Tìm theo
Hydromorphone
Các tên gọi khác (13 ) :
  • (-)-(5R)-4,5-Epoxy-3-hydroxy-9alpha-methylmorphinan-6-one
  • 4,5-Epoxy-3-hydroxy-17-methylmorphinan-6-one
  • 4,5alpha-Epoxy-3-hydroxy-17-methyl-6-morphinanone
  • 6-Deoxy-7,8-dihydro-6-oxomorphine
  • 7,8-Dihydromorphinone
  • Dihydromorfinon
  • Dihydromorphinone
  • Dimorphone
  • Hidromorfona
  • Hydromorfona
  • Hydromorphone
  • Hydromorphonum
  • Idromorfone
Thuốc giảm đau có opioid
Thuốc Gốc
Small Molecule
CAS: 466-99-9
ATC: N02AA03
ĐG : Abbott Laboratories Ltd. , http://www.abbott.com
CTHH: C17H19NO3
PTK: 285.3377
An opioid analgesic derived from morphine and used mainly as an analgesic. It has a shorter duration of action and is more potent than morphine. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H19NO3
Phân tử khối
285.3377
Monoisotopic mass
285.136493479
InChI
InChI=1S/C17H19NO3/c1-18-7-6-17-10-3-5-13(20)16(17)21-15-12(19)4-2-9(14(15)17)8-11(10)18/h2,4,10-11,16,19H,3,5-8H2,1H3/t10-,11+,16-,17-/m0/s1
InChI Key
InChIKey=WVLOADHCBXTIJK-YNHQPCIGSA-N
IUPAC Name
(1S,5R,13R,17R)-10-hydroxy-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
hydromorphone
SMILES
[H][C@@]12OC3=C(O)C=CC4=C3[C@@]11CCN(C)[C@]([H])(C4)[C@]1([H])CCC2=O
Độ tan chảy
266.5 °C
Độ hòa tan
4.39e+00 g/l
logP
0.9
logS
-1.8
pKa (strongest acidic)
10.11
pKa (Strongest Basic)
8.59
PSA
49.77 Å2
Refractivity
78.26 m3·mol-1
Polarizability
30.02 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Hydromorphone is a hydrogenated ketone derivative of morphine that acts as a narcotic analgesic. It has a shorter duration of action than morphine. Hydromorphone is approximately 8 times more potent on a milligram basis than morphine. In addition, hydromorphone is better absorbed orally than is morphine. In clinical settings, Hydromorphone exerts its principal pharmacological effect on the central nervous system and gastrointestinal tract. Its primary actions of therapeutic value are analgesia and sedation. Hydromorphone appears to increase the patient's tolerance for pain and to decrease discomfort, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Opioids also produce respiratory depression by direct action on brain stem respiratory centers.
Cơ Chế Tác Dụng : An opioid analgesic derived from morphine and used mainly as an analgesic. It has a shorter duration of action and is more potent than morphine. [PubChem] Hydromorphone is a narcotic analgesic; its principal therapeutic effect is relief of pain. Hydromorphone interacts predominantly with the opioid mu-receptors. 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. In clinical settings, Hydromorphone exerts its principal pharmacological effect on the central nervous system and gastrointestinal tract. Hydromorphone also binds with kappa-receptors which are thought to mediate spinal analgesia, miosis and sedation.
Dược Động Học :
▧ Absorption :
Better absorbed orally than morphine
▧ Protein binding :
20%
▧ Metabolism :
Primarily hepatic. After absorption hydromorphone is metabolized by the liver to the glucuronide conjugate which is then excreted in the urine. Hydromorphone is metabolized to the major metabolites hydromorphone-3-glucuronide, hydromorphone-3-glucoside and dihydroisomorphine-6-glucuronide.
▧ Route of Elimination :
Only a small amount of the hydromorphone dose is excreted unchanged in the urine. Most of the dose is excreted as hydromorphone-3-glucuronide along with minor amounts of 6-hydroxy reduction metabolites.
▧ Half Life :
2.6 hours (oral); 18.6 hours for sustained release Palladone
▧ Clearance :
* 1.96 L/min
Độc Tính : Hydromorphone is a schedule II narcotic which can lead to physical dependence or addiction. High doses lead to respiratory depression, nausea, and vomiting. Overdoses lead to extreme somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, and sometimes bradycardia and hypotension. In severe overdosage, apnea, circulatory collapse, cardiac arrest and death may occur.
Chỉ Định : For the relief of moderate to severe pain such as that due to surgery, cancer, trauma/injury, or burns.
Tương Tác Thuốc :
  • Alvimopan Increases levels by receptor binding competition. Discontinue opioid administration at least 7 days prior to administrating Alvimopan.
  • Eltrombopag Increases levels of Hydromorphone via metabolism decrease. UDP-glucuronosyltransferase inhibition with unclear significance.
  • Triprolidine The CNS depressants, Triprolidine and Hydromorphone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Capsule, extended release - Oral
Liquid - Intramuscular
Liquid - Intravenous
Liquid - Oral
Powder, for solution - Intravenous
Solution - Intravenous
Suppository - Rectal
Syrup - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Dilaudid
  • Công ty :
    Sản phẩm biệt dược : EXALGO
  • Công ty :
    Sản phẩm biệt dược : Palladone
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00327
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5284570
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508700
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07042
ChemSpider
http://www.chemspider.com/Chemical-Structure.4447624.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0527-1353-01
PharmGKB
http://www.pharmgkb.org/drug/PA449918
Wikipedia
http://en.wikipedia.org/wiki/Hydromorphone
RxList
http://www.rxlist.com/cgi/generic/hydromorphone.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/dil1137.shtml
Drugs.com
http://www.drugs.com/cdi/hydromorphone.html
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