Tìm theo
Ketobemidone
Các tên gọi khác (9 ) :
  • Cetobemidona
  • Cetobemidone
  • Cetobemidonum
  • Cliradon
  • Cymidon
  • Ketobemidone
  • Ketodur
  • Ketogan
  • Ketorax
Thuốc giảm đau có opioid
Thuốc Gốc
Small Molecule
CAS: 469-79-4
ATC: N02AB01
CTHH: C15H21NO2
PTK: 247.3327
Ketobemidone is a powerful opioid analgesic. Its effectiveness against pain is in the same range as morphine, and it also has some NMDA-antagonist properties. This makes it useful for some types of pain that don't respond well to other opioids. The most commonly cited equalisation ratio for analgesic doses is 25 mg of ketobemidone hydrobromide to 60 mg of morphine hydrochloride or sulfate and circa 8 mg of ketobemidone by injection.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H21NO2
Phân tử khối
247.3327
Monoisotopic mass
247.157228921
InChI
InChI=1S/C15H21NO2/c1-3-14(18)15(7-9-16(2)10-8-15)12-5-4-6-13(17)11-12/h4-6,11,17H,3,7-10H2,1-2H3
InChI Key
InChIKey=ALFGKMXHOUSVAD-UHFFFAOYSA-N
IUPAC Name
1-[4-(3-hydroxyphenyl)-1-methylpiperidin-4-yl]propan-1-one
Traditional IUPAC Name
ketobemidone
SMILES
CCC(=O)C1(CCN(C)CC1)C1=CC(O)=CC=C1
Độ tan chảy
156.5 °C
Độ hòa tan
3.01e+00 g/l
logP
2.49
logS
-1.9
pKa (strongest acidic)
9.44
pKa (Strongest Basic)
8.09
PSA
40.54 Å2
Refractivity
73.12 m3·mol-1
Polarizability
27.83 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Cơ Chế Tác Dụng : Ketobemidone is a powerful opioid analgesic. Its effectiveness against pain is in the same range as morphine, and it also has some NMDA-antagonist properties. This makes it useful for some types of pain that don't respond well to other opioids. The most commonly cited equalisation ratio for analgesic doses is 25 mg of ketobemidone hydrobromide to 60 mg of morphine hydrochloride or sulfate and circa 8 mg of ketobemidone by injection. Ketobemidone (Cliradon, Ketogan, Ketodur, Cymidon, Ketorax, &c.) is a powerful opioid analgesic. Its effectiveness against pain is in the same range as morphine, and it also has some NMDA-antagonist properties. This makes it useful for some types of pain that don't respond well to other opioids. The most commonly cited equalisation ratio for analgesic doses is 25 mg of ketobemidone hydrobromide to 60 mg of morphine hydrochloride or sulfate and circa 8 mg of ketobemidone by injection.
Dược Động Học :
▧ Absorption :
34% (oral), 44% (rectal)
▧ Metabolism :
Ketobemidone is mainly metabolised by conjugation of the phenolic hydroxyl group, and by N-desmethylation. Only about 13-24% is excreted unchanged after iv. administration.
▧ Half Life :
Plasma half-life: 2.42 +/- 0.41 h (m +/- SD). Elimination half-life: 3.27 +/- 0.32 h
Độc Tính : Base: Rat Intravenous LD50: 10 mg/kg; Mouse Intravenous LD50: 14 mg/kg. Hydrochloride salt: Rat Oral LD50: 215 mg/kg; Rat Intravenous LD50: 40 mg/kg
Chỉ Định : For the treatment of all types of severe pain, such as postoperative, cancer, kidney stones and fractures.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Pfizer
    Sản phẩm biệt dược : Cliradon
  • Công ty : Pfizer
    Sản phẩm biệt dược : Ketogan
  • Công ty : Pfizer
    Sản phẩm biệt dược : Ketorax
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06738
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C11792
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08100
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50045604
Wikipedia
http://en.wikipedia.org/wiki/Ketobemidone
... loading
... loading