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'''Esmirtazapine''' ('''Org 50081''') is a [[drug]] which is under development by [[Organon]] for the treatment of [[insomnia]] and [[vasomotor]] [[symptom]]s (e.g., [[hot flash]]es) associated with [[menopause]].<ref name="urlFuture Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net">{{cite web | url = http://www.neurotransmitter.net/newdrugs.html | title = Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net | format = | work = | accessdate = }}</ref><ref name="urlA Long-Term Safety Study of Org 50081 in Elderly Outpatients With Chronic Primary Insomnia (176005)(P05697) - Full Text View - ClinicalTrials.gov">{{cite web | url = http://clinicaltrials.gov/ct2/show/NCT00561574 | title = A Long-Term Safety Study of Org 50081 in Elderly Outpatients With Chronic Primary Insomnia (176005)(P05697) - Full Text View - ClinicalTrials.gov | format = | work = | accessdate = }}</ref><ref name="pmid18673166">{{cite journal | author = Teegarden BR, Al Shamma H, Xiong Y | title = 5-HT(2A) inverse-agonists for the treatment of insomnia | journal = Current Topics in Medicinal Chemistry | volume = 8 | issue = 11 | pages = 969–76 | year = 2008 | pmid = 18673166 | doi = | url = }}</ref><ref name="pmid19775194">{{cite journal | author = Lewis V | title = Undertreatment of menopausal symptoms and novel options for comprehensive management | journal = Current Medical Research and Opinion | volume = 25 | issue = 11 | pages = 2689–98 | year = 2009 | month = November | pmid = 19775194 | doi = 10.1185/03007990903240519 | url = http://informahealthcare.com/doi/abs/10.1185/03007990903240519}}</ref> As of 2009 it is in [[phase III]] [[clinical trial]]s.<ref name="urlFuture Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net">{{cite web | url = http://www.neurotransmitter.net/newdrugs.html | title = Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net | format = | work = | accessdate = }}</ref> Esmirtazapine is the ''S''(+)-[[enantiomer]] of [[mirtazapine]] and possesses similar overall [[pharmacology]], including [[receptor_antagonist|antagonist]] actions at [[H1 receptor|H<sub>1</sub>]], [[5-HT2_receptor|5-HT<sub>2</sub>]], and [[alpha-2 adrenergic receptor|α<sub>2</sub>-adrenergic receptor]]s.<ref name="urlFuture Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net">{{cite web | url = http://www.neurotransmitter.net/newdrugs.html | title = Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net | format = | work = | accessdate = }}</ref><ref name="isbn0-521-88663-5">{{cite book | author = | title = Depression and bipolar disorder: Stahl's essential psychopharmacology | publisher = Cambridge University Press | location = Cambridge, UK | year = 2008 | pages = | isbn = 0-521-88663-5 | oclc = | doi = | url = http://books.google.com/books?id=zqvVZOea2JAC&lpg=PA112&dq=esmirtazapine&as_brr=3&pg=PA112#v=onepage&q=&f=false}}</ref> |
'''Esmirtazapine''' ('''Org 50081''') is a [[drug]] which is under development by [[Organon]] for the treatment of [[insomnia]] and [[vasomotor]] [[symptom]]s (e.g., [[hot flash]]es) associated with [[menopause]].<ref name="urlFuture Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net">{{cite web | url = http://www.neurotransmitter.net/newdrugs.html | title = Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net | format = | work = | accessdate = }}</ref><ref name="urlA Long-Term Safety Study of Org 50081 in Elderly Outpatients With Chronic Primary Insomnia (176005)(P05697) - Full Text View - ClinicalTrials.gov">{{cite web | url = http://clinicaltrials.gov/ct2/show/NCT00561574 | title = A Long-Term Safety Study of Org 50081 in Elderly Outpatients With Chronic Primary Insomnia (176005)(P05697) - Full Text View - ClinicalTrials.gov | format = | work = | accessdate = }}</ref><ref name="pmid18673166">{{cite journal | author = Teegarden BR, Al Shamma H, Xiong Y | title = 5-HT(2A) inverse-agonists for the treatment of insomnia | journal = Current Topics in Medicinal Chemistry | volume = 8 | issue = 11 | pages = 969–76 | year = 2008 | pmid = 18673166 | doi = | url = }}</ref><ref name="pmid19775194">{{cite journal | author = Lewis V | title = Undertreatment of menopausal symptoms and novel options for comprehensive management | journal = Current Medical Research and Opinion | volume = 25 | issue = 11 | pages = 2689–98 | year = 2009 | month = November | pmid = 19775194 | doi = 10.1185/03007990903240519 | url = http://informahealthcare.com/doi/abs/10.1185/03007990903240519}}</ref> As of 2009 it is in [[phase III]] [[clinical trial]]s.<ref name="urlFuture Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net">{{cite web | url = http://www.neurotransmitter.net/newdrugs.html | title = Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net | format = | work = | accessdate = }}</ref> Esmirtazapine is the ''S''(+)-[[enantiomer]] of [[mirtazapine]] and possesses similar overall [[pharmacology]], including [[receptor_antagonist|antagonist]]/[[inverse agonist]] actions at [[H1 receptor|H<sub>1</sub>]], [[5-HT2_receptor|5-HT<sub>2</sub>]], and [[alpha-2 adrenergic receptor|α<sub>2</sub>-adrenergic receptor]]s.<ref name="urlFuture Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net">{{cite web | url = http://www.neurotransmitter.net/newdrugs.html | title = Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net | format = | work = | accessdate = }}</ref><ref name="isbn0-521-88663-5">{{cite book | author = | title = Depression and bipolar disorder: Stahl's essential psychopharmacology | publisher = Cambridge University Press | location = Cambridge, UK | year = 2008 | pages = | isbn = 0-521-88663-5 | oclc = | doi = | url = http://books.google.com/books?id=zqvVZOea2JAC&lpg=PA112&dq=esmirtazapine&as_brr=3&pg=PA112#v=onepage&q=&f=false}}</ref> |
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== See also == |
== See also == |
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Revision as of 07:03, 7 March 2010
| File:Esmirtazapine.png | |
| Clinical data | |
|---|---|
| ATC code |
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| Pharmacokinetic data | |
| Metabolism | Liver (CYP2D6)[1] |
| Identifiers | |
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| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.056.994 |
| Chemical and physical data | |
| Formula | C21H23N3O4 |
| Molar mass | 381.43 g/mol g·mol−1 |
| 3D model (JSmol) | |
| Melting point | 114 to 116 °C (237 to 241 °F) |
| Solubility in water | Soluble in methanol and chloroform mg/mL (20 °C) |
| |
Esmirtazapine (Org 50081) is a drug which is under development by Organon for the treatment of insomnia and vasomotor symptoms (e.g., hot flashes) associated with menopause.[2][3][4][5] As of 2009 it is in phase III clinical trials.[2] Esmirtazapine is the S(+)-enantiomer of mirtazapine and possesses similar overall pharmacology, including antagonist/inverse agonist actions at H1, 5-HT2, and α2-adrenergic receptors.[2][6]
See also
References
- ^ "A population analysis on the effects of the CYP2D6 deficiency on pharmacokinetics and exposure of esmirtazapine in healthy volunteers" (PDF).
- ^ a b c "Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net".
- ^ "A Long-Term Safety Study of Org 50081 in Elderly Outpatients With Chronic Primary Insomnia (176005)(P05697) - Full Text View - ClinicalTrials.gov".
- ^ Teegarden BR, Al Shamma H, Xiong Y (2008). "5-HT(2A) inverse-agonists for the treatment of insomnia". Current Topics in Medicinal Chemistry. 8 (11): 969–76. PMID 18673166.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ Lewis V (2009). "Undertreatment of menopausal symptoms and novel options for comprehensive management". Current Medical Research and Opinion. 25 (11): 2689–98. doi:10.1185/03007990903240519. PMID 19775194.
{{cite journal}}: Unknown parameter|month=ignored (help) - ^ Depression and bipolar disorder: Stahl's essential psychopharmacology. Cambridge, UK: Cambridge University Press. 2008. ISBN 0-521-88663-5.
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