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biperiden 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	374	514-65-8

Description:

Molecule	Description
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 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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

Status: OFM

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

Drug dosage:

Dose	Unit	Route
10	mg	O
10	mg	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	30 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	24 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	12 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	12 L/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	1 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.64 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.10 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Sept. 8, 1959	FDA	ABBVIE

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Neuroleptic malignant syndrome	292.22	30.17	87	5894	11969	63471072
Suicide attempt	180.87	30.17	96	5885	60822	63422219
Intentional overdose	152.77	30.17	92	5889	74060	63408981
Drug interaction	146.41	30.17	141	5840	228990	63254051
Intentional self-injury	135.34	30.17	60	5921	25627	63457414
Hyperprolactinaemia	120.40	30.17	34	5947	3866	63479175
Salivary hypersecretion	117.42	30.17	39	5942	7627	63475414
Restlessness	109.29	30.17	54	5927	29399	63453642
Drug abuse	107.13	30.17	73	5908	72445	63410596
Psychotic symptom	103.59	30.17	25	5956	1536	63481505

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Neuroleptic malignant syndrome	254.75	27.75	104	6600	17830	34932397
Colitis ischaemic	166.43	27.75	58	6646	6417	34943810
Schizophrenia	157.10	27.75	60	6644	8606	34941621
Intentional self-injury	117.89	27.75	56	6648	13715	34936512
Salivary hypersecretion	115.37	27.75	48	6656	8596	34941631
Delusion	103.94	27.75	50	6654	12585	34937642
Extrapyramidal disorder	97.04	27.75	48	6656	12832	34937395
Sopor	96.73	27.75	47	6657	12089	34938138
Psychotic disorder	85.29	27.75	55	6649	24397	34925830
Suicide attempt	74.56	27.75	61	6643	39055	34911172

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Neuroleptic malignant syndrome	518.06	24.32	185	12154	27374	79704675
Schizophrenia	224.85	24.32	86	12253	15354	79716695
Salivary hypersecretion	220.75	24.32	83	12256	14141	79717908
Intentional self-injury	216.71	24.32	104	12235	32315	79699734
Suicide attempt	210.45	24.32	141	12198	82791	79649258
Delusion	201.56	24.32	86	12253	20337	79711712
Extrapyramidal disorder	186.51	24.32	84	12255	22595	79709454
Sopor	179.39	24.32	92	12247	32918	79699131
Colitis ischaemic	162.61	24.32	68	12271	15291	79716758
Restlessness	142.34	24.32	89	12250	46403	79685646

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N04AA02	NERVOUS SYSTEM ANTI-PARKINSON DRUGS ANTICHOLINERGIC AGENTS Tertiary amines
CHEBI has role	CHEBI:48407	antiparkinson agent
CHEBI has role	CHEBI:48876	muscarinic antagonists
CHEBI has role	CHEBI:50370	parasympatholytics
CHEBI has role	CHEBI:66956	antidyskinetic agent
FDA EPC	N0000175574	Anticholinergic
FDA MoA	N0000175370	Cholinergic Antagonists
MeSH PA	D018726	Anti-Dyskinesia Agents
MeSH PA	D000978	Antiparkinson Agents
MeSH PA	D002491	Central Nervous System Agents

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

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Disease	Relation	SNOMED_ID	DOID
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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN	ANTAGONIST	Kd	9.32	IUPHAR	CHEMBL
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN	ANTAGONIST	Kd	8.20	IUPHAR
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN	ANTAGONIST	Kd	8.41	IUPHAR
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN	ANTAGONIST	Kd	8.62	IUPHAR
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	8.20	PDSP
Neuronal acetylcholine receptor subunit alpha-2	Ion channel	Q15822	ACHA2_HUMAN				WOMBAT-PK

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External reference:

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ID	Source
001644	NDDF
001645	NDDF
001646	NDDF
0FRP6G56LD	UNII
10020007	SNOMEDCT_US
1235-82-1	SECONDARY_CAS_RN
151311	RXNORM
2381	PUBCHEM_CID
387359004	SNOMEDCT_US
4018474	VANDF

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Pharmaceutical products:

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