Overview
| Trade Names: | Quetiapin hemifumarate; Quetiapine fumarate; Quetiapine hemifumarate; Seroquel |
|---|---|
| PharmGKB Accession Id: | PA451201 |
Description
Quetiapine is indicated for the treatment of schizophrenia as well as for the treatment of acute manic episodes associated with bipolar I disorder. The antipsychotic effect of quetiapine is thought by some to be mediated through antagonist activity at dopamine and serotonin receptors. Specifically the D1 and D2 dopamine, the alpha 1 adrenoreceptor and alpha 2 adrenoreceptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes are antagonized. Quetiapine also has an antagonistic effect on the histamine H1 receptor. (source: Drug Bank)
Indication
For the treatment of schizophrenia and acute manic episodes associated with bipolar I disorder, as either monotherapy or adjunct therapy to lithium or divalproex. (source: Drug Bank)
ATC Therapeutic Category
- N05AH:Diazepines, oxazepines and thiazepines
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
The mechanism of action of quetiapine, as with other drugs used to treat schizophrenia, is unknown. However, it is thought that the drug's therapeutic activity in schizophrenia is mediated through a combination of dopamine type 2 (D2) and serotonin type 2 (5HT<sub>2</sub>) receptor antagonism. Although quetiapine is known to bind other receptors with similar affinity, only the dopamine D2 and serotonin 5HT<sub>2</sub> receptor binding is responsible for quetiapine's therapeutic activity in schizophrenia. (source: Drug Bank)
Pharmacology
Quetiapine is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Quetiapine is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT<sub>2</sub>), and dopamine type 2 (D2) receptors. Quetiapine is an antagonist at serotonin 5-HT<sub>1A</sub> and 5HT<sub>2</sub>, dopamine D1 and D2, histamine H1, and adrenergic alpha 1 and alpha 2 receptors. Quetiapine has no significant affinity for cholinergic muscarinic or benzodiazepine receptors. Drowsiness and orthostatic hypotension associated with use of quetiapine may be explained by its antagonism of histamine H1 and adrenergic alpha 1 receptors, respectively. Quetiapine's antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug. (source: Drug Bank)
Food Interactions
Avoid alcohol.
Take without regard to meals.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic. The major metabolic pathways are sulfoxidation, mediated by cytochrome P450 3A4 (CYP3A4), and oxidation. The major metabolites of quetiapine are inactive. (source: Drug Bank)
Protein Binding
83% (source: Drug Bank)
Absorption
Rapidly and well absorbed. (source: Drug Bank)
Toxicity
Symptoms of overdose include drowsiness and sedation, tachycardia, and hypotension. (source: Drug Bank)
Isomeric SMILES Code:
c1ccc2c(c1)C(=Nc3ccccc3S2)N4CCN(CC4)CCOCCO (source: Drug Bank)
Curated Annotations (
)
-
rs951439
at chr1:161300315
in
RGS4
This variant is associated with differential antipsychotic treatment response in individuals of african descent. Patients with african descent and rs951439 genotype CC responded better to perphenazine treatment compared with ziprasidone or quetiapine treatments. Patient with European descent and rs951439 TT genotype responded better to risperidone than those with CC genotype. However, no association was find between this variant and incidence or age at onset in schizophrenia as well as treatment responses in Finnish patients.- Related Drugs:
- perphenazine, quetiapine, risperidone, ziprasidone
- Related Diseases:
- Schizophrenia
- Evidence:
-
PMID:16604300
PMID:17588543
PMID:18204343
-
rs2661319
at chr1:161306401
in
RGS4
This variant is associated with differential antipsychotic treatment response in individuals of african descent and chinese descent.- Related Drugs:
- perphenazine, quetiapine, risperidone, ziprasidone
- Related Diseases:
- Schizophrenia
- Evidence:
-
PMID:17588543
PMID:18204343
-
rs2842030
at chr1:161307119
in
RGS4
This variant is associated with differential antipsychotic treatment response in individuals of african descent. Patient with rs2842030 TT genotype responded better to perphenazine treatment than by quatiapine, risperidone or ziprasidone. Patient with European descent and rs2842030 GG genotype responded better to risperidone than those with TT genotype.No association was found between this variant and increased susceptibility to the etiology of schizophrenia in Han Chinese.- Related Drugs:
- perphenazine, quetiapine, risperidone, ziprasidone
- Related Diseases:
- Schizophrenia
- Evidence:
-
PMID:16904822
PMID:17588543
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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CYP2D6 |
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Publications |
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CYP3A |
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Publications |
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CYP3A4 |
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Publications |
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CYP3A5 |
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Publications |
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DRD4 |
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Publications |
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KCNH2 |
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Publications |
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PRKCB |
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Publications |
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RGS4 |
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Variants |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
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tamoxifen |
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Publications |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| clarithromycin |
|
This macrolide increases the effect/toxicity of quetiapine (source: Drug Bank) |
| donepezil |
|
Possible antagonism of action (source: Drug Bank) |
| erythromycin |
|
This macrolide increases the effect/toxicity of quetiapine (source: Drug Bank) |
| ethotoin |
|
Phenytoin decreases the effect of quetiapine (source: Drug Bank) |
| fosphenytoin |
|
Phenytoin decreases the effect of quetiapine (source: Drug Bank) |
| galantamine |
|
Possible antagonism of action (source: Drug Bank) |
| ketoconazole |
|
Ketoconazole increases effect/toxicity of quetiapine (source: Drug Bank) |
| mephenytoin |
|
Phenytoin decreases the effect of quetiapine (source: Drug Bank) |
| phenytoin |
|
Phenytoin decreases the effect of quetiapine (source: Drug Bank) |
| quinupristin |
|
This combination presents an increased risk of toxicity (source: Drug Bank) |
| rivastigmine |
|
Possible antagonism of action (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
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Body Weight Changes |
|
Publications |
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Hyperlipidemias |
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Publications |
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Parkinson Disease |
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Publications |
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Psychotic Disorders |
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Publications |
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Schizophrenia |
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Publications, Variants |
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Weight gain |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
LinkOuts
Common Searches
Search PubMed
Search Medline Plus
Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.