Identification
- Summary
Olanzapine is an antipsychotic drug used in the management of schizophrenia, bipolar 1 disorder, and agitation associated with these disorders.
- Brand Names
- Lybalvi, Olazax, Symbyax, Zalasta, Zypadhera, Zyprexa
- Generic Name
- Olanzapine
- DrugBank Accession Number
- DB00334
- Background
Olanzapine is a thienobenzodiazepine classified as an atypical or second-generation antipsychotic agent.2 The second-generation antipsychotics were introduced in the 90s and quickly gained traction due to their impressive efficacy, reduced risk for extrapyramidal side effects and reduced susceptibility to drug-drug interactions.5 Olanzapine very closely resembles clozapine and only differs by two additional methyl groups and the absence of a chloride moiety.10 It was discovered by scientists at Eli Lilly and approved to be marketed in the US in 1996.8
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Olanzapine (DB00334)
- Weight
- Average: 312.432
Monoisotopic: 312.14086735 - Chemical Formula
- C17H20N4S
- Synonyms
- 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine
- Olanzapin
- Olanzapina
- Olanzapine
- Olanzapinum
- External IDs
- LY 170053
- LY-170053
Pharmacology
- Indication
Olanzapine was initially used orally and intramuscularly for the chronic treatment of schizophrenia in patients over 13 years old and other psychiatric disorders such as bipolar I disorder including mixed or manic episodes.6
Olanzapine is also indicated, in combination with lithium or valproate for the short-term treatment of acute manic or mixed episodes associated with bipolar I disorder in adults.Label
As well, olanzapine is indicated, in combination with fluoxetine for the treatment of episodes of depression associated with bipolar disorder type 1 and treatment-resistant depression in patients over 10 years old.6
Olanzapine is also approved for the management of psychomotor agitation associated with schizophrenia and bipolar I mania.Label
Schizophrenia is a complex biochemical brain disorder that affects the person's ability to differentiate reality. It is usually observed as the presence of delusions, hallucinations, social withdrawal and disturbed thinking.11
Bipolar disorder is a mental health condition defined by periods of extreme mood disturbances. It is categorized in different types from which type 1 is known to involve episodes of severe mania and often depression while type 2 presents less severe forms of mania.12
Olanzapine is also indicated in combination with samidorphan for the treatment of bipolar I disorder, either as an adjunct to lithium or valproate or as monotherapy for the acute treatment of manic or mixed episodes or as maintenance therapy, and for the treatment of schizophrenia in adults.16
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Acute agitation •••••••••••• •••••••••• ••••••• ••• ••••••••• •••••••••• ••••••• ••• ••••••••••• •••••••• •••••••• •••••••••• ••••••• •••••••••••• ••• •••••••• Treatment of Acute agitation •••••••••••• •••••••••• ••••••• ••• ••••••••• •••••••••• ••••••• ••• ••••••••••• •••••••• •••••••• •••••••••• ••••••• •••••••••••• ••• •••••••• Management of Bipolar 1 disorder •••••••••••• Used in combination to treat Bipolar disorder with manic or mixed episodes Regimen in combination with: Valproic acid (DB00313), Lithium cation (DB01356) •••••••••••• ••••• •••••• Treatment of Delirium ••• ••••• - Contraindications & Blackbox Warnings
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The effect of olanzapine in the D2 receptor is reported to produce the positive effects of this drug such as a decrease in hallucinations, delusions, disorganized speech, disorganized thought, and disorganized behavior. On the other hand, its effect on the serotonin 5HT2A receptor prevents the onset of anhedonia, flat affect, alogia, avolition and poor attention.6 Based on the specific mechanism of action, olanzapine presents a higher affinity for the dopamine D2 receptor when compared to the rest of the dopamine receptor isotypes. This characteristic significantly reduces the presence of side effects.10
Clinical trials for the original use of olanzapine demonstrated significant effectiveness in the treatment of schizophrenia and bipolar disorder in adults and acute manic or mixed episodes associated with bipolar disorder in adolescents.4
The effect of olanzapine on dopamine and serotonin receptors has been suggested to reduce chemotherapy-induced nausea and vomiting as those receptors are suggested to be involved in this process. For this effect, several clinical trials have been conducted and it has been shown that olanzapine can produce a significant increase in total control of nausea and vomiting.1 In a high-level study of the effect of olanzapine for this condition, a complete response on the delay phase was observed in 84% of the individual and control of emesis of over 80% despite the phase.3
- Mechanism of action
The activity of olanzapine is achieved by the antagonism of multiple neuronal receptors including the dopamine receptor D1, D2, D3 and D4 in the brain, the serotonin receptors 5HT2A, 5HT2C, 5HT3 and 5HT6, the alpha-1 adrenergic receptor, the histamine receptor H1 and multiple muscarinic receptors.1,3
As abovementioned, olanzapine presents a wide profile of targets, however, its antagonistic effect towards the dopamine D2 receptor in the mesolimbic pathway is key as it blocks dopamine from having a potential action at the post-synaptic receptor. The binding of olanzapine to the dopamine D2 receptors is easily dissociable and hence, it allows for a certain degree of dopamine neurotransmission.6
On the other hand, olanzapine acts in the serotonin 5HT2A receptors in the frontal cortex in a similar manner than the reported on dopamine D2 receptors. This determined effect allows for a decrease in adverse effects.6
Target Actions Organism A5-hydroxytryptamine receptor 2A antagonistHumans ADopamine D2 receptor antagonistHumans UDopamine D1 receptor antagonistHumans UDopamine D5 receptor antagonistHumans UDopamine D3 receptor antagonistHumans UDopamine D4 receptor antagonistHumans U5-hydroxytryptamine receptor 2C antagonistHumans U5-hydroxytryptamine receptor 3A antagonistHumans U5-hydroxytryptamine receptor 6 antagonistHumans UHistamine H1 receptor antagonistHumans UAlpha-1A adrenergic receptor antagonistHumans UAlpha-1B adrenergic receptor antagonistHumans UMuscarinic acetylcholine receptor M1 antagonistHumans UMuscarinic acetylcholine receptor M2 antagonistHumans UMuscarinic acetylcholine receptor M3 antagonistHumans UMuscarinic acetylcholine receptor M4 antagonistHumans UD(1) dopamine receptor antagonistHumans NBeta adrenergic receptor inhibitorHumans U5-hydroxytryptamine receptor 1 inhibitorHumans NGABA(A) Receptor Benzodiazepine Binding Site inhibitorHumans - Absorption
Olanzapine presents a linear pharmacokinetic profile and, after daily administration, it reaches steady-state in about a week.6 Under the administration of a normal dosage of olanzapine, the steady-state plasma concentration does not seem to exceed 150 ng/ml with an AUC of 333 ng/h/ml.7,10
The absorption of olanzapine is not affected by the concomitant administration of food. The pharmacokinetic profile of olanzapine is characterized by reaching peak plasma concentration of 156.9 ng/ml approximately 6 hours after oral administration.8
- Volume of distribution
The volume of distribution of olanzapine is reported to be of 1000 liters which indicate a large distribution throughout the body.6
- Protein binding
Olanzapine is largely bound to plasma proteins and hence, about 93% of the administered dose is bound. The main proteins for binding are albumin and alpha-1 acid glycoprotein.6
- Metabolism
Olanzapine is greatly metabolized in the liver, which represents around 40% of the administered dose, mainly by the activity of glucuronide enzymes and by the cytochrome P450 system. From the CYP system, the main metabolic enzymes are CYP1A2 and CYP2D6.6 As part of the phase I metabolism, the major circulating metabolites of olanzapine, accounting for approximate 50-60% of this phase, are the 10-N-glucuronide and the 4'-N-desmethyl olanzapine which are clinically inactive and formed by the activity of CYP1A2.8 On the other hand, CYP2D6 catalyzes the formation of 2-OH olanzapine and the flavin-containing monooxygenase (FMO3) is responsible for N-oxide olanzapine.9
On the phase II metabolism of olanzapine, UGT1A4 is the key player by generating direct conjugation forms of olanzapine.9
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- Route of elimination
Olanzapine is mainly eliminated through metabolism and hence, only 7% of the eliminated drug can be found as the unchanged form. It is mainly excreted in the urine which represents around 53% of the excreted dose followed by the feces that represent about 30%.6
- Half-life
Olanzapine presents a half-life ranging between 21 to 54 hours with an average half-life of 30 hours.6
- Clearance
The mean clearance rate of olanzapine is of 29.4 L/hour however, some studies have reported an apparent clearance of 25 L/h.10
- Adverse Effects
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The toxicity symptoms of olanzapine are known to include somnolence, mydriasis, blurred vision, respiratory depression, hypotension, extrapyramidal symptoms and anticholinergic effects. The overdosage effects in children are generally associated with more significant side effects.7
The maximum registered dosage of olanzapine in clinical trials was of 300 mg and it was reported to present drowsiness and slurred speech. However, on post-marketing surveillance, a wide range of symptoms have been presented including agitation, dysarthria, tachycardia, extrapyramidal symptoms, and reduced consciousness. One case of overdosage-driven death was reported after ingestion of 450 mg of olanzapine. In the cases of acute overdosage, the establishment of adequate oxygenation and ventilation, gastric lavage and administration of activated charcoal with a laxative is recommended.Label
In carcinogenesis studies, olanzapine was showed to present an increase in the incidence of liver hemangiomas and hemangiosarcomas as well as mammary gland adenomas, and adenocarcinomas. On fertility studies, there was solely found impairment in male mating performance and delays in ovulation. There is no evidence of mutagenic, genotoxic potential not adverse events on fertility.Label
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details 5-hydroxytryptamine receptor 1A --- (C;C) CC Allele (homozygous) Effect Directly Studied The presence of this polymorphism in HTR1A may indicate a higher level of efficacy in improving negative symptoms of schizophrenia when treated with olanzapine. Details
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of adverse effects can be increased when 1,2-Benzodiazepine is combined with Olanzapine. Abaloparatide The risk or severity of adverse effects can be increased when Olanzapine is combined with Abaloparatide. Abametapir The serum concentration of Olanzapine can be increased when it is combined with Abametapir. Abatacept The metabolism of Olanzapine can be increased when combined with Abatacept. Abiraterone The serum concentration of Olanzapine can be increased when it is combined with Abiraterone. - Food Interactions
- Avoid alcohol. Alcohol may potentiate CNS adverse effects and orthostatic hypotension.
- Take with or without food. The absorption of olanzapine is unaffected by food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Olanzapine hydrochloride 0Q8K2L0MC3 783334-36-1 MFURKUWVJOJUHP-UHFFFAOYSA-N Olanzapine pamoate X7S6Q4MHCB 221373-18-8 ZIMCQJVMPKQQPB-UHFFFAOYSA-N Olanzapine tartrate 0KNI3MFH5F 491828-16-1 NFEUHAIRXOEOTJ-LREBCSMRSA-N - Product Images
- International/Other Brands
- Aedon (G.L. Pharma) / Amulsin (Sanitas) / Apisco (LKM) / Apsico (LKM) / Arkolamyl (Mylan) / Caprilon (Lavipharm) / CO Olanzapine (Cobalt) / Deprex (Square) / Dominazol (Stein) / Dopin (Daksh) / Egolanza (EGIS) / Elynza (Elynza) / Frenial (Biogen) / Jolyon-MD (Lupin) / Kozylex (Quisisana) / Lanopin (Molekule) / Lanzapin (Biogened) / Lanzep (Renata) / Lapenza (Smart Intermed) / Lapozan (Medochemie) / Lazapix (Portfarma)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Act Olanzapine Tablet 10 mg Oral Actavis Pharma Company 2009-10-15 2018-04-30 Canada 
Act Olanzapine Tablet 2.5 mg Oral Actavis Pharma Company 2009-10-15 2018-04-30 Canada Act Olanzapine Tablet 20 mg Oral Actavis Pharma Company 2009-10-15 2018-04-30 Canada Act Olanzapine Tablet 7.5 mg Oral Actavis Pharma Company 2009-10-15 2018-04-30 Canada Act Olanzapine Tablet 15 mg Oral Actavis Pharma Company 2009-10-15 2018-04-30 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Abbott-olanzapine ODT Tablet, orally disintegrating 15 mg Oral Abbott Laboratories 2014-12-03 2015-12-31 Canada Abbott-olanzapine ODT Tablet, orally disintegrating 10 mg Oral Abbott 2014-09-17 2015-12-31 Canada Abbott-olanzapine ODT Tablet, orally disintegrating 5 mg Oral Bgp Pharma Ulc 2014-09-17 2015-12-31 Canada Accel-olanzapine Tablet 10 mg Oral Accel Pharma Inc 2014-09-04 2015-11-09 Canada Accel-olanzapine Tablet 5 mg Oral Accel Pharma Inc 2014-09-04 2015-11-09 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image FLUXOPIN 12 MG/25 MG KAPSÜL ,30 KAPSÜL Olanzapine (12 mg) + Fluoxetine hydrochloride (25 mg) Capsule Oral Deva Holding A.S. 2020-08-14 2018-10-26 Turkey 
FLUXOPIN 12 MG/50 MG KAPSÜL ,30 KAPSÜL Olanzapine (12 mg) + Fluoxetine hydrochloride (50 mg) Capsule Oral Deva Holding A.S. 2020-08-14 2018-10-26 Turkey FLUXOPIN 3 MG/25 MG KAPSÜL ,30 KAPSÜL Olanzapine (3 mg) + Fluoxetine hydrochloride (25 mg) Capsule Oral Deva Holding A.S. 2020-08-14 2018-10-26 Turkey FLUXOPIN 6 MG/25 MG KAPSÜL ,30 KAPSÜL Olanzapine (6 mg) + Fluoxetine hydrochloride (25 mg) Capsule Oral Deva Holding A.S. 2020-08-14 2018-10-26 Turkey FLUXOPIN 6 MG/50 MG KAPSÜL ,30 KAPSÜL Olanzapine (6 mg) + Fluoxetine hydrochloride (50 mg) Capsule Oral Deva Holding A.S. 2020-08-14 2018-10-26 Turkey - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image ZYPREXA 10 MG IM ENJ. SOL. ICIN TOZ ICEREN FLAKON Olanzapine (10 mg) Injection, powder, for solution Intramuscular LİLLY İLAÇ TİC. LTD. ŞTİ. 2018-02-20 2022-04-11 Turkey
Categories
- ATC Codes
- N05AH53 — Olanzapine and samidorphan
- N05AH — Diazepines, oxazepines, thiazepines and oxepines
- N05A — ANTIPSYCHOTICS
- N05 — PSYCHOLEPTICS
- N — NERVOUS SYSTEM
- Drug Categories
- Adrenergic alpha-1 Receptor Antagonists
- Adrenergic alpha-Antagonists
- Adrenergic Antagonists
- Agents producing tachycardia
- Anticholinergic Agents
- Antidepressive Agents
- Antiemetics
- Antipsychotic Agents
- Antipsychotic Agents (Second Generation [Atypical])
- Autonomic Agents
- Benzazepines
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 Inhibitors (weak)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (weak)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (weak)
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Diazepines, Oxazepines, Thiazepines and Oxepines
- Dopamine Antagonists
- Dopamine D2 Receptor Antagonists
- Gastrointestinal Agents
- Heterocyclic Compounds, Fused-Ring
- Histamine Antagonists
- Histamine H1 Antagonists
- Histamine H2 Antagonists
- Hyperglycemia-Associated Agents
- Hypotensive Agents
- Muscarinic Antagonists
- Nervous System
- Neurotransmitter Agents
- P-glycoprotein substrates
- Peripheral Nervous System Agents
- Potential QTc-Prolonging Agents
- Psycholeptics
- Psychotropic Drugs
- QTc Prolonging Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin 5-HT2C Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Antagonists
- Tranquilizing Agents
- UGT1A4 substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as benzodiazepines. These are organic compounds containing a benzene ring fused to either isomers of diazepine(unsaturated seven-member heterocycle with two nitrogen atoms replacing two carbon atoms).
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Benzodiazepines
- Sub Class
- Not Available
- Direct Parent
- Benzodiazepines
- Alternative Parents
- Thienodiazepines / 2,3,5-trisubstituted thiophenes / N-methylpiperazines / N-arylated-2-aminothiophenes / 1,4-diazepines / Imidolactams / Benzenoids / Heteroaromatic compounds / Trialkylamines / Secondary amines show 5 more
- Substituents
- 1,4-diazinane / 2,3,5-trisubstituted thiophene / 2-aminothiophene / Amidine / Amine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Benzodiazepine / Carboxylic acid amidine show 18 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- N-arylpiperazine, N-methylpiperazine, benzodiazepine (CHEBI:7735)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- N7U69T4SZR
- CAS number
- 132539-06-1
- InChI Key
- KVWDHTXUZHCGIO-UHFFFAOYSA-N
- InChI
- InChI=1S/C17H20N4S/c1-12-11-13-16(21-9-7-20(2)8-10-21)18-14-5-3-4-6-15(14)19-17(13)22-12/h3-6,11,19H,7-10H2,1-2H3
- IUPAC Name
- 5-methyl-8-(4-methylpiperazin-1-yl)-4-thia-2,9-diazatricyclo[8.4.0.0^{3,7}]tetradeca-1(14),3(7),5,8,10,12-hexaene
- SMILES
- CN1CCN(CC1)C1=NC2=CC=CC=C2NC2=C1C=C(C)S2
References
- Synthesis Reference
- US6020487
- General References
- Chelkeba L, Gidey K, Mamo A, Yohannes B, Matso T, Melaku T: Olanzapine for chemotherapy-induced nausea and vomiting: systematic review and meta-analysis. Pharm Pract (Granada). 2017 Jan-Mar;15(1):877. doi: 10.18549/PharmPract.2017.01.877. Epub 2017 Mar 15. [Article]
- Martel ML, Klein LR, Rivard RL, Cole JB: A Large Retrospective Cohort of Patients Receiving Intravenous Olanzapine in the Emergency Department. Acad Emerg Med. 2016 Jan;23(1):29-35. doi: 10.1111/acem.12842. Epub 2015 Dec 31. [Article]
- Yang T, Liu Q, Lu M, Ma L, Zhou Y, Cui Y: Efficacy of olanzapine for the prophylaxis of chemotherapy-induced nausea and vomiting: a meta-analysis. Br J Clin Pharmacol. 2017 Jul;83(7):1369-1379. doi: 10.1111/bcp.13242. Epub 2017 Mar 23. [Article]
- Brunner E, Falk DM, Jones M, Dey DK, Shatapathy CC: Olanzapine in pregnancy and breastfeeding: a review of data from global safety surveillance. BMC Pharmacol Toxicol. 2013 Aug 1;14:38. doi: 10.1186/2050-6511-14-38. [Article]
- Malhotra K, Vu P, Wang DH, Lai H, Faziola LR: Olanzapine-Induced Neutropenia. Ment Illn. 2015 Jun 23;7(1):5871. doi: 10.4081/mi.2015.5871. eCollection 2015 Feb 24. [Article]
- Thomas K, Saadabadi A: Olanzapine . [Article]
- Chue P, Singer P: A review of olanzapine-associated toxicity and fatality in overdose. J Psychiatry Neurosci. 2003 Jul;28(4):253-61. [Article]
- Green W. (2001). Child & adolescent clinical psychopharmacology (3rd ed.). Lippincott Williams & Wilkins. [ISBN:0-7817-5950-1]
- Ng C., Lin K., Singh B. and Chiu E. (2008). Ethno-psychopharmacology. Cambridge University Press. [ISBN:978-0-521-87363-5]
- Schatzberg A. and Nemeroff C. (2017). The american psychiatric association publishing textbook of psychopharmacology (5th ed.). American Psychiatric Association Publishing. [ISBN:978-161-5371-228]
- Canadian Mental Health Association [Link]
- NIH [Link]
- Mylan-Olanzapine. Product monograph [Link]
- FDA Approved Drug Products: Zyprexa (olanzapine) [Link]
- FDA Approved Drug Products: Zyprexa (olanzapine) tablets and powder [Link]
- FDA Approved Drug Products: LYBALVI (olanzapine and samidorphan) tablets [Link]
- External Links
- Human Metabolome Database
- HMDB0005012
- KEGG Drug
- D00454
- KEGG Compound
- C07322
- PubChem Compound
- 4585
- PubChem Substance
- 46507666
- ChemSpider
- 10442212
- BindingDB
- 35254
- 61381
- ChEBI
- 7735
- ChEMBL
- CHEMBL715
- ZINC
- ZINC000052957434
- Therapeutic Targets Database
- DAP000022
- PharmGKB
- PA450688
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Olanzapine
- FDA label
- Download (418 KB)
- MSDS
- Download (232 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Not Available Healthy Male Volunteers 1 4 Completed Not Available Schizoaffective Disorders / Schizophrenia 1 4 Completed Basic Science Diabetes 2 4 Completed Basic Science Diabetes / Schizophrenia 1 4 Completed Basic Science Healthy Subjects (HS) 1
Pharmacoeconomics
- Manufacturers
- Eli lilly and co
- Packagers
- Advanced Pharmaceutical Services Inc.
- AQ Pharmaceuticals Inc.
- Block Drug Co. Inc.
- Cardinal Health
- Catalent Pharma Solutions
- Comprehensive Consultant Services Inc.
- Dispensing Solutions
- Eli Lilly & Co.
- Heartland Repack Services LLC
- Lake Erie Medical and Surgical Supply
- Lilly Del Caribe Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Neuman Distributors Inc.
- PD-Rx Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Rebel Distributors Corp.
- Remedy Repack
- Resource Optimization and Innovation LLC
- Sandhills Packaging Inc.
- Stat Rx Usa
- Dosage Forms
Form Route Strength Tablet, orally disintegrating Oral 10.0 MG Tablet, orally disintegrating Oral 5.0 MG Tablet Oral 7.500 mg Tablet Oral 10.00 mg Tablet, film coated Oral Tablet Oral 10.000 mg Tablet, effervescent 10 mg Tablet, effervescent 15 mg Tablet, effervescent 2.5 mg Tablet, effervescent Tablet, effervescent 5 mg Tablet, effervescent 7.5 mg Tablet, film coated Oral 10.00 mg Tablet, film coated Oral 5.00 mg Tablet, film coated Oral 5.0 MG Tablet, film coated Oral 15 MG Tablet, film coated Oral 2.5 MG Tablet, coated Oral 15 MG Tablet, coated Oral 2.5 MG Tablet, coated Oral 20 MG Tablet, coated Oral 7.5 MG Tablet, film coated Oral 20 mg Tablet, film coated Oral 7.5 mg Tablet, orally disintegrating Oral 2.5 MG Tablet, orally disintegrating Oral 7.5 MG Tablet, orally disintegrating Oral Solution Oral 5 MG/ML Tablet, coated Oral 1000000 mg Injection, powder, for solution Intramuscular 10 MG Tablet Oral Injection, powder, for solution Intramuscular 10 mg/2mL Injection, powder, lyophilized, for solution Intramuscular 10 mg/1 Injection, powder, lyophilized, for solution Intramuscular 10 mg/2mL Tablet, film coated Oral 10 mg/1 Tablet, film coated Oral 15 mg/1 Tablet, film coated Oral 2.5 mg/1 Tablet, film coated Oral 20 mg/1 Tablet, film coated Oral 5 mg/1 Tablet, film coated Oral 7.5 mg/1 Tablet, orally disintegrating Oral 10 mg/1 Tablet, orally disintegrating Oral 15 mg/1 Tablet, orally disintegrating Oral 20 mg/1 Tablet, orally disintegrating Oral 5 mg/1 Capsule Oral Tablet, film coated Oral 10 mg Tablet Oral 10 mg Tablet Oral 5 mg Tablet, film coated Oral 5 mg Tablet Oral 5.000 mg Tablet Oral 10.0 mg Tablet Oral 15.0 mg Tablet Oral 20.0 mg Tablet Oral 5.0 mg Tablet Oral 2.5 mg Tablet Oral 7.5 mg Tablet Oral 500000 mg Injection, powder, lyophilized, for solution Intramuscular 10 mg Injection, powder, for suspension, extended release Intramuscular 210 mg Injection, powder, for suspension, extended release Intramuscular 300 mg Injection, powder, for suspension, extended release Intramuscular 405 mg Powder Intramuscular; Parenteral 210 MG Powder Intramuscular; Parenteral 300 MG Powder Intramuscular; Parenteral 405 MG Tablet Oral 10 mg/1 Tablet Oral 15 mg/1 Tablet Oral 2.5 mg/1 Tablet Oral 20 mg/1 Tablet Oral 5 mg/1 Tablet Oral 7.5 mg/1 Tablet, film coated Oral Tablet, for suspension Oral 10 MG Tablet, for suspension Oral 15 MG Tablet, for suspension Oral 20 MG Tablet, for suspension Oral 5 MG Injection, powder, lyophilized, for solution Intramuscular 1000000 mg Tablet Oral 15 mg Tablet Oral 20 mg Injection, powder, for solution Intramuscular Solution Parenteral 10.000 mg Powder, for solution Intramuscular 10 mg / vial Kit Intramuscular 210 mg/1.4mL Kit Intramuscular 300 mg/2.0mL Kit Intramuscular 405 mg/2.7mL Tablet Oral 5.0000 mg Tablet, orally disintegrating Oral 15 mg Tablet, orally disintegrating Oral 20 mg Tablet, soluble Oral Tablet, orally disintegrating Oral 10 mg Tablet, orally disintegrating Oral 5 mg Tablet, soluble Oral 10 mg Tablet, soluble Oral 5 mg Tablet, coated Oral 10 mg Tablet, coated Oral 5 mg - Prices
Unit description Cost Unit Zyprexa relprevv 405 mg vial 1287.9USD vial Zyprexa relprevv 300 mg vial 954.0USD vial Zyprexa relprevv 210 mg vial 667.8USD vial ZyPREXA Zydis 30 10 mg Dispersible Tablet Box 562.35USD box ZyPREXA Zydis 30 5 mg Dispersible Tablet Box 385.63USD box Zyprexa 10 mg vial 35.69USD vial Zyprexa zydis 20 mg tablet 34.87USD tablet Zyprexa 20 mg tablet 34.37USD tablet Zyprexa zydis 15 mg tablet 26.45USD tablet Zyprexa 15 mg tablet 21.14USD tablet Symbyax 12-25 mg capsule 20.62USD capsule Symbyax 12-50 mg capsule 20.62USD capsule Zyprexa zydis 10 mg tablet 18.02USD tablet Symbyax 6-50 mg capsule 14.56USD capsule Zyprexa 10 mg tablet 14.09USD tablet Symbyax 6-25 mg capsule 13.69USD capsule Zyprexa zydis 5 mg tablet 12.36USD tablet Zyprexa 7.5 mg tablet 11.23USD tablet Symbyax 3-25 mg capsule 10.01USD capsule Zyprexa 5 mg tablet 8.92USD tablet Zyprexa Zydis 10 mg Disintegrating Tablet 7.86USD tablet Zyprexa 2.5 mg tablet 7.1USD tablet Apo-Olanzapine 15 mg Tablet 6.64USD tablet Co Olanzapine 15 mg Tablet 6.64USD tablet Novo-Olanzapine 15 mg Tablet 6.64USD tablet Pms-Olanzapine 15 mg Tablet 6.64USD tablet Apo-Olanzapine 10 mg Tablet 4.43USD tablet Co Olanzapine 10 mg Tablet 4.43USD tablet Novo-Olanzapine 10 mg Tablet 4.43USD tablet Pms-Olanzapine 10 mg Tablet 4.43USD tablet Zyprexa Zydis 5 mg Disintegrating Tablet 3.93USD tablet Co Olanzapine Odt 10 mg Disintegrating Tablet 3.54USD tablet Novo-Olanzapine Od 10 mg Disintegrating Tablet 3.54USD tablet Pms-Olanzapine Odt 10 mg Disintegrating Tablet 3.54USD tablet Sandoz Olanzapine Odt 10 mg Disintegrating Tablet 3.54USD tablet Apo-Olanzapine 7.5 mg Tablet 3.32USD tablet Co Olanzapine 7.5 mg Tablet 3.32USD tablet Novo-Olanzapine 7.5 mg Tablet 3.32USD tablet Pms-Olanzapine 7.5 mg Tablet 3.32USD tablet Apo-Olanzapine 5 mg Tablet 2.21USD tablet Co Olanzapine 5 mg Tablet 2.21USD tablet Novo-Olanzapine 5 mg Tablet 2.21USD tablet Pms-Olanzapine 5 mg Tablet 2.21USD tablet Co Olanzapine Odt 5 mg Disintegrating Tablet 1.77USD tablet Novo-Olanzapine Od 5 mg Disintegrating Tablet 1.77USD tablet Pms-Olanzapine Odt 5 mg Disintegrating Tablet 1.77USD tablet Sandoz Olanzapine Odt 5 mg Disintegrating Tablet 1.77USD tablet Apo-Olanzapine 2.5 mg Tablet 1.11USD tablet Co Olanzapine 2.5 mg Tablet 1.11USD tablet Novo-Olanzapine 2.5 mg Tablet 1.11USD tablet Pms-Olanzapine 2.5 mg Tablet 1.11USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6251895 No 2001-06-26 2018-03-23 US 
US5229382 No 1993-07-20 2011-04-23 US CA2216372 No 2007-11-20 2016-03-22 Canada CA2041113 No 1998-07-14 2011-04-24 Canada US6960577 No 2005-11-01 2017-11-01 US US5945416 No 1999-08-31 2017-03-24 US US6169084 No 2001-01-02 2018-09-30 US US8778960 No 2014-07-15 2032-02-13 US US9126977 No 2015-09-08 2031-08-23 US US9517235 No 2016-12-13 2031-08-23 US US10716785 No 2020-07-21 2031-08-23 US US10300054 No 2019-05-28 2031-08-23 US US9119848 No 2015-09-01 2031-08-30 US US7956187 No 2011-06-07 2021-10-31 US US8252929 No 2012-08-28 2021-10-31 US US7262298 No 2007-08-28 2025-11-23 US US11185541 No 2021-11-30 2031-08-23 US US11241425 No 2011-08-23 2031-08-23 US US11351166 No 2011-08-23 2031-08-23 US US11707466 No 2021-11-12 2041-11-12 US US11793805 No 2011-08-23 2031-08-23 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 189-195 °C 'MSDS' boiling point (°C) 476 ºC 'MSDS' water solubility Partly miscible 'MSDS' logP 4.094 'MSDS' pKa 10.57 Mylan-Olanzapine product monograph - Predicted Properties
Property Value Source Water Solubility 0.0942 mg/mL ALOGPS logP 3.61 ALOGPS logP 3.39 Chemaxon logS -3.5 ALOGPS pKa (Strongest Acidic) 15.67 Chemaxon pKa (Strongest Basic) 7.24 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 30.87 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 93.87 m3·mol-1 Chemaxon Polarizability 35.35 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9645 Blood Brain Barrier + 0.9652 Caco-2 permeable + 0.5993 P-glycoprotein substrate Substrate 0.8524 P-glycoprotein inhibitor I Inhibitor 0.6888 P-glycoprotein inhibitor II Inhibitor 0.7204 Renal organic cation transporter Inhibitor 0.7715 CYP450 2C9 substrate Non-substrate 0.7493 CYP450 2D6 substrate Substrate 0.8918 CYP450 3A4 substrate Substrate 0.5421 CYP450 1A2 substrate Inhibitor 0.6454 CYP450 2C9 inhibitor Non-inhibitor 0.6914 CYP450 2D6 inhibitor Inhibitor 0.608 CYP450 2C19 inhibitor Inhibitor 0.572 CYP450 3A4 inhibitor Non-inhibitor 0.9526 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.707 Ames test Non AMES toxic 0.7009 Carcinogenicity Non-carcinogens 0.9369 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.6972 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9483 hERG inhibition (predictor II) Inhibitor 0.7569
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 182.6556742 predictedDarkChem Lite v0.1.0 [M-H]- 184.4327742 predictedDarkChem Lite v0.1.0 [M-H]- 166.1846 predictedDeepCCS 1.0 (2019) [M+H]+ 183.3909742 predictedDarkChem Lite v0.1.0 [M+H]+ 184.6764742 predictedDarkChem Lite v0.1.0 [M+H]+ 168.5426 predictedDeepCCS 1.0 (2019) [M+Na]+ 183.0629742 predictedDarkChem Lite v0.1.0 [M+Na]+ 174.63574 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Virus receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
- Gene Name
- HTR2A
- Uniprot ID
- P28223
- Uniprot Name
- 5-hydroxytryptamine receptor 2A
- Molecular Weight
- 52602.58 Da
References
- McDonald LM, Moran PM, Vythelingum GN, Joseph MH, Stephenson JD, Gray JA: Enhancement of latent inhibition by two 5-HT2A receptor antagonists only when given at both pre-exposure and conditioning. Psychopharmacology (Berl). 2003 Sep;169(3-4):321-31. Epub 2002 Aug 9. [Article]
- Moresco RM, Cavallaro R, Messa C, Bravi D, Gobbo C, Galli L, Lucignani G, Colombo C, Rizzo G, Velona I, Smeraldi E, Fazio F: Cerebral D2 and 5-HT2 receptor occupancy in Schizophrenic patients treated with olanzapine or clozapine. J Psychopharmacol. 2004 Sep;18(3):355-65. [Article]
- Sharpley AL, Attenburrow ME, Hafizi S, Cowen PJ: Olanzapine increases slow wave sleep and sleep continuity in SSRI-resistant depressed patients. J Clin Psychiatry. 2005 Apr;66(4):450-4. [Article]
- Yatham LN, Goldstein JM, Vieta E, Bowden CL, Grunze H, Post RM, Suppes T, Calabrese JR: Atypical antipsychotics in bipolar depression: potential mechanisms of action. J Clin Psychiatry. 2005;66 Suppl 5:40-8. [Article]
- Padin JF, Rodriguez MA, Dominguez E, Dopeso-Reyes IG, Buceta M, Cano E, Sotelo E, Brea J, Caruncho HJ, Isabel Cadavid M, Castro M, Isabel Loza M: Parallel regulation by olanzapine of the patterns of expression of 5-HT2A and D3 receptors in rat central nervous system and blood cells. Neuropharmacology. 2006 Sep;51(4):923-32. Epub 2006 Aug 14. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S: Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Potassium channel regulator activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
- Gene Name
- DRD2
- Uniprot ID
- P14416
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Naiker DV, Catts SV, Catts VS, Bedi KS, Bryan-Lluka LJ: Dose determination of haloperidol, risperidone and olanzapine using an in vivo dopamine D2-receptor occupancy method in the rat. Eur J Pharmacol. 2006 Jul 1;540(1-3):87-90. Epub 2006 May 11. [Article]
- Weizman T, Pick CG, Backer MM, Rigai T, Bloch M, Schreiber S: The antinociceptive effect of amisulpride in mice is mediated through opioid mechanisms. Eur J Pharmacol. 2003 Oct 8;478(2-3):155-9. [Article]
- Jordan S, Regardie K, Johnson JL, Chen R, Kambayashi J, McQuade R, Kitagawa H, Tadori Y, Kikuchi T: In vitro functional characteristics of dopamine D2 receptor partial agonists in second and third messenger-based assays of cloned human dopamine D2Long receptor signalling. J Psychopharmacol. 2007 Aug;21(6):620-7. Epub 2006 Nov 8. [Article]
- Thacker SK, Perna MK, Ward JJ, Schaefer TL, Williams MT, Kostrzewa RM, Brown RW: The effects of adulthood olanzapine treatment on cognitive performance and neurotrophic factor content in male and female rats neonatally treated with quinpirole. Eur J Neurosci. 2006 Oct;24(7):2075-83. [Article]
- Lencz T, Robinson DG, Xu K, Ekholm J, Sevy S, Gunduz-Bruce H, Woerner MG, Kane JM, Goldman D, Malhotra AK: DRD2 promoter region variation as a predictor of sustained response to antipsychotic medication in first-episode schizophrenia patients. Am J Psychiatry. 2006 Mar;163(3):529-31. [Article]
- Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S: Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- DRD1
- Uniprot ID
- P21728
- Uniprot Name
- D(1A) dopamine receptor
- Molecular Weight
- 49292.765 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- DRD5
- Uniprot ID
- P21918
- Uniprot Name
- D(1B) dopamine receptor
- Molecular Weight
- 52950.5 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
- Gene Name
- DRD3
- Uniprot ID
- P35462
- Uniprot Name
- D(3) dopamine receptor
- Molecular Weight
- 44224.335 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Sh3 domain binding
- Specific Function
- Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
- Gene Name
- DRD4
- Uniprot ID
- P21917
- Uniprot Name
- D(4) dopamine receptor
- Molecular Weight
- 48359.86 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Hutchison KE, Ray L, Sandman E, Rutter MC, Peters A, Davidson D, Swift R: The effect of olanzapine on craving and alcohol consumption. Neuropsychopharmacology. 2006 Jun;31(6):1310-7. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
- Gene Name
- HTR2C
- Uniprot ID
- P28335
- Uniprot Name
- 5-hydroxytryptamine receptor 2C
- Molecular Weight
- 51820.705 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Zhang JY, Kowal DM, Nawoschik SP, Lou Z, Dunlop J: Distinct functional profiles of aripiprazole and olanzapine at RNA edited human 5-HT2C receptor isoforms. Biochem Pharmacol. 2006 Feb 14;71(4):521-9. Epub 2005 Dec 5. [Article]
- Overstreet DH, Knapp DJ, Breese GR: Drug challenges reveal differences in mediation of stress facilitation of voluntary alcohol drinking and withdrawal-induced anxiety in alcohol-preferring P rats. Alcohol Clin Exp Res. 2007 Sep;31(9):1473-81. Epub 2007 Jul 11. [Article]
- Theisen FM, Haberhausen M, Firnges MA, Gregory P, Reinders JH, Remschmidt H, Hebebrand J, Antel J: No evidence for binding of clozapine, olanzapine and/or haloperidol to selected receptors involved in body weight regulation. Pharmacogenomics J. 2007 Aug;7(4):275-81. Epub 2006 Sep 19. [Article]
- Wood MD, Scott C, Clarke K, Cato KJ, Patel N, Heath J, Worby A, Gordon L, Campbell L, Riley G, Davies CH, Gribble A, Jones DN: Pharmacological profile of antipsychotics at monoamine receptors: atypicality beyond 5-HT2A receptor blockade. CNS Neurol Disord Drug Targets. 2006 Aug;5(4):445-52. [Article]
- Hertel P: Comparing sertindole to other new generation antipsychotics on preferential dopamine output in limbic versus striatal projection regions: mechanism of action. Synapse. 2006 Dec 1;60(7):543-52. [Article]
- Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gate...
- Gene Name
- HTR3A
- Uniprot ID
- P46098
- Uniprot Name
- 5-hydroxytryptamine receptor 3A
- Molecular Weight
- 55279.835 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Serotonin receptor activity
- Specific Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
- Gene Name
- HTR6
- Uniprot ID
- P50406
- Uniprot Name
- 5-hydroxytryptamine receptor 6
- Molecular Weight
- 46953.625 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Histamine receptor activity
- Specific Function
- In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Poyurovsky M, Pashinian A, Levi A, Weizman R, Weizman A: The effect of betahistine, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Int Clin Psychopharmacol. 2005 Mar;20(2):101-3. [Article]
- Rasmussen K, Benvenga MJ, Bymaster FP, Calligaro DO, Cohen IR, Falcone JF, Hemrick-Luecke SK, Martin FM, Moore NA, Nisenbaum LK, Schaus JM, Sundquist SJ, Tupper DE, Wiernicki TR, Nelson DL: Preclinical pharmacology of FMPD [6-fluoro-10-[3-(2-methoxyethyl)-4-methyl-piperazin-1-yl]-2-methyl-4H-3-thia-4,9- diaza-benzo[f]azulene]: a potential novel antipsychotic with lower histamine H1 receptor affinity than olanzapine. J Pharmacol Exp Ther. 2005 Dec;315(3):1265-77. Epub 2005 Sep 1. [Article]
- Altschuler EL, Kast RE: Using histamine (H1) antagonists, in particular atypical antipsychotics, to treat anemia of chronic disease via interleukin-6 suppression. Med Hypotheses. 2005;65(1):65-7. [Article]
- Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S: Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27. [Article]
- Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1B
- Uniprot ID
- P35368
- Uniprot Name
- Alpha-1B adrenergic receptor
- Molecular Weight
- 56835.375 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S: Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM1
- Uniprot ID
- P11229
- Uniprot Name
- Muscarinic acetylcholine receptor M1
- Molecular Weight
- 51420.375 Da
References
- Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S: Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled acetylcholine receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM2
- Uniprot ID
- P08172
- Uniprot Name
- Muscarinic acetylcholine receptor M2
- Molecular Weight
- 51714.605 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM3
- Uniprot ID
- P20309
- Uniprot Name
- Muscarinic acetylcholine receptor M3
- Molecular Weight
- 66127.445 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Guanyl-nucleotide exchange factor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM4
- Uniprot ID
- P08173
- Uniprot Name
- Muscarinic acetylcholine receptor M4
- Molecular Weight
- 53048.65 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Components:
References
- Fernandez J, Alonso JM, Andres JI, Cid JM, Diaz A, Iturrino L, Gil P, Megens A, Sipido VK, Trabanco AA: Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. J Med Chem. 2005 Mar 24;48(6):1709-12. [Article]
- Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [Article]
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Receptor signaling protein activity
- Specific Function
- Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately e...
Components:
| Name | UniProt ID |
|---|---|
| Beta-1 adrenergic receptor | P08588 |
| Beta-2 adrenergic receptor | P07550 |
| Beta-3 adrenergic receptor | P13945 |
References
- Bymaster FP, Calligaro DO, Falcone JF, Marsh RD, Moore NA, Tye NC, Seeman P, Wong DT: Radioreceptor binding profile of the atypical antipsychotic olanzapine. Neuropsychopharmacology. 1996 Feb;14(2):87-96. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Components:
| Name | UniProt ID |
|---|---|
| 5-hydroxytryptamine receptor 1A | P08908 |
| 5-hydroxytryptamine receptor 1B | P28222 |
| 5-hydroxytryptamine receptor 1D | P28221 |
| 5-hydroxytryptamine receptor 1E | P28566 |
| 5-hydroxytryptamine receptor 1F | P30939 |
References
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function
- Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Components:
References
- Brafford MV, Glode A: Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting. J Adv Pract Oncol. 2014 Jan;5(1):24-9. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Callaghan JT, Bergstrom RF, Ptak LR, Beasley CM: Olanzapine. Pharmacokinetic and pharmacodynamic profile. Clin Pharmacokinet. 1999 Sep;37(3):177-93. [Article]
- Thomas K, Saadabadi A: Olanzapine . [Article]
- Rao ML, Hiemke C, Grasmader K, Baumann P: [Olanzapine: pharmacology, pharmacokinetics and therapeutic drug monitoring]. Fortschr Neurol Psychiatr. 2001 Nov;69(11):510-7. doi: 10.1055/s-2001-18381. [Article]
- SYMBYAX (olanzapine and fluoxetine HCl capsules) - FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Trimethylamine monooxygenase activity
- Specific Function
- Involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. It N-oxygenates primary aliphatic alkylamines as well as secondary and tertiary amines. Plays an impor...
- Gene Name
- FMO3
- Uniprot ID
- P31513
- Uniprot Name
- Dimethylaniline monooxygenase [N-oxide-forming] 3
- Molecular Weight
- 60032.975 Da
References
- Callaghan JT, Bergstrom RF, Ptak LR, Beasley CM: Olanzapine. Pharmacokinetic and pharmacodynamic profile. Clin Pharmacokinet. 1999 Sep;37(3):177-93. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- Current data regarding this enzyme inhibition is limited to in vitro studies, which is also indicated on the FDA label.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Olanzapine FDA label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Protein homodimerization activity
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
- Gene Name
- UGT1A4
- Uniprot ID
- P22310
- Uniprot Name
- UDP-glucuronosyltransferase 1-4
- Molecular Weight
- 60024.535 Da
References
- Ng C., Lin K., Singh B. and Chiu E. (2008). Ethno-psychopharmacology. Cambridge University Press. [ISBN:978-0-521-87363-5]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- The total cytochrome P450 inhibition of olanzapine is <0.3%. The ki for CYP3A mediated formation of 1'-hydroxymidazolam is is 491, with an IC50 of 14.65µM.
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Ring BJ, Binkley SN, Vandenbranden M, Wrighton SA: In vitro interaction of the antipsychotic agent olanzapine with human cytochromes P450 CYP2C9, CYP2C19, CYP2D6 and CYP3A. Br J Clin Pharmacol. 1996 Mar;41(3):181-6. [Article]
- Gervasini G, Caballero MJ, Carrillo JA, Benitez J: Comparative cytochrome p450 in vitro inhibition by atypical antipsychotic drugs. ISRN Pharmacol. 2013;2013:792456. doi: 10.1155/2013/792456. Epub 2013 Feb 13. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- The total cytochrome P450 inhibition of olanzapine is <0.3%. The ki for CYP3A mediated formation of 1'-hydroxymidazolam is is 491, with an IC50 of 14.65µM.
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Components:
| Name | UniProt ID |
|---|---|
| Cytochrome P450 3A4 | P08684 |
| Cytochrome P450 3A43 | Q9HB55 |
| Cytochrome P450 3A5 | P20815 |
| Cytochrome P450 3A7 | P24462 |
References
- Ring BJ, Binkley SN, Vandenbranden M, Wrighton SA: In vitro interaction of the antipsychotic agent olanzapine with human cytochromes P450 CYP2C9, CYP2C19, CYP2D6 and CYP3A. Br J Clin Pharmacol. 1996 Mar;41(3):181-6. [Article]
- Gervasini G, Caballero MJ, Carrillo JA, Benitez J: Comparative cytochrome p450 in vitro inhibition by atypical antipsychotic drugs. ISRN Pharmacol. 2013;2013:792456. doi: 10.1155/2013/792456. Epub 2013 Feb 13. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
- Gene Name
- ORM1
- Uniprot ID
- P02763
- Uniprot Name
- Alpha-1-acid glycoprotein 1
- Molecular Weight
- 23511.38 Da
References
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Boulton DW, DeVane CL, Liston HL, Markowitz JS: In vitro P-glycoprotein affinity for atypical and conventional antipsychotics. Life Sci. 2002 May 31;71(2):163-9. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55