Tìm theo
Eszopiclone
Các tên gọi khác (9 ) :
  • (+)-(5S)-6-(5-Chloropyridin-2-yl)-7-oxo-6,7-dihydro-5H-pyrrolo(3,4-b)pyrazin-5-yl 4-methylpiperazine-1-carboxylate
  • (+)-(5S)-6-(5-chloropyridin-2-yl)-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazin-5-yl-4-methylpiperazine-1-carboxylate
  • (+)-Zopiclone
  • (S)-6-(5-Chloro-2-pyridinyl)- 7-oxo- 6,7-dihydro- 5H-pyrrolo[3,4-b]pyrazin-5-yl- 4-methyl- 1-piperazinecarboxylate
  • (S)-Zopiclone
  • 1-Piperazinecarobxylic acid,4-methyl-,(5S)-6-(5-chloro-2-pyridinyl)-6,7-dihydro-7-oxo-5H-pyrrolo[3,4-b]pyrazin-5-yl ester
  • Esopiclone
  • Estorra
  • Eszopiclone
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 138729-47-2
ATC: N05CF04
ĐG : A-S Medication Solutions LLC , http://orders.a-smeds.com
CTHH: C17H17ClN6O3
PTK: 388.808
Eszopiclone, marketed by Sepracor under the brand-name Lunesta, is a nonbenzodiazepine hypnotic agent (viz., a sedative) used as a treatment for insomnia. Eszopiclone is the active stereoisomer of zopiclone, and belongs to the class of drugs known as cyclopyrrones. Its main selling point is that it is approved by the U.S. Food and Drug Administration for long-term use, unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H17ClN6O3
Phân tử khối
388.808
Monoisotopic mass
388.105066147
InChI
InChI=1S/C17H17ClN6O3/c1-22-6-8-23(9-7-22)17(26)27-16-14-13(19-4-5-20-14)15(25)24(16)12-3-2-11(18)10-21-12/h2-5,10,16H,6-9H2,1H3/t16-/m0/s1
InChI Key
InChIKey=GBBSUAFBMRNDJC-INIZCTEOSA-N
IUPAC Name
(5S)-6-(5-chloropyridin-2-yl)-7-oxo-5H,6H,7H-pyrrolo[3,4-b]pyrazin-5-yl 4-methylpiperazine-1-carboxylate
Traditional IUPAC Name
eszopiclone
SMILES
CN1CCN(CC1)C(=O)O[C@@H]1N(C(=O)C2=NC=CN=C12)C1=NC=C(Cl)C=C1
Độ hòa tan
very slightly soluble
logP
0.8
logS
-2.6
pKa (strongest acidic)
13.04
pKa (Strongest Basic)
6.89
PSA
91.76 Å2
Refractivity
95.89 m3·mol-1
Polarizability
37.67 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
6
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Eszopiclone is a nonbenzodiazepine hypnotic, pyrrolopyrazine derivative of the cyclopyrrolone class and is indicated for the short-term treatment of insomnia. While Eszopiclone is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Eszopiclone binds selectively to the brain alpha subunit of the GABA A omega-1 receptor.
Cơ Chế Tác Dụng : Eszopiclone, marketed by Sepracor under the brand-name Lunesta, is a nonbenzodiazepine hypnotic agent (viz., a sedative) used as a treatment for insomnia. Eszopiclone is the active stereoisomer of zopiclone, and belongs to the class of drugs known as cyclopyrrones. Its main selling point is that it is approved by the U.S. Food and Drug Administration for long-term use, unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia. The mechanism of action of Eszopiclone is not completely understood. It is thought that Eszopiclone acts on the benzodiazepine receptors as an agonist and interacts with GABA-receptor complexes.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration
▧ Protein binding :
52-59%
▧ Metabolism :
Following oral administration, eszopiclone is extensively metabolized by oxidation and demethylation.
▧ Route of Elimination :
Up to 75% of an oral dose of racemic zopiclone is excreted in the urine, primarily as metabolites.
▧ Half Life :
6 hours
Độc Tính : Side effects include viral infection, dry mouth, dizziness, hallucinations, infection, rash, and unpleasant taste, with this relationship clearest for unpleasant taste depending on doses.
Chỉ Định : For the treatment of insomnia
Tương Tác Thuốc :
  • Telithromycin Telithromycin may reduce clearance of Eszopiclone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Eszopiclone if Telithromycin is initiated, discontinued or dose changed.
  • Triprolidine The CNS depressants, Triprolidine and Eszopiclone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of eszopiclone by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of eszopiclone if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet, film coated - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Lunesta 1 mg tablet
    Giá bán buôn : USD >7.24
    Đơn vị tính : tablet
  • Biệt dược thương mại : Lunesta 3 mg tablet
    Giá bán buôn : USD >7.28
    Đơn vị tính : tablet
  • Biệt dược thương mại : Lunesta 2 mg tablet
    Giá bán buôn : USD >8.08
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty : LKM
    Sản phẩm biệt dược : Dorplen
  • Công ty : Opsonin
    Sản phẩm biệt dược : Esleep
  • Công ty : Silesia
    Sản phẩm biệt dược : Eszop
  • Công ty : Sun
    Sản phẩm biệt dược : Fulnite
  • Công ty : Roemmers
    Sản phẩm biệt dược : Inductal
  • Công ty : Tecnoquimicas
    Sản phẩm biệt dược : Isoklon
  • Công ty : Sunovion
    Sản phẩm biệt dược : Lunesta
  • Công ty : Saval
    Sản phẩm biệt dược : Nirvan
  • Công ty : Andromaco
    Sản phẩm biệt dược : Noptic
  • Công ty : Medipharm
    Sản phẩm biệt dược : Plessir
  • Công ty : Sanitas
    Sản phẩm biệt dược : Sanilent
  • Công ty : Aristopharma
    Sản phẩm biệt dược : Sleepil
  • Công ty : Eskayef
    Sản phẩm biệt dược : Sominex
  • Công ty : Acme
    Sản phẩm biệt dược : Sono
  • Công ty : Drugtech
    Sản phẩm biệt dược : Valnoc
  • Công ty : Tasly
    Sản phẩm biệt dược : Wen Fei
  • Công ty : Incepta
    Sản phẩm biệt dược : Zopilone
  • Công ty : Chile
    Sản phẩm biệt dược : Zopinon
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00402
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=969472
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505809
ChemSpider
http://www.chemspider.com/Chemical-Structure.839530.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=26265
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0339-4162-11
PharmGKB
http://www.pharmgkb.org/drug/PA162630444
Wikipedia
http://en.wikipedia.org/wiki/Eszopiclone
RxList
http://www.rxlist.com/cgi/generic3/lunesta.htm
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