium may increase the anticholinergic activities of Orphenadrine.
AlfentanilAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
AlprazolamAlprazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
AmitriptylineAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
AmobarbitalAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
AmoxapineAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
AripiprazoleAripiprazole may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
AsenapineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
AzelastineAzelastine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
BaclofenBaclofen may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Botulinum Toxin Type AOrphenadrine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BOrphenadrine may increase the anticholinergic activities of Botulinum Toxin Type B.
BrexpiprazoleBrexpiprazole may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
BromazepamBromazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
BrompheniramineBrompheniramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
BuprenorphineBuprenorphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
BuspironeBuspirone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ButabarbitalButabarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ButorphanolButorphanol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
CarbamazepineCarbamazepine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
CarbinoxamineCarbinoxamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
CarisoprodolCarisoprodol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
CetirizineCetirizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ChlordiazepoxideChlordiazepoxide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ChlorphenamineChlorphenamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ChlorpromazineChlorpromazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ChlorzoxazoneChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
CimetropiumOrphenadrine may increase the anticholinergic activities of Cimetropium Bromide.
ClemastineClemastine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ClobazamClobazam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ClomipramineClomipramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ClonazepamClonazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ClonidineClonidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ClorazepateClorazepate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ClozapineClozapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
CyclizineCyclizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
CyclobenzaprineCyclobenzaprine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
CyproheptadineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
DantroleneDantrolene may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
DesfluraneDesflurane may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
DesipramineDesipramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
DesloratadineDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Dexchlorpheniramine maleateDexchlorpheniramine maleate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
DiazepamDiazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
DimenhydrinateDimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
DiphenhydramineDiphenhydramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
DoxepinDoxepin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
EfavirenzEfavirenz may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
EluxadolineOrphenadrine may increase the activities of Eluxadoline.
EntacaponeEntacapone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
EstazolamEstazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
EszopicloneEszopiclone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
EthanolEthanol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
EthosuximideEthosuximide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
EthotoinEthotoin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
EzogabineEzogabine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
FelbamateFelbamate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
FentanylFentanyl may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
FexofenadineFexofenadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
FlibanserinFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
FlunarizineFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
FlupentixolFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
FluphenazineFluphenazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
FlurazepamFlurazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
FosphenytoinFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
GabapentinGabapentin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
gabapentin enacarbilgabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Gamma Hydroxybutyric AcidGamma Hydroxybutyric Acid may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Glucagon recombinant.
GuanfacineGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
HaloperidolHaloperidol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
HydrocodoneHydrocodone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
HydromorphoneHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
IloperidoneIloperidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ImipramineImipramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Orphenadrine.
IsofluraneIsoflurane may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Orphenadrine.
KetamineKetamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
LamotrigineLamotrigine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
LevetiracetamLevetiracetam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
LevocabastineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
LevocetirizineLevocetirizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
LevorphanolLevorphanol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
LoratadineLoratadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
LorazepamLorazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
LoxapineLoxapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
LurasidoneLurasidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MaprotilineMaprotiline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MeclizineMeclizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MeprobamateMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MetaxaloneMetaxalone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MethadoneMethadone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MethocarbamolMethocarbamol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MethohexitalMethohexital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MethotrimeprazineMethotrimeprazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MethsuximideMethsuximide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MetyrosineOrphenadrine may increase the sedative activities of Metyrosine.
MidazolamMidazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MirabegronThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Mirabegron.
MirtazapineMirtazapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
MorphineMorphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
NalbuphineNalbuphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
NitrazepamNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Nitrous oxideNitrous oxide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
NortriptylineNortriptyline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OlanzapineOlanzapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OlopatadineOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxazepamOxazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxycodoneOxycodone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxymorphoneOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PaliperidonePaliperidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeOrphenadrine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Paroxetine.
PentazocinePentazocine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PentobarbitalPentobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PerphenazinePerphenazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PethidinePethidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PhenobarbitalPhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PhenytoinPhenytoin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PimozidePimozide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PipotiazinePipotiazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PizotifenPizotifen may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PomalidomidePomalidomide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Potassium ChlorideOrphenadrine may increase the ulcerogenic activities of Potassium Chloride.
PramipexoleOrphenadrine may increase the sedative activities of Pramipexole.
PramlintidePramlintide may increase the anticholinergic activities of Orphenadrine.
PregabalinPregabalin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PrimidonePrimidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ProchlorperazineProchlorperazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Orphenadrine.
PromazinePromazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PromethazinePromethazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PropofolPropofol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ProtriptylineProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
QuazepamQuazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
QuetiapineQuetiapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
RamelteonRamelteon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
RamosetronOrphenadrine may increase the activities of Ramosetron.
RemifentanilRemifentanil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ReserpineReserpine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
RisperidoneRisperidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
RopiniroleOrphenadrine may increase the sedative activities of Ropinirole.
RotigotineOrphenadrine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Orphenadrine.
ScopolamineScopolamine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Scopolamine butylbromideScopolamine butylbromide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
SecobarbitalSecobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Orphenadrine.
SevofluraneSevoflurane may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
StiripentolStiripentol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
SufentanilSufentanil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Orphenadrine.
SuvorexantSuvorexant may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TacrineThe therapeutic efficacy of Orphenadrine can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TasimelteonTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TemazepamTemazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TetrabenazineTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ThalidomideThalidomide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ThioridazineThioridazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ThiothixeneThiothixene may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TiagabineTiagabine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TiotropiumOrphenadrine may increase the anticholinergic activities of Tiotropium.
TizanidineTizanidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TolcaponeTolcapone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TopiramateTopiramate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TramadolTramadol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TriazolamTriazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Orphenadrine.
TrifluoperazineTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TrimipramineTrimipramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
TriprolidineTriprolidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Orphenadrine.
VigabatrinVigabatrin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ZaleplonZaleplon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ZiconotideZiconotide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ZiprasidoneZiprasidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ZolpidemZolpidem may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ZonisamideZonisamide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ZopicloneZopiclone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ZuclopenthixolZuclopenthixol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Food Interactions
  • Take without regard to meals. Avoid alcohol.

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
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 plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. It mediates neuronal functions in glutamate neurotransmission. Is involved in the cell surface targeting of NMDA receptors (...
Gene Name:
GRIN1
Uniprot ID:
Q05586
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
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 play a role in the development of dendritic spines. May play a role in PPP2CB-NMDAR mediated signaling mechanism (By similarity).
Gene Name:
GRIN3A
Uniprot ID:
Q8TCU5
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 ]
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 catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
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
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 across the membrane, the protein forms a sodium-selective channel through which sodium ions may pass in accordance with their electrochemical gradient. Plays a role in neuropathic pain mechanisms.
Gene Name:
SCN10A
Uniprot ID:
Q9Y5Y9
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
inhibitorinducer
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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 or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23