琥珀酸氯霉素和氯霉素的临床药物动力学。
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安布罗斯PJ
琥珀酸氯霉素和氯霉素的临床药物动力学。
May-Jun Pharmacokinet。1984; 9 (3): 222 - 38。doi: 10.2165 / 00003088-198409030-00004。
- PubMed ID
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6375931 (在PubMed]
- 文摘
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近年来已经有更新对氯霉素的兴趣,主要因为ampicillin-resistant出现的流感嗜血杆菌,婴儿和儿童的细菌性脑膜炎的主要原因。三种制剂的氯霉素在临床实践:最常用的口服的结晶粉末,棕榈酸酯口服作为悬架,和琥珀酸酯注射用。酯都是不活跃的,要求水解氯霉素的抗菌活性。棕榈酸酯水解在小肠吸收之前主动氯霉素。琥珀酸氯霉素作为前体药物,转化为积极的氯霉素虽然在体内循环。各种化验开发确定氯霉素在生物液体的浓度。其中,高效液相色谱和radioenzymatic化验是准确的,精确、具体,且有良好的氯霉素敏感性。它们是快速和对氯霉素治疗药物监测实用。口服生物利用度的水晶氯霉素和氯霉素棕榈酸酯为80%左右。血浆浓度峰值的时间依赖于粒子的大小和与体外溶解和deaggregation率。 The bioavailability of chloramphenicol after intravenous administration of the succinate ester averages approximately 70%, but the range is quite variable. Incomplete bioavailability is the result of renal excretion of unchanged chloramphenicol succinate prior to it being hydrolysed to active chloramphenicol. Plasma protein binding of chloramphenicol is approximately 60% in healthy adults. The drug is extensively distributed to many tissues and body fluids, including cerebrospinal fluid and breast milk, and it crosses the placenta. Reported mean values for the apparent volume of distribution range from 0.6 to 1.0 L/kg. Most of a chloramphenicol dose is metabolised by the liver to inactive products, the chief metabolite being a glucuronide conjugate; only 5 to 15% of chloramphenicol is excreted unchanged in the urine. The elimination half-life is approximately 4 hours. Inaccurate determinations of the pharmacokinetic parameters may result by incorrectly assuming rapid and complete hydrolysis of chloramphenicol succinate. The pharmacokinetics of chloramphenicol succinate have been described by a 2-compartment model. The reported values for the apparent volume of distribution range from 0.2 to 3.1 L/kg.(ABSTRACT TRUNCATED AT 400 WORDS)
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- 药物
- 药物反应
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反应 细节
