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Quetiapine: Difference between revisions

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==Pharmocology==
==Pharmocology==
Quetiapine has the following pharmacological actions:<ref>http://www1.astrazeneca-us.com/pi/Seroquel.pdf</ref><ref>Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compounds | http://www.sciencedirect.com/science/article/pii/S0024320500009115</ref><ref>Neuropsychopharmocology, a fifth generation of progress | http://books.google.co.uk/books?id=BKwkonZwZD0C&pg=PA778&hl=en#v=onepage&q&f=false</ref><ref>http://www.drugs.com/pro/seroquel.html</ref>
This means Quetiapine is a [[dopamine]], [[serotonin]], and [[adrenergic]] [[antagonist]], and a potent [[antihistamine]] with clinically negligible [[anticholinergic]] properties.<ref>http://www1.astrazeneca-us.com/pi/Seroquel.pdf</ref><ref>Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compounds | http://www.sciencedirect.com/science/article/pii/S0024320500009115</ref><ref>Neuropsychopharmocology, a fifth generation of progress | http://books.google.co.uk/books?id=BKwkonZwZD0C&pg=PA778&hl=en#v=onepage&q&f=false</ref><ref>http://www.drugs.com/pro/seroquel.html</ref> Quetiapine binds strongly to serotonin receptors; the drug acts as partial [[agonist]] at 5-HT1A receptors.<ref>Mechanism of Action of Quetiapine | http://psychopharmacologyinstitute.com/antipsychotics/quetiapine/mechanism-of-action/</ref> In terms of its [[antipsychotic]] effects, the precise mechanism of action is unknown, but according to the dopamine theory of schizophrenia, antipsychotic effects might be related to the drug’s ability to reduce dopaminergic neurotransmission in the mesolimbic pathway.
 
*D1 (IC50 = 1268nM), D2 (IC50 = 329nM), D3, and D4 receptor [[antagonist]]
*5-HT1A (IC50 = 717nM) partial agonist, 5-HT2A (IC50 = 148nM), 5-HT2C, and 5-HT7 receptor [[antagonist]]
*α1-adrenergic (IC50 = 94nM) and α2-adrenergic receptor (IC50 = 271nM) [[antagonist]]
*H1 receptor (IC50 = 30nM) [[antagonist]]
*mACh receptor (IC50 = >5000nM) [[antagonist]]
 
This means Quetiapine is a [[dopamine]], [[serotonin]], and [[adrenergic]] [[antagonist]], and a potent [[antihistamine]] with clinically negligible [[anticholinergic]] properties. Quetiapine binds strongly to serotonin receptors; the drug acts as partial [[agonist]] at 5-HT1A receptors.<ref>Mechanism of Action of Quetiapine | http://psychopharmacologyinstitute.com/antipsychotics/quetiapine/mechanism-of-action/</ref> In terms of its [[antipsychotic]] effects, the precise mechanism of action is unknown, but according to the dopamine theory of schizophrenia, antipsychotic effects might be related to the drug’s ability to reduce dopaminergic neurotransmission in the mesolimbic pathway.


==Subjective effects==
==Subjective effects==

Revision as of 14:46, 30 April 2014

Quetiapine
noframe
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The skeletal formula of Quetiapine.
Dosage (oral)
Threshold 10 - 20 mg
Light 20 - 50 mg
Common 50 - 150 mg
Strong 150 - 400 mg
Heavy 400 mg +
Duration (oral)
Onset 5 - 10 minutes
Duration 1.5 - 5 hours
After effects up to 24 hours

Quetiapine (/kwɨˈtaɪ.əpiːn/ kwi-ty-ə-peen) (branded as Seroquel, Xeroquel, Ketipinor) is a short-acting atypical antipsychotic approved for the treatment of schizophrenia, bipolar disorder, and along with an antidepressant to treat major depressive disorder.

Annual sales are approximately $5.7 billion worldwide, with $2.9 billion in the United States.[1] The U.S. patent,[2] which was set to expire in 2011, received a pediatric exclusivity extension which pushed its expiration to March 26, 2012.[3][4] The patent has already expired in Canada. Quetiapine was developed by AstraZeneca from 1992-1996 as an improvement from first generation antipsychotics. It was first approved by the FDA in 1997. There are now several generic versions of quetiapine, such as Quepin, Syquel and Ketipinor.[5]

Chemistry

Pharmocology

This means Quetiapine is a dopamine, serotonin, and adrenergic antagonist, and a potent antihistamine with clinically negligible anticholinergic properties.[6][7][8][9] Quetiapine binds strongly to serotonin receptors; the drug acts as partial agonist at 5-HT1A receptors.[10] In terms of its antipsychotic effects, the precise mechanism of action is unknown, but according to the dopamine theory of schizophrenia, antipsychotic effects might be related to the drug’s ability to reduce dopaminergic neurotransmission in the mesolimbic pathway.

Subjective effects

Physical effects

Cognitive effects

Toxicity and harm potential

Tolerance and addiction potential

Interactions

References