biperiden Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
374 514-65-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • biperiden
  • akineton
  • biperiden hydrochloride
  • biperiden lactate
  • biperiden HCl
A 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.
  • Molecular weight: 311.47
  • Formula: C21H29NO
  • CLOGP: 4.94
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 23.47
  • ALOGS: -4.86
  • ROTB: 5

Drug dosage:

DoseUnitRoute
10 mg O
10 mg P

Approvals:

DateAgencyCompanyOrphan
Sept. 8, 1959 FDA ABBVIE

FDA Adverse Event Reporting System

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 480.71 58.58 93 961 5654 4632284
Intentional self-injury 346.44 58.58 74 980 7309 4630629
Suicide attempt 298.41 58.58 80 974 20762 4617176
Intentional overdose 276.21 58.58 76 978 21690 4616248
Delirium 255.25 58.58 64 990 12688 4625250
Sopor 241.97 58.58 54 1000 6472 4631466
Confusional state 204.19 58.58 73 981 48761 4589177
Dyskinesia 172.60 58.58 44 1010 9231 4628707
Coma 162.28 58.58 48 1006 17471 4620467
Disorientation 150.49 58.58 42 1012 12417 4625521
Somnolence 140.58 58.58 54 1000 43606 4594332
Tremor 139.09 58.58 51 1003 36208 4601730
Agitation 138.91 58.58 46 1008 24154 4613784
Extrapyramidal disorder 127.83 58.58 31 1023 5275 4632663
Ileus paralytic 122.19 58.58 25 1029 1956 4635982
Blood creatine phosphokinase increased 120.83 58.58 37 1017 15062 4622876
Overdose 115.98 58.58 47 1007 43512 4594426
Restlessness 114.58 58.58 32 1022 9437 4628501
Altered state of consciousness 110.59 58.58 30 1024 7941 4629997
Drug abuse 98.49 58.58 37 1017 27910 4610028
Drug interaction 95.18 58.58 46 1008 64462 4573476
Megacolon 94.77 58.58 17 1037 657 4637281
Logorrhoea 93.80 58.58 18 1036 1010 4636928
Intentional product misuse 89.58 58.58 31 1023 18462 4619476
Urinary incontinence 89.50 58.58 25 1029 7355 4630583
Inappropriate affect 87.45 58.58 15 1039 445 4637493
Fall 86.88 58.58 46 1008 78000 4559938
Tachycardia 84.08 58.58 34 1020 31111 4606827
Aggression 81.87 58.58 27 1027 13872 4624066
Hyponatraemia 80.78 58.58 31 1023 24699 4613239
Rhabdomyolysis 80.29 58.58 29 1025 19529 4618409
Condition aggravated 78.29 58.58 39 1015 58132 4579806
Sedation 74.97 58.58 22 1032 7695 4630243
Psychotic disorder 71.79 58.58 23 1031 10772 4627166
Pyrexia 70.78 58.58 45 1009 107099 4530839
Parkinsonism 68.21 58.58 17 1037 3216 4634722
Inappropriate antidiuretic hormone secretion 67.28 58.58 18 1036 4496 4633442
Hallucination, auditory 67.10 58.58 18 1036 4543 4633395
Colitis ischaemic 65.88 58.58 16 1038 2719 4635219
Salivary hypersecretion 64.75 58.58 16 1038 2921 4635017
Muscle rigidity 64.67 58.58 17 1037 3970 4633968
Dysphagia 62.46 58.58 26 1028 25505 4612433
Disorganised speech 60.81 58.58 10 1044 228 4637710
Mydriasis 60.71 58.58 16 1038 3772 4634166

Pharmacologic Action:

SourceCodeDescription
ATC N04AA02 NERVOUS SYSTEM
ANTI-PARKINSON DRUGS
ANTICHOLINERGIC AGENTS
Tertiary amines
CHEBI has role CHEBI:136860 antidote to sarin poisoning
CHEBI has role CHEBI:66956 antidyskinesia agent
CHEBI has role CHEBI:48876 muscarinic antagonist
CHEBI has role CHEBI:50370 parasympatholytic
CHEBI has role CHEBI:48407 antiparkinson drug
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
MeSH PA D010276 Parasympatholytics
MeSH PA D018373 Peripheral Nervous System Agents
FDA EPC N0000175574 Anticholinergic

Drug Use (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

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.2 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 Kd 9.32 IUPHAR CHEMBL
Muscarinic acetylcholine receptor M5 GPCR Ki 8.20 PDSP
Neuronal acetylcholine receptor subunit alpha-2 Ion channel WOMBAT-PK
Muscarinic acetylcholine receptor M2 GPCR ANTAGONIST Kd 8.20 IUPHAR
Muscarinic acetylcholine receptor M3 GPCR ANTAGONIST Kd 8.41 IUPHAR
Muscarinic acetylcholine receptor M4 GPCR ANTAGONIST Kd 8.62 IUPHAR

External reference:

IDSource
D001712 MESH_DESCRIPTOR_UI
4019635 VUID
N0000147728 NUI
C0005578 UMLSCUI
D00779 KEGG_DRUG
09TD6C5147 UNII
7085-45-2 SECONDARY_CAS_RN
915 INN_ID
65041000 SNOMEDCT_US
4019635 VANDF
001644 NDDF
1589 RXNORM
387359004 SNOMEDCT_US
4285 MMSL
d00972 MMSL
CHEMBL1101 ChEMBL_ID
DB00810 DRUGBANK_ID
CHEBI:3112 CHEBI
7128 IUPHAR_LIGAND_ID
2381 PUBCHEM_CID
CHEMBL1201035 ChEMBL_ID
CHEMBL1201067 ChEMBL_ID
C036432 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None