Tìm theo
Oxycodone
Các tên gọi khác (9 ) :
  • (-)-14-Hydroxydihydrocodeinone
  • 4,5-Epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one
  • 4,5alpha-Epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one
  • Dihydro-14-hydroxycodeinone
  • Dihydrohydroxycodeinone
  • Dihydroxycodeinone
  • Oxicodona
  • Oxycodone
  • Oxycodonum
Thuốc giảm đau có opioid
Thuốc Gốc
Small Molecule
CAS: 76-42-6
ATC: N02AA05
ĐG : 4uOrtho LLC , http://www.4udr.com
CTHH: C18H21NO4
PTK: 315.3636
Semisynthetic derivative of codeine that acts as a narcotic analgesic more potent and addicting than codeine. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H21NO4
Phân tử khối
315.3636
Monoisotopic mass
315.147058165
InChI
InChI=1S/C18H21NO4/c1-19-8-7-17-14-10-3-4-12(22-2)15(14)23-16(17)11(20)5-6-18(17,21)13(19)9-10/h3-4,13,16,21H,5-9H2,1-2H3/t13-,16+,17+,18-/m1/s1
InChI Key
InChIKey=BRUQQQPBMZOVGD-XFKAJCMBSA-N
IUPAC Name
(1S,5R,13R,17S)-17-hydroxy-10-methoxy-4-methyl-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10-trien-14-one
Traditional IUPAC Name
oxycodone
SMILES
[H][C@@]12OC3=C(OC)C=CC4=C3[C@@]11CCN(C)[C@]([H])(C4)[C@]1(O)CCC2=O
Độ tan chảy
219 °C
Độ hòa tan
100 mg/ml
logP
0.3
logS
-1.8
pKa (strongest acidic)
13.56
pKa (Strongest Basic)
8.21
PSA
59 Å2
Refractivity
84.04 m3·mol-1
Polarizability
32.8 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Oxycodone, a semisynthetic opiate agonist derived from the opioid alkaloid, thebaine, is similar to other phenanthrene derivatives such as hydrocodone and morphine. Oxycodone is available in combination with aspirin or acetaminophen to control pain and restless leg and Tourette syndromes.
Cơ Chế Tác Dụng : Semisynthetic derivative of codeine that acts as a narcotic analgesic more potent and addicting than codeine. [PubChem] Oxycodone acts as a weak agonist at mu, kappa, and delta opioid receptors within the central nervous system (CNS). Oxycodone primarily affects mu-type opioid receptors, which are coupled with G-protein receptors and function as modulators, both positive and negative, of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is inhibited. Opioids such as oxycodone also inhibit the release of vasopressin, somatostatin, insulin, and glucagon. Opioids close N-type voltage-operated calcium channels (kappa-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (mu and delta receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Dược Động Học :
▧ Absorption :
Well absorbed with an oral bioavailability of 60% to 87%
▧ Volume of Distribution :
* 2.6 L/kg
▧ Protein binding :
45%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Oxycodone and its metabolites are excreted primarily via the kidney.
▧ Half Life :
4.5 hours
▧ Clearance :
* 0.8 L/min [adults]
Độc Tính : Symptoms of overdose include respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, bradycardia, hypotension, and death.
Chỉ Định : For the treatment of diarrhoea, pulmonary oedema and for the relief of moderate to moderately severe pain.
Tương Tác Thuốc :
  • Alvimopan Increases levels by receptor binding competition. Discontinue opioid administration at least 7 days prior to administrating Alvimopan.
  • Cimetidine Cimetidine, a moderate CYP3A4 inhibitor, may decrease the metabolism of oxycodone. Monitor for changes in the therapeutic and adverse effects of oxycodone if cimetidine is initiated, discontinued or dose changed.
  • Citalopram Increased risk of serotonin syndrome
  • Escitalopram Increased risk of serotonin syndrome
  • Fluoxetine Increased risk of serotonin syndrome
  • Fluvoxamine Increased risk of serotonin syndrome
  • Paroxetine Increased risk of serotonin syndrome
  • Sertraline Increased risk of serotonin syndrome
  • Triprolidine The CNS depressants, Triprolidine and Oxycodone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Suppository - Rectal
Tablet - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Oxanest
  • Công ty :
    Sản phẩm biệt dược : Oxecta
  • Công ty :
    Sản phẩm biệt dược : Oxycontin
  • Công ty :
    Sản phẩm biệt dược : OxyIR
  • Công ty :
    Sản phẩm biệt dược : Roxicodone
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00497
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5284603
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508908
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08018
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05312
ChemSpider
http://www.chemspider.com/Chemical-Structure.4447649.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0406-0552-01
PharmGKB
http://www.pharmgkb.org/drug/PA450741
Wikipedia
http://en.wikipedia.org/wiki/Oxycodone
RxList
http://www.rxlist.com/cgi/generic/oxyco.htm
Drugs.com
http://www.drugs.com/oxycodone.html
... loading
... loading