Tìm theo
Oxymorphone
Các tên gọi khác (9 ) :
  • 14-Hydroxydihydromorphinone
  • Dihydrohydroxymorphinone
  • Dihydroxymorphinone
  • EN3202
  • Numorphan
  • Opana
  • Oximorphonum
  • Oxymorphine
  • Oxymorphone
Thuốc giảm đau có opioid
Thuốc Gốc
Small Molecule
CAS: 76-41-5
ĐG : Bristol-Myers Squibb Co. , http://www.bms.com
CTHH: C17H19NO4
PTK: 301.3371
An opioid analgesic with actions and uses similar to those of morphine, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H19NO4
Phân tử khối
301.3371
Monoisotopic mass
301.131408101
InChI
InChI=1S/C17H19NO4/c1-18-7-6-16-13-9-2-3-10(19)14(13)22-15(16)11(20)4-5-17(16,21)12(18)8-9/h2-3,12,15,19,21H,4-8H2,1H3/t12-,15+,16+,17-/m1/s1
InChI Key
InChIKey=UQCNKQCJZOAFTQ-ISWURRPUSA-N
IUPAC Name
(1S,5R,13R,17S)-10,17-dihydroxy-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
oxymorphone
SMILES
[H][C@@]12OC3=C(O)C=CC4=C3[C@@]11CCN(C)[C@]([H])(C4)[C@]1(O)CCC2=O
Độ tan chảy
248-249 °C
Độ hòa tan
2.4E+004 mg/L
logP
0.83
logS
-1.1
pKa (strongest acidic)
7.34
pKa (Strongest Basic)
10.93
PSA
70 Å2
Refractivity
79.56 m3·mol-1
Polarizability
30.77 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.17
Dược Lực Học : Oxymorphone is a semi-synthetic opioid substitute for morphine. It is a potent analgesic. Opioid analgesics exert their principal pharmacologic effects on the CNS and the gastrointestinal tract. The principal actions of therapeutic value are analgesia and sedation. Opioids produce respiratory depression by direct action on brain stem respiratory centers. The mechanism of respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to increases in carbon dioxide tension and to electrical stimulation.
Cơ Chế Tác Dụng : An opioid analgesic with actions and uses similar to those of morphine, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092) Oxymorphone interacts predominantly with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, with high densities in the posterior amygdala, hypothalamus, thalamus, nucleus caudatus, putamen, and certain cortical areas. They are also found on the terminal axons of primary afferents within laminae I and II (substantia gelatinosa) of the spinal cord and in the spinal nucleus of the trigeminal nerve. Also, it has been shown that oxymorphone binds to and inhibits GABA inhibitory interneurons via mu-receptors. These interneurons normally inhibit the descending pain inhibition pathway. So, without the inhibitory signals, pain modulation can proceed downstream.
Dược Động Học :

▧ Metabolism :
Oxymorphone undergoes extensive hepatic metabolism in humans. After a 10 mg oral dose, 49% was excreted over a five-day period in the urine. Of this, 82% was excreted in the first 24 hours after administration. The recovered drug-related products contained the oxymorphone (1.9%), the conjugate of oxymorphone (44.1%), the 6(beta)-carbinol produced by 6-keto reduction of oxymorphone (0.3%), and the conjugates of 6(beta)-carbinol (2.6%) and 6(alpha)-carbinol (0.1%).
▧ Route of Elimination :
Oxymorphone is highly metabolized, principally in the liver, and undergoes reduction or conjugation with glucuronic acid to form both active and inactive products. Because oxymorphone is extensively metabolized, <1% of the administered dose is excreted unchanged in the urine.
▧ Half Life :
1.3 (+/-0.7) hours
Độc Tính : Oxymorphone overdosage is characterized by respiratory depression, extreme somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, and sometimes bradycardia and hypotension. In a severe case of overdose, apnea, circulatory collapse, cardiac arrest, and death may occur. Intravenous mouse LD50 is 172 mg/kg.
Chỉ Định : For 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.
  • Cimetidine Increases the effect of the narcotic
  • Triprolidine The CNS depressants, Triprolidine and Oxymorphone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Suppository - Rectal
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Numorphan
  • Công ty :
    Sản phẩm biệt dược : Opana
  • Công ty :
    Sản phẩm biệt dược : OPANA ER
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01192
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5284604
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505296
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08019
ChemSpider
http://www.chemspider.com/Chemical-Structure.4447650.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50001707
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/63481-612-70
PharmGKB
http://www.pharmgkb.org/drug/PA450748
Wikipedia
http://en.wikipedia.org/wiki/Oxymorphone
RxList
http://www.rxlist.com/cgi/generic2/oxymorphone.htm
Drugs.com
http://www.drugs.com/cdi/oxymorphone.html
... loading
... loading