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:

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

Approvals:

Date	Agency	Company	Orphan
Sept. 8, 1959	FDA	ABBVIE

FDA Adverse Event Reporting System (Female)

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	268.73	32	81	5327	11397	56275262
Suicide attempt	183.86	32	96	5312	57740	56228919
Drug interaction	150.91	32	139	5269	209616	56077043
Extrapyramidal disorder	123.60	32	46	5362	12310	56274349
Hyperprolactinaemia	117.32	32	33	5375	3628	56283031
Intentional overdose	114.90	32	75	5333	68042	56218617
Intentional self-injury	104.42	32	50	5358	24942	56261717
Psychotic symptom	101.14	32	24	5384	1345	56285314
Sopor	97.07	32	45	5363	20877	56265782
Salivary hypersecretion	92.14	32	32	5376	7018	56279641
Dyskinesia	91.44	32	48	5360	29060	56257599
Restlessness	89.71	32	46	5362	26540	56260119
Drug abuse	84.66	32	62	5346	67548	56219111
Delusion	84.54	32	34	5374	11181	56275478
Schizophrenia	79.73	32	32	5376	10467	56276192
Oromandibular dystonia	78.79	32	16	5392	431	56286228
Tremor	76.78	32	75	5333	121014	56165645
Akathisia	74.92	32	29	5379	8623	56278036
Logorrhoea	69.93	32	20	5388	2332	56284327
Inappropriate affect	63.32	32	15	5393	834	56285825
Dysarthria	62.85	32	42	5366	39508	56247151
Toxicity to various agents	60.56	32	90	5318	224474	56062185
Somnolence	58.32	32	75	5333	163338	56123321
Agitation	56.08	32	45	5363	55991	56230668
Dystonia	55.37	32	26	5382	12395	56274264
Parkinsonism	55.32	32	24	5384	9522	56277137
Persecutory delusion	55.22	32	17	5391	2553	56284106
Confabulation	54.29	32	11	5397	293	56286366
Hallucination, auditory	54.09	32	25	5383	11499	56275160
Altered state of consciousness	53.14	32	31	5377	22990	56263669
Sluggishness	52.66	32	19	5389	4649	56282010
Blood creatine phosphokinase increased	52.56	32	33	5375	27919	56258740
Negative symptoms in schizophrenia	50.74	32	9	5399	114	56286545
Muscle rigidity	49.62	32	23	5385	10648	56276011
Coma	49.52	32	43	5365	59612	56227047
Galactorrhoea	48.28	32	17	5391	3878	56282781
Psychomotor hyperactivity	48.27	32	22	5386	9798	56276861
Rhabdomyolysis	45.75	32	35	5373	40623	56246036
Urinary incontinence	43.61	32	30	5378	29555	56257104
Cogwheel rigidity	42.81	32	13	5395	1864	56284795
Rabbit syndrome	42.04	32	9	5399	315	56286344
Hyperammonaemic encephalopathy	40.86	32	13	5395	2172	56284487
Eosinophilic myocarditis	40.54	32	9	5399	374	56286285
Catatonia	40.50	32	15	5393	3949	56282710
Stupor	40.31	32	15	5393	4003	56282656
Blood prolactin increased	39.33	32	14	5394	3295	56283364
Reduced facial expression	39.09	32	12	5396	1784	56284875
Drug monitoring procedure incorrectly performed	36.23	32	7	5401	145	56286514
Accommodation disorder	35.33	32	8	5400	364	56286295
Resting tremor	34.82	32	9	5399	717	56285942
Serotonin syndrome	34.71	32	25	5383	26465	56260194
Distractibility	34.21	32	8	5400	420	56286239
Bradykinesia	34.11	32	14	5394	4840	56281819
Delirium	33.97	32	30	5378	42487	56244172
Parkinsonian gait	33.76	32	8	5400	445	56286214
Urinary retention	33.41	32	25	5383	28049	56258610
Fatigue	32.20	32	18	5390	788534	55498125
Depressed level of consciousness	32.09	32	33	5375	56400	56230259
Arthralgia	32.04	32	5	5403	501664	55784995

FDA Adverse Event Reporting System (Male)

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	248.61	26.85	101	6100	16768	31674375
Colitis ischaemic	169.16	26.85	58	6143	5994	31685149
Schizophrenia	159.97	26.85	65	6136	10765	31680378
Intentional self-injury	140.60	26.85	63	6138	13252	31677891
Extrapyramidal disorder	118.85	26.85	54	6147	11724	31679419
Salivary hypersecretion	115.83	26.85	47	6154	7745	31683398
Delusion	102.42	26.85	49	6152	11948	31679195
Sopor	98.06	26.85	47	6154	11505	31679638
Psychotic disorder	86.44	26.85	54	6147	22239	31668904
Dyskinesia	79.43	26.85	50	6151	20860	31670283
Akathisia	78.70	26.85	35	6166	7218	31683925
Sedation	71.15	26.85	45	6156	18920	31672223
Altered state of consciousness	69.27	26.85	46	6155	21005	31670138
Muscle rigidity	68.34	26.85	35	6166	9862	31681281
Blood creatine phosphokinase increased	65.77	26.85	59	6142	41915	31649228
Oropharyngeal spasm	64.95	26.85	13	6188	153	31690990
Restlessness	62.62	26.85	45	6156	23316	31667827
Depressed level of consciousness	59.96	26.85	54	6147	38547	31652596
Psychiatric symptom	59.79	26.85	23	6178	3288	31687855
Self-injurious ideation	59.51	26.85	19	6182	1568	31689575
Aggression	57.59	26.85	52	6149	37239	31653904
Pneumonia aspiration	52.07	26.85	50	6151	38676	31652467
Delirium	51.07	26.85	51	6150	41370	31649773
Parkinsonism	49.82	26.85	26	6175	7610	31683533
Stupor	49.06	26.85	19	6182	2765	31688378
Rhabdomyolysis	48.62	26.85	61	6140	63520	31627623
Persecutory delusion	48.48	26.85	18	6183	2334	31688809
Suicide attempt	48.03	26.85	47	6154	37201	31653942
Hallucination, auditory	47.60	26.85	28	6173	10332	31680811
Patient restraint	46.67	26.85	9	6192	86	31691057
Dysphagia	43.56	26.85	55	6146	57621	31633522
Ileus paralytic	42.84	26.85	21	6180	5387	31685756
Post-injection delirium sedation syndrome	41.97	26.85	11	6190	449	31690694
Postoperative respiratory failure	39.82	26.85	8	6193	96	31691047
Drug interaction	39.29	26.85	109	6092	208434	31482709
Psychomotor retardation	36.25	26.85	16	6185	3236	31687907
Psychomotor hyperactivity	35.84	26.85	22	6179	8765	31682378
Megacolon	35.44	26.85	13	6188	1629	31689514
Intentional overdose	35.33	26.85	42	6159	41347	31649796
Overdose	33.95	26.85	60	6141	84604	31606539
Tardive dyskinesia	33.63	26.85	18	6183	5541	31685602
Psychotic symptom	32.29	26.85	12	6189	1560	31689583
Shock	31.87	26.85	30	6171	22615	31668528
Polydipsia	31.84	26.85	15	6186	3525	31687618
Tension	29.48	26.85	12	6189	1989	31689154
Agitation	29.33	26.85	44	6157	54125	31637018
Drug screen false positive	28.77	26.85	9	6192	694	31690449
Sudden death	28.07	26.85	23	6178	14434	31676709
Tremor	27.88	26.85	52	6149	76368	31614775
Social avoidant behaviour	27.82	26.85	13	6188	3000	31688143
Fatigue	27.21	26.85	16	6185	335190	31355953

FDA Adverse Event Reporting System (Geriatric)

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	487.09	25.71	176	11268	25831	70891169
Intentional self-injury	230.21	25.71	109	11335	31541	70885459
Extrapyramidal disorder	226.54	25.71	95	11349	20655	70896345
Schizophrenia	224.94	25.71	89	11355	16679	70900321
Delusion	200.06	25.71	85	11359	19080	70897920
Salivary hypersecretion	196.01	25.71	75	11369	12850	70904150
Sopor	180.49	25.71	92	11352	31175	70885825
Suicide attempt	179.86	25.71	128	11316	79382	70837618
Dyskinesia	156.96	25.71	92	11352	40982	70876018
Colitis ischaemic	148.51	25.71	63	11381	14074	70902926
Drug interaction	145.45	25.71	237	11207	381204	70535796
Restlessness	144.44	25.71	88	11356	42040	70874960
Akathisia	139.91	25.71	58	11386	12235	70904765
Psychotic symptom	122.54	25.71	35	11409	2403	70914597
Altered state of consciousness	120.53	25.71	77	11367	39945	70877055
Blood creatine phosphokinase increased	118.96	25.71	90	11354	61173	70855827
Hyperprolactinaemia	109.94	25.71	37	11407	4376	70912624
Muscle rigidity	107.94	25.71	55	11389	18595	70898405
Persecutory delusion	101.29	25.71	35	11409	4482	70912518
Parkinsonism	99.91	25.71	49	11395	15276	70901724
Psychotic disorder	97.60	25.71	66	11378	37635	70879365
Hallucination, auditory	97.29	25.71	51	11393	18277	70898723
Intentional overdose	96.52	25.71	98	11346	98337	70818663
Tremor	96.38	25.71	122	11322	155502	70761498
Rhabdomyolysis	95.10	25.71	96	11348	95664	70821336
Agitation	87.98	25.71	91	11353	93284	70823716
Aggression	87.08	25.71	68	11376	48378	70868622
Delirium	85.66	25.71	81	11363	74533	70842467
Stupor	85.33	25.71	34	11410	6475	70910525
Pneumonia aspiration	83.97	25.71	74	11370	62215	70854785
Depressed level of consciousness	83.80	25.71	86	11358	87345	70829655
Psychomotor hyperactivity	79.22	25.71	42	11402	15391	70901609
Psychiatric symptom	74.41	25.71	31	11413	6613	70910387
Ileus paralytic	72.42	25.71	33	11411	8728	70908272
Dystonia	69.65	25.71	42	11402	19664	70897336
Sedation	67.99	25.71	58	11386	46673	70870327
Psychomotor retardation	65.67	25.71	27	11417	5571	70911429
Drug abuse	64.87	25.71	98	11346	147158	70769842
Oromandibular dystonia	63.50	25.71	17	11427	917	70916083
Somnolence	62.45	25.71	119	11325	215487	70701513
Self-injurious ideation	60.18	25.71	22	11422	3316	70913684
Oropharyngeal spasm	58.22	25.71	13	11431	325	70916675
Fatigue	57.31	25.71	31	11413	824288	70092712
Logorrhoea	55.70	25.71	22	11422	4092	70912908
Dysarthria	55.56	25.71	59	11385	62254	70854746
Arthralgia	54.91	25.71	8	11436	503382	70413618
Megacolon	53.94	25.71	20	11424	3136	70913864
Coma	53.64	25.71	70	11374	91774	70825226
Inappropriate affect	52.47	25.71	16	11428	1378	70915622
Nausea	51.05	25.71	38	11406	852050	70064950
Tardive dyskinesia	50.89	25.71	27	11417	9902	70907098
Catatonia	50.02	25.71	25	11419	8108	70908892
Treatment noncompliance	48.60	25.71	48	11396	46526	70870474
Headache	47.90	25.71	17	11427	580388	70336612
Patient restraint	47.50	25.71	9	11435	96	70916904
Post-injection delirium sedation syndrome	47.15	25.71	12	11432	530	70916470
Intentional product misuse	46.99	25.71	61	11383	79534	70837466
Social avoidant behaviour	46.40	25.71	20	11424	4636	70912364
Dysphagia	45.33	25.71	72	11372	112762	70804238
Overdose	44.63	25.71	90	11354	169655	70747345
Pain	44.59	25.71	23	11421	628793	70288207
Negative symptoms in schizophrenia	44.42	25.71	9	11435	139	70916861
Confabulation	43.83	25.71	11	11433	459	70916541
Blood prolactin increased	40.31	25.71	17	11427	3737	70913263
Bradykinesia	40.15	25.71	21	11423	7481	70909519
Mental impairment	39.44	25.71	28	11416	17227	70899773
Irritability	39.14	25.71	39	11405	38186	70878814
Sluggishness	38.72	25.71	19	11425	5924	70911076
Pain in extremity	38.71	25.71	4	11440	328078	70588922
Disorientation	38.32	25.71	47	11397	57876	70859124
Postoperative respiratory failure	37.82	25.71	8	11436	154	70916846
Urinary incontinence	37.63	25.71	38	11406	37804	70879196
Hyperammonaemic encephalopathy	37.55	25.71	17	11427	4426	70912574
Hypothermia	37.18	25.71	29	11415	20565	70896435
Intestinal pseudo-obstruction	37.03	25.71	14	11430	2316	70914684
Reduced facial expression	36.90	25.71	14	11430	2338	70914662
Eosinophilic myocarditis	36.79	25.71	11	11433	886	70916114
Sudden death	36.60	25.71	29	11415	21035	70895965
Rabbit syndrome	36.57	25.71	9	11435	346	70916654
Galactorrhoea	35.28	25.71	15	11429	3363	70913637
Drug monitoring procedure incorrectly performed	35.14	25.71	9	11435	408	70916592
Toxicity to various agents	34.28	25.71	137	11307	382035	70534965
Shock	33.78	25.71	37	11407	40388	70876612
Urinary retention	33.75	25.71	42	11402	52478	70864522
Asthenia	33.52	25.71	16	11428	457650	70459350
Accommodation disorder	33.08	25.71	9	11435	516	70916484
Refusal of treatment by patient	32.39	25.71	19	11425	8451	70908549
Hallucination, visual	32.02	25.71	31	11413	29306	70887694
Dysphoria	31.16	25.71	15	11429	4483	70912517
Mutism	31.06	25.71	12	11432	2104	70914896
Leukocytosis	30.90	25.71	35	11409	39633	70877367
Cogwheel rigidity	30.40	25.71	13	11431	2955	70914045
Distractibility	30.21	25.71	9	11435	716	70916284
Dyspnoea	29.90	25.71	49	11395	770011	70146989
Drug level increased	29.82	25.71	33	11411	36436	70880564
Akinesia	29.73	25.71	13	11431	3118	70913882
Disorganised speech	29.27	25.71	11	11433	1790	70915210
Faecaloma	28.72	25.71	19	11425	10432	70906568
Medication error	28.09	25.71	40	11404	56872	70860128
Back pain	27.97	25.71	5	11439	271147	70645853
Electrocardiogram QT prolonged	27.79	25.71	49	11395	83468	70833532
White blood cell count increased	27.38	25.71	44	11400	69529	70847471
Polydipsia	27.11	25.71	15	11429	5973	70911027
Disturbance in attention	27.08	25.71	34	11410	42860	70874140
Drug screen false positive	27.07	25.71	9	11435	1024	70915976
Neutrophil count increased	26.81	25.71	27	11417	26768	70890232
Thinking abnormal	26.27	25.71	19	11425	12032	70904968
Inappropriate antidiuretic hormone secretion	26.17	25.71	25	11419	23251	70893749
Electrocardiogram J wave	25.92	25.71	5	11439	59	70916941

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N04AA02	NERVOUS SYSTEM ANTI-PARKINSON DRUGS ANTICHOLINERGIC AGENTS Tertiary amines
FDA MoA	N0000175370	Cholinergic Antagonists
FDA EPC	N0000175574	Anticholinergic
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
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

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

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
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

🐶 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:

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

External reference:

ID	Source
4019635	VUID
N0000147728	NUI
D00779	KEGG_DRUG
151311	RXNORM
4018474	VANDF
4018475	VANDF
4019635	VANDF
C0005578	UMLSCUI
CHEBI:3112	CHEBI
CHEMBL1101	ChEMBL_ID
CHEMBL1201035	ChEMBL_ID
CHEMBL1201067	ChEMBL_ID
DB00810	DRUGBANK_ID
D001712	MESH_DESCRIPTOR_UI
2381	PUBCHEM_CID
7128	IUPHAR_LIGAND_ID
C036432	MESH_SUPPLEMENTAL_RECORD_UI
915	INN_ID
1235-82-1	SECONDARY_CAS_RN
7085-45-2	SECONDARY_CAS_RN
0FRP6G56LD	UNII
4285	MMSL
d00972	MMSL
001644	NDDF
001645	NDDF
001646	NDDF
10020007	SNOMEDCT_US
387359004	SNOMEDCT_US
61742009	SNOMEDCT_US
65041000	SNOMEDCT_US

Pharmaceutical products:

None