trihexyphenidyl ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
vasodilators 2745 144-11-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • trihexyphenidyl
  • trihexyphenidyl hydrochloride
  • benzhexol
  • benzhexol hydrochloride
  • trihexyphenidyl HCl
  • benzhexol HCl
One of the centrally acting MUSCARINIC ANTAGONISTS used for treatment of PARKINSONIAN DISORDERS and drug-induced extrapyramidal movement disorders and as an antispasmodic.
  • Molecular weight: 301.47
  • Formula: C20H31NO
  • CLOGP: 5.15
  • LIPINSKI: 1
  • HAC: 2
  • HDO: 1
  • TPSA: 23.47
  • ALOGS: -4.98
  • ROTB: 5

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 10 mg/mL Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.63 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
May 13, 1949 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dystonia 101.18 26.66 35 3336 13784 63471867
Dyskinesia 88.27 26.66 40 3331 31962 63453689
Coma 77.28 26.66 46 3325 64318 63421333
Extrapyramidal disorder 64.99 26.66 25 3346 13259 63472392
Parkinsonism 59.61 26.66 22 3349 10417 63475234
Muscle rigidity 57.53 26.66 22 3349 11478 63474173
Myoclonus 53.97 26.66 23 3348 15845 63469806
Drug interaction 53.16 26.66 63 3308 229068 63256583
Neuroleptic malignant syndrome 53.01 26.66 21 3350 12035 63473616
Tardive dyskinesia 48.84 26.66 18 3353 8484 63477167
Somnolence 47.95 26.66 53 3318 178632 63307019
Apraxia 45.97 26.66 12 3359 1809 63483842
Hyperchloraemia 45.14 26.66 10 3361 753 63484898
Tremor 43.98 26.66 44 3327 132195 63353456
Hypernatraemia 43.30 26.66 16 3355 7593 63478058
Hyperreflexia 43.29 26.66 15 3356 5919 63479732
Perseveration 42.47 26.66 8 3363 267 63485384
Urinary retention 39.86 26.66 23 3348 30278 63455373
Suicide attempt 37.94 26.66 29 3342 60889 63424762
Transient aphasia 33.35 26.66 5 3366 39 63485612
Intentional overdose 32.94 26.66 29 3342 74123 63411528
Onychophagia 30.55 26.66 5 3366 72 63485579
Disorientation 29.56 26.66 21 3350 39431 63446220
Hallucination, auditory 29.04 26.66 14 3357 12810 63472841
Drug screen false positive 28.09 26.66 7 3364 877 63484774
Electrocardiogram QT prolonged 27.88 26.66 24 3347 59506 63426145
Oculogyric crisis 27.88 26.66 8 3363 1713 63483938
Hallucination 27.52 26.66 23 3348 54794 63430857
Mental disorder 27.15 26.66 17 3354 25902 63459749
Ataxia 26.79 26.66 14 3357 15181 63470470

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Neuroleptic malignant syndrome 120.68 24.10 57 5124 17877 34933873
Coma 119.91 24.10 78 5103 45600 34906150
Wrong patient received product 118.12 24.10 34 5147 2620 34949130
Cerebral artery thrombosis 93.63 24.10 22 5159 758 34950992
Brain scan abnormal 90.99 24.10 22 5159 858 34950892
Hallucination 90.91 24.10 69 5112 51429 34900321
Extrapyramidal disorder 89.89 24.10 42 5139 12838 34938912
Failure to suspend medication 77.75 24.10 17 5164 421 34951329
Dystonia 77.64 24.10 36 5145 10809 34940941
Areflexia 68.02 24.10 23 5158 3008 34948742
Somnolence 66.52 24.10 82 5099 111034 34840716
Tardive dyskinesia 60.21 24.10 25 5156 5765 34945985
Respiratory distress 56.81 24.10 45 5136 35620 34916130
Parkinsonism 49.03 24.10 24 5157 8114 34943636
Accidental death 48.74 24.10 17 5164 2439 34949311
Pneumonia aspiration 42.71 24.10 41 5140 41862 34909888
Rhabdomyolysis 41.84 24.10 51 5130 68112 34883638
Hemiplegia 40.33 24.10 20 5161 6952 34944798
Cerebral amyloid angiopathy 39.55 24.10 8 5173 134 34951616
Dyskinesia 37.22 24.10 29 5152 22384 34929366
Disease recurrence 36.11 24.10 28 5153 21462 34930288
Facial paralysis 34.81 24.10 21 5160 10713 34941037
Ischaemic stroke 33.35 24.10 25 5156 18225 34933525
Toxicity to various agents 33.33 24.10 84 5097 200278 34751472
Drug abuse 32.47 24.10 55 5126 99041 34852709
Miosis 31.82 24.10 19 5162 9516 34942234
Salivary gland cancer stage IV 28.82 24.10 5 5176 34 34951716
Antipsychotic drug level increased 28.18 24.10 13 5168 3852 34947898
Spleen congestion 28.12 24.10 7 5174 308 34951442
Neutrophil count increased 28.06 24.10 22 5159 17124 34934626
Catatonia 27.83 24.10 14 5167 5011 34946739
Prothrombin level decreased 27.05 24.10 9 5172 1119 34950631
Faecaloma 26.94 24.10 14 5167 5363 34946387
Delusion 26.93 24.10 19 5162 12616 34939134
Bezoar 26.82 24.10 9 5172 1148 34950602
Akathisia 26.64 24.10 16 5165 8093 34943657
Compulsive shopping 26.39 24.10 7 5174 397 34951353
Delirium 25.49 24.10 32 5149 43959 34907791
Portal tract inflammation 25.17 24.10 5 5176 76 34951674
Psychotic disorder 25.04 24.10 24 5157 24428 34927322
Unmasking of previously unidentified disease 24.77 24.10 8 5173 906 34950844
Sexually inappropriate behaviour 24.75 24.10 7 5174 505 34951245
Dysarthria 24.59 24.10 28 5153 34754 34916996

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Coma 188.47 21.24 121 8017 100528 79635722
Neuroleptic malignant syndrome 167.83 21.24 73 8065 27486 79708764
Dystonia 164.83 21.24 67 8071 21332 79714918
Extrapyramidal disorder 154.35 21.24 65 8073 22614 79713636
Dyskinesia 115.04 21.24 66 8072 44707 79691543
Parkinsonism 107.73 21.24 46 8092 16538 79719712
Tardive dyskinesia 98.51 21.24 38 8100 10533 79725717
Hallucination 97.31 21.24 76 8062 85669 79650581
Somnolence 96.16 21.24 120 8018 238861 79497389
Wrong patient received product 86.89 21.24 28 8110 4590 79731660
Brain scan abnormal 86.79 21.24 21 8117 1202 79735048
Cerebral artery thrombosis 83.59 21.24 20 8118 1091 79735159
Failure to suspend medication 76.89 21.24 16 8122 458 79735792
Rhabdomyolysis 69.60 21.24 68 8070 103063 79633187
Muscle rigidity 66.77 21.24 35 8103 19847 79716403
Drug abuse 62.65 21.24 80 8058 162611 79573639
Pneumonia aspiration 60.49 21.24 52 8086 66915 79669335
Areflexia 59.17 21.24 22 8116 5512 79730738
Oculogyric crisis 55.94 21.24 18 8120 2934 79733316
Tremor 55.29 21.24 77 8061 170006 79566244
Respiratory distress 54.11 21.24 46 8092 58293 79677957
Drug interaction 53.03 21.24 125 8013 415058 79321192
Hypernatraemia 50.12 21.24 26 8112 14425 79721825
Suicide attempt 49.18 21.24 51 8087 82881 79653369
Catatonia 46.22 21.24 21 8117 8735 79727515
Salivary hypersecretion 44.81 21.24 24 8114 14200 79722050
Poisoning deliberate 43.69 21.24 26 8112 18802 79717448
Accidental death 42.03 21.24 16 8122 4275 79731975
Delirium 41.35 21.24 47 8091 84580 79651670
Psychotic disorder 41.18 21.24 34 8104 41368 79694882
Akathisia 40.73 21.24 22 8116 13237 79723013
Delusion 39.23 21.24 25 8113 20398 79715852
Hallucination, auditory 38.93 21.24 25 8113 20668 79715582
Disorientation 37.92 21.24 39 8099 62737 79673513
Faecaloma 37.80 21.24 20 8118 11544 79724706
Antipsychotic drug level increased 36.95 21.24 16 8122 5941 79730309
Pain 36.82 21.24 13 8125 703789 79032461
Diarrhoea 35.79 21.24 23 8115 880466 78855784
Urinary retention 35.69 21.24 36 8102 56594 79679656
Cerebral amyloid angiopathy 35.40 21.24 8 8130 339 79735911
Neutrophil count increased 35.36 21.24 27 8111 29369 79706881
Hyperchloraemia 34.83 21.24 10 8128 1111 79735139
Myoclonus 34.59 21.24 26 8112 27634 79708616
Perseveration 34.33 21.24 8 8130 389 79735861
Apraxia 32.87 21.24 12 8126 2855 79733395
White blood cell count increased 32.37 21.24 39 8099 74594 79661656
Abnormal behaviour 32.30 21.24 28 8110 36393 79699857
Miosis 32.01 21.24 20 8118 15769 79720481
Hyperreflexia 31.73 21.24 16 8122 8369 79727881
Agitation 30.67 21.24 44 8094 99671 79636579
Hemiplegia 30.48 21.24 19 8119 14920 79721330
Toxicity to various agents 30.17 21.24 103 8035 421437 79314813
Disease recurrence 29.56 21.24 29 8109 44080 79692170
Facial paralysis 29.03 21.24 21 8117 21051 79715199
Ischaemic stroke 28.43 21.24 25 8113 33106 79703144
Fatigue 28.35 21.24 32 8106 929695 78806555
Spleen congestion 28.17 21.24 7 8131 447 79735803
Salivary gland cancer stage IV 27.62 21.24 5 8133 67 79736183
Hyperammonaemia 27.52 21.24 16 8122 11077 79725173
Schizophrenia 27.44 21.24 18 8120 15422 79720828
Prothrombin level decreased 27.01 21.24 9 8129 1635 79734615
Sexually inappropriate behaviour 26.91 21.24 7 8131 538 79735712
Hallucination, visual 26.70 21.24 24 8114 32705 79703545
Bezoar 26.24 21.24 10 8128 2678 79733572
Respiratory depression 26.04 21.24 22 8116 27608 79708642
Arthralgia 25.96 21.24 13 8125 571790 79164460
Sudden death 25.60 21.24 20 8118 22491 79713759
Dysarthria 25.58 21.24 33 8105 67589 79668661
Onychophagia 25.51 21.24 5 8133 105 79736145
Psychiatric symptom 25.38 21.24 13 8125 7022 79729228
Cognitive disorder 24.71 21.24 33 8105 69893 79666357
Portal tract inflammation 24.64 21.24 5 8133 126 79736124
Disturbance in attention 24.44 21.24 28 8110 50773 79685477
On and off phenomenon 24.43 21.24 10 8128 3230 79733020
Drug ineffective for unapproved indication 24.25 21.24 28 8110 51210 79685040
Bradykinesia 23.74 21.24 13 8125 8030 79728220
Ataxia 23.73 21.24 20 8118 25019 79711231
Persecutory delusion 23.49 21.24 11 8127 4898 79731352
Intentional overdose 23.19 21.24 40 8098 105920 79630330
Parkinsonian gait 23.07 21.24 7 8131 941 79735309
Confusional state 22.98 21.24 78 8060 317919 79418331
Psychomotor skills impaired 22.81 21.24 11 8127 5226 79731024
Headache 22.76 21.24 20 8118 653752 79082498
Labelled drug-disease interaction issue 22.58 21.24 4 8134 47 79736203
Altered state of consciousness 22.52 21.24 25 8113 43797 79692453
Impulse-control disorder 22.49 21.24 8 8130 1766 79734484
Electrocardiogram QT prolonged 22.29 21.24 36 8102 90350 79645900
Fanconi syndrome 22.17 21.24 9 8129 2847 79733403
Drug screen false positive 21.99 21.24 7 8131 1102 79735148
Pneumoconiosis 21.46 21.24 5 8133 243 79736007
Unmasking of previously unidentified disease 21.34 21.24 8 8130 2049 79734201
Macroprolactinaemia 21.28 21.24 3 8135 6 79736244
Choking 21.24 21.24 14 8124 12087 79724163

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N04AA01 NERVOUS SYSTEM
ANTI-PARKINSON DRUGS
ANTICHOLINERGIC AGENTS
Tertiary amines
MeSH PA D018726 Anti-Dyskinesia Agents
MeSH PA D000978 Antiparkinson Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D018727 Muscarinic Antagonists
MeSH PA D018377 Neurotransmitter Agents

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Postencephalitic parkinsonism indication 19972008 DOID:14332
Parkinsonism indication 32798002
Parkinson's disease indication 49049000 DOID:14330
Extrapyramidal disease indication 76349003
Arteriosclerotic Parkinsonism indication
Urinary tract obstruction contraindication 7163005 DOID:5200
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Severe chronic ulcerative colitis contraindication 14311001
Disorder of autonomic nervous system contraindication 15241006
Toxic megacolon contraindication 28536002 DOID:1770
Atony of colon contraindication 29479008
Shigellosis contraindication 36188001
Hypertensive disorder contraindication 38341003 DOID:10763
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Achalasia of esophagus contraindication 45564002 DOID:9164
Chronic heart failure contraindication 48447003
Dysuria contraindication 49650001
Paralytic ileus contraindication 55525008 DOID:8442
Ulcerative colitis contraindication 64766004 DOID:8577
Hiatal hernia contraindication 84089009 DOID:12642
Open-angle glaucoma contraindication 84494001 DOID:1067
Kidney disease contraindication 90708001 DOID:557
Thyrotoxicosis contraindication 90739004 DOID:7997
Myasthenia gravis contraindication 91637004 DOID:437
Tardive dyskinesia contraindication 102449007
Dysentery contraindication 111939009
Gastrointestinal obstruction contraindication 126765001
Bleeding contraindication 131148009
Gastroesophageal reflux disease contraindication 235595009 DOID:8534
Disease of liver contraindication 235856003 DOID:409
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Fever contraindication 386661006
Angle-closure glaucoma contraindication 392291006 DOID:13550
Pseudomembranous enterocolitis contraindication 397683000
Gastric ulcer contraindication 397825006 DOID:10808
Disorder of coronary artery contraindication 414024009




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.23 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Muscarinic acetylcholine receptor M1 GPCR ANTAGONIST IC50 8.89 CHEMBL CHEMBL
Muscarinic acetylcholine receptor M2 GPCR IC50 7.73 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 7.35 DRUG MATRIX
Muscarinic acetylcholine receptor M4 GPCR IC50 8.17 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR IC50 7.99 CHEMBL
Cytochrome P450 2D6 Enzyme IC50 5.61 DRUG MATRIX
Muscarinic acetylcholine receptor M3 GPCR IC50 7.58 CHEMBL

External reference:

IDSource
4019959 VUID
N0000148044 NUI
D00787 KEGG_DRUG
52-49-3 SECONDARY_CAS_RN
4017900 VANDF
4019959 VANDF
C0041009 UMLSCUI
CHEBI:9720 CHEBI
CHEMBL1490 ChEMBL_ID
DB00376 DRUGBANK_ID
CHEMBL1092 ChEMBL_ID
D014282 MESH_DESCRIPTOR_UI
5572 PUBCHEM_CID
7315 IUPHAR_LIGAND_ID
1318 INN_ID
6RC5V8B7PO UNII
10811 RXNORM
2986 MMSL
5628 MMSL
d00970 MMSL
001641 NDDF
004664 NDDF
2190009 SNOMEDCT_US
387120000 SNOMEDCT_US
387336005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0121-0658 SOLUTION 2 mg ORAL ANDA 23 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0121-0658 SOLUTION 2 mg ORAL ANDA 23 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0121-0658 SOLUTION 2 mg ORAL ANDA 23 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-5335 TABLET 2 mg ORAL ANDA 9 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-5337 TABLET 5 mg ORAL ANDA 9 sections
Trihexyphenidyl hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-0675 TABLET 2 mg ORAL ANDA 9 sections
Trihexyphenidyl hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-0676 TABLET 5 mg ORAL ANDA 9 sections
Trihexyphenidyl Hydrochloride Human Prescription Drug Label 1 16571-160 TABLET 2 mg ORAL ANDA 21 sections
Trihexyphenidyl Hydrochloride Human Prescription Drug Label 1 16571-161 TABLET 5 mg ORAL ANDA 21 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50090-2994 TABLET 2 mg ORAL ANDA 9 sections
TRIHEXYPHENIDYL HYDROCHLORIDE Human Prescription Drug Label 1 50090-5205 TABLET 5 mg ORAL ANDA 10 sections
TRIHEXYPHENIDYL HYDROCHLORIDE Human Prescription Drug Label 1 50090-5205 TABLET 5 mg ORAL ANDA 10 sections
TRIHEXYPHENIDYL HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 51407-265 TABLET 2 mg ORAL ANDA 10 sections
TRIHEXYPHENIDYL HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 51407-265 TABLET 2 mg ORAL ANDA 10 sections
TRIHEXYPHENIDYL HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 51407-265 TABLET 2 mg ORAL ANDA 10 sections
TRIHEXYPHENIDYL HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 51407-266 TABLET 5 mg ORAL ANDA 10 sections
TRIHEXYPHENIDYL HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 51407-266 TABLET 5 mg ORAL ANDA 10 sections
TRIHEXYPHENIDYL HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 51407-266 TABLET 5 mg ORAL ANDA 10 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 53808-0633 TABLET 2 mg ORAL ANDA 10 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 53808-0634 TABLET 5 mg ORAL ANDA 10 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 53808-0696 TABLET 5 mg ORAL ANDA 9 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 54738-554 TABLET 2 mg ORAL ANDA 10 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 54738-555 TABLET 5 mg ORAL ANDA 10 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 61748-054 SYRUP 2 mg ORAL ANDA 21 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 61748-054 SYRUP 2 mg ORAL ANDA 21 sections
Trihexyphenidyl Hydrochloride Human Prescription Drug Label 1 63850-0021 TABLET 2 mg ORAL ANDA 19 sections
Trihexyphenidyl Hydrochloride Human Prescription Drug Label 1 63850-0022 TABLET 5 mg ORAL ANDA 19 sections
Trihexyphenidyl Hydrochloride Human Prescription Drug Label 1 64725-0161 TABLET 5 mg ORAL ANDA 20 sections
Trihexyphenidyl Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68151-2782 TABLET 2 mg ORAL ANDA 9 sections
Trihexyphenidyl Hydrochloride Human Prescription Drug Label 1 69452-241 TABLET 2 mg ORAL ANDA 20 sections