Tìm theo
Pentazocine
Các tên gọi khác (5 ) :
  • Fortral
  • Pentazocin
  • Pentazocina
  • Pentazocine
  • Pentazocinum
Thuốc giảm đau có opioid
Thuốc Gốc
Small Molecule
CAS: 359-83-1
ATC: N02AD01
ĐG : A-S Medication Solutions LLC , http://orders.a-smeds.com
CTHH: C19H27NO
PTK: 285.4238
The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H27NO
Phân tử khối
285.4238
Monoisotopic mass
285.209264491
InChI
InChI=1S/C19H27NO/c1-13(2)7-9-20-10-8-19(4)14(3)18(20)11-15-5-6-16(21)12-17(15)19/h5-7,12,14,18,21H,8-11H2,1-4H3/t14-,18+,19+/m0/s1
InChI Key
InChIKey=VOKSWYLNZZRQPF-GDIGMMSISA-N
IUPAC Name
(1R,9R,13R)-1,13-dimethyl-10-(3-methylbut-2-en-1-yl)-10-azatricyclo[7.3.1.0^{2,7}]trideca-2,4,6-trien-4-ol
Traditional IUPAC Name
pentazocine
SMILES
C[C@H]1[C@H]2CC3=CC=C(O)C=C3[C@]1(C)CCN2CC=C(C)C
Độ tan chảy
146.3 °C
Độ hòa tan
1.22e-01 g/l
logP
4.64
logS
-3.4
pKa (strongest acidic)
7.59
pKa (Strongest Basic)
12.4
PSA
23.47 Å2
Refractivity
89.8 m3·mol-1
Polarizability
33.86 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.88
Dược Lực Học : Pentazocine is a potent analgesic which when administered orally in a 50 mg dose appears equivalent in analgesic effect to 60 mg (1 grain) of codeine. Onset of significant analgesia usually occurs between 15 and 30 minutes after oral administration, and duration of action is usually three hours or longer. Onset and duration of action and the degree of pain relief are related both to dose and the severity of pretreatment pain. Pentazocine weakly antagonizes the analgesic effects of morphine and meperidine; in addition, it produces incomplete reversal of cardiovascular, respiratory, and behavioral depression induced by morphine and meperidine. Pentazocine has about 1/50 the antagonistic activity of nalorphine. It also has sedative activity.
Cơ Chế Tác Dụng : The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97) The preponderance of evidence suggests that pentazocine antagonizes the opioid effects by competing for the same receptor sites, especially the opioid mu receptor.
Dược Động Học :
▧ Absorption :
Well absorbed from the gastro-intestinal tract.
▧ Metabolism :
Hepatic
▧ Half Life :
2 to 3 hours
Chỉ Định : For the relief of moderate to severe pain.
Tương Tác Thuốc :
  • Alvimopan Increases levels by receptor binding competition. Discontinue opioid administration at least 7 days prior to administrating Alvimopan.
  • Triprolidine The CNS depressants, Triprolidine and Pentazocine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Solution - Intravenous
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Talwin 30 mg/ml
    Giá bán buôn : USD >1.64
    Đơn vị tính : ml
  • Biệt dược thương mại : Talwin 30 mg/ml ampul
    Giá bán buôn : USD >4.86
    Đơn vị tính : ml
  • Biệt dược thương mại : Talwin 30 mg/ml vial
    Giá bán buôn : USD >14.78
    Đơn vị tính : ml
  • Biệt dược thương mại : Talwin 50 mg Tablet
    Giá bán buôn : USD >0.47
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Fortal
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Fortral
  • Công ty : Terapia
    Sản phẩm biệt dược : Fortwin
  • Công ty : L.B.S.
    Sản phẩm biệt dược : Pangon
  • Công ty : Daiichi Sankyo
    Sản phẩm biệt dược : Pentagin
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Sosegon
  • Công ty : Beximco
    Sản phẩm biệt dược : Stopain
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Talwin
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Talwin PX
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00652
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=441278
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506363
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07421
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00498
ChemSpider
http://www.chemspider.com/Chemical-Structure.390041.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50001028
PharmGKB
http://www.pharmgkb.org/drug/PA164744326
Wikipedia
http://en.wikipedia.org/wiki/Pentazocine
RxList
http://www.rxlist.com/cgi/generic/pentazocine.htm
Drugs.com
http://www.drugs.com/cdi/pentazocine.html
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