olanzapine indications/contra

Stem definitionDrug idCAS RN
psychoactive 1982 132539-06-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • olanzapine pamoate
  • olanzapine embonate
  • zyprexa relprevv
  • olanzapine pamoate monohydrate
  • olanzapine
  • zyprexa
  • LY 170053
  • LY-170053
The mechanism of action of olanzapine, as with other drugs having efficacy in schizophrenia, is unknown. However, it has been proposed that this drug’s efficacy in schizophrenia is mediated through a combination of dopamine and serotonin type 2 (5HT2) antagonism. The mechanism of action of olanzapine in the treatment of acute manic or mixed episodes associated with bipolar I disorder is unknown.
  • Molecular weight: 312.44
  • Formula: C17H20N4S
  • CLOGP: 2.86
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 30.87
  • ALOGS: -3.52
  • ROTB: 0

Drug dosage:

DoseUnitRoute
10 mg O
10 mg P
10 mg P

Approvals:

DateAgencyCompanyOrphan
Sept. 30, 1996 FDA LILLY

FDA Adverse Event Reporting System

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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 3598.44 28.57 801 16548 3640 3364870
Weight increased 3523.59 28.57 1145 16204 25595 3342915
Overdose 3131.62 28.57 1113 16236 32865 3335645
Completed suicide 2234.68 28.57 850 16499 30264 3338246
Diabetes mellitus 2164.46 28.57 657 16692 11476 3357034
Toxicity to various agents 2004.60 28.57 884 16465 46170 3322340
Sedation 1507.61 28.57 426 16923 5675 3362835
Agitation 1507.47 28.57 565 16784 19141 3349369
Suicide attempt 1417.43 28.57 510 16839 15337 3353173
Psychotic disorder 1373.48 28.57 430 16919 8304 3360206
Somnolence 1357.59 28.57 602 16747 31602 3336908
Prescribed overdose 1315.59 28.57 320 17029 2246 3366264
Intentional overdose 1309.02 28.57 476 16873 14749 3353761
Electrocardiogram QT prolonged 1146.14 28.57 395 16954 10400 3358110
Extrapyramidal disorder 1031.90 28.57 285 17064 3458 3365052
Drug interaction 1030.31 28.57 562 16787 46250 3322260
Coma 1020.97 28.57 377 16972 12175 3356335
Type 2 diabetes mellitus 1018.46 28.57 275 17074 3046 3365464
Blood triglycerides increased 994.58 28.57 289 17060 4261 3364249
Blood creatine phosphokinase increased 974.91 28.57 368 16981 12645 3355865
Tachycardia 948.34 28.57 426 16923 22945 3345565
Confusional state 930.35 28.57 490 16859 37508 3331002
Exposure during pregnancy 887.26 28.57 428 16921 27135 3341375
Off label use 866.78 28.57 528 16821 53449 3315061
Rhabdomyolysis 838.88 28.57 348 17001 15381 3353129
Intentional self-injury 812.97 28.57 255 17094 4930 3363580
Aggression 787.85 28.57 304 17045 11081 3357429
Catatonia 780.85 28.57 187 17162 1213 3367297
Neutropenia 761.56 28.57 411 16938 32975 3335535
Schizophrenia 760.14 28.57 209 17140 2485 3366025

Pharmacologic Action:

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SourceCodeDescription
ATC N05AH03 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Diazepines, oxazepines, thiazepines and oxepines
CHEBI has role CHEBI:37956 histamine antagonist
CHEBI has role CHEBI:48876 muscarinic antagonist
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:50919 antiemetic
CHEBI has role CHEBI:50949 serotonin uptake inhibitor
CHEBI has role CHEBI:65191 second generation antipsychotic
MeSH PA D000932 Antiemetics
MeSH PA D014150 Antipsychotic Agents
MeSH PA D001337 Autonomic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D014179 Neurotransmitter Uptake Inhibitors
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D018490 Serotonin Agents
MeSH PA D017367 Serotonin Uptake Inhibitors
MeSH PA D014149 Tranquilizing Agents
FDA EPC N0000175430 Atypical Antipsychotic

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Mixed bipolar I disorder indication 16506000 DOID:3312
Schizophrenia indication 58214004
Bipolar disorder in remission indication 85248005
Bipolar affective disorder, current episode manic indication 191618007
Bipolar affective disorder, current episode depression indication 191627008 DOID:3312
Major depressive disorder indication 370143000
Agitation associated with Bipolar Mania indication
Agitation associated with Schizophrenia indication
Depression Treatment Adjunct indication
Delirium contraindication 2776000
Suicidal thoughts contraindication 6471006
Weight gain finding contraindication 8943002
Sinus tachycardia contraindication 11092001
Hypercholesterolemia contraindication 13644009
Bipolar disorder contraindication 13746004 DOID:3312
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Senile dementia contraindication 15662003
Agranulocytosis contraindication 17182001 DOID:12987
Lowered convulsive threshold contraindication 19260006
Cirrhosis of liver contraindication 19943007 DOID:5082
Myocardial infarction contraindication 22298006 DOID:5844
Hypovolemia contraindication 28560003
Orthostatic hypotension contraindication 28651003
Dehydration contraindication 34095006
Upper gastrointestinal hemorrhage contraindication 37372002
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Syndrome of inappropriate vasopressin secretion contraindication 55004003 DOID:3401
Paralytic ileus contraindication 55525008 DOID:8442
Hyperlipidemia contraindication 55822004 DOID:1168
Anorexia nervosa contraindication 56882008 DOID:8689
Abnormal sexual function contraindication 56925008 DOID:1876
Hepatic failure contraindication 59927004
Cerebrovascular disease contraindication 62914000 DOID:6713
Blood coagulation disorder contraindication 64779008 DOID:1247
Sedation contraindication 72641008
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Heart failure contraindication 84114007 DOID:6000
Epilepsy contraindication 84757009 DOID:1826
Leukopenia contraindication 84828003 DOID:615
Hyponatremia contraindication 89627008
Tardive dyskinesia contraindication 102449007
Seizure disorder contraindication 128613002 DOID:1826
Liver function tests abnormal contraindication 166603001
Cerebrovascular accident contraindication 230690007 DOID:6713
Mania contraindication 231494001
Hypomania contraindication 231496004
Disease of liver contraindication 235856003 DOID:409
Metabolic syndrome X contraindication 237602007 DOID:14221
Hyperprolactinemia contraindication 237662005 DOID:12700
Transient ischemic attack contraindication 266257000 DOID:224
Esophageal dysmotility contraindication 266434009 DOID:9192
Benign prostatic hyperplasia contraindication 266569009 DOID:2883
Hypertriglyceridemia contraindication 302870006
Neutropenic disorder contraindication 303011007 DOID:1227
Serotonin syndrome contraindication 371089000
Coma contraindication 371632003
At risk for aspiration contraindication 371736008
Angle-closure glaucoma contraindication 392291006 DOID:13550
Myocardial ischemia contraindication 414795007 DOID:3393
Obesity contraindication 414916001 DOID:9970
Carcinoma of female breast contraindication 447782002
Smokes tobacco daily contraindication 449868002
Chemotherapy-induced nausea and vomiting off-label use 236084000

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.59 Basic
pKa2 5.72 Basic
pKa3 0.66 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 210MG BASE/VIAL ZYPREXA RELPREVV ELI LILLY CO N022173 Dec. 11, 2009 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 6169084 Sept. 30, 2018 A METHOD OF TREATING HUMAN SUFFERING FROM OR SUSCEPTIBLE TO PSYCHOSIS.
EQ 300MG BASE/VIAL ZYPREXA RELPREVV ELI LILLY CO N022173 Dec. 11, 2009 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 6169084 Sept. 30, 2018 A METHOD OF TREATING HUMAN SUFFERING FROM OR SUSCEPTIBLE TO PSYCHOSIS.
EQ 405MG BASE/VIAL ZYPREXA RELPREVV ELI LILLY CO N022173 Dec. 11, 2009 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 6169084 Sept. 30, 2018 A METHOD OF TREATING HUMAN SUFFERING FROM OR SUSCEPTIBLE TO PSYCHOSIS.

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 8.32 WOMBAT-PK CHEMBL
D(2) dopamine receptor GPCR ANTAGONIST Ki 8.52 WOMBAT-PK CHEMBL
D(4) dopamine receptor GPCR ANTAGONIST Ki 8.80 WOMBAT-PK
5-hydroxytryptamine receptor 1E GPCR AGONIST Ki 5.70 IUPHAR
Sodium-dependent serotonin transporter Transporter Ki 6.26 DRUG MATRIX
Alpha-1D adrenergic receptor GPCR Ki 7.59 DRUG MATRIX
5-hydroxytryptamine receptor 1A GPCR Kd 5.90 CHEMBL
D(3) dopamine receptor GPCR ANTAGONIST Ki 8.10 WOMBAT-PK
5-hydroxytryptamine receptor 2C GPCR ANTAGONIST Ki 7.96 WOMBAT-PK
5-hydroxytryptamine receptor 1F GPCR Ki 6.51 WOMBAT-PK
Alpha-1B adrenergic receptor GPCR Ki 6.58 WOMBAT-PK
5-hydroxytryptamine receptor 3A Ion channel Ki 6.69 WOMBAT-PK
Alpha-2C adrenergic receptor GPCR Ki 7.54 WOMBAT-PK
5-hydroxytryptamine receptor 1D GPCR Ki 6.12 WOMBAT-PK
5-hydroxytryptamine receptor 1B GPCR Ki 6.23 WOMBAT-PK
Aldehyde oxidase Enzyme IC50 5.22 WOMBAT-PK
Muscarinic acetylcholine receptor M5 GPCR Ki 8.05 WOMBAT-PK
Muscarinic acetylcholine receptor M4 GPCR Ki 7.68 WOMBAT-PK
Muscarinic acetylcholine receptor M3 GPCR Ki 7.14 WOMBAT-PK
Muscarinic acetylcholine receptor M2 GPCR Ki 7.10 WOMBAT-PK
Muscarinic acetylcholine receptor M1 GPCR Ki 7.51 WOMBAT-PK
Histamine H2 receptor GPCR Ki 7.36 WOMBAT-PK
Histamine H1 receptor GPCR Ki 8.15 WOMBAT-PK
D(1B) dopamine receptor GPCR Ki 7.05 WOMBAT-PK
Alpha-2B adrenergic receptor GPCR Ki 7.09 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 7.72 WOMBAT-PK
5-hydroxytryptamine receptor 7 GPCR Ki 6.98 WOMBAT-PK
5-hydroxytryptamine receptor 6 GPCR Ki 8.10 WOMBAT-PK
5-hydroxytryptamine receptor 2B GPCR Ki 7.92 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.74 WOMBAT-PK
Alpha-2A adrenergic receptor GPCR Ki 6.49 WOMBAT-PK
D(1A) dopamine receptor GPCR Ki 7.40 WOMBAT-PK
5-hydroxytryptamine receptor 5A GPCR Ki 5.92 PDSP
Beta-2 adrenergic receptor GPCR Ki 5.30 PDSP
Beta-1 adrenergic receptor GPCR Ki 5.30 PDSP
FAD-linked sulfhydryl oxidase ALR Enzyme AC50 6.43 CHEMBL
Arachidonate 15-lipoxygenase Enzyme IC50 5.56 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR Ki 7.68 DRUG MATRIX
5-hydroxytryptamine receptor 1B GPCR Ki 6.36 DRUG MATRIX
Transporter Transporter Ki 5.70 CHEMBL
Transporter Transporter Ki 6.02 CHEMBL
D(3) dopamine receptor GPCR Ki 7.41 CHEMBL
Serotonin 2 (5-HT2) receptor GPCR Ki 7.92 CHEMBL
Adrenergic receptor alpha-2 GPCR Ki 5.54 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 7.66 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 6.21 CHEMBL
D(1A) dopamine receptor GPCR Ki 7.70 CHEMBL
Histamine H1 receptor GPCR Ki 9.52 CHEMBL
D(2) dopamine receptor GPCR Ki 7.90 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 8.40 CHEMBL
D(4) dopamine receptor GPCR Ki 7.30 CHEMBL
Histamine H1 receptor GPCR Ki 8.20 CHEMBL
5-hydroxytryptamine receptor 6 GPCR ANTAGONIST Ki 8.60 IUPHAR
Alpha-1A adrenergic receptor GPCR IC50 7.19 CHEMBL
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 7 IUPHAR

External reference:

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IDSource
DB00334 DRUGBANK_ID
47 IUPHAR_LIGAND_ID
4020996 VUID
N0000148465 NUI
C0171023 UMLSCUI
D00454 KEGG_DRUG
CHEMBL715 ChEMBL_ID
4020996 VANDF
N0000007422 NDFRT
N0000148465 NDFRT
006204 NDDF
61381 RXNORM
d04050 MMSL
172501 MMSL
5198 MMSL
108441004 SNOMEDCT_US
386849001 SNOMEDCT_US
4585 PUBCHEM_CID
CHEMBL1201741 ChEMBL_ID
N7U69T4SZR UNII
6956 INN_ID
221373-18-8 SECONDARY_CAS_RN
C076029 MESH_SUPPLEMENTAL_RECORD_UI
CHEBI:7735 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Symbyax HUMAN PRESCRIPTION DRUG LABEL 2 0002-3230 CAPSULE 3 mg ORAL NDA 20 sections
Symbyax HUMAN PRESCRIPTION DRUG LABEL 2 0002-3231 CAPSULE 6 mg ORAL NDA 20 sections
Symbyax HUMAN PRESCRIPTION DRUG LABEL 2 0002-3232 CAPSULE 12 mg ORAL NDA 20 sections
Symbyax HUMAN PRESCRIPTION DRUG LABEL 2 0002-3233 CAPSULE 6 mg ORAL NDA 20 sections
Symbyax HUMAN PRESCRIPTION DRUG LABEL 2 0002-3234 CAPSULE 12 mg ORAL NDA 20 sections
Zyprexa HUMAN PRESCRIPTION DRUG LABEL 1 0002-4112 TABLET 2.50 mg ORAL NDA 20 sections
Zyprexa HUMAN PRESCRIPTION DRUG LABEL 1 0002-4115 TABLET 5 mg ORAL NDA 20 sections
Zyprexa HUMAN PRESCRIPTION DRUG LABEL 1 0002-4116 TABLET 7.50 mg ORAL NDA 20 sections
Zyprexa HUMAN PRESCRIPTION DRUG LABEL 1 0002-4117 TABLET 10 mg ORAL NDA 20 sections
Zyprexa HUMAN PRESCRIPTION DRUG LABEL 1 0002-4415 TABLET 15 mg ORAL NDA 20 sections
Zyprexa HUMAN PRESCRIPTION DRUG LABEL 1 0002-4420 TABLET 20 mg ORAL NDA 20 sections
ZYPREXA HUMAN PRESCRIPTION DRUG LABEL 1 0002-4453 TABLET, ORALLY DISINTEGRATING 5 mg ORAL NDA 20 sections
ZYPREXA HUMAN PRESCRIPTION DRUG LABEL 1 0002-4454 TABLET, ORALLY DISINTEGRATING 10 mg ORAL NDA 20 sections
ZYPREXA HUMAN PRESCRIPTION DRUG LABEL 1 0002-4455 TABLET, ORALLY DISINTEGRATING 15 mg ORAL NDA 20 sections
ZYPREXA HUMAN PRESCRIPTION DRUG LABEL 1 0002-4456 TABLET, ORALLY DISINTEGRATING 20 mg ORAL NDA 20 sections
ZYPREXA HUMAN PRESCRIPTION DRUG LABEL 1 0002-7597 INJECTION, POWDER, FOR SOLUTION 10 mg INTRAMUSCULAR NDA 20 sections
ZYPREXA HUMAN PRESCRIPTION DRUG LABEL 1 0002-7635 KIT 210 mg INTRAMUSCULAR NDA 21 sections
ZYPREXA HUMAN PRESCRIPTION DRUG LABEL 1 0002-7636 KIT 300 mg INTRAMUSCULAR NDA 21 sections
ZYPREXA HUMAN PRESCRIPTION DRUG LABEL 1 0002-7637 KIT 405 mg INTRAMUSCULAR NDA 21 sections
Olanzapine HUMAN PRESCRIPTION DRUG LABEL 1 0093-5105 TABLET, FILM COATED 20 mg ORAL ANDA 20 sections
Olanzapine HUMAN PRESCRIPTION DRUG LABEL 1 0093-5245 TABLET, ORALLY DISINTEGRATING 5 mg ORAL ANDA 20 sections
Olanzapine HUMAN PRESCRIPTION DRUG LABEL 1 0093-5246 TABLET, ORALLY DISINTEGRATING 10 mg ORAL ANDA 20 sections
Olanzapine HUMAN PRESCRIPTION DRUG LABEL 1 0093-5247 TABLET, ORALLY DISINTEGRATING 15 mg ORAL ANDA 20 sections
Olanzapine HUMAN PRESCRIPTION DRUG LABEL 1 0093-5248 TABLET, ORALLY DISINTEGRATING 20 mg ORAL ANDA 20 sections
Olanzapine and Fluoxetine HUMAN PRESCRIPTION DRUG LABEL 2 0093-5503 CAPSULE 3 mg ORAL ANDA 20 sections
Olanzapine and Fluoxetine HUMAN PRESCRIPTION DRUG LABEL 2 0093-5504 CAPSULE 6 mg ORAL ANDA 20 sections
Olanzapine and Fluoxetine HUMAN PRESCRIPTION DRUG LABEL 2 0093-5505 CAPSULE 6 mg ORAL ANDA 20 sections
Olanzapine and Fluoxetine HUMAN PRESCRIPTION DRUG LABEL 2 0093-5506 CAPSULE 12 mg ORAL ANDA 20 sections
Olanzapine and Fluoxetine HUMAN PRESCRIPTION DRUG LABEL 2 0093-5507 CAPSULE 12 mg ORAL ANDA 20 sections
Olanzapine HUMAN PRESCRIPTION DRUG LABEL 1 0093-5767 TABLET, FILM COATED 2.50 mg ORAL ANDA 20 sections