Tìm theo
Glutethimide
Các tên gọi khác (2) :
  • 2-Ethyl-2-phenylglutarimide
  • Doriden
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 77-21-4
ATC: N05CE01
CTHH: C13H15NO2
PTK: 217.2637
A hypnotic and sedative. Its use has been largely superseded by other drugs. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H15NO2
Phân tử khối
217.2637
Monoisotopic mass
217.110278729
InChI
InChI=1S/C13H15NO2/c1-2-13(10-6-4-3-5-7-10)9-8-11(15)14-12(13)16/h3-7H,2,8-9H2,1H3,(H,14,15,16)
InChI Key
InChIKey=JMBQKKAJIKAWKF-UHFFFAOYSA-N
IUPAC Name
3-ethyl-3-phenylpiperidine-2,6-dione
Traditional IUPAC Name
glutethimide
SMILES
CCC1(CCC(=O)NC1=O)C1=CC=CC=C1
Độ tan chảy
78-81
Độ hòa tan
999 mg/L (at 30 °C)
logP
1.90
logS
-2.34
pKa (strongest acidic)
11.69
pKa (Strongest Basic)
-6.7
PSA
46.17 Å2
Refractivity
60.65 m3·mol-1
Polarizability
23.15 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
9.2
Dược Lực Học : Glutethimide is a hypnotic sedative that was introduced in 1954 as a safe alternative to barbiturates to treat insomnia. Before long, however, it had become clear that glutethimide was just as likely to cause addiction and caused similarly severe withdrawal symptoms.
Cơ Chế Tác Dụng : A hypnotic and sedative. Its use has been largely superseded by other drugs. [PubChem] Glutethimide seems to be a GABA agonist which helps induced sedation. It also induces CYP 2D6. When taken with codeine, it enables the body to convert higher amounts of the codeine (higher than the average 5 - 10%) to morphine. The general sedative effect also adds to the power of the combination.
Dược Động Học :
▧ Absorption :
Variable
▧ Metabolism :
Hepatic. Glutethimide is almost completely metabolized.
▧ Route of Elimination :
glutethimide is inactivated by conjugation and the metabolites are excreted in urine, only 2% of the parent substance is excreted in urine, up to 2% of the dose has been reported to be found in the faeces.
▧ Half Life :
10-12 hours
Độc Tính : In adults, death has been reported after 5 g. The usual lethal dose is 10 to 20g, although survival after a dose of 28 g has been reported.
Chỉ Định : For the treatment of insomnia.
Tương Tác Thuốc :
  • Acenocoumarol Glutethimide may decrease the anticoagulant effect of acenocoumarol.
  • Anisindione Glutethimide may decrease the anticoagulant effect of anisindione.
  • Dicoumarol Glutethimide may decrease the anticoagulant effect of dicumarol.
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Rivastigmine Possible antagonism of action
  • Triprolidine The CNS depressants, Triprolidine and Glutethimide, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Warfarin Glutethimide may decrease the serum concentration of warfarin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of warfarin if glutethimide is initiated, discontinued or dose changed.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : U.S.V .
    Sản phẩm biệt dược : Doriden
  • Công ty :
    Sản phẩm biệt dược : Elrodorm
  • Công ty : Polfa Pabianice
    Sản phẩm biệt dược : Glimid
  • Công ty : Balkanpharma
    Sản phẩm biệt dược : Glutethimid
  • Công ty :
    Sản phẩm biệt dược : Noxyron
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01437
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3487
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506283
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07489
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00532
ChemSpider
http://www.chemspider.com/Chemical-Structure.3367.html
PharmGKB
http://www.pharmgkb.org/drug/PA164749505
Wikipedia
http://en.wikipedia.org/wiki/Glutethimide
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