Quetiapine drug data and news

Quetiapine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Quetiapine
Brand Names/Synonyms CHEMBANK1802; Quetiapin Hemifumarate; Quetiapine; Quetiapine Fumarate; Quetiapine Hemifumarate; Seroquel; ZD5077
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.
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Description Not Available
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 (5HT2), and dopamine type 2 (D2) receptors. Quetiapine is an antagonist at serotonin 5-HT1A and 5HT2, 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.
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 (5HT2) receptor antagonism. Although quetiapine is known to bind other receptors with similar affinity, only the dopamine D2 and serotonin 5HT2 receptor binding is responsible for quetiapine's therapeutic activity in schizophrenia.
Quetiapine News
(When available)

TODDLERS USED AS DRUG GUINEA PIGS?  16 May 2006
...that a Massachusetts hospital is currently recruiting pre-schoolers to test the safety and effectiveness of a powerful antipsychotic drug called Quetiapine. ... - Free Market News Network,

Understanding and Managing Psychosis in Late Life  May 15, 2006
For older patients with schizophrenia or psychosis of AD, risperidone (Risperdal), olanzapine (Zyprexa) and quetiapine (Seroquel) are currently the three most ... - Psychiatric Times,

Innovations: Geriatric Psychiatry: Diagnosis and Treatment of ...  May 10, 2006
Olanzapine has also been shown to effective and well tolerated at dosages of 5 to 10 mg per day (8). Data for quetiapine, ziprasidone, and aripiprazole are ... - Psychiatric Services (subscription)

Recent Developments in Antipsychotic Use in Adults  Apr 20, 2006
Having to titrate dose over time rather than starting at an efficacious dose is also an obstacle, and here clozapine, quetiapine (Seroquel), ziprasidone and ... - Psychiatric Times,

Psychiatric Decision Making in the Adoption of a New Antipsychotic ...  May 4, 2006
Woodward ND, Purdon SE, Meltzer HY, et al: A meta-analysis of neuropsychological change to clozapine, olanzapine, quetiapine, and risperidone in schizophrenia. ... - Psychiatric Services (subscription)

Behavioral and Pharmacologic Treatment of Aggression in Children ...  May 10, 2006
Clozapine (Clozaril), quetiapine (Seroquel), olanzapine (Zyprexa) and ziprasidone (Geodon) have been evaluated in small or uncontrolled studies and case ... - Psychiatric Times,

Parkinson Disease Guidelines Aid Diagnosis, Management  May 9, 2006
...recommended for managing dementia. Clozapine and quetiapine are recommended for psychosis symptoms. Another important consideration ... - Journal of American Medical Association (subscription),

Antipsychotic Drug Use Growing Fastest Among Children  May 2, 2006
...the latest generation of antipsychotics - known as atypical antipsychotics, including risperidone, olanzapine, clozapine, ziprasidone and quetiapine - at a ... - YubaNet,

Cortical Serotonin 5-HT 2A Receptor Binding and Social ...  Apr 28, 2006
Jones HM, Travis MJ, Mulligan R, Bressan RA, Visvikis D, Gacinovic S, Ell PJ, Kerwin RW, Pilowsky LS: In vivo 5-HT2A receptor blockade by quetiapine: an R91150 ... - Am J Psychiatry (subscription)

Schizophrenia gene function offers hope for drug R&D  Apr 23, 2006
The newer atypical antipsychotic medications (such as clozapine, risperidone, olanzapine, quetiapine, ziprasidone and aripiprazole) are usually preferred over ... - DrugResearcher.com,

Seroquel big, and could get bigger  Apr 23, 2006
...year. Seroquel, whose chemical name is quetiapine fumarate, belongs to a class of drugs known as atypical antipsychotics. Seroquel ... - The News Journal,

Dosage Forms TABLET
Drug_Category Antipsychotics; ATC:N05AH04
Absorption Rapidly and well absorbed.
Interactions -->Interactions for Quetiapine:

The risks of using SEROQUEL in combination with other drugs have not been extensively evaluated in systematic studies. Given the primary CNS effects of SEROQUEL, caution should be used when it is taken in combination with other centrally acting drugs. SEROQUEL potentiated the cognitive and motor effects of alcohol in a clinical trial in subjects with selected psychotic disorders, and alcoholic beverages should be avoided while taking SEROQUEL.

Because of its potential for inducing hypotension, SEROQUEL may enhance the effects of certain antihypertensive agents. SEROQUEL may antagonize the effects of levodopa and dopamine agonists.

The Effect of Other Drugs on Quetiapine

Phenytoin: Coadministration of quetiapine (250 mg tid) and phenytoin (100 mg tid) increased the mean oral clearance of quetiapine by 5-fold. Increased doses of SEROQUEL may be required to maintain control of symptoms of schizophrenia in patients receiving quetiapine and phenytoin, or other hepatic enzyme inducers (e.g., carbamazepine, barbiturates, rifampin, glucocorticoids). Caution should be taken if phenytoin is withdrawn and replaced with a non-inducer (e.g., valproate).

Divalproex: Coadministration of quetiapine (150 mg bid) and divalproex (500 mg bid) increased the mean maximum plasma concentration of quetiapine at steady state by 17% without affecting the extent of absorption or mean oral clearance.

Thioridazine: Thioridazine (200 mg bid) increased the oral clearance of quetiapine (300 mg bid) by 65%.

Cimetidine: Administration of multiple daily doses of cimetidine (400 mg tid for 4 days) resulted in a 20% decrease in the mean oral clearance of quetiapine (150 mg tid). Dosage adjustment for quetiapine is not required when it is given with cimetidine.

P450 3A Inhibitors: Coadministration of ketoconazole (200 mg once daily for 4 days), a potent inhibitor of cytochrome P4503A, reduced oral clearance of quetiapine by 84%, resulting in a 335% increase in maximum plasma concentration of quetiapine. Caution is indicated when SEROQUEL is administered with ketoconazole and other inhibitors of cytochrome P450 3A (e.g., itraconazole, fluconazole, and erythromycin).

Fluoxetine, Imipramine, Haloperidol, and Risperidone: Coadministration of fluoxetine (60 mg once daily); imipramine (75 mg bid), haloperidol (7.5 mg bid), or risperidone (3 mg bid) with quetiapine (300 mg bid) did not alter the steady-state pharmacokinetics of quetiapine.

Effect of Quetiapine on Other Drugs

Lorazepam: The mean oral clearance of lorazepam (2 mg, single dose) was reduced by 20% in the presence of quetiapine administered as 250 mg tid dosing.

Divalproex: The mean maximum concentration and extent of absorption of total and free valproic acid at steady state were decreased by 10 to 12% when divalproex (500 mg bid) was administered with quetiapine (150 mg bid). The mean oral clearance of total valproic acid (administered as divalproex 500 mg bid) was increased by 11% in the presence of quetiapine (150 mg bid). The changes were not significant

Lithium: Concomitant administration of quetiapine (250 mg tid) with lithium had no effect on any of the steady-state pharmacokinetic parameters of lithium.

Antipyrine: Administration of multiple daily doses up to 750 mg/day (on a tid schedule) of quetiapine to subjects with selected psychotic disorders had no clinically relevant effect on the clearance of antipyrine or urinary recovery of antipyrine metabolites. These results indicate that quetiapine does not significantly induce hepatic enzymes responsible for cytochrome P450 mediated metabolism of antipyrine.

Toxicity Symptoms of overdose include drowsiness and sedation, tachycardia, and hypotension.
Organisms Affected Humans and other mammals
Chemical IUPAC Name Not Available
Chemical Formula C21H25N3O2S
Molecular Weight 383.508 g/mol
Smiles String C1CN(CCN1CCOCCO)C2=NC3=CC=CC=C3SC4=CC=CC=C42
Melting Point Not Available
Water Solubility Moderate
State Solid (white to off-white crystalline powder)
LogP/Hphobicity 2.296
Isoelectric Point Not Available
Biotransformation Hepatic. The major metabolic pathways are sulfoxidation, mediated by cytochrome P450 3A4 (CYP3A4), and oxidation. The major metabolites of quetiapine are inactive.
Half Life 6 hours
Protein Binding [%] 83%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Quetiapine.html
http://www.rxlist.com/cgi/generic2/quetiap.htm
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ser1402.shtml
Drug Type Approved Drug
Accession No APRD00675
CAS Registry Number 111974-69-7
KEGG Compound ID C07397
PubChem ID SID:66188
PharmGKB ID PA451201
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2240862

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