拉贝洛尔的临床药物动力学。

文章的细节

引用

复制到剪贴板

麦克尼尔JJ,路易WJ

拉贝洛尔的临床药物动力学。

Pharmacokinet。1984; 3 - 4月9日(2):157 - 67。doi: 10.2165 / 00003088-198409020-00003。

PubMed ID

6370541 (在PubMed

]

文摘

拉贝洛尔是第一个一类新的抗高血压药物与α-和beta-adrenoceptor阻塞属性出现在同一个分子。其功效已经被双盲研究证实所有等级的治疗高血压和心绞痛。药物的剂量相关的副作用主要是体位低血压。拉贝洛尔的临床配方由相同比例的4个光学异构体。其中一个(RR异构体)可能是负责药品的beta-adrenoceptor封锁,另一个(SR异构体)产生大部分alpha-blockade。大多数目前药代动力学信息关于拉贝洛尔从研究利用荧光的测定,但这最近取代更具体的高压液相色谱(HPLC)程序。拉贝洛尔口服后迅速吸收血浆浓度峰值一般是在2小时内完成。的生物利用度在不同的学科从10%到80%不等。平均生物利用度被报道与随着年龄的增长,价值约30%在30 - 40年的年龄,大约65%在80年。也有证据表明,生物利用度增加适度当药物与食物。 About 50% of the drug is bound in the plasma. The apparent volume of distribution at equilibrium varies from approximately 200 to over 800L, suggesting that concentration of labetalol occurs in extravascular sites. Radiochemical analysis in animals has shown high levels of accumulation in the lung, liver and kidney with little present in brain tissue. This is in keeping with the relatively low lipid solubility of labetalol. The half-life of labetalol in plasma is 3 to 3.5 hours. The drug is eliminated mainly by hepatic metabolism with the production of several biologically inactive glucuronides which in turn are excreted in the urine and bile. Approximately 85% of labetalol in the blood is removed during a single passage through the liver; thus, like propranolol, labetalol's clearance is probably flow dependent (i.e. it is sensitive to alterations in hepatic blood flow). Small doses of the drug (i.e. 300mg daily) have been shown to reduce antipyrine clearance by approximately 15%, and further studies are necessary to determine whether high doses produce a greater, possibly clinically significant, inhibition of mixed-function oxidase activity. After both single doses and during long term treatment the plasma concentration-time profile of labetalol shows marked variation between different individuals.(ABSTRACT TRUNCATED AT 400 WORDS)

beplay体育安全吗DrugBank数据引用了这篇文章

药物

拉贝洛尔