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药品详细

Morphine(吗啡)

化学结构式图
中文名
吗啡
英文名
Morphine
分子式
C17H19NO3
化学名
(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
分子量
Average: 285.3377
Monoisotopic: 285.136493479
CAS号
57-27-2
ATC分类
G04B 未知;N02A 未知;N02A 未知;N02A 未知;N04B 未知;R05D 未知;R05D 未知;S01X 其他眼科用药;D10A Anti-Acne Preparations for Topical Use
药物类型
small molecule
阶段
approved
商品名
Apokyn;Astramorph PF;Avinza;Depodur;Dulcontin;Duramorph PF;Duromorph;Epimorph;Kadian;l-Morphine;M-Eslon;M.O.S;Meconium;Morfina;Morphia;Morphine Extra-Forte;Morphine Forte;Morphine H.P;Morphinism;Morphitec;Morphium;Moscontin;Ms Contin;MS/L;MS/S;MSIR;Nepenthe;OMS Concentrate;Oramorph SR;Ospalivina;Rescudose;RMS Uniserts;Roxanol;Roxanol 100;Roxanol UD;Statex;Statex Drops;
同义名
(-)-Heroin hydrochloride;(-)-Morphine;D-(-)-Morphine;Diacetylmorphine hydrochloride;Diamorphine hydrochloride;Heroin hydrochloride;Heroine hydrochloride;Morphin;Morphina;Morphine Sulfate;Morphinum;O,O'-Diacetylmorphine hydrochloride;
基本介绍

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]

生产厂家
  • Actavis
  • Actavis elizabeth llc
  • App pharmaceuticals llc
  • Baxter healthcare corp anesthesia and critical care
  • Clonmel healthcare ltd
  • Ekr therapeutics inc
  • Endo pharmaceuticals inc
  • Hospira inc
  • King pharmaceuticals inc
  • Kv pharmaceutical co
  • Mallinckrodt chemical inc
  • Mallinckrodt inc
  • Meridian medical technologies inc
  • Purdue pharma lp
  • Roxane laboratories inc
  • Watson laboratories inc
  • Xanodyne pharmaceutics inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Kilpatrick GJ, Smith TW: Morphine-6-glucuronide: actions and mechanisms. Med Res Rev. 2005 Sep;25(5):521-44. Pubmed
  2. Loguinov AV, Anderson LM, Crosby GJ, Yukhananov RY: Gene expression following acute morphine administration. Physiol Genomics. 2001 Aug 28;6(3):169-81. Pubmed
剂型
Form Route Strength
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
规格
Unit description Cost Unit
Depodur 15 mg/1.5 ml vial 618.18 USD ml
Roxanol 20 mg/ml Solution 120ml Bottle 95.98 USD bottle
Morphine Sulfate 20 mg/5ml Solution 500ml Bottle 65.05 USD bottle
Apokyn 30 mg/3 ml cartridge 52.48 USD ml
Morphine Sulfate 10 mg/5ml Solution 500ml Bottle 38.55 USD bottle
Kadian er 200 mg capsule 35.43 USD capsule
Kadian er 100 mg capsule 23.01 USD capsule
Roxanol 20 mg/ml Solution 30ml Bottle 22.99 USD bottle
Morphine Sulfate 10 mg/5ml Solution 100ml Bottle 21.99 USD bottle
Oramorph sr 60 mg tablet 21.76 USD tablet
Ms contin 200 mg tablet 21.5 USD tablet
Kadian er 80 mg capsule 18.66 USD capsule
Roxanol 20 mg/ml Solution 240ml Bottle 17.99 USD bottle
Avinza 90 mg capsule 17.56 USD capsule
Oramorph sr 100 mg tablet 17.16 USD tablet
Kadian 100 mg 24 Hour Capsule 16.93 USD capsule
MS Contin 200 mg 12 Hour tablet 16.32 USD tablet
Kadian 100 mg capsule sr 16.25 USD capsule
Kadian er 60 mg capsule 14.31 USD capsule
AVINza 90 mg 24 Hour Capsule 13.21 USD capsule
Kadian 80 mg capsule sr 12.96 USD capsule
Avinza 120 mg capsule 12.07 USD capsule
Kadian er 50 mg capsule 11.76 USD capsule
Ms contin 100 mg tablet 11.75 USD tablet
Avinza 60 mg capsule 11.58 USD capsule
AVINza 120 mg 24 Hour Capsule 11.33 USD capsule
Avinza 75 mg capsule 10.79 USD capsule
Morphine sulfate powder 10.61 USD g
Avinza 45 mg capsule 10.22 USD capsule
Kadian 60 mg 24 Hour Capsule 9.06 USD capsule
Morphine Sulfate CR 200 mg 12 Hour tablet 8.97 USD tablet
MS Contin 100 mg 12 Hour tablet 8.89 USD tablet
Morphine sulf 30 mg suppository 8.44 USD suppository
AVINza 60 mg 24 Hour Capsule 8.36 USD capsule
Ms contin 60 mg tablet 7.95 USD tablet
Infumorph 10 mg/ml ampul p-f 7.8 USD ml
Kadian 50 mg 24 Hour Capsule 7.71 USD capsule
Kadian er 30 mg capsule 7.13 USD capsule
Oramorph sr 30 mg tablet 6.83 USD tablet
Morphine sulf 20 mg suppository 6.71 USD suppository
Kadian er 10 mg capsule 6.35 USD capsule
Morphine sulf 10 mg suppository 6.25 USD suppository
Avinza 30 mg capsule 6.0 USD capsule
MS Contin 60 mg 12 Hour tablet 5.71 USD tablet
Kadian er 20 mg capsule 5.69 USD capsule
Ms Contin 200 mg Sustained-Release Tablet 5.62 USD tablet
Kadian 30 mg 24 Hour Capsule 4.8 USD capsule
Kadian 20 mg 24 Hour Capsule 4.76 USD capsule
AVINza 30 mg 24 Hour Capsule 4.47 USD capsule
Morphine sulf 5 mg suppository 4.45 USD suppository
Morphine Sulfate CR 100 mg 12 Hour tablet 4.33 USD tablet
M-Eslon 200 mg Extended-Release Capsule 4.3 USD capsule
Oramorph sr 15 mg tablet 4.12 USD tablet
Ms contin cr 30 mg tablet 4.09 USD tablet
Kadian 10 mg capsule sr 4.05 USD capsule
Morphine Hp 50 50 mg/ml 4.01 USD ml
Kadian 10 mg 24 Hour Capsule 4.0 USD capsule
Ms contin 15 mg tablet 3.58 USD tablet
MS Contin 30 mg 12 Hour tablet 3.26 USD tablet
Novo-Morphine Sr 200 mg Sustained-Release Tablet 3.09 USD tablet
Pms-Morphine Sulfate Sr 200 mg Sustained-Release Tablet 3.09 USD tablet
Ms Contin 100 mg Sustained-Release Tablet 3.02 USD tablet
Morphine Sulfate CR 60 mg 12 Hour tablet 3.0 USD tablet
Morphine Hp 25 25 mg/ml 2.9 USD ml
Statex 30 mg Suppository 2.55 USD suppository
Kadian 100 mg Sustained-Release Capsule 2.35 USD capsule
Statex 20 mg Suppository 2.32 USD suppository
Morphine Lp Epidural 1 mg/ml 2.24 USD ml
M-Eslon 100 mg Extended-Release Capsule 2.15 USD capsule
MS Contin 15 mg 12 Hour tablet 2.13 USD tablet
Ms Contin 60 mg Sustained-Release Tablet 1.98 USD tablet
Statex 10 mg Suppository 1.95 USD suppository
Morph sulf 5 mg/0.25 ml vial 1.83 USD vial
Statex 5 mg Suppository 1.75 USD suppository
Novo-Morphine Sr 100 mg Sustained-Release Tablet 1.66 USD tablet
Pms-Morphine Sulfate Sr 100 mg Sustained-Release Tablet 1.66 USD tablet
Morphine Sulfate CR 30 mg 12 Hour tablet 1.63 USD tablet
Morphine 8 mg/ml ampule 1.56 USD ml
Kadian 50 mg Sustained-Release Capsule 1.35 USD capsule
Duramorph 0.5 mg/ml ampul 1.31 USD ml
Astramorph-pf 1 mg/ml ampul 1.15 USD ml
Ms Contin 30 mg Sustained-Release Tablet 1.13 USD tablet
Morphine Lp Epidural 0.5 mg/ml 1.12 USD ml
Morphine Sulfate 15 mg/ml 1.03 USD ml
Morphine Sulfate 10 mg/ml 1.02 USD ml
Novo-Morphine Sr 60 mg Sustained-Release Tablet 1.01 USD tablet
Pms-Morphine Sulfate Sr 60 mg Sustained-Release Tablet 1.01 USD tablet
Ratio-Morphine Sulfate Sr 60 mg Sustained-Release Tablet 1.01 USD tablet
M-Eslon 60 mg Extended-Release Capsule 1.0 USD capsule
Statex 50 mg/ml Drops 0.99 USD ml
Morphine Sulfate CR 15 mg 12 Hour tablet 0.93 USD tablet
Duramorph 1 mg/ml ampul 0.91 USD ml
M.O.S.-Sr 60 mg Sustained-Release Tablet 0.89 USD tablet
Morphine 50 mg/25 ml-d5w syr 0.86 USD ml
Morphine-ns 10 mg/ml syringe 0.86 USD ml
Morphine-ns 5 mg/ml syringe 0.8 USD ml
Ms Contin 15 mg Sustained-Release Tablet 0.75 USD tablet
Morphine 5 mg/ml vial 0.74 USD ml
Kadian 20 mg Sustained-Release Capsule 0.73 USD capsule
Astramorph-pf 0.5 mg/ml amp 0.72 USD ml
Morphine Sulfate 15 mg tablet 0.65 USD tablet
Morphine Sulfate 30 mg tablet 0.65 USD tablet
Morphine 1 mg/ml vial p-f 0.6 USD ml
Morphine-ns 1 mg/ml syringe 0.58 USD ml
Novo-Morphine Sr 30 mg Sustained-Release Tablet 0.57 USD tablet
Pms-Morphine Sulfate Sr 30 mg Sustained-Release Tablet 0.57 USD tablet
Ratio-Morphine Sulfate Sr 30 mg Sustained-Release Tablet 0.57 USD tablet
M-Eslon 30 mg Extended-Release Capsule 0.56 USD capsule
Morphine 0.5 mg/ml vial 0.55 USD ml
Morphine sulfate 50 mg/ml vial 0.55 USD ml
Morphine sulfate ir 30 mg tablet 0.55 USD tablet
Ratio-Morphine 20 mg/ml Syrup 0.55 USD syrup
Statex 20 mg/ml Drops 0.52 USD ml
M.O.S.-Sr 30 mg Sustained-Release Tablet 0.51 USD tablet
Morphine 1 mg/ml syringe 0.48 USD ml
Morphine 10 mg/ml vial 0.48 USD ml
Ms.Ir 30 mg Tablet 0.48 USD tablet
Morphine sulfate 25 mg/ml vial 0.43 USD ml
Morphine sulf 1 mg/ml vial 0.4 USD ml
M.O.S. Sulfate 50 mg Tablet 0.39 USD tablet
Statex 50 mg Tablet 0.39 USD tablet
Kadian 10 mg Sustained-Release Capsule 0.38 USD capsule
M-Eslon 15 mg Extended-Release Capsule 0.38 USD capsule
Ms.Ir 20 mg Tablet 0.38 USD tablet
Novo-Morphine Sr 15 mg Sustained-Release Tablet 0.37 USD tablet
Pms-Morphine Sulfate Sr 15 mg Sustained-Release Tablet 0.37 USD tablet
Ratio-Morphine Sulfate Sr 15 mg Sustained-Release Tablet 0.37 USD tablet
M-Eslon 10 mg Extended-Release Capsule 0.33 USD capsule
Morphine sulfate ir 15 mg tablet 0.32 USD tablet
Morphine 15 mg/ml vial 0.3 USD ml
Morphine-ns 25 mg/25 ml syr 0.26 USD ml
M.O.S. Sulfate 25 mg Tablet 0.25 USD tablet
Statex 25 mg Tablet 0.25 USD tablet
Ms.Ir 10 mg Tablet 0.21 USD tablet
Ratio-Morphine 10 mg/ml Syrup 0.19 USD syrup
M.O.S. Sulfate 10 mg Tablet 0.19 USD tablet
Statex 10 mg Tablet 0.19 USD tablet
Morphine-ns 5 mg/ml 0.16 USD ml
Morphine-ns 55 mg/55 ml syr 0.14 USD ml
Ms.Ir 5 mg Tablet 0.14 USD tablet
M.O.S. Sulfate 5 mg Tablet 0.12 USD tablet
Statex 5 mg Tablet 0.12 USD tablet
Morphine 1 mg/ml-d5w 100 ml 0.1 USD ml
Morphine-ns 150 mg/150 ml 0.1 USD ml
Statex 5 mg/ml Syrup 0.08 USD ml
Morphine 1 mg/ml-d5w 250 ml 0.06 USD ml
Ratio-Morphine 5 mg/ml Syrup 0.05 USD syrup
Ratio-Morphine 1 mg/ml Syrup 0.02 USD syrup
Statex 1 mg/ml Syrup 0.02 USD ml
化合物类型
Type small molecule
Classes
  • Morphine and Derivatives
Substructures
  • Morphinans
  • Benzofurans
  • Hydroxy Compounds
  • Alkanes and Alkenes
  • Naphthalenes
  • Phenols and Derivatives
  • Morphine and Derivatives
  • Ethers
  • Benzene and Derivatives
  • Phenylpiperidines
  • Methoxyphenols
  • Aliphatic and Aryl Amines
  • Catechols
  • Phenethylamines
  • Heterocyclic compounds
  • Aromatic compounds
  • Anisoles
  • Phenylpropylamines
  • Alcohols and Polyols
  • Cyclohexenes and Derivatives
  • Phenyl Esters
  • Amphetamines
  • Catecholamines and Derivatives
  • Piperidines
适应症
PARKINSON 帕金森氏症;
药理
Indication For the relief and treatment of severe pain.
Pharmacodynamics 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.
Mechanism of action 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.
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]
Toxicity 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.
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00405 Codeine Pathway SMP00405
Smp00406 Morphine Pathway SMP00406
Smp00407 Heroin Pathway SMP00407
理化性质
Properties
State solid
Melting point 255oC (sulfate salt)
Experimental Properties
Property Value Source
water solubility 149 mg/L (60 mg/mL for sulfate salt) PhysProp
logP 0.8 PhysProp
logS -3.28 [ADME Research, USCD] PhysProp
pKa 8.21 Various sources
Predicted Properties
Property Value Source
water solubility 1.02e+01 g/l ALOGPS
logP 0.99 ALOGPS
logP 0.9 ChemAxon Molconvert
logS -1.4 ALOGPS
pKa 13.78 ChemAxon Molconvert
hydrogen acceptor count 4 ChemAxon Molconvert
hydrogen donor count 2 ChemAxon Molconvert
polar surface area 52.93 ChemAxon Molconvert
rotatable bond count 0 ChemAxon Molconvert
refractivity 80.12 ChemAxon Molconvert
polarizability 29.95 ChemAxon Molconvert
药物相互作用
Drug Interaction
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.
Rifampin Rifampin decreases the effect of morphine/codeine
食物相互作用
  • Avoid alcohol.
  • Take with food.
  • To avoid constipation: increase your daily intake of fiber (beans, whole grains, vegetables).

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