biperiden indications/contra

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

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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 287.44 48.43 57 666 4384 3380752
Intentional self-injury 278.63 48.43 57 666 5128 3380008
Suicide attempt 224.92 48.43 59 664 15788 3369348
Sopor 211.41 48.43 43 680 3721 3381415
Intentional overdose 179.37 48.43 49 674 15176 3369960
Delirium 171.20 48.43 43 680 9585 3375551
Confusional state 154.35 48.43 54 669 37944 3347192
Overdose 132.87 48.43 47 676 33931 3351205
Coma 118.30 48.43 34 689 12518 3372618
Somnolence 116.17 48.43 42 681 32162 3352974
Altered state of consciousness 113.55 48.43 28 695 5730 3379406
Tachycardia 101.38 48.43 35 688 23336 3361800
Blood creatine phosphokinase increased 95.21 48.43 29 694 12984 3372152
Agitation 95.16 48.43 32 691 19674 3365462
Ileus paralytic 93.73 48.43 19 704 1589 3383547
Dyskinesia 92.68 48.43 25 698 7260 3377876
Megacolon 87.21 48.43 15 708 509 3384627
Aggression 85.94 48.43 26 697 11359 3373777
Drug abuse 85.44 48.43 29 694 18301 3366835
Tremor 84.01 48.43 32 691 28112 3357024
Drug interaction 71.43 48.43 33 690 46779 3338357
Intentional product misuse 70.72 48.43 23 700 12678 3372458
Rhabdomyolysis 69.78 48.43 24 699 15705 3369431
Restlessness 69.25 48.43 20 703 7418 3377718
Extrapyramidal disorder 67.66 48.43 17 706 3726 3381410
Colitis ischaemic 60.46 48.43 14 709 2174 3382962
Akathisia 57.72 48.43 14 709 2649 3382487
Schizophrenia 57.56 48.43 14 709 2680 3382456
Pyrexia 56.94 48.43 34 689 81081 3304055
Pneumonia aspiration 56.91 48.43 17 706 7071 3378065

Pharmacologic Action:

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SourceCodeDescription
ATC N04AA02 NERVOUS SYSTEM
ANTI-PARKINSON DRUGS
ANTICHOLINERGIC AGENTS
Tertiary amines
FDA EPC N0000175574 Anticholinergic
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 D001337 Autonomic 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

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Postencephalitic parkinsonism indication 19972008 DOID:14332
Parkinsonism indication 32798002 DOID:13548
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 DOID:12385
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:2527
Thyrotoxicosis contraindication 90739004 DOID:7997
Myasthenia gravis contraindication 91637004 DOID:437
Tardive dyskinesia contraindication 102449007
Dysentery contraindication 111939009 DOID:13250
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 DOID:2883
Retention of urine contraindication 267064002
Fever contraindication 386661006
Angle-closure glaucoma contraindication 392291006 DOID:13550
Pseudomembranous enterocolitis contraindication 397683000 DOID:0060185
Gastric ulcer contraindication 397825006 DOID:10808
Disorder of coronary artery contraindication 414024009

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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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:

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IDSource
4019635 VUID
N0000147728 NUI
C0005578 UMLSCUI
7128 IUPHAR_LIGAND_ID
D00779 KEGG_DRUG
09TD6C5147 UNII
7085-45-2 SECONDARY_CAS_RN
915 INN_ID
DB00810 DRUGBANK_ID
4019635 VANDF
N0000007878 NDFRT
N0000147728 NDFRT
001644 NDDF
1589 RXNORM
387359004 SNOMEDCT_US
65041000 SNOMEDCT_US
4285 MMSL
d00972 MMSL
CHEMBL1101 ChEMBL_ID
2381 PUBCHEM_CID
CHEMBL1201035 ChEMBL_ID
CHEMBL1201067 ChEMBL_ID
D001712 MESH_DESCRIPTOR_UI
C036432 MESH_SUPPLEMENTAL_RECORD_UI
CHEMBL3085495 ChEMBL_ID
CHEBI:3112 CHEBI

Pharmaceutical products:

None