Tìm theo
Dezocine
Các tên gọi khác (3) :
  • (-)-13beta-amino-5,6,7,8,9,10,11alpha,12-Octahydro-5alpha-methyl-5,11-methanobenzocyclodecen-3-ol
  • Dezocina
  • Dezocinum
Thuốc giảm đau có opioid
Thuốc Gốc
Small Molecule
CAS: 53648-55-8
ATC: N02AX03
CTHH: C16H23NO
PTK: 245.3599
Dezocine is a partial opiate drug and is used for pain management. Dezocine is a very effective alternative to fentanyl when administered during outpatient laparoscopy, although is associated with an increased incidence of postoperative nausea.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H23NO
Phân tử khối
245.3599
Monoisotopic mass
245.177964363
InChI
InChI=1S/C16H23NO/c1-16-8-4-2-3-5-12(15(16)17)9-11-6-7-13(18)10-14(11)16/h6-7,10,12,15,18H,2-5,8-9,17H2,1H3/t12-,15-,16+/m0/s1
InChI Key
InChIKey=VTMVHDZWSFQSQP-VBNZEHGJSA-N
IUPAC Name
(1R,9S,15S)-15-amino-1-methyltricyclo[7.5.1.0^{2,7}]pentadeca-2,4,6-trien-4-ol
Traditional IUPAC Name
dezocine
SMILES
[H][C@@]12CC3=CC=C(O)C=C3[C@@](C)(CCCCC1)[C@H]2N
Độ hòa tan
1.40e-02 g/l
logP
3.3
logS
-4.2
pKa (strongest acidic)
10.43
pKa (Strongest Basic)
9.67
PSA
46.25 Å2
Refractivity
74.19 m3·mol-1
Polarizability
28.49 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Dezocine is a parenteral narcotic analgesic possessing both agonist and antagonist activity. It is similar to morphine with respect to analgesic potency and onset and duration of action. The narcotic antagonist activity is greater than that of pentazocine.
Cơ Chế Tác Dụng : Dezocine is a partial opiate drug and is used for pain management. Dezocine is a very effective alternative to fentanyl when administered during outpatient laparoscopy, although is associated with an increased incidence of postoperative nausea. Dezocine is a opioid analgesic drug of mixed agonist-antagonist type. It binds with stereospecific receptors at many sites within the central nervous system (CNS) to alter processes affecting both the perception of pain and the emotional response to pain. At least 2 of these types of receptors (mu and kappa) mediate analgesia. Mu receptors are widely distributed throughout the CNS, especially in the limbic system (frontal cortex, temporal cortex, amygdala, and hippocampus), thalamus, striatum, hypothalamus, and midbrain as well as laminae I, II, IV, and V of the dorsal horn in the spinal cord. Kappa receptors are localized primarily in the spinal cord and in the cerebral cortex.
Dược Động Học :
▧ Absorption :
Rapid and complete following intramuscular administration.
▧ Metabolism :
Hepatic, via conjugation (glucuronidation).
▧ Half Life :
Elimination half-life following intramuscular administration averages 2.2 hours. Elimination half-life following a 5mg intravenous dose averages 1.7 to 2.6 hours (range 0.6 to 4.4 hours) while a 10mg dose averages 2.4 to 2.6 hours (range 1.2 to 7.4 hours). In patients with hepatic cirrhosis, the half-life is increased by 30 to 50%.
Độc Tính : Symptoms of overdose include cold and clammy skin, confusion, nervousness, or severe restlessness, convulsions (seizures), severe dizziness, severe drowsiness, low blood pressure, pinpoint pupils of eyes, slow heartbeat, slow or troubled breathing and severe weakness.
Chỉ Định : Indicated in the treatment 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 Dezocine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Dalgan
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01209
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08010
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00838
PharmGKB
http://www.pharmgkb.org/drug/PA164746059
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