Tìm theo
Morphine
Các tên gọi khác (12 ) :
  • (-)-Morphine
  • (−)-morphine
  • (5alpha,6alpha)-17-Methyl-7,8-didehydro-4,5-epoxymorphinan-3,6-diol
  • (5alpha,6alpha)-Didehydro-4,5-epoxy-17-methylmorphinan-3,6-diol
  • (5R,6S,9R,13S,14R)-4,5-Epoxy-N-methyl-7-morphinen-3,6-diol
  • (7R,7AS,12bs)-3-methyl-2,3,4,4a,7,7a-hexahydro-1H-4,12-methano[1]benzofuro[3,2-e]isoquinoline-7,9-diol
  • Morfina
  • Morphia
  • Morphin
  • Morphine
  • Morphinum
  • Morphium
Thuốc giảm đau, hạ sốt, chống viêm không steroid, điều trị Gút và các bệnh xương khớp
Thuốc Gốc
Small Molecule
CAS: 57-27-2
ATC: G04BE07, N02AA01, N02AA04, N04BC07, R05DA01, R05DA05, S01XA06, D10AX30
ĐG : Actavis Group , http://www.actavis.com
CTHH: C17H19NO3
PTK: 285.3377
The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
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/h2-5,10-11,13,16,19-20H,6-8H2,1H3/t10-,11+,13-,16-,17-/m0/s1
InChI Key
InChIKey=BQJCRHHNABKAKU-KBQPJGBKSA-N
IUPAC Name
(1S,5R,13R,14S,17R)-4-methyl-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10,15-tetraene-10,14-diol
Traditional IUPAC Name
morphine
SMILES
[H][[email protected]@]12OC3=C(O)C=CC4=C3[[email protected]@]11CCN(C)[[email protected]]([H])(C4)[[email protected]]1([H])C=C[[email protected]@H]2O
Độ tan chảy
255 °C
Độ hòa tan
149 mg/L (at 20 °C)
logP
0.89
logS
-3.28
pKa (strongest acidic)
10.26
pKa (Strongest Basic)
9.12
PSA
52.93 Å2
Refractivity
80.12 m3·mol-1
Polarizability
29.95 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.21 (at 25 °C)
Dược Lực Học : Morphine is a narcotic pain management agent indicated for the relief of pain in patients who require opioid analgesics for more than a few days. Morphine 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. In clinical settings, morphine exerts its principal pharmacological effect on the central nervous system and gastrointestinal tract. Its primary actions of therapeutic value are analgesia and sedation. Morphine 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 : The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle. [PubChem] The precise mechanism of the analgesic action of morphine is unknown. However, specific CNS opiate receptors have been identified and likely play a role in the expression of analgesic effects. Morphine first acts on the mu-opioid receptors. 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. It has been shown that morphine binds to and inhibits GABA inhibitory interneurons. These interneurons normally inhibit the descending pain inhibition pathway. So, without the inhibitory signals, pain modulation can proceed downstream.
Dược Động Học :
▧ Absorption :
Bioavailability is approximately 30%.
▧ Volume of Distribution :
* 1 to 6 L/kg
▧ Protein binding :
30-40%
▧ Metabolism :
Primarily hepatic (90%), converted to dihydromorphinone and normorphine. Also converted to morphine-3-glucuronide (M3G) and morphine-6-glucuronide. Virtually all morphine is converted to glucuronide metabolites; only a small fraction (less than 5%) of absorbed morphine is demethylated.
▧ Route of Elimination :
A small amount of glucuronide conjugates are excreted in bile, with minor enterohepatic recycling. Seven to 10% of administered morphine sulfate is excreted in the feces.
▧ Half Life :
2-4 hours
▧ Clearance :
* 20 – 30 mL/min/kg [Adult] * 1852 +/- 116 mL/min [Chinese] * 1495 +/- 80 mL/min [Caucasian]
Độc Tính : LD50 = 461 mg/kg (rat, oral), 600 mg/kg (mouse, oral). Human lethal dose by ingestion is 120-250 mg of morphine sulfate. Symptoms of overdose include cold, clammy skin, flaccid muscles, fluid in the lungs, lowered blood pressure, "pinpoint" or dilated pupils, sleepiness leading to stupor and coma, slowed breathing, and slow pulse rate.
Chỉ Định : For the relief and treatment of severe pain.
Tương Tác Thuốc :
  • Alvimopan Increases levels by receptor binding competition. Discontinue opioid administration at least 7 days prior to administrating Alvimopan.
  • Eltrombopag Eltrombopag increases Morphine levels via decreasing metabolism. UDP-glucuronosyltransferase inhibition with unclear significance.
  • Rifampicin Rifampin decreases the effect of morphine/codeine
  • Triprolidine The CNS depressants, Triprolidine and Morphine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Trovafloxacin Morphine may reduce serum levels of Trovafloxacin decreasing the efficacy of the antibiotic. IV doses of morphine should be administered at least 2 hours after a dose of Trovafloxacin given in a fasting state or 4 hours after if given in a fed state.
Liều Lượng & Cách Dùng : Capsule, extended release - Oral
Liquid - Intramuscular
Liquid - Intravenous
Soap - Topical
Solution - Epidural
Solution - Intramuscular
Solution - Intravenous
Solution / drops - Oral
Suppository - Rectal
Syrup - Oral
Tablet - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Avinza
  • Công ty :
    Sản phẩm biệt dược : Duramorph
  • Công ty :
    Sản phẩm biệt dược : Kadian
  • Công ty :
    Sản phẩm biệt dược : Kapanol
  • Công ty :
    Sản phẩm biệt dược : MS Contin
  • Công ty :
    Sản phẩm biệt dược : MSIR
  • Công ty :
    Sản phẩm biệt dược : Oramorph
  • Công ty :
    Sản phẩm biệt dược : Roxanol
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