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Identification
NameBiperiden
Accession NumberDB00810  (APRD00725)
TypeSmall Molecule
GroupsApproved
DescriptionA muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine. [PubChem]
Structure
Thumb
Synonyms
1-Bicyclo[2.2.1]hept-5-en-2-yl-1-phenyl-3-piperidin-1-yl-propan-1-ol
alpha-5-Norbornen-2-yl-alpha-phenyl-1-piperidinepropanol
alpha-Bicyclo[2.2.1]hept-5-en-2-yl-alpha-phenyl-1-piperidinepropanol
Beperiden
Biperidene
Biperideno
Biperidenum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Akineton Tab 2mgTablet2 mgOralAbbott Laboratories, Limited1985-12-312007-07-31Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AkinetonAbbott
BilinoWinston
IpsatolOrion
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Biperiden hydrochloride
Thumb
  • InChI Key: RDNLAULGBSQZMP-UHFFFAOYNA-N
  • Monoisotopic Mass: 347.201592294
  • Average Mass: 347.922
DBSALT000804
Biperiden lactate
ThumbNot applicableDBSALT001327
Categories
UNII0FRP6G56LD
CAS number514-65-8
WeightAverage: 311.4611
Monoisotopic: 311.224914555
Chemical FormulaC21H29NO
InChI KeyYSXKPIUOCJLQIE-UHFFFAOYSA-N
InChI
InChI=1S/C21H29NO/c23-21(19-7-3-1-4-8-19,11-14-22-12-5-2-6-13-22)20-16-17-9-10-18(20)15-17/h1,3-4,7-10,17-18,20,23H,2,5-6,11-16H2
IUPAC Name
1-{bicyclo[2.2.1]hept-5-en-2-yl}-1-phenyl-3-(piperidin-1-yl)propan-1-ol
SMILES
OC(CCN1CCCCC1)(C1CC2CC1C=C2)C1=CC=CC=C1
Pharmacology
IndicationFor use as an adjunct in the therapy of all forms of parkinsonism and control of extrapyramidal disorders secondary to neuroleptic drug therapy.
Structured Indications Not Available
PharmacodynamicsBiperiden is a weak peripheral anticholinergic agent. It has, therefore, some antisecretory, antispasmodic and mydriatic effects. In addition, biperiden possesses nicotinolytic activity. The parenteral form of biperiden is an effective and reliable agent for the treatment of acute episodes of extrapyramidal disturbances sometimes seen during treatment with neuroleptic agents. Akathisia, akinesia, dyskinetic tremors, rigor, oculogyric crisis, spasmodic torticollis, and profuse sweating are markedly reduced or eliminated. With parenteral biperiden, these drug-induced disturbances are rapidly brought under control.
Mechanism of actionParkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as biperiden is considered to relate to competitive antagonism of acetylcholine at cholinergic receptors in the corpus striatum, which then restores the balance.
TargetKindPharmacological actionActionsOrganismUniProt ID
Muscarinic acetylcholine receptor M1Proteinyes
antagonist
HumanP11229 details
Neuronal acetylcholine receptor subunit alpha-2Proteinyes
antagonist
HumanQ15822 details
Related Articles
Absorption87% bioavailability
Volume of distributionNot Available
Protein binding60%
Metabolism

The metabolism of biperiden is not completely understood, but does involve hydroxylation.

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityLD50=760 mg/kg (Orally in rats). Signs of overdose include dilated and sluggish pupils, warm, dry skin, facial flushing, decreased secretions of the mouth, pharynx, nose, and bronchi, foul-smelling breath, elevated temperature, tachycardia, cardiac arrhythmias, decreased bowel sounds, urinary retention, delirium, disorientation, anxiety, hallucinations, illusions, confusion, incoherence, agitation, hyperactivity, ataxia, loss of memory, paranoia, combativeness, and seizures.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of Biperiden can be decreased when used in combination with 1,10-Phenanthroline.Experimental
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Biperiden.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Biperiden.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Biperiden.Approved, Vet Approved
AclidiniumAclidinium may increase the anticholinergic activities of Biperiden.Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Biperiden.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Biperiden.Experimental
AlfentanilThe risk or severity of adverse effects can be increased when Biperiden is combined with Alfentanil.Approved, Illicit
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Biperiden.Approved, Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Biperiden is combined with Alphacetylmethadol.Experimental, Illicit
AmbenoniumThe therapeutic efficacy of Biperiden can be decreased when used in combination with Ambenonium.Approved
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Biperiden.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Biperiden.Approved
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Anisotropine Methylbromide is combined with Biperiden.Approved
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Biperiden.Approved
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Biperiden.Approved, Investigational
AtazanavirThe serum concentration of Atazanavir can be increased when it is combined with Biperiden.Approved, Investigational
AtenololThe serum concentration of Atenolol can be increased when it is combined with Biperiden.Approved
Atracurium besylateThe risk or severity of adverse effects can be increased when Atracurium besylate is combined with Biperiden.Approved
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Biperiden.Approved, Vet Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Biperiden.Approved, Investigational
BenactyzineThe risk or severity of adverse effects can be increased when Biperiden is combined with Benactyzine.Withdrawn
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Biperiden.Approved
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Biperiden.Approved
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Biperiden.Approved, Vet Approved
BezitramideThe risk or severity of adverse effects can be increased when Biperiden is combined with Bezitramide.Experimental, Illicit, Withdrawn
BoceprevirThe serum concentration of Boceprevir can be increased when it is combined with Biperiden.Approved
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Biperiden.Approved
Botulinum Toxin Type ABiperiden may increase the anticholinergic activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BBiperiden may increase the anticholinergic activities of Botulinum Toxin Type B.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Biperiden.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Biperiden.Approved, Investigational
BuprenorphineThe risk or severity of adverse effects can be increased when Biperiden is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe risk or severity of adverse effects can be increased when Biperiden is combined with Butorphanol.Approved, Illicit, Vet Approved
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Biperiden.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Biperiden.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Biperiden.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Biperiden.Approved
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Biperiden.Approved, Investigational
CarfentanilThe risk or severity of adverse effects can be increased when Biperiden is combined with Carfentanil.Illicit, Vet Approved
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Biperiden.Approved
CeritinibThe serum concentration of Ceritinib can be increased when it is combined with Biperiden.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Biperiden.Withdrawn
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Biperiden.Approved, Vet Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Biperiden is combined with Chlorphenoxamine.Withdrawn
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Biperiden.Approved, Vet Approved
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Biperiden.Approved
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Biperiden.Approved
CimetropiumBiperiden may increase the anticholinergic activities of Cimetropium.Experimental
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Biperiden.Approved, Investigational
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Biperiden.Approved
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Biperiden.Approved
ClarithromycinThe serum concentration of Clarithromycin can be increased when it is combined with Biperiden.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Biperiden.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Biperiden.Approved, Investigational
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Biperiden.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Biperiden.Approved, Nutraceutical
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Biperiden.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Biperiden.Approved
CodeineThe risk or severity of adverse effects can be increased when Biperiden is combined with Codeine.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Biperiden.Approved
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Biperiden.Approved
CoumaphosThe therapeutic efficacy of Biperiden can be decreased when used in combination with Coumaphos.Vet Approved
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Biperiden.Approved
CyclopentolateThe risk or severity of adverse effects can be increased when Biperiden is combined with Cyclopentolate.Approved
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Biperiden.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Biperiden.Approved
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Biperiden.Approved
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Biperiden.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Biperiden.Approved
DarifenacinThe risk or severity of adverse effects can be increased when Darifenacin is combined with Biperiden.Approved, Investigational
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Biperiden.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Biperiden.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Biperiden.Approved
DecamethoniumThe therapeutic efficacy of Biperiden can be decreased when used in combination with Decamethonium.Approved
DemecariumThe therapeutic efficacy of Biperiden can be decreased when used in combination with Demecarium.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Biperiden is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Biperiden.Approved, Investigational, Vet Approved
DexetimideThe risk or severity of adverse effects can be increased when Biperiden is combined with Dexetimide.Withdrawn
DextromoramideThe risk or severity of adverse effects can be increased when Biperiden is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Biperiden is combined with Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Biperiden is combined with Dezocine.Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Biperiden.Approved, Illicit, Vet Approved
DichlorvosThe therapeutic efficacy of Biperiden can be decreased when used in combination with Dichlorvos.Vet Approved
DicyclomineThe risk or severity of adverse effects can be increased when Dicyclomine is combined with Biperiden.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Biperiden.Approved
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Biperiden.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Biperiden.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Biperiden is combined with Dihydrocodeine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Biperiden is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Biperiden is combined with Dihydromorphine.Experimental, Illicit
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Biperiden.Illicit
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Biperiden.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Biperiden is combined with Diphenoxylate.Approved, Illicit
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Biperiden.Approved
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Biperiden.Approved, Investigational
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Biperiden.Approved, Investigational, Vet Approved
DonepezilThe therapeutic efficacy of Biperiden can be decreased when used in combination with Donepezil.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Biperiden.Approved, Investigational
DPDPEThe risk or severity of adverse effects can be increased when Biperiden is combined with DPDPE.Investigational
DronabinolBiperiden may increase the tachycardic activities of Dronabinol.Approved, Illicit
EchothiophateThe therapeutic efficacy of Biperiden can be decreased when used in combination with Echothiophate.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Biperiden.Approved
EdrophoniumThe therapeutic efficacy of Biperiden can be decreased when used in combination with Edrophonium.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Biperiden.Approved, Investigational
EluxadolineBiperiden may increase the constipating activities of Eluxadoline.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Biperiden.Approved, Investigational
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Biperiden.Approved, Investigational
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Biperiden.Approved, Vet Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Biperiden.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be increased when it is combined with Biperiden.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Biperiden.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Biperiden.Approved
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Biperiden.Approved
EthylmorphineThe risk or severity of adverse effects can be increased when Biperiden is combined with Ethylmorphine.Approved, Illicit
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Biperiden.Approved
EtorphineThe risk or severity of adverse effects can be increased when Biperiden is combined with Etorphine.Illicit, Vet Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Biperiden.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Biperiden.Approved
FentanylThe risk or severity of adverse effects can be increased when Biperiden is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenthionThe therapeutic efficacy of Biperiden can be decreased when used in combination with Fenthion.Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Biperiden.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Biperiden.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Biperiden.Approved
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Biperiden.Approved
GalantamineThe therapeutic efficacy of Biperiden can be decreased when used in combination with Galantamine.Approved
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Biperiden.Approved
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Biperiden.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Biperiden.Approved
Ginkgo bilobaThe therapeutic efficacy of Biperiden can be decreased when used in combination with Ginkgo biloba.Approved, Nutraceutical
Glucagon recombinantThe risk or severity of adverse effects can be increased when Biperiden is combined with Glucagon recombinant.Approved
GlycopyrroniumBiperiden may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Biperiden.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Biperiden.Withdrawn
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Biperiden.Approved
HeroinThe risk or severity of adverse effects can be increased when Biperiden is combined with Heroin.Approved, Illicit
HexamethoniumThe risk or severity of adverse effects can be increased when Biperiden is combined with Hexamethonium.Experimental
HomatropineThe risk or severity of adverse effects can be increased when Biperiden is combined with Homatropine.Approved
Huperzine AThe therapeutic efficacy of Biperiden can be decreased when used in combination with Huperzine A.Investigational
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Biperiden.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Biperiden is combined with Hydrocodone.Approved, Illicit
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Biperiden.Approved, Vet Approved
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Biperiden.Approved
HydromorphoneThe risk or severity of adverse effects can be increased when Biperiden is combined with Hydromorphone.Approved, Illicit
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Biperiden.Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Biperiden.Approved
IdelalisibThe serum concentration of Idelalisib can be increased when it is combined with Biperiden.Approved
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Biperiden.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Biperiden.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Biperiden.Approved
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Biperiden.Approved
IndinavirThe serum concentration of Indinavir can be increased when it is combined with Biperiden.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Biperiden.Approved, Investigational
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Biperiden.Approved
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Biperiden.Approved, Investigational
IsoflurophateThe therapeutic efficacy of Biperiden can be decreased when used in combination with Isoflurophate.Approved, Withdrawn
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Biperiden.Investigational
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Biperiden.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Biperiden.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Biperiden is combined with Ketobemidone.Approved
KetoconazoleThe serum concentration of Ketoconazole can be increased when it is combined with Biperiden.Approved, Investigational
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Biperiden.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Biperiden.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Biperiden.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Biperiden.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Biperiden.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Biperiden.Approved
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Biperiden.Approved, Investigational
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Biperiden.Approved, Investigational
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Biperiden is combined with Levomethadyl Acetate.Approved
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Biperiden.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Biperiden is combined with Levorphanol.Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Biperiden.Approved
LofentanilThe risk or severity of adverse effects can be increased when Biperiden is combined with Lofentanil.Illicit
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Biperiden.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Biperiden.Approved
MalathionThe therapeutic efficacy of Biperiden can be decreased when used in combination with Malathion.Approved, Investigational
MannitolThe serum concentration of Mannitol can be increased when it is combined with Biperiden.Approved, Investigational
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Biperiden.Approved
MefloquineThe therapeutic efficacy of Biperiden can be decreased when used in combination with Mefloquine.Approved
MemantineThe therapeutic efficacy of Biperiden can be decreased when used in combination with Memantine.Approved, Investigational
MethadoneThe risk or severity of adverse effects can be increased when Biperiden is combined with Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Biperiden is combined with Methadyl Acetate.Approved, Illicit
Methanesulfonyl FluorideThe therapeutic efficacy of Biperiden can be decreased when used in combination with Methanesulfonyl Fluoride.Investigational
MethanthelineThe risk or severity of adverse effects can be increased when Biperiden is combined with Methantheline.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Biperiden.Approved
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Biperiden.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Biperiden.Approved, Vet Approved
MetixeneThe risk or severity of adverse effects can be increased when Biperiden is combined with Metixene.Approved
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Biperiden.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Biperiden.Approved, Investigational
MianserinMianserin may increase the anticholinergic activities of Biperiden.Approved
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Biperiden.Approved, Illicit
MinaprineThe therapeutic efficacy of Biperiden can be decreased when used in combination with Minaprine.Approved
MirabegronThe risk or severity of adverse effects can be increased when Biperiden is combined with Mirabegron.Approved
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Biperiden.Approved, Investigational
MorphineThe serum concentration of Morphine can be increased when it is combined with Biperiden.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Biperiden.Approved, Investigational
N-butylscopolammonium bromideThe risk or severity of adverse effects can be increased when Biperiden is combined with N-butylscopolammonium bromide.Vet Approved
NabiloneBiperiden may increase the tachycardic activities of Nabilone.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Biperiden.Approved
NalbuphineThe risk or severity of adverse effects can be increased when Biperiden is combined with Nalbuphine.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Biperiden.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Biperiden.Approved, Vet Approved
NelfinavirThe serum concentration of Nelfinavir can be increased when it is combined with Biperiden.Approved
NeostigmineThe therapeutic efficacy of Biperiden can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Biperiden.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Biperiden.Approved
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Biperiden.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Biperiden.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Biperiden.Approved
NormethadoneThe risk or severity of adverse effects can be increased when Biperiden is combined with Normethadone.Approved, Illicit
NVA237The risk or severity of adverse effects can be increased when Biperiden is combined with NVA237.Investigational
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Biperiden.Approved, Investigational
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Biperiden.Approved
OpiumThe risk or severity of adverse effects can be increased when Biperiden is combined with Opium.Approved, Illicit
OrphenadrineThe risk or severity of adverse effects can be increased when Biperiden is combined with Orphenadrine.Approved
OsimertinibThe serum concentration of Osimertinib can be increased when it is combined with Biperiden.Approved
OxybutyninThe risk or severity of adverse effects can be increased when Biperiden is combined with Oxybutynin.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Biperiden is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Biperiden is combined with Oxymorphone.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Biperiden.Approved
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Biperiden.Approved, Vet Approved
PancuroniumThe risk or severity of adverse effects can be increased when Biperiden is combined with Pancuronium.Approved
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Biperiden.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Biperiden.Approved
PentazocineThe risk or severity of adverse effects can be increased when Biperiden is combined with Pentazocine.Approved, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Biperiden is combined with Pentolinium.Approved
PethidineThe risk or severity of adverse effects can be increased when Biperiden is combined with Pethidine.Approved
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Biperiden.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Biperiden.Approved, Vet Approved
PhysostigmineThe therapeutic efficacy of Biperiden can be decreased when used in combination with Physostigmine.Approved
PipecuroniumThe risk or severity of adverse effects can be increased when Biperiden is combined with Pipecuronium.Approved
PirenzepineThe risk or severity of adverse effects can be increased when Pirenzepine is combined with Biperiden.Approved
PiritramideThe risk or severity of adverse effects can be increased when Biperiden is combined with Piritramide.Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Biperiden.Approved
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Biperiden.Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Biperiden.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Biperiden.Approved
Potassium ChlorideBiperiden may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PramlintidePramlintide may increase the anticholinergic activities of Biperiden.Approved, Investigational
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Biperiden.Approved
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Biperiden.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Biperiden.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Biperiden.Approved, Vet Approved
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Biperiden.Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Biperiden.Approved, Vet Approved
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Biperiden.Approved
PropiverineThe risk or severity of adverse effects can be increased when Biperiden is combined with Propiverine.Investigational
PropranololThe serum concentration of Propranolol can be increased when it is combined with Biperiden.Approved, Investigational
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Biperiden.Approved
PyridostigmineThe therapeutic efficacy of Biperiden can be decreased when used in combination with Pyridostigmine.Approved
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Biperiden.Approved
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Biperiden.Approved
QuinidineThe risk or severity of adverse effects can be increased when Biperiden is combined with Quinidine.Approved
QuinineThe serum concentration of Quinine can be increased when it is combined with Biperiden.Approved
RamosetronBiperiden may increase the constipating activities of Ramosetron.Approved
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Biperiden.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Biperiden.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Biperiden is combined with Remifentanil.Approved
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Biperiden.Approved
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Biperiden.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Biperiden.Approved, Investigational
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Biperiden.Approved, Investigational
RitonavirThe serum concentration of Ritonavir can be increased when it is combined with Biperiden.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Biperiden.Approved
RivastigmineThe therapeutic efficacy of Biperiden can be decreased when used in combination with Rivastigmine.Approved, Investigational
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Biperiden.Approved, Investigational
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Biperiden.Approved, Vet Approved
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Biperiden.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Biperiden.Approved
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Biperiden is combined with Scopolamine butylbromide.Approved
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Biperiden.Approved, Investigational
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Biperiden.Approved
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Biperiden.Approved
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Biperiden.Approved
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Biperiden.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Biperiden.Approved
SolifenacinThe risk or severity of adverse effects can be increased when Biperiden is combined with Solifenacin.Approved
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Biperiden.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Biperiden.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Biperiden.Experimental
SufentanilThe risk or severity of adverse effects can be increased when Biperiden is combined with Sufentanil.Approved, Investigational
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Biperiden.Approved
TacrineThe therapeutic efficacy of Biperiden can be decreased when used in combination with Tacrine.Withdrawn
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Biperiden.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Biperiden.Approved
TapentadolThe risk or severity of adverse effects can be increased when Biperiden is combined with Tapentadol.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Biperiden.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Biperiden.Approved
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Biperiden.Approved
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Biperiden.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Biperiden.Approved
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Biperiden.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Biperiden.Approved
TiotropiumBiperiden may increase the anticholinergic activities of Tiotropium.Approved
TolterodineThe risk or severity of adverse effects can be increased when Biperiden is combined with Tolterodine.Approved, Investigational
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Biperiden.Approved
TopiramateThe risk or severity of adverse effects can be increased when Biperiden is combined with Topiramate.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Biperiden.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Biperiden.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Biperiden is combined with Tramadol.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Biperiden.Approved
TrichlorfonThe therapeutic efficacy of Biperiden can be decreased when used in combination with Trichlorfon.Vet Approved
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Biperiden.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Biperiden.Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Biperiden is combined with Trimethaphan.Approved
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Biperiden.Approved
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Biperiden.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Biperiden is combined with Tubocurarine.Approved
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Biperiden.Approved
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Biperiden.Approved
VecuroniumThe risk or severity of adverse effects can be increased when Biperiden is combined with Vecuronium.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Biperiden.Approved
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Biperiden.Approved
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Biperiden.Approved
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Biperiden.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Biperiden.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Biperiden.Approved
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Biperiden.Approved
Food Interactions
  • Avoid alcohol.
  • Take with food.
References
Synthesis Reference

Peter Klein, “Method for the production of biperiden II.” U.S. Patent US20040152899, issued August 05, 2004.

US20040152899
General References
  1. Nishiyama K, Mizuno T, Sakuta M, Kurisaki H: Chronic dementia in Parkinson's disease treated by anticholinergic agents. Neuropsychological and neuroradiological examination. Adv Neurol. 1993;60:479-83. [PubMed:8420174 ]
External Links
ATC CodesN04AA02
AHFS Codes
  • 12:08.04
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9669
Blood Brain Barrier+0.9808
Caco-2 permeable+0.6422
P-glycoprotein substrateSubstrate0.7189
P-glycoprotein inhibitor IInhibitor0.6211
P-glycoprotein inhibitor IINon-inhibitor0.8284
Renal organic cation transporterInhibitor0.7592
CYP450 2C9 substrateNon-substrate0.8119
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5193
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9084
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9056
CYP450 3A4 inhibitorNon-inhibitor0.9041
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9558
Ames testNon AMES toxic0.8194
CarcinogenicityNon-carcinogens0.9309
BiodegradationNot ready biodegradable0.8756
Rat acute toxicity2.6495 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.6982
hERG inhibition (predictor II)Non-inhibitor0.6332
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Abbott laboratories
Packagers
Dosage forms
FormRouteStrength
TabletOral2 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point114 °CPhysProp
water solubility25.1 mg/LNot Available
logP4.25SANGSTER (1993)
Predicted Properties
PropertyValueSource
Water Solubility0.00426 mg/mLALOGPS
logP4.28ALOGPS
logP3.54ChemAxon
logS-4.9ALOGPS
pKa (Strongest Acidic)13.82ChemAxon
pKa (Strongest Basic)9.3ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area23.47 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity97.02 m3·mol-1ChemAxon
Polarizability36.74 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (7.72 KB)
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)splash10-0002-9000000000-92eb93b999cf7f5ec519View in MoNA
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpropylamines. These are compounds containing a phenylpropylamine moiety, which consists of a phenyl group substituted at the third carbon by an propan-1-amine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylpropylamines
Direct ParentPhenylpropylamines
Alternative Parents
Substituents
  • Phenylpropylamine
  • Aralkylamine
  • Piperidine
  • Tertiary alcohol
  • 1,3-aminoalcohol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Aromatic alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
Molecular Weight:
51420.375 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. Hosoi R, Kobayashi K, Watanabe Y, Inoue O: Evaluation of in vivo binding properties of 3H-NMPB and 3H-QNB in mouse brain. J Neural Transm (Vienna). 1999;106(7-8):583-92. [PubMed:10907719 ]
  4. Pehl C, Wendl B, Kaess H, Pfeiffer A: Effects of two anticholinergic drugs, trospium chloride and biperiden, on motility and evoked potentials of the oesophagus. Aliment Pharmacol Ther. 1998 Oct;12(10):979-84. [PubMed:9798802 ]
  5. Eltze M: Multiple mechanisms of action: the pharmacological profile of budipine. J Neural Transm Suppl. 1999;56:83-105. [PubMed:10370904 ]
  6. Eltze M, Galvan M: Involvement of muscarinic M2 and M3, but not of M1 and M4 receptors in vagally stimulated contractions of rabbit bronchus/trachea. Pulm Pharmacol. 1994 Apr;7(2):109-20. [PubMed:8081071 ]
  7. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Drug binding
Specific Function:
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
Gene Name:
CHRNA2
Uniprot ID:
Q15822
Molecular Weight:
59764.82 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 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [PubMed:12438524 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23