Quetiapine

Identification

Summary

Quetiapine is an atypical antipsychotic agent used for the management of bipolar disorder, schizophrenia, and major depressive disorder.

Brand Names
Seroquel
Generic Name
Quetiapine
DrugBank Accession Number
DB01224
Background

Initially approved by the FDA in 1997, quetiapine is a second-generation atypical antipsychotic used in schizophrenia, major depression, and bipolar disorder.19 Quetiapine demonstrates a high level of therapeutic efficacy and low risk of adverse effects during long-term treatment. It is well-tolerated and a suitable option for some patients with high sensitivity to other drugs, such as clozapine and olanzapine.1

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 383.507
Monoisotopic: 383.166747749
Chemical Formula
C21H25N3O2S
Synonyms
  • 2-[2-(4-Dibenzo[b,f][1,4]thiazepin-11-yl-1-piperazinyl)ethoxy]ethanol
  • Quetiapina
  • Quétiapine
  • Quetiapine
  • Quetiapinum

Pharmacology

Indication

Quetiapine is used in the symptomatic treatment of schizophrenia. In addition, it may be used for the management of acute manic or mixed episodes in patients with bipolar I disorder, as a monotherapy or combined with other drugs. It may be used to manage depressive episodes in bipolar disorder. In addition to the above indications, quetiapine is used in combination with antidepressant drugs for the treatment of major depression.19

Some off-label uses for this drug include the management of post-traumatic stress disorder (PTSD), generalized anxiety disorder, and psychosis associated with Parkinson's disease.7,10,18

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Adjunct therapy in management ofBipolar 1 disorder••••••••••••••••••• ••••••• •••••••• •••••••• ••••••• •••• ••••••• ••••••• •••• ••••••• •••••••• •••••••• ••••••• ••••••••••• •••••••• •••••••
Adjunct therapy in management ofBipolar 1 disorder••••••••••••••••••• •••••••• •••••••• ••••••• •••• ••••••• •••••••• •••••••• ••••••• ••••••••••• •••••••• •••••••• ••••••• ••••••• •••• ••••••
Management ofGeneralized anxiety disorder••• •••••
Adjunct therapy in treatment ofMajor depressive disorders••••••••••••••••••• •••••••• •••••••• ••••••• •••• ••••••• •••••••• •••••••• ••••••• ••••••••••• •••••••• •••••••
Treatment ofManic episode••••••••••••••••••• ••••••• •••••••• •••••••• ••••••• •••• ••••••• ••••••• •••• ••••••• •••••••• •••••••• ••••••• ••••••••••• •••••••• •••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Quetiapine improves the positive and negative symptoms of schizophrenia and major depression by acting on various neurotransmitter receptors, such as the serotonin and dopamine receptors. In bipolar disorder, it improves both depressive and manic symptoms.1,8,9

A note on suicidality in young patients and administration in the elderly

Quetiapine can cause suicidal thinking or behavior in children and adolescents and should not be given to children under 10 years of age. It is important to monitor for suicidality if this drug is given to younger patients. In addition, this drug is not indicated for the treatment of psychosis related to dementia due to an increased death rate in elderly patients taking this drug.19

Mechanism of action

Although the mechanism of action of quetiapine is not fully understood, several proposed mechanisms exist. In schizophrenia, its actions could occur from the antagonism of dopamine type 2 (D2) and serotonin 2A (5HT2A) receptors. In bipolar depression and major depression, quetiapine's actions may be attributed to the binding of this drug or its metabolite to the norepinephrine transporter. Additional effects of quetiapine, including somnolence, orthostatic hypotension, and anticholinergic effects, may result from the antagonism of H1 receptors, adrenergic α1 receptors, and muscarinic M1 receptors, respectively.1,7,19

TargetActionsOrganism
A5-hydroxytryptamine receptor 2A
antagonist
Humans
ADopamine D2 receptor
antagonist
Humans
U5-hydroxytryptamine receptor 1A
antagonist
partial agonist
Humans
U5-hydroxytryptamine receptor 1B
ligand
Humans
U5-hydroxytryptamine receptor 1D
ligand
Humans
U5-hydroxytryptamine receptor 1E
ligand
Humans
U5-hydroxytryptamine receptor 2C
ligand
Humans
U5-hydroxytryptamine receptor 3A
ligand
Humans
U5-hydroxytryptamine receptor 6
antagonist
Humans
U5-hydroxytryptamine receptor 7
ligand
Humans
UDopamine D1 receptor
antagonist
Humans
UDopamine D5 receptor
ligand
Humans
UDopamine D3 receptor
ligand
Humans
UDopamine D4 receptor
ligand
Humans
UHistamine H1 receptor
antagonist
Humans
UAlpha-1 adrenergic receptors
antagonist
Humans
UAlpha-2A adrenergic receptor
antagonist
Humans
UAlpha-2B adrenergic receptor
antagonist
Humans
UAlpha-2C adrenergic receptor
antagonist
Humans
UMuscarinic acetylcholine receptor M1
antagonist
Humans
UMuscarinic acetylcholine receptor M2
ligand
Humans
UMuscarinic acetylcholine receptor M3
antagonist
Humans
UMuscarinic acetylcholine receptor M4
ligand
Humans
UMuscarinic acetylcholine receptor M5
ligand
Humans
Absorption

Quetiapine is rapidly and well absorbed after administration of an oral dose. Steady-state is achieved within 48 hours15 Peak plasma concentrations are achieved within 1.5 hours. The bioavailability of a tablet is 100%. The steady-state Cmax of quetiapine in Han Chinese patients with schizophrenia after a 300 mg oral dose of the extended released formulation was approximately 467 ng/mL and the AUC at steady-state was 5094 ng·h/mL.17 Absorption of quetiapine is affected by food, with Cmax increased by 25% and AUC increased by 15%.19

Volume of distribution

Quetiapine distributes throughout body tissues. The apparent volume of distribution of this drug is about 10±4 L/kg.19

Protein binding

The protein binding of quetiapine is 83%.5,19

Metabolism

The metabolism of quetiapine occurs mainly in the liver. Sulfoxidation and oxidation are the main metabolic pathways of this drug. According to in vitro studies, cytochrome P450 3A4 metabolizes quetiapine to an inactive sulfoxide metabolite and also participates in the metabolism of its active metabolite, N-desalkyl quetiapine. CYP2D6 also regulates the metabolism of quetiapine. In one study, three metabolites of N-desalkylquetiapine were identified. Two of the metabolites were identified as N-desalkylquetiapine sulfoxide and 7-hydroxy-N-desalkylquetiapine. CYP2D6 has been found to be responsible for metabolism of quetiapine to 7-hydroxy-N-desalkylquetiapine, a pharmacologically active metabolite. Individual differences in CYP2D6 metabolism may be present, which may affect the concentrations of the active metabolite.4,11,19

Hover over products below to view reaction partners

Route of elimination

After an oral dose of radiolabeled quetiapine, less than 1% of unchanged drug was detected in the urine8, suggesting that quetiapine is heavily metabolized. About 73% of a dose was detected in the urine, and about 20% in the feces.5,19

Half-life

The average terminal half-life of quetiapine is about 6-7 hours.8,19

Clearance

The clearance of quetiapine healthy volunteers in the fasted state during a clinical study was 101.04±39.11 L/h.16 Elderly patients may require lower doses of quetiapine, as clearance in these patients may be reduced by up to 50%.19 Those with liver dysfunction may also require lower doses.14

Adverse Effects
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Toxicity

The oral LD50 if quetiapine in rats is 2000 mg/kg.20

Overdose information

Some signs and symptoms of a quetiapine overdose include sedation, drowsiness, tachycardia, and hypotension. Clinical trials demonstrate that overdoses of up to 30 grams of quetiapine did not result in death. A lethal outcome was reported in a clinical trial after an overdose of 13.6 grams of quetiapine. In the case of an acute overdose, ensure to maintain an airway and provide adequate ventilation and oxygenation. Gastric lavage following intubation (if necessary) along with activated charcoal and a laxative may be considered. The possibility of obtundation, seizure or dystonic reaction of the head and neck following overdose may create a risk of aspiration with induced emesis. Cardiac monitoring should also take place.19

A note on QT-interval prolongation in an overdose

Postmarketing reports reveal increases in the cardiac QT interval in cases of quetiapine overdose, concomitant illness, and in those taking drugs that increase QT interval or affect electrolyte levels.19 Note that disopyramide, procainamide, and quinidine may exert additive QT-prolonging effects when administered in patients who have overdosed with quetiapine, and should be avoided.12,13,19

Pathways
PathwayCategory
Quetiapine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Quetiapine is combined with 1,2-Benzodiazepine.
AbacavirAbacavir may decrease the excretion rate of Quetiapine which could result in a higher serum level.
AbaloparatideThe risk or severity of adverse effects can be increased when Quetiapine is combined with Abaloparatide.
AbametapirThe serum concentration of Quetiapine can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Quetiapine can be increased when combined with Abatacept.
Food Interactions
  • Avoid alcohol.
  • Take with or without food. If taken with food, take with a light meal.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Quetiapine fumarate2S3PL1B6UJ111974-72-2ZTHJULTYCAQOIJ-WXXKFALUSA-N
Product Images
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Act QuetiapineTablet200 mgOralTEVA Canada Limited2008-09-04Not applicableCanada flag
Act QuetiapineTablet150 mgOralTEVA Canada LimitedNot applicableNot applicableCanada flag
Act QuetiapineTablet100 mgOralTEVA Canada Limited2008-09-04Not applicableCanada flag
Act QuetiapineTablet300 mgOralTEVA Canada Limited2008-09-04Not applicableCanada flag
Act QuetiapineTablet25 mgOralTEVA Canada Limited2008-09-04Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Abbott-quetiapineTablet, multilayer, extended release25 mgOralBgp Pharma Ulc2014-06-092015-12-31Canada flag
Abbott-quetiapineTablet, multilayer, extended release100 mgOralBgp Pharma Ulc2014-06-092015-12-31Canada flag
Abbott-quetiapineTablet, multilayer, extended release200 mgOralBgp Pharma Ulc2014-06-132015-12-31Canada flag
Abbott-quetiapineTablet, multilayer, extended release300 mgOralBgp Pharma Ulc2014-06-092015-12-31Canada flag
Accel-quetiapineTablet25 mgOralAccel Pharma Inc2015-03-262017-01-27Canada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
QUETAMEDQuetiapine (25 MG) + Quetiapine (100 MG) + Quetiapine (200 MG)Tablet, coatedOralFairmed Healthcare Gmbh2014-07-08Not applicableItaly flag
QUETAMEDQuetiapine (25 MG) + Quetiapine (100 MG) + Quetiapine (200 MG)Tablet, coatedOralFairmed Healthcare Gmbh2014-07-08Not applicableItaly flag
QUETAMEDQuetiapine (25 MG) + Quetiapine (100 MG) + Quetiapine (200 MG)Tablet, coatedOralFairmed Healthcare Gmbh2014-07-08Not applicableItaly flag
Quetialan 4 Tage Startpackung - FilmtablettenQuetiapine fumarate (25 mg) + Quetiapine fumarate (100 mg)Kit; Tablet, film coatedOralG.L. Pharma Gmb H2007-08-28Not applicableAustria flag
Quetialan 4 Tage Startpackung - FilmtablettenQuetiapine fumarate (25 mg) + Quetiapine fumarate (100 mg)Kit; Tablet, film coatedOralG.L. Pharma Gmb H2007-08-28Not applicableAustria flag

Categories

ATC Codes
N05AH04 — Quetiapine
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as dibenzothiazepines. These are compounds containing a dibenzothiazepine moiety, which consists of two benzene connected by a thiazepine ring.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzothiazepines
Sub Class
Dibenzothiazepines
Direct Parent
Dibenzothiazepines
Alternative Parents
Diarylthioethers / N-alkylpiperazines / Imidolactams / Benzenoids / Trialkylamines / Propargyl-type 1,3-dipolar organic compounds / Dialkyl ethers / Carboxamidines / Azacyclic compounds / Primary alcohols
show 2 more
Substituents
1,4-diazinane / Alcohol / Amidine / Amine / Aromatic heteropolycyclic compound / Aryl thioether / Azacycle / Benzenoid / Carboxylic acid amidine / Dialkyl ether
show 18 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
N-arylpiperazine, N-alkylpiperazine, dibenzothiazepine (CHEBI:8707)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
BGL0JSY5SI
CAS number
111974-69-7
InChI Key
URKOMYMAXPYINW-UHFFFAOYSA-N
InChI
InChI=1S/C21H25N3O2S/c25-14-16-26-15-13-23-9-11-24(12-10-23)21-17-5-1-3-7-19(17)27-20-8-4-2-6-18(20)22-21/h1-8,25H,9-16H2
IUPAC Name
2-[2-(4-{2-thia-9-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(15),3,5,7,9,11,13-heptaen-10-yl}piperazin-1-yl)ethoxy]ethan-1-ol
SMILES
OCCOCCN1CCN(CC1)C1=NC2=CC=CC=C2SC2=CC=CC=C12

References

Synthesis Reference

Kansal VK., Lal K.Suhail, Leonov AD.,(2006).US7687622B2.Retrieved from https://patents.google.com/patent/US7687622B2/en

US4879288
General References
  1. Dev V, Raniwalla J: Quetiapine: a review of its safety in the management of schizophrenia. Drug Saf. 2000 Oct;23(4):295-307. [Article]
  2. Mukaddes NM, Abali O: Quetiapine treatment of children and adolescents with Tourette's disorder. J Child Adolesc Psychopharmacol. 2003 Fall;13(3):295-9. [Article]
  3. Tallerico T, Novak G, Liu IS, Ulpian C, Seeman P: Schizophrenia: elevated mRNA for dopamine D2(Longer) receptors in frontal cortex. Brain Res Mol Brain Res. 2001 Mar 5;87(2):160-5. [Article]
  4. Urichuk L, Prior TI, Dursun S, Baker G: Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab. 2008 Jun;9(5):410-8. [Article]
  5. DeVane CL, Nemeroff CB: Clinical pharmacokinetics of quetiapine: an atypical antipsychotic. Clin Pharmacokinet. 2001;40(7):509-22. doi: 10.2165/00003088-200140070-00003. [Article]
  6. McConville BJ, Arvanitis LA, Thyrum PT, Yeh C, Wilkinson LA, Chaney RO, Foster KD, Sorter MT, Friedman LM, Brown KL, Heubi JE: Pharmacokinetics, tolerability, and clinical effectiveness of quetiapine fumarate: an open-label trial in adolescents with psychotic disorders. J Clin Psychiatry. 2000 Apr;61(4):252-60. doi: 10.4088/jcp.v61n0403. [Article]
  7. Maneeton N, Maneeton B, Woottiluk P, Likhitsathian S, Suttajit S, Boonyanaruthee V, Srisurapanont M: Quetiapine monotherapy in acute treatment of generalized anxiety disorder: a systematic review and meta-analysis of randomized controlled trials. Drug Des Devel Ther. 2016 Jan 12;10:259-76. doi: 10.2147/DDDT.S89485. eCollection 2016. [Article]
  8. Muneer A: Pharmacotherapy of bipolar disorder with quetiapine: a recent literature review and an update. Clin Psychopharmacol Neurosci. 2015 Apr 30;13(1):25-35. doi: 10.9758/cpn.2015.13.1.25. [Article]
  9. Suttajit S, Srisurapanont M, Maneeton N, Maneeton B: Quetiapine for acute bipolar depression: a systematic review and meta-analysis. Drug Des Devel Ther. 2014 Jun 25;8:827-38. doi: 10.2147/DDDT.S63779. eCollection 2014. [Article]
  10. Shotbolt P, Samuel M, David A: Quetiapine in the treatment of psychosis in Parkinson's disease. Ther Adv Neurol Disord. 2010 Nov;3(6):339-50. doi: 10.1177/1756285610389656. [Article]
  11. Bakken GV, Molden E, Knutsen K, Lunder N, Hermann M: Metabolism of the active metabolite of quetiapine, N-desalkylquetiapine in vitro. Drug Metab Dispos. 2012 Sep;40(9):1778-84. doi: 10.1124/dmd.112.045237. Epub 2012 Jun 11. [Article]
  12. Beelen AP, Yeo KT, Lewis LD: Asymptomatic QTc prolongation associated with quetiapine fumarate overdose in a patient being treated with risperidone. Hum Exp Toxicol. 2001 Apr;20(4):215-9. doi: 10.1191/096032701678766778. [Article]
  13. Gajwani P, Pozuelo L, Tesar GE: QT interval prolongation associated with quetiapine (Seroquel) overdose. Psychosomatics. 2000 Jan-Feb;41(1):63-5. doi: 10.1016/S0033-3182(00)71175-3. [Article]
  14. Riedel M, Muller N, Strassnig M, Spellmann I, Severus E, Moller HJ: Quetiapine in the treatment of schizophrenia and related disorders. Neuropsychiatr Dis Treat. 2007 Apr;3(2):219-35. doi: 10.2147/nedt.2007.3.2.219. [Article]
  15. Li KY, Li X, Cheng ZN, Peng WX, Zhang BK, Li HD: Multiple dose pharmacokinetics of quetiapine and some of its metabolites in Chinese suffering from schizophrenia. Acta Pharmacol Sin. 2004 Mar;25(3):390-4. [Article]
  16. Huang X, Zhang S, Ma Y, Yang H, He C, Tian R, Mei H, Liu L, Zhang B: Bioequivalence of two quetiapine extended release tablets in Chinese healthy volunteers under fasting and fed conditions and effects of food on pharmacokinetic profiles. Drug Des Devel Ther. 2018 Dec 31;13:255-264. doi: 10.2147/DDDT.S182965. eCollection 2019. [Article]
  17. Li Q, Su YA, Liu Y, Chen JX, Tan YL, Yang FD, Si TM: Pharmacokinetics and tolerability of extended-release quetiapine fumarate in Han Chinese patients with schizophrenia. Clin Pharmacokinet. 2014 May;53(5):455-65. doi: 10.1007/s40262-013-0127-9. [Article]
  18. Jasdave S. Maan; Abdolreza Saadabadi (2019). Quetiapine. Stat Pearls Publishing.
  19. Quetiapine fumarate fda label [Link]
  20. AstraZeneca SDS: Quetiapine [Link]
Human Metabolome Database
HMDB0005021
KEGG Drug
D08456
KEGG Compound
C07397
PubChem Compound
5002
PubChem Substance
46504800
ChemSpider
4827
BindingDB
50095890
RxNav
51272
ChEBI
8707
ChEMBL
CHEMBL716
ZINC
ZINC000019632628
Therapeutic Targets Database
DAP000001
PharmGKB
PA451201
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Quetiapine
FDA label
Download (273 KB)
MSDS
Download (57.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableDepression, Bipolar1
4CompletedNot AvailableMajor Depressive Disorder (MDD)1
4CompletedNot AvailableSchizophrenia2
4CompletedNot AvailableSchizophrenia / Substance Use Disorders (SUD)1
4CompletedDiagnosticSchizophrenia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Advanced Pharmaceutical Services Inc.
  • AQ Pharmaceuticals Inc.
  • A-S Medication Solutions LLC
  • AstraZeneca Inc.
  • Atlantic Biologicals Corporation
  • Bryant Ranch Prepack
  • Cardinal Health
  • Comprehensive Consultant Services Inc.
  • Coupler Enterprises Inc.
  • Direct Dispensing Inc.
  • Heartland Repack Services LLC
  • Innoviant Pharmacy Inc.
  • Lake Erie Medical and Surgical Supply
  • Murfreesboro Pharmaceutical Nursing Supply
  • Neuman Distributors Inc.
  • Norwich Pharmaceuticals Inc.
  • Nucare Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Rebel Distributors Corp.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Southwood Pharmaceuticals
  • Tya Pharmaceuticals
  • Vangard Labs Inc.
  • Wyeth Pharmaceuticals
Dosage Forms
FormRouteStrength
TabletOral115.120 mg
TabletOral50.000 mg
TabletOral57.566 mg
Tablet, coatedOral
Tablet, coatedOral345.4 mg
Capsule, liquid filledOral25 mg
Capsule, liquid filledOral300 mg
Tablet, film coatedOral25 mg
TabletOral28.750 mg
TabletOral28.783 mg
TabletOral100.000 mg
TabletOral50 mg
TabletOral300.000 mg
Tablet, coatedOral2500000 mg
Tablet, coatedOral20000000 mg
Tablet, coatedOral
Tablet, extended releaseOral
Kit; tablet, film coatedOral
Tablet, film coatedOral150 MG
Tablet, film coatedOral
Tablet, film coatedOral400 MG
Tablet, film coatedOral50 MG
Tablet, extended releaseOral600 MG
Tablet, film coatedOral10000000 mg
Tablet, coatedOral28.78 mg
Tablet, coatedOral230.265 mg
TabletOral100 mg/1
TabletOral150 mg/1
TabletOral200 mg/1
TabletOral25 mg/1
TabletOral300 mg/1
TabletOral400 mg/1
TabletOral50 mg/1
Tablet, film coatedOral150 mg/1
Tablet, film coated, extended releaseOral150 mg/1
Tablet, film coated, extended releaseOral200 mg/1
Tablet, film coated, extended releaseOral300 mg/1
Tablet, film coated, extended releaseOral400 mg/1
Tablet, film coated, extended releaseOral50 mg/1
Tablet, multilayer, extended releaseOral150 mg
TabletOral20000000 mg
Tablet, coatedOral10000000 mg
TabletOral25.000 mg
TabletOral100.00 mg
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral200 mg/1
Tablet, film coatedOral25 mg/1
Tablet, film coatedOral300 mg/1
Tablet, film coatedOral400 mg/1
Tablet, film coatedOral50 mg/1
Tablet, multilayer, extended releaseOral100 mg
Tablet, multilayer, extended releaseOral150 mg / tab
Tablet, multilayer, extended releaseOral200 mg
Tablet, multilayer, extended releaseOral25 mg
Tablet, multilayer, extended releaseOral300 mg
Tablet, film coatedOral
Tablet, film coatedOral100 mg
Tablet, film coatedOral300 mg
TabletOral
TabletOral150.000 mg
Tablet, extended releaseOral150 mg/1
Tablet, extended releaseOral200 mg/1
Tablet, extended releaseOral300 mg/1
Tablet, extended releaseOral400 mg/1
Tablet, extended releaseOral50 mg/1
Tablet, film coated, extended releaseOral200 mg
Tablet, film coated, extended releaseOral300 mg
TabletOral400 mg
Tablet, film coated, extended releaseOral400 mg
Tablet, film coated, extended releaseOral50 mg
Tablet, extended releaseOral200 mg
TabletOral100 mg
TabletOral150 mg
TabletOral200 mg
TabletOral25 mg
TabletOral300 mg
Tablet, film coatedOral200 mg
TabletOral50.0000 mg
Tablet, coatedOral300 mg
Tablet, coatedOral100 mg
Tablet, coatedOral200 mg
Tablet, coatedOral25 mg
Tablet, extended releaseOral150 mg
Tablet, extended releaseOral300 mg
Tablet, extended releaseOral400 mg
Tablet, extended releaseOral50 mg
Prices
Unit descriptionCostUnit
Seroquel 400 mg tablet16.71USD tablet
Seroquel xr 400 mg tablet14.82USD tablet
Seroquel 300 mg tablet14.21USD tablet
Seroquel xr 300 mg tablet12.61USD tablet
Seroquel 200 mg tablet10.84USD tablet
SEROquel XR 200 mg 24 Hour tablet10.0USD tablet
Seroquel xr 200 mg tablet9.62USD tablet
SEROquel XR 150 mg 24 Hour tablet9.09USD tablet
Seroquel xr 150 mg tablet8.74USD tablet
Seroquel 100 mg tablet5.75USD tablet
Seroquel 50 mg tablet5.5USD tablet
SEROquel XR 50 mg 24 Hour tablet5.06USD tablet
Seroquel xr 50 mg tablet4.87USD tablet
Seroquel 300 mg Tablet4.35USD tablet
Seroquel 25 mg tablet3.35USD tablet
Seroquel 200 mg Tablet2.98USD tablet
Apo-Quetiapine 300 mg Tablet2.44USD tablet
Co Quetiapine 300 mg Tablet2.44USD tablet
Jamp-Quetiapine 300 mg Tablet2.44USD tablet
Mylan-Quetiapine 300 mg Tablet2.44USD tablet
Novo-Quetiapine 300 mg Tablet2.44USD tablet
Pms-Quetiapine 300 mg Tablet2.44USD tablet
Ratio-Quetiapine 300 mg Tablet2.44USD tablet
Sandoz Quetiapine 300 mg Tablet2.44USD tablet
Apo-Quetiapine 200 mg Tablet1.67USD tablet
Co Quetiapine 200 mg Tablet1.67USD tablet
Jamp-Quetiapine 200 mg Tablet1.67USD tablet
Mylan-Quetiapine 200 mg Tablet1.67USD tablet
Novo-Quetiapine 200 mg Tablet1.67USD tablet
Pms-Quetiapine 200 mg Tablet1.67USD tablet
Ratio-Quetiapine 200 mg Tablet1.67USD tablet
Sandoz Quetiapine 200 mg Tablet1.67USD tablet
Seroquel 100 mg Tablet1.48USD tablet
Novo-Quetiapine 150 mg Tablet1.42USD tablet
Apo-Quetiapine 100 mg Tablet0.83USD tablet
Co Quetiapine 100 mg Tablet0.83USD tablet
Jamp-Quetiapine 100 mg Tablet0.83USD tablet
Mylan-Quetiapine 100 mg Tablet0.83USD tablet
Novo-Quetiapine 100 mg Tablet0.83USD tablet
Pms-Quetiapine 100 mg Tablet0.83USD tablet
Ratio-Quetiapine 100 mg Tablet0.83USD tablet
Sandoz Quetiapine 100 mg Tablet0.83USD tablet
Seroquel 25 mg Tablet0.56USD tablet
Apo-Quetiapine 25 mg Tablet0.31USD tablet
Co Quetiapine 25 mg Tablet0.31USD tablet
Jamp-Quetiapine 25 mg Tablet0.31USD tablet
Mylan-Quetiapine 25 mg Tablet0.31USD tablet
Novo-Quetiapine 25 mg Tablet0.31USD tablet
Pms-Quetiapine 25 mg Tablet0.31USD tablet
Ratio-Quetiapine 25 mg Tablet0.31USD tablet
Sandoz Quetiapine 25 mg Tablet0.31USD tablet
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Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US4879288No1989-11-072011-09-26US flag
CA2251944No2007-04-102017-05-27Canada flag
US5948437Yes1999-09-072017-11-28US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)174-176https://www.chemicalbook.com/ChemicalProductProperty_US_CB9270451.aspx
boiling point (°C)556.5±60.0 http://www.chemspider.com/Chemical-Structure.4827.html
logP2.81http://www.t3db.ca/toxins/T3D2555
logS-4http://www.t3db.ca/toxins/T3D2555
pKa7.06http://www.t3db.ca/toxins/T3D2555
Predicted Properties
PropertyValueSource
Water Solubility0.0403 mg/mLALOGPS
logP2.93ALOGPS
logP2.81Chemaxon
logS-4ALOGPS
pKa (Strongest Acidic)15.12Chemaxon
pKa (Strongest Basic)7.06Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area48.3 Å2Chemaxon
Rotatable Bond Count5Chemaxon
Refractivity114.09 m3·mol-1Chemaxon
Polarizability42.78 Å3Chemaxon
Number of Rings4Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9155
Blood Brain Barrier+0.9906
Caco-2 permeable-0.6037
P-glycoprotein substrateSubstrate0.8424
P-glycoprotein inhibitor IInhibitor0.9117
P-glycoprotein inhibitor IIInhibitor0.9325
Renal organic cation transporterInhibitor0.5554
CYP450 2C9 substrateNon-substrate0.6438
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateNon-substrate0.6049
CYP450 1A2 substrateInhibitor0.5744
CYP450 2C9 inhibitorNon-inhibitor0.6305
CYP450 2D6 inhibitorInhibitor0.588
CYP450 2C19 inhibitorNon-inhibitor0.7033
CYP450 3A4 inhibitorInhibitor0.7961
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5375
Ames testNon AMES toxic0.7479
CarcinogenicityNon-carcinogens0.869
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6537 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9483
hERG inhibition (predictor II)Inhibitor0.8684
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-0007-9264000000-4758f7f7f4947282ccbb
MS/MS Spectrum - DI-ESI-qTof , NegativeLC-MS/MSsplash10-001i-0039000000-6e58caa07d6f7951f23e
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001i-0089000000-b7b1c7d0bf6bb604c5cb
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0uk9-1390000000-ce855b6e08dee583681b
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-001i-0009000000-846325405daa424f16a3
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-1009000000-1913bb309b971f5a3c42
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0159-0009000000-9c7f2db128493c5293c6
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-9006000000-b0cf94a15b1680baabc5
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-03k9-0296000000-25ef2c5397c5da59d103
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-3192000000-a18b5d971739001b8092
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-202.7059893
predicted
DarkChem Lite v0.1.0
[M-H]-182.08702
predicted
DeepCCS 1.0 (2019)
[M+H]+202.2814893
predicted
DarkChem Lite v0.1.0
[M+H]+184.44502
predicted
DeepCCS 1.0 (2019)
[M+Na]+202.9761893
predicted
DarkChem Lite v0.1.0
[M+Na]+190.53816
predicted
DeepCCS 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
  1. Goldstein JM: Quetiapine fumarate (Seroquel): a new atypical antipsychotic. Drugs Today (Barc). 1999 Mar;35(3):193-210. [Article]
  2. McIntyre RS, Soczynska JK, Woldeyohannes HO, Alsuwaidan M, Konarski JZ: A preclinical and clinical rationale for quetiapine in mood syndromes. Expert Opin Pharmacother. 2007 Jun;8(9):1211-9. [Article]
  3. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  4. 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]
  5. 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]
  6. Quetiapine FDA label [Link]
Details
2. Dopamine D2 receptor
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
  1. Kapur S, Zipursky R, Jones C, Shammi CS, Remington G, Seeman P: A positron emission tomography study of quetiapine in schizophrenia: a preliminary finding of an antipsychotic effect with only transiently high dopamine D2 receptor occupancy. Arch Gen Psychiatry. 2000 Jun;57(6):553-9. [Article]
  2. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  3. Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [Article]
  4. 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]
  5. Quetiapine FDA label [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
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...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. Ichikawa J, Li Z, Dai J, Meltzer HY: Atypical antipsychotic drugs, quetiapine, iloperidone, and melperone, preferentially increase dopamine and acetylcholine release in rat medial prefrontal cortex: role of 5-HT1A receptor agonism. Brain Res. 2002 Nov 29;956(2):349-57. [Article]
  2. McIntyre RS, Soczynska JK, Woldeyohannes HO, Alsuwaidan M, Konarski JZ: A preclinical and clinical rationale for quetiapine in mood syndromes. Expert Opin Pharmacother. 2007 Jun;8(9):1211-9. [Article]
  3. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  4. 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]
  5. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 Da
References
  1. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  2. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that trig...
Gene Name
HTR1E
Uniprot ID
P28566
Uniprot Name
5-hydroxytryptamine receptor 1E
Molecular Weight
41681.57 Da
References
  1. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
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
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  2. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
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
  1. 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]
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
  1. 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]
  2. Bymaster FP, Falcone JF, Bauzon D, Kennedy JS, Schenck K, DeLapp NW, Cohen ML: Potent antagonism of 5-HT(3) and 5-HT(6) receptors by olanzapine. Eur J Pharmacol. 2001 Nov 2;430(2-3):341-9. doi: 10.1016/s0014-2999(01)01399-1. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
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
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
Molecular Weight
53554.43 Da
References
  1. 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]
Details
11. Dopamine D1 receptor
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
  1. 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]
  2. Tauscher J, Hussain T, Agid O, Verhoeff NP, Wilson AA, Houle S, Remington G, Zipursky RB, Kapur S: Equivalent occupancy of dopamine D1 and D2 receptors with clozapine: differentiation from other atypical antipsychotics. Am J Psychiatry. 2004 Sep;161(9):1620-5. doi: 10.1176/appi.ajp.161.9.1620. [Article]
  3. Moallem N, Ray LA: Quetiapine improves response inhibition in alcohol dependent patients: a placebo-controlled pilot study. Pharmacol Biochem Behav. 2012 Jan;100(3):490-3. doi: 10.1016/j.pbb.2011.10.012. Epub 2011 Oct 20. [Article]
Details
12. Dopamine D5 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
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
  1. 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]
  2. Jain M: Quetiapine associated Central Serous Chorioretinopathy: Implicit role of serotonin and dopamine pathways. Indian J Ophthalmol. 2019 Feb;67(2):292-294. doi: 10.4103/ijo.IJO_929_18. [Article]
Details
13. Dopamine D3 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
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
  1. 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]
  2. Vernaleken I, Janouschek H, Raptis M, Hellmann S, Veselinovic T, Brocheler A, Boy C, Cumming P, Hiemke C, Rosch F, Schafer WM, Grunder G: Dopamine D2/3 receptor occupancy by quetiapine in striatal and extrastriatal areas. Int J Neuropsychopharmacol. 2010 Aug;13(7):951-60. doi: 10.1017/S1461145710000374. Epub 2010 Apr 15. [Article]
  3. Bressan RA, Erlandsson K, Jones HM, Mulligan RS, Ell PJ, Pilowsky LS: Optimizing limbic selective D2/D3 receptor occupancy by risperidone: a [123I]-epidepride SPET study. J Clin Psychopharmacol. 2003 Feb;23(1):5-14. doi: 10.1097/00004714-200302000-00002. [Article]
Details
14. Dopamine D4 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
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
  1. 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]
  2. Li P, Snyder GL, Vanover KE: Dopamine Targeting Drugs for the Treatment of Schizophrenia: Past, Present and Future. Curr Top Med Chem. 2016;16(29):3385-3403. doi: 10.2174/1568026616666160608084834. [Article]
Details
15. Histamine H1 receptor
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
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  2. 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]
  3. Quetiapine FDA label [Link]
Kind
Protein group
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...

Components:
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  2. 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]
  3. Shayegan DK, Stahl SM: Atypical antipsychotics: matching receptor profile to individual patient's clinical profile. CNS Spectr. 2004 Oct;9(10 Suppl 11):6-14. [Article]
  4. Quetiapine FDA label [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  2. 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]
  3. Jensen NH, Rodriguiz RM, Caron MG, Wetsel WC, Rothman RB, Roth BL: N-desalkylquetiapine, a potent norepinephrine reuptake inhibitor and partial 5-HT1A agonist, as a putative mediator of quetiapine's antidepressant activity. Neuropsychopharmacology. 2008 Sep;33(10):2303-12. doi: 10.1038/sj.npp.1301646. Epub 2007 Dec 5. [Article]
  4. Riedel M, Muller N, Strassnig M, Spellmann I, Severus E, Moller HJ: Quetiapine in the treatment of schizophrenia and related disorders. Neuropsychiatr Dis Treat. 2007 Apr;3(2):219-35. doi: 10.2147/nedt.2007.3.2.219. [Article]
  5. Jasdave S. Maan; Abdolreza Saadabadi (2019). Quetiapine. Stat Pearls Publishing.
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Epinephrine binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  2. 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]
  3. Suttajit S, Srisurapanont M, Maneeton N, Maneeton B: Quetiapine for acute bipolar depression: a systematic review and meta-analysis. Drug Des Devel Ther. 2014 Jun 25;8:827-38. doi: 10.2147/DDDT.S63779. eCollection 2014. [Article]
  4. Jensen NH, Rodriguiz RM, Caron MG, Wetsel WC, Rothman RB, Roth BL: N-desalkylquetiapine, a potent norepinephrine reuptake inhibitor and partial 5-HT1A agonist, as a putative mediator of quetiapine's antidepressant activity. Neuropsychopharmacology. 2008 Sep;33(10):2303-12. doi: 10.1038/sj.npp.1301646. Epub 2007 Dec 5. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein homodimerization activity
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name
ADRA2C
Uniprot ID
P18825
Uniprot Name
Alpha-2C adrenergic receptor
Molecular Weight
49521.585 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  2. 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]
  3. Uys MM, Shahid M, Harvey BH: Therapeutic Potential of Selectively Targeting the alpha2C-Adrenoceptor in Cognition, Depression, and Schizophrenia-New Developments and Future Perspective. Front Psychiatry. 2017 Aug 14;8:144. doi: 10.3389/fpsyt.2017.00144. eCollection 2017. [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
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  2. 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]
  3. Quetiapine FDA label [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
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
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  2. 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]
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
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  2. 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]
  3. Vehof J, Risselada AJ, Al Hadithy AF, Burger H, Snieder H, Wilffert B, Arends J, Wunderink L, Knegtering H, Wiersma D, Cohen D, Mulder H, Bruggeman R: Association of genetic variants of the histamine H1 and muscarinic M3 receptors with BMI and HbA1c values in patients on antipsychotic medication. Psychopharmacology (Berl). 2011 Jul;216(2):257-65. doi: 10.1007/s00213-011-2211-x. Epub 2011 Feb 19. [Article]
  4. Muller C, Reuter H, Dohmen C: Intoxication after extreme oral overdose of quetiapine to attempt suicide: pharmacological concerns of side effects. Case Rep Med. 2009;2009:371698. doi: 10.1155/2009/371698. Epub 2010 Jan 3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
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
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  2. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
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
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
  2. 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]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
  1. Lin SN, Chang Y, Moody DE, Foltz RL: A liquid chromatographic-electrospray-tandem mass spectrometric method for quantitation of quetiapine in human plasma and liver microsomes: application to study in vitro metabolism. J Anal Toxicol. 2004 Sep;28(6):443-8. doi: 10.1093/jat/28.6.443. [Article]
  2. Bavle AD, Vishwaraj S: Warfarin-quetiapine interaction causing hemorrhage. Indian J Psychiatry. 2016 Jan-Mar;58(1):102-3. doi: 10.4103/0019-5545.174401. [Article]
  3. Cabaleiro T, Lopez-Rodriguez R, Roman M, Ochoa D, Novalbos J, Borobia A, Carcas A, Abad-Santos F: Pharmacogenetics of quetiapine in healthy volunteers: association with pharmacokinetics, pharmacodynamics, and adverse effects. Int Clin Psychopharmacol. 2015 Mar;30(2):82-8. doi: 10.1097/YIC.0000000000000047. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
  1. Lin SN, Chang Y, Moody DE, Foltz RL: A liquid chromatographic-electrospray-tandem mass spectrometric method for quantitation of quetiapine in human plasma and liver microsomes: application to study in vitro metabolism. J Anal Toxicol. 2004 Sep;28(6):443-8. doi: 10.1093/jat/28.6.443. [Article]
  2. Hasselstrom J, Linnet K: In vitro studies on quetiapine metabolism using the substrate depletion approach with focus on drug-drug interactions. Drug Metabol Drug Interact. 2006;21(3-4):187-211. [Article]
  3. Bakken GV, Molden E, Knutsen K, Lunder N, Hermann M: Metabolism of the active metabolite of quetiapine, N-desalkylquetiapine in vitro. Drug Metab Dispos. 2012 Sep;40(9):1778-84. doi: 10.1124/dmd.112.045237. Epub 2012 Jun 11. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Oxygen binding
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
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Lin SN, Chang Y, Moody DE, Foltz RL: A liquid chromatographic-electrospray-tandem mass spectrometric method for quantitation of quetiapine in human plasma and liver microsomes: application to study in vitro metabolism. J Anal Toxicol. 2004 Sep;28(6):443-8. doi: 10.1093/jat/28.6.443. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
  1. Urichuk L, Prior TI, Dursun S, Baker G: Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab. 2008 Jun;9(5):410-8. [Article]
  2. DeVane CL, Nemeroff CB: Clinical pharmacokinetics of quetiapine: an atypical antipsychotic. Clin Pharmacokinet. 2001;40(7):509-22. doi: 10.2165/00003088-200140070-00003. [Article]
  3. Bakken GV, Rudberg I, Christensen H, Molden E, Refsum H, Hermann M: Metabolism of quetiapine by CYP3A4 and CYP3A5 in presence or absence of cytochrome B5. Drug Metab Dispos. 2009 Feb;37(2):254-8. doi: 10.1124/dmd.108.023291. Epub 2008 Nov 20. [Article]
  4. Bakken GV, Molden E, Knutsen K, Lunder N, Hermann M: Metabolism of the active metabolite of quetiapine, N-desalkylquetiapine in vitro. Drug Metab Dispos. 2012 Sep;40(9):1778-84. doi: 10.1124/dmd.112.045237. Epub 2012 Jun 11. [Article]
  5. Dev V, Raniwalla J: Quetiapine: a review of its safety in the management of schizophrenia. Drug Saf. 2000 Oct;23(4):295-307. [Article]
  6. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
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
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Kim KA, Joo HJ, Lee HM, Park JY: Influence of ABCB1 and CYP3A5 genetic polymorphisms on the pharmacokinetics of quetiapine in healthy volunteers. Pharmacogenet Genomics. 2014 Jan;24(1):35-42. doi: 10.1097/FPC.0000000000000020. [Article]
  2. Bakken GV, Rudberg I, Christensen H, Molden E, Refsum H, Hermann M: Metabolism of quetiapine by CYP3A4 and CYP3A5 in presence or absence of cytochrome B5. Drug Metab Dispos. 2009 Feb;37(2):254-8. doi: 10.1124/dmd.108.023291. Epub 2008 Nov 20. [Article]
  3. Flockhart Table of Drug Interactions [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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
  1. 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]
  2. Kim KA, Joo HJ, Lee HM, Park JY: Influence of ABCB1 and CYP3A5 genetic polymorphisms on the pharmacokinetics of quetiapine in healthy volunteers. Pharmacogenet Genomics. 2014 Jan;24(1):35-42. doi: 10.1097/FPC.0000000000000020. [Article]

Drug created at June 13, 2005 13:24 / Updated at March 18, 2024 16:48