biperiden 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
10 mg O
10 mg P

ADMET properties:

PropertyValueReference
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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.594 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.899 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 28.576 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 28.576 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 12.400 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 23.610 % High 1
herg hERG pIC50 5.367 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 6.266 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 17.947 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 11.250 % High 1
kinase-safety-class ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK 42
kinase-selectivity-class AXL,CAMK2D,CDK4,EIF2AK3,EPHB4,GRK2,PDK4,SIK2,STK33 9
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 0.564 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.350 High 1
mh-clint Mouse hepatocyte intrinsic clearance 74.645 High 1
mppb Mouse plasma protein binding (% unbound) 11.390 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.710 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 22.830 % High 1
rat-kpuu-brain Rat brain Kpuu 0.352 % High 1
rh-clint Rat hepatocyte intrinsic clearance 249.459 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 37.330 % High 1
rppb Rat plasma protein binding (% unbound) 14.600 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 544.503 uM High 1

Approvals:

DateAgencyCompanyOrphan
Sept. 8, 1959 FDA ABBVIE

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
Neuroleptic malignant syndrome 412.81 30.79 115 7026 14981 90606325
Suicide attempt 211.90 30.79 108 7033 75291 90546015
Extrapyramidal disorder 203.49 30.79 68 7073 16235 90605071
Drug interaction 198.49 30.79 168 6973 276285 90345021
Intentional overdose 176.35 30.79 103 7038 93731 90527575
Intentional self-injury 144.50 30.79 62 7079 29272 90592034
Hyperprolactinaemia 142.03 30.79 40 7101 5393 90615913
Akathisia 141.03 30.79 47 7094 11112 90610194
Psychotic symptom 129.25 30.79 31 7110 2225 90619081
Sopor 121.07 30.79 52 7089 24592 90596714
Drug abuse 120.32 30.79 77 7064 82270 90539036
Dyskinesia 119.27 30.79 58 7083 36476 90584830
Salivary hypersecretion 117.71 30.79 39 7102 9053 90612253
Schizophrenia 116.71 30.79 44 7097 14870 90606436
Restlessness 114.48 30.79 56 7085 35664 90585642
Somnolence 110.25 30.79 107 7034 208977 90412329
Delusion 98.12 30.79 38 7103 13802 90607504
Muscle rigidity 96.89 30.79 38 7103 14271 90607035
Altered state of consciousness 93.81 30.79 47 7094 31485 90589821
Toxicity to various agents 93.34 30.79 114 7027 287732 90333574
Hallucination, auditory 92.84 30.79 38 7103 15937 90605369
Tremor 91.41 30.79 84 7057 153089 90468217
Oromandibular dystonia 83.03 30.79 17 7124 586 90620720
Dystonia 77.72 30.79 34 7107 16785 90604521
Blood creatine phosphokinase increased 76.35 30.79 42 7099 33981 90587325
Coma 73.09 30.79 54 7087 72578 90548728
Logorrhoea 70.91 30.79 20 7121 2707 90618599
Agitation 67.77 30.79 50 7091 67048 90554258
Persecutory delusion 67.70 30.79 20 7121 3188 90618118
Dysarthria 65.15 30.79 45 7096 54437 90566869
Inappropriate affect 63.46 30.79 15 7126 1010 90620296
Rhabdomyolysis 62.85 30.79 43 7098 51213 90570093
Confabulation 62.02 30.79 12 7129 308 90620998
Parkinsonism 60.37 30.79 27 7114 14038 90607268
Galactorrhoea 60.30 30.79 20 7121 4652 90616654
Psychomotor hyperactivity 59.52 30.79 26 7115 12787 90608519
Mental impairment 55.91 30.79 27 7114 16693 90604613
Sluggishness 55.53 30.79 20 7121 5939 90615367
Resting tremor 55.08 30.79 13 7128 870 90620436
Reduced facial expression 54.24 30.79 16 7125 2537 90618769
Bradykinesia 52.99 30.79 20 7121 6768 90614538
Negative symptoms in schizophrenia 51.95 30.79 9 7132 122 90621184
Blood prolactin increased 48.66 30.79 16 7125 3621 90617685
Cogwheel rigidity 48.30 30.79 14 7127 2088 90619218
Urinary incontinence 47.20 30.79 32 7109 37534 90583772
Pneumonia aspiration 44.71 30.79 32 7109 40908 90580398
Treatment noncompliance 44.40 30.79 35 7106 51692 90569614
Psychomotor retardation 44.35 30.79 16 7125 4773 90616533
Catatonia 44.24 30.79 17 7124 6039 90615267
Ileus paralytic 43.41 30.79 16 7125 5069 90616237
Rabbit syndrome 43.39 30.79 9 7132 331 90620975
Megacolon 43.23 30.79 13 7128 2201 90619105
Hypothermia 42.76 30.79 22 7119 15553 90605753
Arthralgia 41.61 30.79 6 7135 778516 89842790
Hyperammonaemic encephalopathy 40.69 30.79 13 7128 2686 90618620
Urinary retention 40.07 30.79 29 7112 37715 90583591
Depressed level of consciousness 39.67 30.79 38 7103 72746 90548560
Stupor 38.66 30.79 15 7126 5467 90615839
Parkinsonian gait 38.41 30.79 9 7132 583 90620723
Electrocardiogram QT prolonged 37.93 30.79 37 7104 72419 90548887
Serotonin syndrome 37.71 30.79 28 7113 37859 90583447
Tardive dyskinesia 37.60 30.79 18 7123 10912 90610394
Eosinophilic myocarditis 37.11 30.79 9 7132 676 90620630
Accommodation disorder 36.06 30.79 8 7133 406 90620900
Psychotic disorder 35.46 30.79 25 7116 31205 90590101
Stereotypy 35.29 30.79 8 7133 448 90620858
Parkinsonism hyperpyrexia syndrome 34.36 30.79 7 7134 235 90621071
Distractibility 33.66 30.79 8 7133 551 90620755
Oculogyric crisis 33.54 30.79 11 7130 2468 90618838
Mutism 32.88 30.79 10 7131 1759 90619547
Hypertonia 32.47 30.79 13 7128 5142 90616164
Headache 32.06 30.79 14 7127 862732 89758574
Psychiatric decompensation 31.95 30.79 10 7131 1933 90619373
Drug monitoring procedure incorrectly performed 31.93 30.79 7 7134 336 90620970
Delirium 31.57 30.79 40 7101 104319 90516987
Sitting disability 31.48 30.79 7 7134 359 90620947
Cerebral atrophy 31.33 30.79 13 7128 5633 90615673
Hallucinations, mixed 30.80 30.79 13 7128 5876 90615430

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 270.46 25.94 113 7743 21359 42592120
Schizophrenia 165.31 25.94 65 7791 10485 42602994
Colitis ischaemic 158.65 25.94 57 7799 7169 42606310
Extrapyramidal disorder 131.54 25.94 63 7793 16349 42597130
Salivary hypersecretion 119.16 25.94 52 7804 10891 42602588
Intentional self-injury 114.70 25.94 56 7800 15146 42598333
Sopor 112.89 25.94 53 7803 13149 42600330
Megacolon 102.74 25.94 31 7825 2254 42611225
Suicide attempt 101.51 25.94 77 7779 46023 42567456
Delusion 98.51 25.94 50 7806 14684 42598795
Muscle rigidity 89.69 25.94 44 7812 12015 42601464
Psychotic disorder 87.82 25.94 59 7797 29149 42584330
Ileus paralytic 82.16 25.94 36 7820 7605 42605874
Altered state of consciousness 78.27 25.94 55 7801 29204 42584275
Self-injurious ideation 78.24 25.94 24 7832 1844 42611635
Hallucination, auditory 78.24 25.94 43 7813 14821 42598658
Aggression 76.31 25.94 64 7792 44099 42569380
Dyskinesia 75.63 25.94 51 7805 25339 42588140
Intentional overdose 73.68 25.94 67 7789 51389 42562090
Depressed level of consciousness 71.72 25.94 64 7792 47906 42565573
Akathisia 71.41 25.94 36 7820 10415 42603064
Restlessness 69.12 25.94 51 7805 29198 42584281
Blood creatine phosphokinase increased 67.37 25.94 62 7794 48276 42565203
Sedation 67.25 25.94 51 7805 30424 42583055
Psychomotor hyperactivity 66.92 25.94 35 7821 10923 42602556
Persecutory delusion 66.67 25.94 25 7831 3539 42609940
Pneumonia aspiration 65.50 25.94 62 7794 50016 42563463
Parkinsonism 65.07 25.94 34 7822 10589 42602890
Oropharyngeal spasm 62.06 25.94 13 7843 207 42613272
Psychiatric symptom 59 25.94 24 7832 4217 42609262
Stupor 58.55 25.94 22 7834 3131 42610348
Faecaloma 56.14 25.94 26 7830 6244 42607235
Delirium 50.36 25.94 55 7801 52464 42561015
Patient restraint 47.99 25.94 9 7847 78 42613401
Drug interaction 47.89 25.94 132 7724 266867 42346612
Tremor 47.81 25.94 73 7783 96856 42516623
Peritonitis 47.44 25.94 34 7822 18599 42594880
Dysphagia 46.51 25.94 62 7794 72657 42540822
Psychomotor retardation 44.94 25.94 20 7836 4379 42609100
Sinus tachycardia 44.31 25.94 34 7822 20619 42592860
Postoperative respiratory failure 43.85 25.94 9 7847 129 42613350
Dystonia 43.69 25.94 28 7828 12762 42600717
Rhabdomyolysis 43.12 25.94 62 7794 77957 42535522
Post-injection delirium sedation syndrome 39.57 25.94 11 7845 597 42612882
Self-destructive behaviour 39.56 25.94 10 7846 375 42613104
Tardive dyskinesia 36.34 25.94 20 7836 6904 42606575
Polydipsia 35.23 25.94 17 7839 4471 42609008
Psychotic symptom 34.88 25.94 14 7842 2376 42611103
Paraplegia 33.71 25.94 15 7841 3282 42610197
Hyponatraemia 32.34 25.94 63 7793 101399 42512080
Overdose 31.91 25.94 64 7792 105200 42508279
Treatment noncompliance 31.91 25.94 37 7819 37635 42575844
Bezoar 31.54 25.94 11 7845 1265 42612214
Disorientation 31.25 25.94 36 7820 36353 42577126
Tension 31.07 25.94 13 7843 2451 42611028
Olfactory nerve disorder 30.87 25.94 6 7850 64 42613415
Shock 28.77 25.94 31 7825 29090 42584389
Coma 28.76 25.94 42 7814 53512 42559967
Arthralgia 27.30 25.94 3 7853 205235 42408244
Social avoidant behaviour 27.19 25.94 13 7843 3351 42610128
Drug screen false positive 27.09 25.94 9 7847 893 42612586
Pseudohallucination 27.02 25.94 5 7851 40 42613439
Agitation 26.95 25.94 45 7811 64269 42549210
Sudden death 26.45 25.94 23 7833 16606 42596873
Paraparesis 26.36 25.94 11 7845 2060 42611419
Fatigue 26.32 25.94 25 7831 435616 42177863

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
Neuroleptic malignant syndrome 653.81 25.53 223 14370 33836 110540870
Extrapyramidal disorder 319.18 25.53 126 14467 28741 110545965
Suicide attempt 255.73 25.53 163 14430 103231 110471475
Schizophrenia 250.85 25.53 98 14495 21728 110552978
Salivary hypersecretion 231.66 25.53 87 14506 17334 110557372
Intentional self-injury 224.32 25.53 106 14487 37323 110537383
Sopor 220.56 25.53 104 14489 36442 110538264
Delusion 215.55 25.53 90 14503 23665 110551041
Akathisia 200.74 25.53 78 14515 17035 110557671
Drug interaction 199.56 25.53 285 14308 499898 110074808
Muscle rigidity 181.61 25.53 80 14513 23951 110550755
Dyskinesia 173.39 25.53 99 14494 51347 110523359
Hallucination, auditory 171.28 25.53 79 14514 26318 110548388
Altered state of consciousness 168.13 25.53 101 14492 57525 110517181
Colitis ischaemic 163.54 25.53 68 14525 17682 110557024
Intentional overdose 160.95 25.53 136 14457 132365 110442341
Psychotic symptom 152.68 25.53 44 14549 3823 110570883
Restlessness 149.77 25.53 93 14500 56166 110518540
Blood creatine phosphokinase increased 148.53 25.53 102 14491 72975 110501731
Megacolon 139.36 25.53 42 14551 4263 110570443
Persecutory delusion 135.57 25.53 45 14548 6246 110568460
Hyperprolactinaemia 133.63 25.53 45 14548 6530 110568176
Tremor 132.73 25.53 148 14445 202084 110372622
Ileus paralytic 132.35 25.53 52 14541 11685 110563021
Parkinsonism 124.25 25.53 60 14533 22127 110552579
Psychomotor hyperactivity 123.20 25.53 58 14535 20219 110554487
Pneumonia aspiration 118.88 25.53 93 14500 81140 110493566
Aggression 118.78 25.53 82 14511 59128 110515578
Psychotic disorder 115.22 25.53 76 14517 50861 110523845
Dystonia 109.95 25.53 58 14535 25747 110548959
Rhabdomyolysis 107.55 25.53 104 14489 120297 110454409
Depressed level of consciousness 106.01 25.53 100 14493 112178 110462528
Agitation 99.75 25.53 97 14496 112954 110461752
Stupor 94.53 25.53 37 14556 8228 110566478
Somnolence 93.48 25.53 152 14441 297297 110277409
Oromandibular dystonia 91.32 25.53 23 14570 1196 110573510
Psychomotor retardation 89.53 25.53 35 14558 7757 110566949
Self-injurious ideation 89.32 25.53 30 14563 4316 110570390
Coma 87.28 25.53 92 14501 117777 110456929
Psychiatric symptom 80.51 25.53 34 14559 9179 110565527
Delirium 80.35 25.53 94 14499 134931 110439775
Sedation 79.38 25.53 69 14524 69614 110505092
Drug abuse 79.25 25.53 107 14486 177304 110397402
Treatment noncompliance 76.62 25.53 69 14524 72921 110501785
Faecaloma 76.53 25.53 38 14555 14870 110559836
Arthralgia 72.25 25.53 9 14584 779623 109795083
Toxicity to various agents 69.58 25.53 178 14415 480377 110094329
Tardive dyskinesia 67.89 25.53 34 14559 13545 110561161
Dysarthria 64.66 25.53 67 14526 84054 110490652
Nausea 63.24 25.53 43 14550 1235647 109339059
Bradykinesia 62.89 25.53 30 14563 10758 110563948
Dysphagia 61.63 25.53 88 14505 153512 110421194
Headache 58.08 25.53 22 14571 882355 109692351
Electrocardiogram QT prolonged 56.87 25.53 71 14522 108889 110465817
Inappropriate affect 56.82 25.53 17 14576 1682 110573024
Logorrhoea 56.01 25.53 22 14571 4935 110569771
Overdose 55.88 25.53 106 14487 233688 110341018
Oropharyngeal spasm 55.76 25.53 13 14580 487 110574219
Catatonia 55.63 25.53 28 14565 11272 110563434
Disorientation 55.59 25.53 57 14536 70614 110504092
Urinary retention 54.44 25.53 56 14537 69627 110505079
Pain 53.28 25.53 30 14563 954925 109619781
Fatigue 52.58 25.53 50 14543 1215908 109358798
Hypothermia 51.72 25.53 36 14557 26266 110548440
Intentional product misuse 51.64 25.53 75 14518 132829 110441877
Reduced facial expression 51.31 25.53 19 14574 3632 110571074
Cogwheel rigidity 51.08 25.53 19 14574 3679 110571027
Mutism 50.46 25.53 18 14575 3095 110571611
Confabulation 50.02 25.53 12 14581 509 110574197
Irritability 49.77 25.53 45 14548 47764 110526942
Patient restraint 49.39 25.53 9 14584 95 110574611
Social avoidant behaviour 47.53 25.53 20 14573 5349 110569357
Peritonitis 46.95 25.53 37 14556 32570 110542136
Mental impairment 46.90 25.53 32 14561 22607 110552099
Blood prolactin increased 46.88 25.53 19 14574 4623 110570083
Galactorrhoea 45.40 25.53 18 14575 4137 110570569
Post-injection delirium sedation syndrome 45.38 25.53 12 14581 757 110573949
Hyponatraemia 43.96 25.53 92 14501 217561 110357145
Negative symptoms in schizophrenia 42.66 25.53 9 14584 211 110574495
Torticollis 42.48 25.53 16 14577 3205 110571501
Postoperative respiratory failure 42.46 25.53 9 14584 216 110574490
Refusal of treatment by patient 42.31 25.53 22 14571 9472 110565234
Disorganised speech 42.09 25.53 16 14577 3287 110571419
Intestinal pseudo-obstruction 41.85 25.53 16 14577 3340 110571366
Shock 41.74 25.53 43 14550 53545 110521161
Sluggishness 40.96 25.53 20 14573 7547 110567159
Sinus tachycardia 40.76 25.53 39 14554 44454 110530252
Resting tremor 39.83 25.53 13 14580 1710 110572996
Inappropriate antidiuretic hormone secretion 39.51 25.53 34 14559 33817 110540889
Sudden death 37.99 25.53 29 14564 24366 110550340
Urinary incontinence 37.86 25.53 39 14554 48548 110526158
Pain in extremity 37.69 25.53 9 14584 487109 110087597
Rabbit syndrome 37.55 25.53 9 14584 380 110574326
Hyperammonaemic encephalopathy 37.55 25.53 17 14576 5417 110569289
Abnormal behaviour 37.24 25.53 35 14558 39004 110535702
Drug level increased 36.64 25.53 38 14555 47681 110527025
Hypersensitivity 36.56 25.53 5 14588 403993 110170713
Oculogyric crisis 36.36 25.53 15 14578 3817 110570889
Disturbance in attention 34.93 25.53 42 14551 61953 110512753
Polydipsia 34.79 25.53 18 14575 7670 110567036
Olfactory nerve disorder 34.77 25.53 6 14587 45 110574661
Hallucination 34.77 25.53 54 14539 101378 110473328
Leukocytosis 34.56 25.53 39 14554 53789 110520917
Spasmodic dysphonia 34.06 25.53 9 14584 566 110574140
Asthenia 33.79 25.53 25 14568 688974 109885732
Intestinal dilatation 33.77 25.53 14 14579 3606 110571100
Cough 32.94 25.53 10 14583 461631 110113075
Accommodation disorder 32.93 25.53 9 14584 644 110574062
Paraplegia 32.40 25.53 16 14577 6184 110568522
Drug hypersensitivity 32.10 25.53 10 14583 454080 110120626
Dyspnoea 32.05 25.53 61 14532 1106811 109467895
Dysphoria 31.85 25.53 16 14577 6412 110568294
Hypernatraemia 31.80 25.53 23 14570 17810 110556896
Rash 31.76 25.53 37 14556 820927 109753779
Pruritus 31.33 25.53 19 14574 581541 109993165
Drug monitoring procedure incorrectly performed 31.31 25.53 9 14584 774 110573932
White blood cell count increased 31.04 25.53 50 14543 96792 110477914
Neutrophil count increased 31.03 25.53 30 14563 34622 110540084
Suicidal ideation 30.79 25.53 49 14544 93888 110480818
Loss of consciousness 30.72 25.53 75 14518 196231 110378475
Hypertonia 30.52 25.53 17 14576 8389 110566317
Akinesia 30.27 25.53 13 14580 3654 110571052
Swelling 30.25 25.53 5 14588 351036 110223670
Distractibility 30.06 25.53 9 14584 892 110573814
Obsessive-compulsive disorder 30.05 25.53 16 14577 7225 110567481
Eosinophilic myocarditis 29.85 25.53 11 14582 2074 110572632
Hallucination, visual 29.44 25.53 31 14562 39574 110535132
Abdominal discomfort 29.07 25.53 8 14585 393850 110180856
Seizure 28.94 25.53 79 14514 221106 110353600
Parkinsonism hyperpyrexia syndrome 28.77 25.53 8 14585 610 110574096
Drug intolerance 28.64 25.53 9 14584 406503 110168203
Parkinsonian gait 28.52 25.53 9 14584 1063 110573643
Gaze palsy 27.87 25.53 12 14581 3395 110571311
Diarrhoea 27.07 25.53 70 14523 1139435 109435271
Drug screen false positive 26.36 25.53 9 14584 1360 110573346
Tension 26.22 25.53 13 14580 5065 110569641
Self-destructive behaviour 26.21 25.53 8 14585 847 110573859
Thinking abnormal 25.80 25.53 19 14574 15121 110559585
Gastrointestinal necrosis 25.68 25.53 14 14579 6626 110568080
Colectomy total 25.66 25.53 7 14586 497 110574209
Negativism 25.55 25.53 8 14585 921 110573785

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N04AA02 NERVOUS SYSTEM
ANTI-PARKINSON DRUGS
ANTICHOLINERGIC AGENTS
Tertiary amines
FDA MoA N0000175370 Cholinergic Antagonists
FDA EPC N0000175574 Anticholinergic
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35474 anxiolytic drug
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:48407 antiparkinson drug
CHEBI has role CHEBI:48876 muscarinic antagonist
CHEBI has role CHEBI:50370 parasympatholytic
CHEBI has role CHEBI:66956 antidyskinesia agent
CHEBI has role CHEBI:136860 antidote to sarin poisoning
MeSH PA D000978 Antiparkinson Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D010276 Parasympatholytics
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D018726 Anti-Dyskinesia Agents
MeSH PA D018727 Muscarinic Antagonists
CHEBI has role CHEBI:63726 neuroprotective agent

Related Drugs by ATC class:

N04AA Tertiary amines 9 drugs
bornaprinedexetimidemazaticolmetixenephenglutarimideprocyclidineprofenaminetrihexyphenidyltropatepine

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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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 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
Muscarinic acetylcholine receptor M5 GPCR Ki 8.20 PDSP
Neuronal acetylcholine receptor subunit alpha-2 Ion channel WOMBAT-PK

External reference:

IDSource
4019635 VUID
N0000147728 NUI
D00779 KEGG_DRUG
151311 RXNORM
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
915 INN_ID
1235-82-1 SECONDARY_CAS_RN
7085-45-2 SECONDARY_CAS_RN
0FRP6G56LD UNII
4285 MMSL
d00972 MMSL
10020007 SNOMEDCT_US
387359004 SNOMEDCT_US
61742009 SNOMEDCT_US
65041000 SNOMEDCT_US
4018474 VANDF
4018475 VANDF
4019635 VANDF
C036432 MESH_SUPPLEMENTAL_RECORD_UI
001644 NDDF
001645 NDDF
001646 NDDF
0FRP6G56LD INXIGHT DRUGS

Pharmaceutical products:

None