临床药物动力学的吗啡。

文章的细节

引用

复制到剪贴板

眩光PA,沃尔什道明

临床药物动力学的吗啡。

其他药物Monit。1991年1月,13 (1):1。

PubMed ID

2057987 (在PubMed

]

文摘

吗啡(M)是世界卫生组织推荐的是严重癌症疼痛的治疗选择。发展敏感的放射免疫检定法(RIA)和高效液相色谱法在过去的20年中,使得药物动力学的研究,仍不完全理解。RIA派生的数据必须被小心由于anti-sera大代谢物,损伤检测特异性。M的药物动力学已经确定了各种临床情况,但有大interpatient可变性对大多数参数。M是容易吸收的所有航线管理,除了皮肤,可以注射沿着脊骨。等离子体峰值水平达到15 - 20分钟内肌内和皮下政府和口服后30 - 90分钟内。口服后峰值水平远低于肠外路线后,口服米以来经历了广泛的肝脏中初步的新陈代谢。重复管理,oral-parenteral相对效价比是1:3 M可以实施硬膜外或鞘内,也被放在intracerebroventricularly。硬膜外M进入蛛网膜下腔,但也吸收进入体循环。只有5%的剂量穿过硬脑膜。 M administered in the lumbar region is quickly redistributed in the cerebrospinal fluid in a rostral direction, explaining the high incidence of systemic side effects following spinal administration. After absorption, M is rapidly and widely distributed and crosses the blood-brain barrier. With therapeutic doses, plasma protein binding is only 20-35%, and the volume of distribution is 1-6 L/kg. The primary site of M metabolism is the liver, and the dose should be reduced in patients with liver disease. Glucuronidation is the main metabolic pathway, but the principal metabolite, morphine-3-glucuronide (M3G), is inactive. Morphine-6-glucuronide (M6G) is produced in smaller amounts than M3G, but is pharmacologically active and many times more potent than M. The ratio of M6G to M in plasma, after a dose of M, is approximately 10:1, and the ratio does not change with increasing doses or prolonged treatment. Normorphine (NM) is also active, and is formed to a greater extent after oral administration; it is not, however, usually found in plasma. NM may be neurotoxic. M and its metabolites are excreted by the kidney, but urinary free M accounts for less than 10% of an administered dose. In patients with renal insufficiency, the metabolites accumulate, though M itself is still excreted.(ABSTRACT TRUNCATED AT 400 WORDS)

beplay体育安全吗DrugBank数据引用了这篇文章

药物

吗啡