ziprasidone ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
2865 146939-27-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ziprasidone
  • zaprasidone
  • ziprasidone hydrochloride
  • ziprasidone mesylate
  • geodon
  • ziprasidone HCl
  • ziprasidone mesilate
a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone
  • Molecular weight: 412.94
  • Formula: C21H21ClN4OS
  • CLOGP: 4.86
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 48.47
  • ALOGS: -4.76
  • ROTB: 4

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
80 mg O
40 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.21 mg/mL Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 0.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 6.36 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 60 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 5.10 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 3.10 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Feb. 5, 2001 FDA PFIZER

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
Dystonia 1344.29 19.55 376 17796 13443 63457407
Blood prolactin abnormal 1336.16 19.55 280 17892 2799 63468051
Sexual dysfunction 1331.99 19.55 297 17875 4062 63466788
Anosognosia 1093.65 19.55 239 17933 2957 63467893
Disturbance in social behaviour 1024.61 19.55 236 17936 3757 63467093
Sedation 1012.90 19.55 390 17782 38419 63432431
Metabolic disorder 934.55 19.55 241 17931 6262 63464588
Dyskinesia 930.15 19.55 348 17824 31654 63439196
Personality change 846.24 19.55 226 17946 6747 63464103
Suicide attempt 726.33 19.55 352 17820 60566 63410284
Tardive dyskinesia 711.92 19.55 206 17966 8296 63462554
Blood glucose increased 399.74 19.55 266 17906 83490 63387360
Extrapyramidal disorder 398.30 19.55 148 18024 13136 63457714
Completed suicide 384.22 19.55 324 17848 145349 63325501
Akathisia 357.41 19.55 124 18048 9022 63461828
Neuroleptic malignant syndrome 338.40 19.55 128 18044 11928 63458922
Orthostatic hypertension 318.53 19.55 63 18109 455 63470395
Metabolic syndrome 273.13 19.55 68 18104 1520 63469330
Parkinsonism 250.80 19.55 99 18073 10340 63460510
Electrocardiogram QT prolonged 198.18 19.55 152 18020 59378 63411472
Diabetes mellitus 191.27 19.55 145 18027 55665 63415185
Insurance issue 157.41 19.55 61 18111 6060 63464790
Suicidal ideation 156.26 19.55 135 18037 62286 63408564
Psychotic disorder 137.90 19.55 88 18084 25624 63445226
Oculogyric crisis 127.67 19.55 38 18134 1683 63469167
Impulse-control disorder 126.73 19.55 32 18140 758 63470092
Agitation 119.61 19.55 114 18058 59643 63411207
Posture abnormal 112.27 19.55 37 18135 2295 63468555
Mania 110.62 19.55 59 18113 12308 63458542
Blood prolactin increased 108.49 19.55 40 18132 3463 63467387
Tremor 104.59 19.55 157 18015 132082 63338768
Hallucination, auditory 103.08 19.55 57 18115 12767 63458083
Galactorrhoea 101.85 19.55 40 18132 4115 63466735
Dyslipidaemia 94.74 19.55 45 18127 7348 63463502
Arthralgia 93.61 19.55 24 18148 569686 62901164
Obesity 85.67 19.55 70 18102 29882 63440968
Substance abuse 79.68 19.55 35 18137 4772 63466078
Pain 79.47 19.55 58 18114 740570 62730280
Hyperprolactinaemia 76.53 19.55 32 18140 3868 63466982
Cardio-respiratory arrest 76.45 19.55 90 18082 59869 63410981
Paranoia 75.38 19.55 45 18127 11634 63459216
Torsade de pointes 74.82 19.55 47 18125 13304 63457546
Respiratory arrest 74.42 19.55 67 18105 32578 63438272
Personality change due to a general medical condition 73.11 19.55 16 18156 198 63470652
Weight increased 72.20 19.55 200 17972 260592 63210258
Coma 69.74 19.55 89 18083 64275 63406575
Anxiety 69.50 19.55 176 17996 217365 63253485
Intentional overdose 68.76 19.55 95 18077 74057 63396793
Depression 67.01 19.55 163 18009 196329 63274521
Joint swelling 63.89 19.55 9 18163 327657 63143193
Peripheral swelling 63.57 19.55 3 18169 265939 63204911
Diarrhoea 63.43 19.55 67 18105 715299 62755551
Somnolence 62.81 19.55 150 18022 178535 63292315
Adverse drug reaction 62.04 19.55 94 18078 79620 63391230
Condition aggravated 59.49 19.55 250 17922 401967 63068883
Overdose 58.18 19.55 112 18060 114966 63355884
Infusion related reaction 57.94 19.55 3 18169 245518 63225332
Delusion 56.76 19.55 38 18134 11979 63458871
Pneumonia 55.40 19.55 31 18141 456736 63014114
Arthropathy 54.99 19.55 3 18169 234789 63236061
Rheumatoid arthritis 54.39 19.55 5 18167 253814 63217036
Rapid eye movement sleep behaviour disorder 51.28 19.55 13 18159 313 63470537
Catatonia 50.57 19.55 25 18147 4452 63466398
Insomnia 48.93 19.55 154 18018 215098 63255752
Product use issue 48.18 19.55 4 18168 220516 63250334
Distributive shock 47.32 19.55 17 18155 1366 63469484
Abnormal behaviour 46.92 19.55 43 18129 21383 63449467
Systemic lupus erythematosus 45.06 19.55 4 18168 208914 63261936
Cardiac arrest 44.25 19.55 88 18084 92457 63378393
Off label use 43.82 19.55 79 18093 674383 62796467
Alopecia 43.72 19.55 21 18151 337515 63133335
Muscle rigidity 41.83 19.55 31 18141 11469 63459381
Psychomotor hyperactivity 41.63 19.55 30 18142 10633 63460217
Swelling 40.74 19.55 14 18158 275364 63195486
Abdominal discomfort 40.00 19.55 21 18151 320864 63149986
Treatment failure 39.88 19.55 5 18167 199038 63271812
Blood triglycerides increased 39.56 19.55 31 18141 12457 63458393
Drug ineffective 38.75 19.55 462 17710 1044303 62426547
Mental disorder 38.27 19.55 42 18130 25877 63444973
Nasopharyngitis 37.48 19.55 13 18159 254244 63216606
Fatigue 37.44 19.55 130 18042 887898 62582952
Aggression 36.30 19.55 39 18133 23459 63447391
Symptom recurrence 36.01 19.55 15 18157 1795 63469055
General physical health deterioration 35.96 19.55 7 18165 201395 63269455
Reduced facial expression 34.81 19.55 15 18157 1951 63468899
Sinusitis 34.43 19.55 11 18161 226642 63244208
Restlessness 33.91 19.55 42 18130 29411 63441439
Toxicity to various agents 33.63 19.55 150 18022 247100 63223750
Infection 33.29 19.55 12 18160 229161 63241689
Type 2 diabetes mellitus 33.29 19.55 63 18109 63805 63407045
Wound 32.95 19.55 4 18168 163259 63307591
Maternal exposure during pregnancy 32.87 19.55 11 18161 220051 63250799
Swollen tongue 32.86 19.55 45 18127 34755 63436095
Cardiac hypertrophy 32.61 19.55 12 18160 1033 63469817
Rabbit syndrome 32.06 19.55 9 18163 323 63470527
Pyrexia 31.50 19.55 54 18118 470424 63000426
Mental status changes 31.22 19.55 47 18125 39552 63431298
Cough 29.88 19.55 24 18148 292719 63178131
Tachyphrenia 29.42 19.55 12 18160 1362 63469488
Pain in extremity 29.32 19.55 31 18141 331455 63139395
Seizure 29.28 19.55 94 18078 132540 63338310
Product substitution issue 29.13 19.55 29 18143 15967 63454883
Cognitive disorder 29.01 19.55 55 18117 55760 63415090
Abdominal pain 28.79 19.55 25 18147 293431 63177419
Torticollis 28.49 19.55 13 18159 1936 63468914
Infarction 27.63 19.55 14 18158 2627 63468223
Pericarditis 27.10 19.55 3 18169 131576 63339274
Glossodynia 26.60 19.55 9 18163 178867 63291983
Back pain 26.53 19.55 22 18150 264123 63206727
Drug intolerance 26.04 19.55 30 18142 308631 63162219
Echolalia 25.73 19.55 7 18165 223 63470627
Thrombocytopenia 25.45 19.55 6 18166 151151 63319699
Drug withdrawal syndrome 25.42 19.55 35 18137 27159 63443691
Drooling 25.21 19.55 15 18157 3853 63466997
Hypersensitivity 25.17 19.55 28 18144 292657 63178193
Trismus 25.15 19.55 15 18157 3870 63466980
Rhabdomyolysis 24.96 19.55 45 18127 43906 63426944
Pruritus 24.62 19.55 41 18131 361412 63109438
Posturing 24.30 19.55 8 18164 494 63470356
Bruxism 23.84 19.55 14 18158 3511 63467339
Headache 23.81 19.55 97 18075 633144 62837706
Exposure via ingestion 23.56 19.55 13 18159 2896 63467954
Irritability 22.71 19.55 36 18136 31658 63439192
Cogwheel rigidity 22.25 19.55 11 18161 1959 63468891
Sinus bradycardia 22.21 19.55 24 18148 14527 63456323
Haemoglobin decreased 22.19 19.55 7 18165 145478 63325372
Withdrawal syndrome 22.19 19.55 28 18144 19969 63450881
Blister 22.16 19.55 5 18167 129809 63341041
Mobility decreased 22.07 19.55 4 18168 121155 63349695
Dyspnoea 22.02 19.55 106 18066 661207 62809643
Suicidal behaviour 21.95 19.55 12 18160 2627 63468223
Amenorrhoea 21.90 19.55 20 18152 9894 63460956
Organ failure 21.81 19.55 12 18160 2659 63468191
Malaise 21.70 19.55 55 18117 415899 63054951
Shock 21.63 19.55 30 18142 23433 63447417
Diabetic coma 21.51 19.55 8 18164 709 63470141
Nausea 21.49 19.55 150 18022 854321 62616529
Stereotypy 21.22 19.55 7 18165 435 63470415
Anaemia 21.18 19.55 32 18140 293398 63177452
Coprolalia 21.01 19.55 4 18168 23 63470827
Drug screen positive 20.89 19.55 13 18159 3616 63467234
Thinking abnormal 20.69 19.55 20 18152 10623 63460227
Gestational diabetes 20.66 19.55 18 18154 8378 63462472
Rash 20.39 19.55 87 18085 560784 62910066
Injection site pain 20.24 19.55 6 18166 129794 63341056
Hepatic enzyme increased 20.12 19.55 17 18155 202311 63268539
Granulocytopenia 19.98 19.55 15 18157 5657 63465193
Apathy 19.94 19.55 18 18154 8776 63462074
Schizophrenia 19.91 19.55 19 18153 9933 63460917
Personality disorder 19.66 19.55 15 18157 5796 63465054

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
Dystonia 465.86 22.26 169 12949 10676 34933137
Akathisia 403.64 22.26 141 12977 7968 34935845
Antipsychotic drug level below therapeutic 329.44 22.26 92 13026 2455 34941358
Therapeutic product effect variable 309.84 22.26 87 13031 2369 34941444
Disinhibition 307.95 22.26 92 13026 3134 34940679
Neuroleptic malignant syndrome 307.64 22.26 145 12973 17789 34926024
Euphoric mood 307.45 22.26 105 13013 5536 34938277
Dyskinesia 302.97 22.26 154 12964 22259 34921554
Obsessive-compulsive disorder 297.13 22.26 102 13016 5462 34938351
Anosognosia 287.98 22.26 68 13050 905 34942908
Suicide attempt 286.91 22.26 180 12938 38936 34904877
Blood prolactin abnormal 283.03 22.26 67 13051 902 34942911
Tardive dyskinesia 270.19 22.26 96 13022 5694 34938119
Increased appetite 246.87 22.26 96 13022 7333 34936480
Disturbance in social behaviour 244.57 22.26 68 13050 1783 34942030
Sedation 240.02 22.26 129 12989 20877 34922936
Weight increased 226.79 22.26 223 12895 92810 34851003
Sexual dysfunction 200.77 22.26 79 13039 6224 34937589
Extrapyramidal disorder 199.08 22.26 97 13021 12783 34931030
Metabolic disorder 188.44 22.26 68 13050 4215 34939598
Obesity 169.57 22.26 87 13031 12791 34931022
Personality change 144.88 22.26 59 13059 5080 34938733
Aggression 131.02 22.26 112 13006 38852 34904961
Priapism 129.47 22.26 54 13064 4940 34938873
Completed suicide 115.37 22.26 162 12956 98006 34845807
Electrocardiogram QT prolonged 114.39 22.26 106 13012 40846 34902967
Psychotic disorder 111.39 22.26 84 13034 24368 34919445
Leukaemia 106.78 22.26 46 13072 4557 34939256
Dyslipidaemia 105.57 22.26 53 13065 7435 34936378
Suicidal ideation 102.22 22.26 99 13019 40289 34903524
Agitation 101.19 22.26 116 13002 57283 34886530
Irritability 99.76 22.26 79 13039 24611 34919202
Bruxism 97.24 22.26 33 13085 1702 34942111
Oppositional defiant disorder 95.20 22.26 25 13093 524 34943289
Decreased eye contact 92.88 22.26 24 13094 471 34943342
Homicidal ideation 90.26 22.26 35 13083 2647 34941166
Blood prolactin increased 89.01 22.26 31 13087 1729 34942084
Catatonia 87.19 22.26 41 13077 4984 34938829
Therapeutic product effect incomplete 83.81 22.26 99 13019 50442 34893371
Hallucination, auditory 80.14 22.26 52 13066 11865 34931948
Leukopenia 78.65 22.26 107 13011 62749 34881064
Drug ineffective 77.68 22.26 357 12761 456394 34487419
Serotonin syndrome 76.72 22.26 62 13056 19871 34923942
Oculogyric crisis 76.62 22.26 27 13091 1559 34942254
Trismus 71.53 22.26 29 13089 2466 34941347
Prescribed overdose 70.46 22.26 46 13072 10601 34933212
Delusion 67.93 22.26 48 13070 12587 34931226
Schizoaffective disorder 65.67 22.26 23 13095 1304 34942509
Toxicity to various agents 64.66 22.26 193 12925 200169 34743644
Mania 62.71 22.26 41 13077 9470 34934343
Diarrhoea 61.73 22.26 35 13083 389877 34553936
Blood glucose increased 59.61 22.26 97 13021 66621 34877192
Swollen tongue 59.55 22.26 47 13071 14558 34929255
Crying 55.91 22.26 32 13086 5830 34937983
Pneumonia 55.33 22.26 34 13084 362593 34581220
Psychomotor hyperactivity 55.10 22.26 38 13080 9584 34934229
Choreoathetosis 54.80 22.26 19 13099 1045 34942768
Paranoia 53.91 22.26 41 13077 12027 34931786
Anxiety 53.13 22.26 116 13002 99312 34844501
Anaemia 51.93 22.26 12 13106 233323 34710490
Speech disorder 48.77 22.26 54 13064 25632 34918181
Coordination abnormal 48.08 22.26 32 13086 7612 34936201
Dacryostenosis congenital 46.23 22.26 9 13109 43 34943770
Parkinsonism 43.93 22.26 31 13087 8107 34935706
Abnormal behaviour 43.16 22.26 50 13068 24919 34918894
Tic 42.64 22.26 19 13099 2039 34941774
Type 2 diabetes mellitus 41.84 22.26 40 13078 15992 34927821
Schizophrenia 39.94 22.26 30 13088 8636 34935177
Muscle rigidity 36.87 22.26 31 13087 10487 34933326
Blood creatine phosphokinase increased 35.75 22.26 62 13056 44795 34899018
Granulocytopenia 35.41 22.26 25 13093 6542 34937271
Diabetes mellitus 35.05 22.26 63 13055 46810 34897003
Tremor 34.95 22.26 88 13030 82499 34861314
Affect lability 34.84 22.26 20 13098 3663 34940150
Mood altered 34.76 22.26 28 13090 8924 34934889
Pruritus 34.26 22.26 6 13112 141975 34801838
Anger 33.59 22.26 31 13087 11853 34931960
Hypotonia neonatal 33.03 22.26 14 13104 1331 34942482
Blood triglycerides increased 32.61 22.26 33 13085 14126 34929687
Somnolence 31.98 22.26 103 13015 111013 34832800
Torticollis 31.66 22.26 13 13105 1141 34942672
Rhabdomyolysis 31.35 22.26 75 13043 68088 34875725
Pyrexia 31.27 22.26 48 13070 332965 34610848
Cough 30.92 22.26 9 13109 150131 34793682
Acute kidney injury 30.55 22.26 42 13076 304946 34638867
Off label use 30.18 22.26 71 13047 419453 34524360
Grandiosity 29.76 22.26 9 13109 319 34943494
Hyperkinesia 29.36 22.26 14 13104 1754 34942059
Blunted affect 28.93 22.26 9 13109 351 34943462
Feminisation acquired 28.75 22.26 6 13112 43 34943770
Insomnia 28.71 22.26 95 13023 103812 34840001
Arthralgia 28.67 22.26 14 13104 170027 34773786
Overweight 28.47 22.26 14 13104 1876 34941937
Disease progression 27.34 22.26 4 13114 108073 34835740
Opisthotonus 26.63 22.26 9 13109 458 34943355
Product prescribing issue 26.59 22.26 14 13104 2165 34941648
Death 26.56 22.26 70 13048 397979 34545834
Thrombocytopenia 26.13 22.26 13 13105 156234 34787579
Overdose 24.92 22.26 83 13035 90976 34852837
Bipolar disorder 24.63 22.26 16 13102 3653 34940160
Myopathy toxic 24.63 22.26 9 13109 577 34943236
Neonatal respiratory depression 23.48 22.26 8 13110 417 34943396
Febrile neutropenia 23.47 22.26 11 13107 136838 34806975
Thinking abnormal 23.41 22.26 19 13099 6118 34937695
Asthenia 23.32 22.26 35 13083 245216 34698597
Depressed mood 22.79 22.26 32 13086 19285 34924528
Streptococcal infection 22.47 22.26 17 13101 4944 34938869

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
Blood prolactin abnormal 1471.77 18.92 314 23490 3287 79717297
Dystonia 1411.40 18.92 435 23369 20964 79699620
Sexual dysfunction 1355.83 18.92 339 23465 7424 79713160
Anosognosia 1240.28 18.92 275 23529 3489 79717095
Disturbance in social behaviour 1143.29 18.92 271 23533 4699 79715885
Sedation 1048.41 18.92 439 23365 51456 79669128
Dyskinesia 1024.12 18.92 414 23390 44359 79676225
Metabolic disorder 1001.62 18.92 276 23528 8894 79711690
Personality change 914.88 18.92 263 23541 9907 79710677
Suicide attempt 760.35 18.92 407 23397 82525 79638059
Completed suicide 532.95 18.92 498 23306 245269 79475315
Neuroleptic malignant syndrome 528.68 18.92 225 23579 27334 79693250
Tardive dyskinesia 503.50 18.92 168 23636 10403 79710181
Akathisia 421.61 18.92 156 23648 13103 79707481
Blood glucose increased 414.84 18.92 313 23491 114662 79605922
Extrapyramidal disorder 385.30 18.92 170 23634 22509 79698075
Orthostatic hypertension 285.13 18.92 63 23741 782 79719802
Parkinsonism 267.79 18.92 120 23684 16464 79704120
Metabolic syndrome 251.32 18.92 72 23732 2668 79717916
Electrocardiogram QT prolonged 236.33 18.92 204 23600 90182 79630402
Suicidal ideation 211.19 18.92 178 23626 76162 79644422
Obesity 205.55 18.92 129 23675 34996 79685588
Psychotic disorder 193.30 18.92 132 23672 41270 79679314
Insurance issue 176.86 18.92 66 23738 5667 79714917
Oculogyric crisis 173.30 18.92 55 23749 2897 79717687
Diabetes mellitus 163.72 18.92 156 23648 78234 79642350
Aggression 162.26 18.92 129 23675 50829 79669755
Dyslipidaemia 162.11 18.92 76 23728 11557 79709027
Agitation 147.73 18.92 165 23639 99550 79621034
Hallucination, auditory 146.79 18.92 86 23718 20607 79699977
Blood prolactin increased 141.59 18.92 51 23753 3960 79716624
Catatonia 121.37 18.92 57 23747 8699 79711885
Adverse drug reaction 114.34 18.92 119 23685 66273 79654311
Weight increased 114.13 18.92 254 23550 277132 79443452
Decreased eye contact 112.93 18.92 30 23774 835 79719749
Oppositional defiant disorder 108.48 18.92 26 23778 471 79720113
Posture abnormal 106.57 18.92 41 23763 3825 79716759
Drug ineffective 105.52 18.92 614 23190 1080299 78640285
Respiratory arrest 102.42 18.92 105 23699 57445 79663139
Irritability 101.66 18.92 90 23714 41054 79679530
Impulse-control disorder 99.80 18.92 32 23772 1742 79718842
Delusion 99.77 18.92 67 23737 20356 79700228
Antipsychotic drug level below therapeutic 97.91 18.92 29 23775 1209 79719375
Diarrhoea 97.08 18.92 73 23731 880416 78840168
Mania 89.43 18.92 60 23744 18200 79702384
Anxiety 88.39 18.92 215 23589 248297 79472287
Bruxism 87.62 18.92 36 23768 3990 79716594
Galactorrhoea 87.59 18.92 35 23769 3611 79716973
Psychomotor hyperactivity 86.47 18.92 57 23747 16792 79703792
Pneumonia 83.19 18.92 47 23757 660199 79060385
Homicidal ideation 82.40 18.92 33 23771 3424 79717160
Arthralgia 82.22 18.92 34 23770 571769 79148815
Condition aggravated 82.18 18.92 331 23473 500793 79219791
Paranoia 79.11 18.92 57 23747 19375 79701209
Priapism 73.98 18.92 33 23771 4472 79716112
Type 2 diabetes mellitus 73.58 18.92 88 23716 57034 79663550
Disinhibition 73.21 18.92 28 23776 2570 79718014
Cardio-respiratory arrest 71.02 18.92 121 23683 108389 79612195
Serotonin syndrome 70.93 18.92 77 23727 44950 79675634
Euphoric mood 70.81 18.92 38 23766 7688 79712896
Cardiac arrest 70.00 18.92 157 23647 171939 79548645
Pain 69.28 18.92 65 23739 703737 79016847
Therapeutic product effect variable 68.87 18.92 25 23779 1984 79718600
Trismus 67.88 18.92 33 23771 5434 79715150
Depression 67.09 18.92 178 23626 216612 79503972
Hyperprolactinaemia 66.53 18.92 31 23773 4645 79715939
Overdose 65.04 18.92 159 23645 184047 79536537
Obsessive-compulsive disorder 62.44 18.92 32 23772 5895 79714689
Granulocytopenia 61.90 18.92 40 23764 11391 79709193
Joint swelling 61.72 18.92 7 23797 288639 79431945
Insomnia 60.01 18.92 185 23619 244985 79475599
Personality change due to a general medical condition 59.81 18.92 14 23790 228 79720356
Toxicity to various agents 59.36 18.92 266 23538 421274 79299310
Tremor 59.18 18.92 146 23658 169937 79550647
Pyrexia 58.58 18.92 70 23734 678639 79041945
Muscle rigidity 58.31 18.92 48 23756 19834 79700750
Increased appetite 57.79 18.92 39 23765 11939 79708645
Peripheral swelling 56.50 18.92 7 23797 269610 79450974
Infusion related reaction 56.42 18.92 3 23801 230234 79490350
Rhabdomyolysis 55.96 18.92 106 23698 103025 79617559
Anaemia 55.50 18.92 32 23772 444983 79275601
Torsade de pointes 55.34 18.92 46 23758 19266 79701318
Abnormal behaviour 55.13 18.92 61 23743 36360 79684224
Substance abuse 54.96 18.92 36 23768 10490 79710094
Mental disorder 50.12 18.92 54 23750 31248 79689336
Cough 49.22 18.92 24 23780 366765 79353819
Choreoathetosis 48.14 18.92 18 23786 1552 79719032
Intentional overdose 48.00 18.92 101 23703 105859 79614725
Blood triglycerides increased 47.97 18.92 44 23760 20996 79699588
Rheumatoid arthritis 47.32 18.92 4 23800 208466 79512118
Nausea 47.03 18.92 139 23665 957057 78763527
Coma 46.83 18.92 97 23707 100552 79620032
Rapid eye movement sleep behaviour disorder 46.13 18.92 13 23791 453 79720131
Abdominal pain 44.46 18.92 31 23773 389538 79331046
Off label use 44.36 18.92 132 23672 907083 78813501
Nasopharyngitis 43.64 18.92 11 23793 253870 79466714
Coordination abnormal 43.01 18.92 38 23766 17274 79703310
Swollen tongue 42.81 18.92 58 23746 42512 79678072
Malaise 42.77 18.92 50 23754 489819 79230765
General physical health deterioration 41.75 18.92 15 23789 275223 79445361
Arthropathy 41.31 18.92 3 23801 177108 79543476
Blood creatine phosphokinase increased 41.00 18.92 72 23732 66018 79654566
Abdominal discomfort 40.96 18.92 12 23792 250715 79469869
Torticollis 40.85 18.92 18 23786 2369 79718215
Exposure via ingestion 40.67 18.92 23 23781 5151 79715433
Schizoaffective disorder 39.34 18.92 17 23787 2135 79718449
Grandiosity 38.90 18.92 12 23792 575 79720009
Speech disorder 38.66 18.92 63 23741 54382 79666202
Pain in extremity 37.78 18.92 32 23772 364506 79356078
Pruritus 36.94 18.92 38 23766 394610 79325974
Somnolence 36.77 18.92 155 23649 238826 79481758
Mood altered 36.23 18.92 35 23769 17812 79702772
Alopecia 36.13 18.92 12 23792 231343 79489241
Thrombocytopenia 36.11 18.92 17 23787 265242 79455342
Febrile neutropenia 36.04 18.92 12 23792 230987 79489597
Restlessness 36.04 18.92 56 23748 46436 79674148
Distributive shock 35.72 18.92 17 23787 2670 79717914
Crying 35.57 18.92 39 23765 23004 79697580
Dyspnoea 35.49 18.92 134 23670 856891 78863693
Hyperkinesia 35.47 18.92 17 23787 2712 79717872
Rabbit syndrome 35.36 18.92 10 23794 353 79720231
Reduced facial expression 35.26 18.92 17 23787 2748 79717836
Fatigue 34.96 18.92 151 23653 929576 78791008
Schizophrenia 34.63 18.92 32 23772 15408 79705176
Cognitive disorder 34.42 18.92 69 23735 69857 79650727
Tic 34.02 18.92 17 23787 2969 79717615
Haemoglobin decreased 33.85 18.92 12 23792 222107 79498477
Infection 33.66 18.92 15 23789 241697 79478887
Renal impairment 33.27 18.92 4 23800 157779 79562805
COVID-19 33.24 18.92 4 23800 157670 79562914
Symptom recurrence 31.87 18.92 15 23789 2299 79718285
Intentional product use issue 31.73 18.92 4 23800 152108 79568476
Disease progression 31.65 18.92 8 23796 184354 79536230
Swelling 30.89 18.92 13 23791 216698 79503886
Affect lability 30.57 18.92 26 23778 11233 79709351
Headache 29.85 18.92 98 23706 653674 79066910
Sinusitis 29.05 18.92 11 23793 195490 79525094
Posturing 28.42 18.92 11 23793 1042 79719542
Gastrointestinal haemorrhage 28.24 18.92 5 23799 147714 79572870
Stomatitis 27.99 18.92 5 23799 146752 79573832
Acute kidney injury 27.96 18.92 72 23732 519332 79201252
Tachyphrenia 27.16 18.92 13 23791 2067 79718517
Mental status changes 27.09 18.92 61 23743 66898 79653686
Thinking abnormal 27.07 18.92 26 23778 13135 79707449
Asthenia 26.73 18.92 72 23732 511617 79208967
Erythema 26.48 18.92 17 23787 223273 79497311
Anger 26.41 18.92 29 23775 17133 79703451
Overweight 26.18 18.92 16 23788 4134 79716450
Rash 26.18 18.92 87 23717 578271 79142313
Stereotypy 25.97 18.92 10 23794 935 79719649
Injection site pain 25.70 18.92 4 23800 129834 79590750
Feminisation acquired 25.59 18.92 5 23799 32 79720552
Maternal exposure during pregnancy 25.29 18.92 5 23799 136533 79584051
Bradypnoea 25.19 18.92 18 23786 6034 79714550
Sepsis 25.13 18.92 26 23778 269402 79451182
Spasmodic dysphonia 24.13 18.92 7 23797 271 79720313
Systemic lupus erythematosus 23.38 18.92 4 23800 121145 79599439
Drooling 23.22 18.92 17 23787 5917 79714667
Contraindicated product administered 23.18 18.92 9 23795 157529 79563055
Hallucination 23.11 18.92 67 23737 85678 79634906
Treatment failure 23.08 18.92 11 23793 170475 79550109
Drug screen positive 22.89 18.92 17 23787 6046 79714538
Treatment noncompliance 22.70 18.92 49 23755 52219 79668365
Sperm concentration decreased 22.34 18.92 5 23799 66 79720518
Corneal reflex decreased 22.17 18.92 7 23797 362 79720222
Wound 22.06 18.92 4 23800 116175 79604409
Decreased appetite 22.06 18.92 43 23761 342375 79378209
Echolalia 21.94 18.92 7 23797 375 79720209
Sinus bradycardia 21.82 18.92 32 23772 25215 79695369
Depressed mood 21.69 18.92 46 23758 48434 79672150
Back pain 21.56 18.92 36 23768 304144 79416440
Abdominal pain upper 21.55 18.92 21 23783 223798 79496786
Product prescribing issue 21.52 18.92 14 23790 4031 79716553
Ventricular arrhythmia 21.15 18.92 19 23785 8821 79711763
Myopathy toxic 21.14 18.92 9 23795 1089 79719495
Interstitial lung disease 21.12 18.92 4 23800 112596 79607988
Vomiting 20.98 18.92 115 23689 665713 79054871
Cardiac failure 20.94 18.92 10 23794 154832 79565752
Obsessive thoughts 20.88 18.92 9 23795 1123 79719461
Blister 20.86 18.92 5 23799 119471 79601113
Pressure of speech 20.18 18.92 9 23795 1219 79719365
Diabetic coma 20.02 18.92 9 23795 1242 79719342
Muscle contractions involuntary 19.95 18.92 13 23791 3752 79716832
Infarction 19.93 18.92 14 23790 4568 79716016
Drug intolerance 19.90 18.92 30 23774 264089 79456495
Influenza 19.74 18.92 7 23797 129599 79590985
Mobility decreased 19.66 18.92 6 23798 122169 79598415
Urticaria 19.48 18.92 16 23788 185185 79535399
Bipolar disorder 19.31 18.92 17 23787 7690 79712894
Weight decreased 19.27 18.92 49 23755 355149 79365435
Streptococcal infection 19.22 18.92 18 23786 8812 79711772
Poisoning 18.97 18.92 30 23774 25242 79695342

FDA Adverse Event Reporting System (Pediatric)

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
Dacryostenosis congenital 39.35 29.74 8 117 8 89659
Opisthotonus 35.79 29.74 8 117 17 89650

Pharmacologic Action:

SourceCodeDescription
ATC N05AE04 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Indole derivatives
FDA EPC N0000175430 Atypical Antipsychotic
MeSH PA D014150 Antipsychotic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D015259 Dopamine Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D018490 Serotonin Agents
MeSH PA D012702 Serotonin Antagonists
MeSH PA D014149 Tranquilizing Agents
CHEBI has role CHEBI:35471 psychotropic drugs
CHEBI has role CHEBI:35476 neuroleptics
CHEBI has role CHEBI:37956 antihistamines
CHEBI has role CHEBI:48279 serotonin antagonists
CHEBI has role CHEBI:48561 dopaminergic antagonists
CHEBI has role CHEBI:48876 muscarinic antagonists

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

DiseaseRelationSNOMED_IDDOID
Mixed bipolar I disorder indication 16506000 DOID:3312
Schizophrenia indication 58214004 DOID:5419
Bipolar disorder in remission indication 85248005
Bipolar affective disorder, current episode manic indication 191618007
Agitation associated with Schizophrenia indication
Bipolar affective disorder, current episode depression off-label use 191627008 DOID:3312
Depression Treatment Adjunct off-label use
Tachyarrhythmia contraindication 6285003
Suicidal thoughts contraindication 6471006
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Senile dementia contraindication 15662003
Agranulocytosis contraindication 17182001 DOID:12987
Myocardial infarction contraindication 22298006 DOID:5844
Hypovolemia contraindication 28560003
Orthostatic hypotension contraindication 28651003
Torsades de pointes contraindication 31722008
Dehydration contraindication 34095006
Dysphagia contraindication 40739000
Hypokalemia contraindication 43339004
Conduction disorder of the heart contraindication 44808001
Bradycardia contraindication 48867003
Hyperlipidemia contraindication 55822004 DOID:1168
Hepatic failure contraindication 59927004
Cerebrovascular disease contraindication 62914000 DOID:6713
Diabetes mellitus contraindication 73211009 DOID:9351
Extrapyramidal disease contraindication 76349003
Hyperglycemia contraindication 80394007 DOID:4195
Heart failure contraindication 84114007 DOID:6000
Epilepsy contraindication 84757009 DOID:1826
Leukopenia contraindication 84828003 DOID:615
Kidney disease contraindication 90708001 DOID:557
Tardive dyskinesia contraindication 102449007
Prolonged QT interval contraindication 111975006
Hypomagnesemia contraindication 190855004
Decompensated cardiac failure contraindication 195111005
Metabolic syndrome X contraindication 237602007 DOID:14221
Neutropenic disorder contraindication 303011007 DOID:1227
Severe diarrhea contraindication 409587002
Breastfeeding (mother) contraindication 413712001
Myocardial ischemia contraindication 414795007 DOID:3393
Obesity contraindication 414916001 DOID:9970
Acquired torsion dystonia contraindication 433493000
Congenital long QT syndrome contraindication 442917000
Carcinoma of female breast contraindication 447782002




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.26 acidic
pKa2 7.35 Basic
pKa3 0.27 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 20MG BASE GEODON VIATRIS N020825 Feb. 5, 2001 RX CAPSULE ORAL Jan. 28, 2025 INFORMATION ADDED TO SECTION 8.4 OF THE LABELING TO DESCRIBE THE RESULTS FROM PEDIATRIC STUDIES
EQ 40MG BASE GEODON VIATRIS N020825 Feb. 5, 2001 RX CAPSULE ORAL Jan. 28, 2025 INFORMATION ADDED TO SECTION 8.4 OF THE LABELING TO DESCRIBE THE RESULTS FROM PEDIATRIC STUDIES
EQ 60MG BASE GEODON VIATRIS N020825 Feb. 5, 2001 RX CAPSULE ORAL Jan. 28, 2025 INFORMATION ADDED TO SECTION 8.4 OF THE LABELING TO DESCRIBE THE RESULTS FROM PEDIATRIC STUDIES
EQ 80MG BASE GEODON VIATRIS N020825 Feb. 5, 2001 RX CAPSULE ORAL Jan. 28, 2025 INFORMATION ADDED TO SECTION 8.4 OF THE LABELING TO DESCRIBE THE RESULTS FROM PEDIATRIC STUDIES

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
D(2) dopamine receptor GPCR ANTAGONIST Ki 8.32 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 9.40 WOMBAT-PK CHEMBL
Beta-2 adrenergic receptor GPCR Ki 5.30 PDSP
D(1A) dopamine receptor GPCR Ki 8.02 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 6.30 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.92 WOMBAT-PK
Sodium-dependent serotonin transporter Transporter IC50 7 WOMBAT-PK
Sodium-dependent noradrenaline transporter Transporter Ki 7.36 PDSP
5-hydroxytryptamine receptor 1A GPCR EC50 8.47 WOMBAT-PK
5-hydroxytryptamine receptor 2B GPCR Ki 7.57 PDSP
5-hydroxytryptamine receptor 2C GPCR ANTAGONIST Ki 8.89 WOMBAT-PK
5-hydroxytryptamine receptor 6 GPCR Ki 7.22 WOMBAT-PK
5-hydroxytryptamine receptor 7 GPCR Ki 8.30 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 8 WOMBAT-PK
Alpha-2B adrenergic receptor GPCR Ki 7.32 PDSP
D(3) dopamine receptor GPCR ANTAGONIST Ki 8.14 WOMBAT-PK
D(1B) dopamine receptor GPCR Ki 6.82 PDSP
Histamine H1 receptor GPCR Ki 7.33 WOMBAT-PK
Histamine H2 receptor GPCR Ki 5.46 PDSP
Muscarinic acetylcholine receptor M1 GPCR Ki 6.55 WOMBAT-PK
Muscarinic acetylcholine receptor M2 GPCR Ki 5.52 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 5 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 5.80 PDSP
Muscarinic acetylcholine receptor M5 GPCR Ki 5.80 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 8.70 WOMBAT-PK
Alpha-2C adrenergic receptor GPCR Ki 7.11 PDSP
Sodium-dependent dopamine transporter Transporter WOMBAT-PK
D(4) dopamine receptor GPCR ANTAGONIST Ki 7.30 WOMBAT-PK
5-hydroxytryptamine receptor 3A Ion channel Ki 6.40 WOMBAT-PK
Alpha-1B adrenergic receptor GPCR Ki 8.05 PDSP
5-hydroxytryptamine receptor 5A GPCR Ki 6.54 PDSP
5-hydroxytryptamine receptor 1E GPCR Ki 6.44 WOMBAT-PK
Aspartate aminotransferase, cytoplasmic Enzyme IC50 5.27 CHEMBL
5-hydroxytryptamine receptor 1B GPCR AGONIST Ki 8.30 IUPHAR
Histone H1.0 Nuclear other Ki 7.82 CHEMBL
Beta-1 adrenergic receptor GPCR Ki 5.59 PDSP
Alpha-1A adrenergic receptor GPCR Ki 9.30 CHEMBL
Histamine H1 receptor GPCR Ki 7.80 CHEMBL
D(2) dopamine receptor GPCR Ki 8.32 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 9.38 CHEMBL
Histamine H1 receptor GPCR IC50 6.82 CHEMBL
Transporter Transporter Ki 7.32 CHEMBL
Adrenergic receptor alpha-1 GPCR Ki 7.96 CHEMBL

External reference:

IDSource
4021249 VUID
N0000148690 NUI
D02100 KEGG_DRUG
138982-67-9 SECONDARY_CAS_RN
199191-69-0 SECONDARY_CAS_RN
4021249 VANDF
4030214 VANDF
4030215 VANDF
C0380393 UMLSCUI
CHEBI:10119 CHEBI
CHEMBL708 ChEMBL_ID
CHEMBL1375743 ChEMBL_ID
CHEMBL1712 ChEMBL_ID
CHEMBL3989833 ChEMBL_ID
CHEMBL1200997 ChEMBL_ID
DB00246 DRUGBANK_ID
C092292 MESH_SUPPLEMENTAL_RECORD_UI
60854 PUBCHEM_CID
59 IUPHAR_LIGAND_ID
7155 INN_ID
6UKA5VEJ6X UNII
115698 RXNORM
16791 MMSL
187736 MMSL
331404 MMSL
41113 MMSL
d04747 MMSL
009104 NDDF
009105 NDDF
009579 NDDF
129479007 SNOMEDCT_US
373389002 SNOMEDCT_US
409356003 SNOMEDCT_US
409357007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0052 CAPSULE 20 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0052 CAPSULE 20 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0052 CAPSULE 20 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0054 CAPSULE 40 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0054 CAPSULE 40 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0054 CAPSULE 40 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0056 CAPSULE 60 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0056 CAPSULE 60 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0056 CAPSULE 60 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0058 CAPSULE 80 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0058 CAPSULE 80 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0058 CAPSULE 80 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0352 CAPSULE 20 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0352 CAPSULE 20 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0352 CAPSULE 20 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0354 CAPSULE 40 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0354 CAPSULE 40 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0354 CAPSULE 40 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0356 CAPSULE 60 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0356 CAPSULE 60 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0356 CAPSULE 60 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0358 CAPSULE 80 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0358 CAPSULE 80 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-0358 CAPSULE 80 mg ORAL NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-1203 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAMUSCULAR NDA 30 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-1203 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAMUSCULAR NDA 30 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-3920 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAMUSCULAR NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-3920 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAMUSCULAR NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-3920 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAMUSCULAR NDA 32 sections
Geodon HUMAN PRESCRIPTION DRUG LABEL 1 0049-3960 CAPSULE 20 mg ORAL NDA 32 sections