Identification

Name
Trihexyphenidyl
Accession Number
DB00376  (APRD00070)
Type
Small Molecule
Groups
Approved
Description

One of the centrally acting muscarinic antagonists used for treatment of parkinsonian disorders and drug-induced extrapyramidal movement disorders and as an antispasmodic. [PubChem]

Structure
Thumb
Synonyms
  • (RS)-1-cyclohexyl-1-phenyl-3-(1-piperidyl)propan-1-ol
  • Apo-trihex
  • Benzhexol Hydrochloride
  • Trihexifenidilo
  • Trihexyphenidyl
  • Trihexyphénidyle
  • Trihexyphenidylum
External IDs
Win 511
Product Ingredients
IngredientUNIICASInChI Key
Trihexyphenidyl HydrochlorideAO61G82577 52-49-3QDWJJTJNXAKQKD-UHFFFAOYNA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aparkane Tab 2mgTablet2 mgOralIcn Pharmaceuticals1973-12-312005-04-26Canada
Aparkane Tab 5mgTablet5 mgOralIcn Pharmaceuticals1973-12-312005-04-26Canada
Artane Elx 2mg/5mlElixir2 mgOralLederle Cyanamid Canada Inc.1967-12-311999-08-12Canada
Artane Tab 2mgTablet2 mgOralLederle Cyanamid Canada Inc.1951-12-311999-04-12Canada
Artane Tab 5mgTablet5 mgOralLederle Cyanamid Canada Inc.1951-12-311997-01-14Canada
Novo-hexidyl 2mgTablet2 mgOralNovopharm Limited1968-12-312005-08-10Canada
Novo-hexidyl 5mgTablet5 mgOralNovopharm Limited1967-12-312005-08-10Canada
Nu-trihexyphenidylTablet5 mgOralNu Pharm IncNot applicableNot applicableCanada
Nu-trihexyphenidylTablet2 mgOralNu Pharm IncNot applicableNot applicableCanada
PMS TrihexyphenidylTablet5 mgOralPharmascience Inc1987-12-31Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Trihexyphenidyl HydrochlorideTablet2 mg/1OralRichmond Pharmaceuticals1998-12-24Not applicableUs
Trihexyphenidyl HydrochlorideTablet2 mg/1OralRemedy Repack2017-06-06Not applicableUs
Trihexyphenidyl HydrochlorideSolution2 mg/5mLOralPharmaceutical Associates, Inc.1997-05-15Not applicableUs
Trihexyphenidyl HydrochlorideTablet2 mg/1OralRemedy Repack2014-04-042016-12-21Us
Trihexyphenidyl HydrochlorideTablet2 mg/1OralAvera Mc Kennan Hospital2015-08-17Not applicableUs
Trihexyphenidyl HydrochlorideTablet2 mg/1OralRemedy Repack2016-06-15Not applicableUs
Trihexyphenidyl HydrochlorideSolution2 mg/5mLOralMikart, Inc.1999-10-04Not applicableUs
Trihexyphenidyl HydrochlorideTablet5 mg/1OralRemedy Repack2014-08-262017-02-02Us
Trihexyphenidyl hydrochlorideTablet2 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs1998-02-06Not applicableUs00591 5335 01 nlmimage10 501da84d
Trihexyphenidyl HydrochlorideTablet5 mg/1OralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
International/Other Brands
ACA (Atlantic) / Acamed (Medifive) / Altant (Panbiotic) / Artane (Sanofi Aventis) / Artine (The Central) / Atan (Newai Chem) / Benzhexol (Johnson) / Benzox (Li Ta) / Bexol (Intas) / Broflex (Alliance) / Cyclodol (Grindeks) / Dyskinil (Crescent) / Ea Ten (Heng Hsin) / Hexymer (Mersifarma) / Hipokinon (Psicofarma) / Lahexy (La Pharmaceuticals) / Pacitane (Wyeth) / Pakisonal (Takata Seiyaku) / Parales (Psyco Remedies) / Parcisol (Milve) / Pargitan (Nevada Pharma) / Parkin (Micro Synapse) / Parkinane (Eisai) / Parkines (Towa Yakuhin) / Parkinidyl (CCPC) / Parkisan (Balkanpharma) / Parkitane (Sun) / Parkizol (Hikma) / Tonaril (Chile)
Categories
UNII
6RC5V8B7PO
CAS number
144-11-6
Weight
Average: 301.4662
Monoisotopic: 301.240564619
Chemical Formula
C20H31NO
InChI Key
HWHLPVGTWGOCJO-UHFFFAOYSA-N
InChI
InChI=1S/C20H31NO/c22-20(18-10-4-1-5-11-18,19-12-6-2-7-13-19)14-17-21-15-8-3-9-16-21/h1,4-5,10-11,19,22H,2-3,6-9,12-17H2
IUPAC Name
1-cyclohexyl-1-phenyl-3-(piperidin-1-yl)propan-1-ol
SMILES
OC(CCN1CCCCC1)(C1CCCCC1)C1=CC=CC=C1

Pharmacology

Indication

Indicated for the treatment of parkinson's disease and extrapyramidal reactions caused by drugs.

Structured Indications
Pharmacodynamics

Trihexyphenidyl is an anticholinergic used in the symptomatic treatment of all etiologic groups of parkinsonism and drug induced extrapyramidal reactions (except tardive dyskinesia). Trihexyphenidyl possesses both anticholinergic and antihistaminic effects, although only the former has been established as therapeutically significant in the management of parkinsonism.

Mechanism of action

Trihexyphenidyl is a selective M1 muscarinic acetylcholine receptor antagonist. It is able to discriminate between the M1 (cortical or neuronal) and the peripheral muscarinic subtypes (cardiac and glandular). Trihexyphenidyl partially blocks cholinergic activity in the CNS, which is responsible for the symptoms of Parkinson's disease. It is also thought to increase the availability of dopamine, a brain chemical that is critical in the initiation and smooth control of voluntary muscle movement.

TargetActionsOrganism
AMuscarinic acetylcholine receptor M1
antagonist
Human
UMuscarinic acetylcholine receptor M2
antagonist
Human
UMuscarinic acetylcholine receptor M3
antagonist
Human
UMuscarinic acetylcholine receptor M4
antagonist
Human
UMuscarinic acetylcholine receptor M5
antagonist
Human
Absorption

Trihexyphenidyl is rapidly absorbed from the gastrointestinal tract.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life

3.3-4.1 hours

Clearance
Not Available
Toxicity

Symptoms of overdose include mydriasis, dryness of mucous membranes, red face, atonic states of bowels and bladder, and hyperthermia in high doses. Central consequences are agitation, confusion, and hallucinations. An untreated overdose may be fatal, particular in children. Premortal signs are respiratory depression and cardiac arrest.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with 1,10-Phenanthroline.Experimental
AclidiniumAclidinium may increase the anticholinergic activities of Trihexyphenidyl.Approved
AlcuroniumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Alcuronium.Experimental
AlfentanilThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Alphaprodine.Illicit
AmbenoniumThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Ambenonium.Approved
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Anisotropine Methylbromide.Approved
AtracuriumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Atracurium.Experimental
Atracurium besylateThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Atracurium besylate.Approved
AtropineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Atropine.Approved, Vet Approved
BenactyzineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Benactyzine.Withdrawn
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Trihexyphenidyl.Approved
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Trihexyphenidyl.Approved
BezitramideThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Bezitramide.Experimental, Illicit, Withdrawn
BiperidenThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Biperiden.Approved
BornaprineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Bornaprine.Experimental
Botulinum Toxin Type ATrihexyphenidyl may increase the anticholinergic activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BTrihexyphenidyl may increase the anticholinergic activities of Botulinum Toxin Type B.Approved
BuprenorphineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Butorphanol.Approved, Illicit, Vet Approved
CarfentanilThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Carfentanil.Illicit, Vet Approved
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Trihexyphenidyl.Approved, Vet Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Chlorphenoxamine.Withdrawn
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Trihexyphenidyl.Approved
CimetropiumTrihexyphenidyl may increase the anticholinergic activities of Cimetropium.Experimental
CodeineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Codeine.Approved, Illicit
CoumaphosThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Coumaphos.Vet Approved
CyclopenthiazideThe serum concentration of Cyclopenthiazide can be increased when it is combined with Trihexyphenidyl.Experimental
CyclopentolateThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Cyclopentolate.Approved
DarifenacinThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Darifenacin.Approved, Investigational
DecamethoniumThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Decamethonium.Approved
DemecariumThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Demecarium.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Desloratadine.Approved, Investigational
DexetimideThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Dexetimide.Withdrawn
DextromoramideThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Dezocine.Approved
DichlorvosThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Dichlorvos.Vet Approved
DicyclomineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Dicyclomine.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Dihydrocodeine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Dihydromorphine.Experimental, Illicit
DiphenoxylateThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Diphenoxylate.Approved, Illicit
DistigmineThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Distigmine.Experimental
DonepezilThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Donepezil.Approved
DPDPEThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with DPDPE.Investigational
DronabinolTrihexyphenidyl may increase the tachycardic activities of Dronabinol.Approved, Illicit
EchothiophateThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Echothiophate.Approved
EdrophoniumThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Edrophonium.Approved
EluxadolineTrihexyphenidyl may increase the constipating activities of Eluxadoline.Approved
EmeproniumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Emepronium.Experimental
EtanautineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Etanautine.Experimental
EthopropazineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Ethopropazine.Approved
EthylmorphineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Ethylmorphine.Approved, Illicit
EtorphineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Etorphine.Illicit, Vet Approved
EtybenzatropineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Etybenzatropine.Experimental
FentanylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenthionThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Fenthion.Vet Approved
FesoterodineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Fesoterodine.Approved
GalantamineThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Galantamine.Approved
GallamineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Gallamine.Experimental
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Gallamine Triethiodide.Approved
Ginkgo bilobaThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Ginkgo biloba.Approved, Nutraceutical
Glucagon recombinantThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Glucagon recombinant.Approved
GlycopyrroniumTrihexyphenidyl may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Heroin.Approved, Illicit
HexamethoniumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Hexamethonium.Experimental
HomatropineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Homatropine.Approved
Huperzine AThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Huperzine A.Investigational
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Trihexyphenidyl.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Hydrocodone.Approved, Illicit
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Trihexyphenidyl.Approved
HydromorphoneThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Hydromorphone.Approved, Illicit
HyoscyamineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Hyoscyamine.Approved
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Trihexyphenidyl.Approved
IpidacrineThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Ipidacrine.Experimental
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Trihexyphenidyl.Approved
IsoflurophateThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Isoflurophate.Approved, Withdrawn
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Trihexyphenidyl.Investigational
KetobemidoneThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Ketobemidone.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Levomethadyl Acetate.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Levorphanol.Approved
LofentanilThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Lofentanil.Illicit
MalathionThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Malathion.Approved, Investigational
MazaticolThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Mazaticol.Experimental
MecamylamineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Mecamylamine.Approved
MefloquineThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Mefloquine.Approved
MemantineThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Memantine.Approved, Investigational
MeptazinolThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Meptazinol.Experimental
MethadoneThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Methadyl Acetate.Approved, Illicit
Methanesulfonyl FluorideThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Methanesulfonyl Fluoride.Investigational
MethanthelineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Methantheline.Approved
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Trihexyphenidyl.Approved
Methyl salicylateThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Methyl salicylate.Approved, Vet Approved
MetixeneThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Metixene.Approved
MetoclopramideThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Metoclopramide.Approved, Investigational
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Trihexyphenidyl.Approved
MianserinMianserin may increase the anticholinergic activities of Trihexyphenidyl.Approved
MinaprineThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Minaprine.Approved
MirabegronThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Mirabegron.Approved
MorphineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Morphine.Approved, Investigational
NabiloneTrihexyphenidyl may increase the tachycardic activities of Nabilone.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Nalbuphine.Approved
NeostigmineThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NicomorphineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Nicomorphine.Experimental
NormethadoneThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Normethadone.Approved, Illicit
OpiumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Opium.Approved, Illicit
OrphenadrineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Orphenadrine.Approved
OtiloniumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Otilonium.Experimental
OxitropiumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Oxitropium.Investigational
OxybutyninThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Oxybutynin.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Oxymorphone.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Oxyphenonium.Approved
PancuroniumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Pancuronium.Approved
ParaoxonThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Paraoxon.Experimental
PentazocineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Pentazocine.Approved, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Pentolinium.Approved
PethidineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Pethidine.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Phenazocine.Experimental
PhenglutarimideThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Phenglutarimide.Experimental
PhenoperidineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Phenoperidine.Experimental
PhysostigmineThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Physostigmine.Approved
PipecuroniumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Pipecuronium.Approved
PirenzepineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Pirenzepine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Piritramide.Investigational
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Trihexyphenidyl.Approved
Potassium ChlorideTrihexyphenidyl may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PramlintidePramlintide may increase the anticholinergic activities of Trihexyphenidyl.Approved, Investigational
ProcyclidineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Procyclidine.Approved
PropanthelineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Propantheline.Approved
PropiverineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Propiverine.Investigational
PyridostigmineThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Pyridostigmine.Approved
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Trihexyphenidyl.Approved
QuinidineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Quinidine.Approved
RamosetronTrihexyphenidyl may increase the constipating activities of Ramosetron.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Remifentanil.Approved
RivastigmineThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Rivastigmine.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Scopolamine.Approved
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Scopolamine butylbromide.Approved, Vet Approved
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Trihexyphenidyl.Approved, Investigational
SolifenacinThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Solifenacin.Approved
SufentanilThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Sufentanil.Approved, Investigational
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Trihexyphenidyl.Approved
TacrineThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Tacrine.Withdrawn
TapentadolThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Tapentadol.Approved
TilidineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Tilidine.Experimental
TiotropiumTrihexyphenidyl may increase the anticholinergic activities of Tiotropium.Approved
TolterodineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Tolterodine.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Tramadol.Approved, Investigational
TrichlorfonThe therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Trichlorfon.Vet Approved
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Trihexyphenidyl.Approved, Vet Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Trimethaphan.Approved
TropatepineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Tropatepine.Experimental
TropicamideThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Tropicamide.Approved
TrospiumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Trospium.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Tubocurarine.Approved
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Trihexyphenidyl.Approved
VecuroniumThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Vecuronium.Approved
Food Interactions
Not Available

References

Synthesis Reference
Not Available
General References
Not Available
External Links
Human Metabolome Database
HMDB14520
KEGG Compound
C07171
PubChem Compound
5572
PubChem Substance
46507717
ChemSpider
5371
BindingDB
81462
ChEBI
9720
ChEMBL
CHEMBL1490
Therapeutic Targets Database
DAP001532
PharmGKB
PA164747026
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Trihexyphenidyl
ATC Codes
N04AA01 — Trihexyphenidyl
AHFS Codes
  • 12:08.04
PDB Entries
Not Available
FDA label
Download (197 KB)
MSDS
Not Available

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedBasic ScienceRosaceas1
2CompletedTreatmentDystonias1
2Not Yet RecruitingTreatmentMalignant Neoplasm of Stomach2
2, 3RecruitingTreatmentMalignant Neoplasm of Stomach2
3RecruitingTreatmentMalignant Neoplasm of Stomach1
4RecruitingTreatmentMalignant Neoplasm of Stomach1
Not AvailableActive Not RecruitingNot AvailableDYT 1 Dystonia / Primary Cervical Dystonia1
Not AvailableRecruitingTreatmentMalignant Neoplasm of Stomach Stage II / Malignant Neoplasm of Stomach Stage IV1

Pharmacoeconomics

Manufacturers
  • Lederle laboratories div american cyanamid co
  • Mikart inc
  • Pharmaceutical assoc inc div beach products
  • Pharmaceutical ventures ltd
  • Schering corp sub schering plough corp
  • Nylos trading co inc
  • Vangard laboratories inc div midway medical co
  • Vintage pharmaceuticals inc
  • Watson laboratories inc
  • West ward pharmaceutical corp
Packagers
Dosage forms
FormRouteStrength
ElixirOral2 mg
ElixirOral0.4 mg
TabletOral2 mg
TabletOral5 mg
SolutionOral2 mg/5mL
SyrupOral2 mg/5mL
TabletOral2 mg/1
TabletOral5 mg/1
Prices
Unit descriptionCostUnit
Trihexyphenidyl HCl 5 mg tablet0.37USD tablet
Trihexyphenidyl 5 mg tablet0.36USD tablet
Trihexyphenidyl HCl 2 mg tablet0.26USD tablet
Trihexyphenidyl 2 mg tablet0.18USD tablet
Apo-Trihex 5 mg Tablet0.07USD tablet
Apo-Trihex 2 mg Tablet0.04USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)258.5 °CNot Available
logP4.49SANGSTER (1993)
Predicted Properties
PropertyValueSource
Water Solubility0.00314 mg/mLALOGPS
logP4.93ALOGPS
logP4.23ChemAxon
logS-5ALOGPS
pKa (Strongest Acidic)13.84ChemAxon
pKa (Strongest Basic)9.32ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area23.47 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity93.21 m3·mol-1ChemAxon
Polarizability36.73 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9156
Blood Brain Barrier+0.9523
Caco-2 permeable+0.6707
P-glycoprotein substrateSubstrate0.6943
P-glycoprotein inhibitor IInhibitor0.5993
P-glycoprotein inhibitor IINon-inhibitor0.7561
Renal organic cation transporterInhibitor0.7563
CYP450 2C9 substrateNon-substrate0.8256
CYP450 2D6 substrateNon-substrate0.7655
CYP450 3A4 substrateNon-substrate0.5746
CYP450 1A2 substrateNon-inhibitor0.9187
CYP450 2C9 inhibitorNon-inhibitor0.9126
CYP450 2D6 inhibitorInhibitor0.8966
CYP450 2C19 inhibitorNon-inhibitor0.9248
CYP450 3A4 inhibitorNon-inhibitor0.8506
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9543
Ames testNon AMES toxic0.8434
CarcinogenicityNon-carcinogens0.9238
BiodegradationNot ready biodegradable0.9253
Rat acute toxicity2.6751 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.6676
hERG inhibition (predictor II)Inhibitor0.5713
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0002-9200000000-2092a098302f5e63b76c
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udi-4119000000-9ed82688d3c1b39f26eb

Taxonomy

Description
This compound belongs to the class of organic compounds known as aralkylamines. These are alkylamines in which the alkyl group is substituted at one carbon atom by an aromatic hydrocarbyl group.
Kingdom
Organic compounds
Super Class
Organic nitrogen compounds
Class
Organonitrogen compounds
Sub Class
Amines
Direct Parent
Aralkylamines
Alternative Parents
Piperidines / Benzene and substituted derivatives / Tertiary alcohols / 1,3-aminoalcohols / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives / Aromatic alcohols
Substituents
Aralkylamine / Monocyclic benzene moiety / Piperidine / Benzenoid / 1,3-aminoalcohol / Tertiary alcohol / Tertiary amine / Tertiary aliphatic amine / Azacycle / Organoheterocyclic compound
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
amine (CHEBI:9720 )

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...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
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. Prus AJ, Pehrson AL, Philibin SD, Wood JT, Vunck SA, Porter JH: The role of M1 muscarinic cholinergic receptors in the discriminative stimulus properties of N-desmethylclozapine and the atypical antipsychotic drug clozapine in rats. Psychopharmacology (Berl). 2009 Apr;203(2):295-301. doi: 10.1007/s00213-008-1262-0. Epub 2008 Aug 7. [PubMed:18685832 ]
  4. Giachetti A, Giraldo E, Ladinsky H, Montagna E: Binding and functional profiles of the selective M1 muscarinic receptor antagonists trihexyphenidyl and dicyclomine. Br J Pharmacol. 1986 Sep;89(1):83-90. [PubMed:2432979 ]
  5. Tanda G, Katz JL: Muscarinic preferential M(1) receptor antagonists enhance the discriminative-stimulus effects of cocaine in rats. Pharmacol Biochem Behav. 2007 Oct;87(4):400-4. Epub 2007 Jun 2. [PubMed:17631384 ]
  6. Dorje F, Wess J, Lambrecht G, Tacke R, Mutschler E, Brann MR: Antagonist binding profiles of five cloned human muscarinic receptor subtypes. J Pharmacol Exp Ther. 1991 Feb;256(2):727-33. [PubMed:1994002 ]
  7. Freedman SB, Beer MS, Harley EA: Muscarinic M1, M2 receptor binding. Relationship with functional efficacy. Eur J Pharmacol. 1988 Oct 26;156(1):133-42. [PubMed:3208836 ]
  8. 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
Unknown
Actions
Antagonist
General Function
G-protein coupled acetylcholine receptor 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...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. Bognar IT, Altes U, Beinhauer C, Kessler I, Fuder H: A muscarinic receptor different from the M1, M2, M3 and M4 subtypes mediates the contraction of the rabbit iris sphincter. Naunyn Schmiedebergs Arch Pharmacol. 1992 Jun;345(6):611-8. [PubMed:1635586 ]
  2. Dorje F, Wess J, Lambrecht G, Tacke R, Mutschler E, Brann MR: Antagonist binding profiles of five cloned human muscarinic receptor subtypes. J Pharmacol Exp Ther. 1991 Feb;256(2):727-33. [PubMed:1994002 ]
  3. Freedman SB, Beer MS, Harley EA: Muscarinic M1, M2 receptor binding. Relationship with functional efficacy. Eur J Pharmacol. 1988 Oct 26;156(1):133-42. [PubMed:3208836 ]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Receptor 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...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
Molecular Weight
66127.445 Da
References
  1. Bognar IT, Altes U, Beinhauer C, Kessler I, Fuder H: A muscarinic receptor different from the M1, M2, M3 and M4 subtypes mediates the contraction of the rabbit iris sphincter. Naunyn Schmiedebergs Arch Pharmacol. 1992 Jun;345(6):611-8. [PubMed:1635586 ]
  2. Dorje F, Wess J, Lambrecht G, Tacke R, Mutschler E, Brann MR: Antagonist binding profiles of five cloned human muscarinic receptor subtypes. J Pharmacol Exp Ther. 1991 Feb;256(2):727-33. [PubMed:1994002 ]
  3. Freedman SB, Beer MS, Harley EA: Muscarinic M1, M2 receptor binding. Relationship with functional efficacy. Eur J Pharmacol. 1988 Oct 26;156(1):133-42. [PubMed:3208836 ]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Guanyl-nucleotide exchange factor 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...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. Bognar IT, Altes U, Beinhauer C, Kessler I, Fuder H: A muscarinic receptor different from the M1, M2, M3 and M4 subtypes mediates the contraction of the rabbit iris sphincter. Naunyn Schmiedebergs Arch Pharmacol. 1992 Jun;345(6):611-8. [PubMed:1635586 ]
  2. Dorje F, Wess J, Lambrecht G, Tacke R, Mutschler E, Brann MR: Antagonist binding profiles of five cloned human muscarinic receptor subtypes. J Pharmacol Exp Ther. 1991 Feb;256(2):727-33. [PubMed:1994002 ]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. Bognar IT, Altes U, Beinhauer C, Kessler I, Fuder H: A muscarinic receptor different from the M1, M2, M3 and M4 subtypes mediates the contraction of the rabbit iris sphincter. Naunyn Schmiedebergs Arch Pharmacol. 1992 Jun;345(6):611-8. [PubMed:1635586 ]
  2. Dorje F, Wess J, Lambrecht G, Tacke R, Mutschler E, Brann MR: Antagonist binding profiles of five cloned human muscarinic receptor subtypes. J Pharmacol Exp Ther. 1991 Feb;256(2):727-33. [PubMed:1994002 ]

Drug created on June 13, 2005 07:24 / Updated on October 02, 2017 04:36