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Quetiapine: Difference between revisions

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Annual sales are approximately $5.7 billion worldwide, with $2.9 billion in the United States.<ref>http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=SEROQUEL</ref> The U.S. patent,<ref>http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPTO%2Fsearch-bool.html&r=1&f=G&l=50&co1=AND&d=PTXT&s1=4,879,288.PN.&OS=PN/4,879,288&RS=PN/4,879,288</ref> which was set to expire in 2011, received a pediatric exclusivity extension which pushed its expiration to March 26, 2012.<ref>http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPTO%2Fsearch-bool.html&r=1&f=G&l=50&co1=AND&d=PTXT&s1=4,879,288.PN.&OS=PN/4,879,288&RS=PN/4,879,288</ref><ref>Blockbuster Drugs That Will Go Generic Soon | http://money.usnews.com/money/blogs/the-best-life/2011/04/29/blockbuster-drugs-that-will-go-generic-soon</ref> 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.<ref>http://www.theodora.com/drugs/quepin_tablets_specifar.html</ref>
Annual sales are approximately $5.7 billion worldwide, with $2.9 billion in the United States.<ref>http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=SEROQUEL</ref> The U.S. patent,<ref>http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPTO%2Fsearch-bool.html&r=1&f=G&l=50&co1=AND&d=PTXT&s1=4,879,288.PN.&OS=PN/4,879,288&RS=PN/4,879,288</ref> which was set to expire in 2011, received a pediatric exclusivity extension which pushed its expiration to March 26, 2012.<ref>http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPTO%2Fsearch-bool.html&r=1&f=G&l=50&co1=AND&d=PTXT&s1=4,879,288.PN.&OS=PN/4,879,288&RS=PN/4,879,288</ref><ref>Blockbuster Drugs That Will Go Generic Soon | http://money.usnews.com/money/blogs/the-best-life/2011/04/29/blockbuster-drugs-that-will-go-generic-soon</ref> 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.<ref>http://www.theodora.com/drugs/quepin_tablets_specifar.html</ref>


Recreational usage of this substance is rare but well documented. It seems to be driven by its sedative and anxiolytic effects (to help with sleep or to 'calm down') rather than by its antipsychotic properties."<ref>Intranasal quetiapine abuse | http://ajp.psychiatryonline.org/article.aspx?articleid=177055</ref> Reports of quetiapine abuse have emerged in medical literature. In addition to oral administration, the drug is sometimes taken intranasally by insufflating pulverized tablets. A 2004 letter to the editor of the American Journal of Psychiatry provided an anecdotal estimate that up to 30% of inmates who were seen for psychiatric services in the Los Angeles County Jail were faking psychotic symptoms in an attempt to obtain quetiapine.<ref>Intranasal quetiapine abuse | http://ajp.psychiatryonline.org/article.aspx?articleid=177055</ref> This drug seems to be more commonly abused in prisons than on the street due to its capacity to be regularly prescribed as a sedative and the unavailability in prison of more commonly abused substances.  
Recreational usage of this substance is uncommon but well documented. It seems to be driven by its sedative and anxiolytic effects (to help with sleep or to 'calm down') rather than by its antipsychotic properties."<ref>Intranasal quetiapine abuse | http://ajp.psychiatryonline.org/article.aspx?articleid=177055</ref> Reports of quetiapine abuse have emerged in medical literature. In addition to oral administration, the drug is sometimes taken intranasally by insufflating pulverized tablets. A 2004 letter to the editor of the American Journal of Psychiatry provided an anecdotal estimate that up to 30% of inmates who were seen for psychiatric services in the Los Angeles County Jail were faking psychotic symptoms in an attempt to obtain quetiapine.<ref>Intranasal quetiapine abuse | http://ajp.psychiatryonline.org/article.aspx?articleid=177055</ref> This drug seems to be more commonly abused in prisons than on the street due to its capacity to be regularly prescribed as a sedative and the unavailability in prison of more commonly abused substances.  


==Chemistry==
==Chemistry==

Revision as of 17:05, 30 April 2014

Quetiapine
noframe
noframe
The skeletal formula of Quetiapine.
Dosage (oral)
Threshold 25 mg
Light 25 - 100 mg
Common 75 - 200 mg
Strong 200 - 300 mg
Heavy 300 mg +
Duration (oral)
4 - 8 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]

Recreational usage of this substance is uncommon but well documented. It seems to be driven by its sedative and anxiolytic effects (to help with sleep or to 'calm down') rather than by its antipsychotic properties."[6] Reports of quetiapine abuse have emerged in medical literature. In addition to oral administration, the drug is sometimes taken intranasally by insufflating pulverized tablets. A 2004 letter to the editor of the American Journal of Psychiatry provided an anecdotal estimate that up to 30% of inmates who were seen for psychiatric services in the Los Angeles County Jail were faking psychotic symptoms in an attempt to obtain quetiapine.[7] This drug seems to be more commonly abused in prisons than on the street due to its capacity to be regularly prescribed as a sedative and the unavailability in prison of more commonly abused substances.

Chemistry

Pharmocology

Quetiapine is a powerful dopamine, serotonin, and adrenergic antagonist, and a potent antihistamine with clinically negligible anticholinergic properties.[8][9][10][11] Quetiapine binds strongly to serotonin receptors; the drug acts as partial agonist at 5-HT1A receptors.[12] 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

The physical effects of Quetiapine can be broken down into 3 components all of which progressively intensify proportional to dosage. These are described below and generally include:

Cognitive effects

The general head space of Quetiapine is often described as one of sleepiness, emptiness, apathy, stupor and zombification. The specific cognitive effects can be broken down into 7 components all of which progressively intensify proportional to dosage. These are described below and generally include:

Medical uses

  • Schizophrenia: There is tentative evidence of the benefit of quetiapine versus placebo in schizophrenia; however, definitive conclusions are not possible due to the high rate of attrition in trials (greater than 50%) and the lack of data on economic outcomes, social functioning, or quality of life.[13]
  • Bipolar disorder: In those with bipolar disorder, quetiapine is used to treat depressive episodes, acute manic episodes associated with bipolar I disorder.[14][15]
  • Major depressove disorder: Quetiapine is effective when used by itself[16] and when used along with other medications in major depressive disorder (MDD).[16][17] However, sedation is often an undesirable side effect.[18]
  • Parkinsons disease: Quetiapine and clozapine are the most widely used medications for the treatment of Parkinson's disease psychosis due to their very low extrapyramidal side effect liability. Owing to the risks associated with clozapine (e.g. agranulocytosis, diabetes mellitus, etc.), clinicians often attempt treatment with quetiapine first, although the evidence to support quetiapine's use for this indication is significantly weaker than that of clozapine.[19][20]
  • Other: The use of low doses of quetiapine for insomnia, while common, is not recommended; there is little evidence of benefit and concerns regarding adverse effects.[21][22] It is sometimes used off-label, often as an augmentation agent, to treat conditions such as Tourette syndrome,[23] musical hallucinations[24] and anxiety disorders.[25]

Toxicity and harm potential

Tolerance and addiction potential

Interactions

References

  1. http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=SEROQUEL
  2. http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPTO%2Fsearch-bool.html&r=1&f=G&l=50&co1=AND&d=PTXT&s1=4,879,288.PN.&OS=PN/4,879,288&RS=PN/4,879,288
  3. http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPTO%2Fsearch-bool.html&r=1&f=G&l=50&co1=AND&d=PTXT&s1=4,879,288.PN.&OS=PN/4,879,288&RS=PN/4,879,288
  4. Blockbuster Drugs That Will Go Generic Soon | http://money.usnews.com/money/blogs/the-best-life/2011/04/29/blockbuster-drugs-that-will-go-generic-soon
  5. http://www.theodora.com/drugs/quepin_tablets_specifar.html
  6. Intranasal quetiapine abuse | http://ajp.psychiatryonline.org/article.aspx?articleid=177055
  7. Intranasal quetiapine abuse | http://ajp.psychiatryonline.org/article.aspx?articleid=177055
  8. http://www1.astrazeneca-us.com/pi/Seroquel.pdf
  9. Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compounds | http://www.sciencedirect.com/science/article/pii/S0024320500009115
  10. Neuropsychopharmocology, a fifth generation of progress | http://books.google.co.uk/books?id=BKwkonZwZD0C&pg=PA778&hl=en#v=onepage&q&f=false
  11. http://www.drugs.com/pro/seroquel.html
  12. Mechanism of Action of Quetiapine | http://psychopharmacologyinstitute.com/antipsychotics/quetiapine/mechanism-of-action/
  13. Quetiapine for schizophrenia | http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD000967.pub2/abstract
  14. Efficacy of Quetiapine Monotherapy in Bipolar I and II Depression: A Double-blind, Placebo-controlled Study (The BOLDER II Study) | http://journals.lww.com/psychopharmacology/pages/articleviewer.aspx?year=2006&issue=12000&article=00009&type=abstract
  15. British National Formulary (BNF) 65. Pharmaceutical Pr; 2013. ISBN 978-0857110848
  16. Second-generation antipsychotics for major depressive disorder and dysthymia | http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD008121.pub2/abstract
  17. Adjunctive Atypical Antipsychotic Treatment for Major Depressive Disorder: A Meta-Analysis of Depression, Quality of Life, and Safety Outcomes | http://www.plosmedicine.org/article/info%3Adoi%2F10.1371%2Fjournal.pmed.1001403
  18. Second-generation antipsychotics for major depressive disorder and dysthymia | http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD008121.pub2/abstract
  19. Quetiapine in the treatment of psychosis in Parkinson’s disease | http://tan.sagepub.com/content/3/6/339
  20. Taylor, D; Carol, P; Shitij, K (2012). The Maudsley prescribing guidelines in psychiatry. West Sussex: Wiley-Blackwell. ISBN 9780470979693.
  21. Safety of Low Doses of Quetiapine When Used for Insomnia | http://aop.sagepub.com/content/46/5/718
  22. Off-Label Use of Atypical Antipsychotics: An Update [Internet] | http://www.ncbi.nlm.nih.gov/pubmed/22132426
  23. Journal of Child and Adolescent Psychopharmacology | http://online.liebertpub.com/doi/abs/10.1089/104454603322572624
  24. Oliver Sacks "Musicophilia" Knopf NY 2007 P.67
  25. Treatment of sleep dysfunction and psychiatric disorders | http://link.springer.com/article/10.1007%2Fs11940-006-0026-6