Esmirtazapine

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Esmirtazapine
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Systematic (IUPAC) name
(S)-1,2,3,4,10,14b-hexahydro-2-methylpyrazino(2,1-a)pyrido(2,3-c)(2)benzazepine
Clinical data
Legal status
  • Uncontrolled
Routes of
administration
Oral
Pharmacokinetic data
Metabolism Liver (CYP2D6)[1]
Identifiers
CAS Number 61337-87-9 YesY
ATC code none
PubChem CID: 3085218
DrugBank DB00316 YesY
ChemSpider 2342166 YesY
UNII 4685R51V7M YesY
KEGG D04055 YesY
Chemical data
Formula C17H19N3
Molecular mass 265.35 g/mol
Physical data
Melting point 114 to 116 °C (237 to 241 °F)
Solubility in water Soluble in methanol and chloroform mg/mL (20 °C)
  (verify)

Esmirtazapine (ORG-50,081) is a drug which was under development by Organon for the treatment of insomnia and vasomotor symptoms (e.g., hot flashes) associated with menopause.[2][3][4][5] Esmirtazapine is the (S)-(+)-enantiomer of mirtazapine and possesses similar overall pharmacology, including inverse agonist actions at H1 and 5-HT2 receptors and antagonist actions at α2-adrenergic receptors.[2][6] As of March 2010, Merck terminated internal clinical development program for esmirtazapine, for hot flashes and insomnia, for strategic reasons.[7]

See also

References

  1. "A population analysis on the effects of the CYP2D6 deficiency on pharmacokinetics and exposure of esmirtazapine in healthy volunteers" (PDF).<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
  2. 2.0 2.1 "Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net".<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
  3. "A Long-Term Safety Study of Org 50081 in Elderly Outpatients With Chronic Primary Insomnia (176005)(P05697) - Full Text View - ClinicalTrials.gov".<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
  4. Lua error in Module:Citation/CS1/Identifiers at line 47: attempt to index field 'wikibase' (a nil value).
  5. Lua error in Module:Citation/CS1/Identifiers at line 47: attempt to index field 'wikibase' (a nil value).
  6. Depression and bipolar disorder: Stahl's essential psychopharmacology. Cambridge, UK: Cambridge University Press. 2008. ISBN 0-521-88663-5.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
  7. http://www.merck.com/investors/financials/form-10-K-2009-final.pdf