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

Stem definitionDrug idCAS RN
psychoactive 1613 1977-10-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • loxapine
  • loxapin
  • oxilapine
  • loxapine succinate
  • cloxazepine
  • loxitane
  • adasuve
  • loxapine hydrochloride
  • loxapine HCl
  • loxipine maleate
An antipsychotic agent used in SCHIZOPHRENIA.
  • Molecular weight: 327.81
  • Formula: C18H18ClN3O
  • CLOGP: 3.68
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 28.07
  • ALOGS: -3.50
  • ROTB: 0

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
9.10 mg Inhal.powder
0.10 g O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 30 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Feb. 25, 1975 FDA

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
Coma 378.17 37.79 146 3836 59509 56228576
Poisoning deliberate 377.72 37.79 96 3886 9857 56278228
Neuroleptic malignant syndrome 221.21 37.79 65 3917 11413 56276672
Extrapyramidal disorder 153.51 37.79 50 3932 12306 56275779
Hepatocellular injury 146.76 37.79 59 3923 26455 56261630
Cholestasis 128.88 37.79 54 3928 26859 56261226
Somnolence 117.55 37.79 95 3887 163318 56124767
Oculogyric crisis 111.34 37.79 25 3957 1499 56286586
Toxicity to various agents 104.50 37.79 102 3880 224462 56063623
Intestinal obstruction 94.68 37.79 44 3938 27927 56260158
Tachycardia 74.79 37.79 61 3921 105815 56182270
Pneumonia aspiration 71.15 37.79 38 3944 32373 56255712
Intentional overdose 69.71 37.79 49 3933 68068 56220017
Benzodiazepine drug level increased 69.69 37.79 12 3970 176 56287909
Catatonia 65.67 37.79 20 3962 3944 56284141
Altered state of consciousness 65.04 37.79 32 3950 22989 56265096
Miosis 63.31 37.79 22 3960 6570 56281515
Galactorrhoea 61.76 37.79 19 3963 3876 56284209
Hypothermia 59.56 37.79 25 3957 12445 56275640
Hyperprolactinaemia 58.64 37.79 18 3964 3643 56284442
Brain death 57.86 37.79 17 3965 2966 56285119
Faecaloma 56.99 37.79 21 3961 7420 56280665
Hepatic cytolysis 55.92 37.79 23 3959 10883 56277202
Cardio-respiratory arrest 52.44 37.79 38 3944 55283 56232802
Antipsychotic drug level above therapeutic 49.68 37.79 12 3970 989 56287096
Rhabdomyolysis 48.08 37.79 32 3950 40626 56247459
Hyperthermia 47.73 37.79 19 3963 8266 56279819
Intestinal pseudo-obstruction 47.08 37.79 11 3971 786 56287299
Hypotension 47.03 37.79 72 3910 250436 56037649
Dystonia 46.58 37.79 21 3961 12400 56275685
Urinary retention 45.53 37.79 27 3955 28047 56260038
Overdose 45.19 37.79 46 3936 105784 56182301
Suicide attempt 42.20 37.79 34 3948 57802 56230283
Cardiogenic shock 41.12 37.79 21 3961 16304 56271781
Myocarditis septic 39.67 37.79 6 3976 36 56288049
Amenorrhoea 39.54 37.79 17 3965 8969 56279116
Asphyxia 39.45 37.79 15 3967 5774 56282311

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
Coma 316.07 37.89 158 6300 40992 31649894
Therapeutic product effect variable 267.46 37.89 65 6393 1873 31689013
Antipsychotic drug level below therapeutic 264.94 37.89 65 6393 1950 31688936
Disinhibition 251.02 37.89 66 6392 2627 31688259
Akathisia 241.28 37.89 80 6378 7173 31683713
Obsessive-compulsive disorder 232.62 37.89 71 6387 4866 31686020
Euphoric mood 207.50 37.89 65 6393 4855 31686031
Increased appetite 191.26 37.89 65 6393 6279 31684607
Neuroleptic malignant syndrome 169.40 37.89 78 6380 16791 31674095
Poisoning deliberate 148.58 37.89 56 6402 7288 31683598
Wrong patient received product 134.25 37.89 40 6418 2519 31688367
Suicide attempt 130.85 37.89 86 6372 37162 31653724
Hepatocellular injury 128.58 37.89 70 6388 21474 31669412
Rhabdomyolysis 117.92 37.89 100 6358 63481 31627405
Extrapyramidal disorder 116.74 37.89 54 6404 11724 31679162
Miosis 99.87 37.89 44 6414 8526 31682360
Therapeutic product effect incomplete 98.39 37.89 77 6381 43619 31647267
Intestinal obstruction 85.76 37.89 53 6405 20557 31670329
Dyslipidaemia 84.82 37.89 36 6422 6370 31684516
Leukaemia 82.49 37.89 31 6427 3994 31686892
Faecaloma 81.62 37.89 32 6426 4624 31686262
Leukopenia 79.66 37.89 77 6381 57751 31633135
Obesity 77.29 37.89 40 6418 11060 31679826
Toxicity to various agents 76.25 37.89 134 6324 181353 31509533
Hypothermia 74.04 37.89 37 6421 9507 31681379
Prescribed overdose 72.38 37.89 36 6422 9156 31681730
Product use in unapproved indication 68.07 37.89 92 6366 99079 31591807
Somnolence 66.35 37.89 91 6367 99354 31591532
Weight increased 61.59 37.89 80 6378 82867 31608019
Colitis ischaemic 60.73 37.89 28 6430 6024 31684862
Hyperleukocytosis 57.15 37.89 19 6439 1710 31689176
Pneumonia aspiration 56.00 37.89 53 6405 38673 31652213
Subileus 53.99 37.89 21 6437 2969 31687917
Fatigue 50.54 37.89 5 6453 335201 31355685
Electrocardiogram QT prolonged 49.30 37.89 49 6409 37938 31652948
Necrotising colitis 48.68 37.89 15 6443 1057 31689829
Hyperthermia 44.85 37.89 27 6431 9977 31680909
Bradypnoea 42.86 37.89 17 6441 2530 31688356
Tachycardia 42.36 37.89 64 6394 76143 31614743
Blood creatine phosphokinase increased 41.76 37.89 47 6411 41927 31648959
Congestive cardiomyopathy 39.71 37.89 22 6436 6960 31683926
Mydriasis 38.23 37.89 21 6437 6531 31684355

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
Coma 690.78 35.79 304 9103 91540 70827497
Poisoning deliberate 490.98 35.79 152 9255 16908 70902129
Neuroleptic malignant syndrome 379.22 35.79 139 9268 25868 70893169
Extrapyramidal disorder 277.03 35.79 104 9303 20646 70898391
Hepatocellular injury 268.24 35.79 128 9279 45963 70873074
Somnolence 190.32 35.79 185 9222 215421 70703616
Rhabdomyolysis 188.15 35.79 131 9276 95629 70823408
Intestinal obstruction 178.78 35.79 92 9315 38733 70880304
Miosis 171.29 35.79 66 9341 14035 70905002
Faecaloma 141.65 35.79 53 9354 10398 70908639
Pneumonia aspiration 135.96 35.79 91 9316 62198 70856839
Hypothermia 134.50 35.79 62 9345 20532 70898505
Wrong patient received product 124.86 35.79 39 9368 4441 70914596
Tachycardia 110.55 35.79 120 9287 158426 70760611
Toxicity to various agents 107.49 35.79 186 9221 381986 70537051
Akathisia 106.03 35.79 45 9362 12248 70906789
Hyperthermia 95.93 35.79 46 9361 16625 70902412
Cholestasis 92.73 35.79 65 9342 47807 70871230
Catatonia 91.43 35.79 36 9371 8097 70910940
Subileus 87.55 35.79 31 9376 5196 70913841
Necrotising colitis 80.57 35.79 20 9387 975 70918062
Cardio-respiratory arrest 80.44 35.79 82 9325 100595 70818442
Altered state of consciousness 79.04 35.79 55 9352 39967 70879070
Fatigue 78.39 35.79 9 9398 824310 70094727
Oculogyric crisis 77.33 35.79 24 9383 2674 70916363
Blood creatine phosphokinase increased 70.25 35.79 61 9346 61202 70857835
Suicide attempt 67.60 35.79 67 9340 79443 70839594
Bladder dilatation 67.58 35.79 20 9387 1897 70917140
Asphyxia 67.08 35.79 31 9376 10311 70908726
Congestive cardiomyopathy 65.45 35.79 31 9376 10895 70908142
Hyperleukocytosis 64.85 35.79 20 9387 2181 70916856
Electrocardiogram QT prolonged 61.25 35.79 65 9342 83452 70835585
Benzodiazepine drug level increased 60.00 35.79 12 9395 213 70918824
Hepatic cytolysis 59.34 35.79 35 9372 19157 70899880
Agitation 58.66 35.79 67 9340 93308 70825729
Bradypnoea 57.30 35.79 23 9384 5436 70913601
Antipsychotic drug level below therapeutic 56.29 35.79 15 9392 970 70918067
Pain 54.66 35.79 9 9398 628807 70290230
Galactorrhoea 52.67 35.79 19 9388 3359 70915678
Respiratory acidosis 52.04 35.79 26 9381 10255 70908782
Distal intestinal obstruction syndrome 51.76 35.79 13 9394 665 70918372
Intentional overdose 50.94 35.79 64 9343 98371 70820666
Faecal vomiting 50.82 35.79 14 9393 1027 70918010
Colitis ischaemic 49.61 35.79 28 9379 14109 70904928
Therapeutic product effect variable 48.12 35.79 15 9392 1695 70917342
Urinary retention 47.88 35.79 46 9361 52474 70866563
Disinhibition 47.67 35.79 16 9391 2285 70916752
Confusional state 46.82 35.79 111 9296 284287 70634750
Housebound 45.93 35.79 11 9396 461 70918576
Aggression 45.24 35.79 43 9364 48403 70870634
Brain death 44.79 35.79 19 9388 5159 70913878
Dystonia 43.44 35.79 29 9378 19677 70899360
Drug interaction 42.67 35.79 129 9278 381312 70537725
Intestinal ischaemia 42.62 35.79 24 9383 12040 70906997
Hyperprolactinaemia 40.87 35.79 17 9390 4396 70914641
Dyspnoea 40.87 35.79 26 9381 770034 70149003
Product use in unapproved indication 40.85 35.79 87 9320 207391 70711646
Psychotic disorder 40.12 35.79 36 9371 37665 70881372
Arthralgia 39.91 35.79 9 9398 503381 70415656
Antipsychotic drug level above therapeutic 38.01 35.79 13 9394 1966 70917071
Drug abuse 37.75 35.79 69 9338 147187 70771850
Diabetic hyperosmolar coma 36.09 35.79 10 9397 749 70918288
Myocarditis septic 35.90 35.79 6 9401 36 70919001

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AH01 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Diazepines, oxazepines, thiazepines and oxepines
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 D014149 Tranquilizing Agents
CHEBI has role CHEBI:35476 neuroleptics
CHEBI has role CHEBI:48561 dopaminergic antagonists

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

DiseaseRelationSNOMED_IDDOID
Bipolar disorder indication 13746004 DOID:3312
Schizophrenia indication 58214004 DOID:5419
Alcoholism contraindication 7200002
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Senile dementia contraindication 15662003
Glaucoma contraindication 23986001 DOID:1686
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Tardive dyskinesia contraindication 102449007
Seizure disorder contraindication 128613002
Hyperprolactinemia contraindication 237662005 DOID:12700
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Coma contraindication 371632003
Carcinoma of female breast contraindication 447782002
Pigmentary Retinopathy contraindication
Drug Induced CNS Depression contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.59 Basic
pKa2 3.24 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
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 8.62 CHEMBL CHEMBL
D(2) dopamine receptor GPCR ANTAGONIST Ki 7.68 CHEMBL CHEMBL
Sodium-dependent noradrenaline transporter Transporter Ki 5.24 PDSP
5-hydroxytryptamine receptor 1A GPCR Ki 5.61 PDSP
5-hydroxytryptamine receptor 2C GPCR ANTAGONIST Ki 8 IUPHAR
5-hydroxytryptamine receptor 6 GPCR Ki 7.82 CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 7.51 PDSP
Alpha-2B adrenergic receptor GPCR Ki 6.97 PDSP
D(3) dopamine receptor GPCR ANTAGONIST IC50 7.66 CHEMBL
D(1B) dopamine receptor GPCR Ki 7.13 PDSP
Histamine H1 receptor GPCR ANTAGONIST Ki 8.20 IUPHAR
Histamine H2 receptor GPCR Ki 6.68 PDSP
Histamine H4 receptor GPCR Ki 5.30 PDSP
Muscarinic acetylcholine receptor M1 GPCR IC50 5.26 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 6.38 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 6.91 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 6.09 PDSP
Muscarinic acetylcholine receptor M5 GPCR Ki 6.83 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 6.41 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 5.46 PDSP
Alpha-2C adrenergic receptor GPCR Ki 7.10 PDSP
D(4) dopamine receptor GPCR ANTAGONIST Ki 8.31 CHEMBL
5-hydroxytryptamine receptor 3A Ion channel Ki 6.72 PDSP
Alpha-1B adrenergic receptor GPCR Ki 7.28 PDSP
5-hydroxytryptamine receptor 5A GPCR Ki 6.11 PDSP
5-hydroxytryptamine receptor 1E GPCR Ki 5.85 PDSP
Potassium channel subfamily K member 2 Ion channel IC50 4.70 CHEMBL
Potassium channel subfamily T member 1 Ion channel ACTIVATOR EC50 5.36 IUPHAR
D(1A) dopamine receptor GPCR Ki 7.27 PDSP
Alpha-2A adrenergic receptor GPCR Ki 6.82 PDSP
D(2) dopamine receptor GPCR Ki 7.68 CHEMBL
5-hydroxytryptamine receptor 2A GPCR IC50 8.22 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 7.37 CHEMBL
5-hydroxytryptamine receptor 2C GPCR IC50 6 CHEMBL
Histamine H1 receptor GPCR IC50 6 CHEMBL
5-hydroxytryptamine receptor 6 GPCR ANTAGONIST Ki 7.80 IUPHAR
Adrenergic receptor alpha-1 GPCR IC50 7.74 CHEMBL

External reference:

IDSource
4019805 VUID
N0000147894 NUI
D00794 KEGG_DRUG
27833-64-3 SECONDARY_CAS_RN
4017917 VANDF
4017918 VANDF
4019805 VANDF
C0024056 UMLSCUI
CHEBI:50841 CHEBI
CHEMBL831 ChEMBL_ID
CHEMBL1201155 ChEMBL_ID
DB00408 DRUGBANK_ID
D008152 MESH_DESCRIPTOR_UI
3964 PUBCHEM_CID
205 IUPHAR_LIGAND_ID
2610 INN_ID
54810-23-0 SECONDARY_CAS_RN
LER583670J UNII
1364415 RXNORM
1308 MMSL
1346 MMSL
196711 MMSL
29026 MMSL
4999 MMSL
5000 MMSL
d00897 MMSL
001522 NDDF
001523 NDDF
001524 NDDF
1971003 SNOMEDCT_US
30745005 SNOMEDCT_US
372789006 SNOMEDCT_US
59270007 SNOMEDCT_US
CHEMBL1201060 ChEMBL_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 0527-1394 CAPSULE 5 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 0527-1395 CAPSULE 10 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 0527-1396 CAPSULE 25 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 0527-1397 CAPSULE 50 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 0591-0369 CAPSULE 5 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 0591-0370 CAPSULE 10 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 0591-0371 CAPSULE 25 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 0591-0372 CAPSULE 50 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 10135-585 TABLET 5 mg ORAL ANDA 19 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 10135-586 TABLET 10 mg ORAL ANDA 19 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 10135-587 TABLET 25 mg ORAL ANDA 19 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 10135-588 TABLET 50 mg ORAL ANDA 19 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 17856-1397 CAPSULE 50 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 35573-436 CAPSULE 5 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 35573-437 CAPSULE 10 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 35573-438 CAPSULE 25 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 35573-439 CAPSULE 50 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 50090-4701 CAPSULE 10 mg ORAL ANDA 21 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 50090-4701 CAPSULE 10 mg ORAL ANDA 21 sections
Adasuve HUMAN PRESCRIPTION DRUG LABEL 1 51097-001 AEROSOL, POWDER 10 mg RESPIRATORY (INHALATION) NDA 31 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 64850-890 CAPSULE 5 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 64850-891 CAPSULE 10 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 64850-892 CAPSULE 25 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 64850-893 CAPSULE 50 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 68151-2875 CAPSULE 5 mg ORAL ANDA 18 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 70518-0283 CAPSULE 10 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 70518-0283 CAPSULE 10 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 70518-0346 CAPSULE 5 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 70518-0346 CAPSULE 5 mg ORAL ANDA 20 sections
Loxapine HUMAN PRESCRIPTION DRUG LABEL 1 70518-0347 CAPSULE 25 mg ORAL ANDA 20 sections