Influence of rifampicin treatment on antipyrine clearance and metabolite formation in patients with tuberculosis.

Influence of rifampicin treatment on antipyrine clearance and metabolite formation in patients with tuberculosis.
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利福平治疗对结核病患者安替比林清除率和代谢物形成的影响。

DOI:
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发表时间:
1984
影响因子:
3.4
通讯作者:
D. Breimer
D. Breimer
中科院分区:
医学3区
文献类型:
--
作者:
M. Teunissen;W. Bakker;J. E. Meerburg;D. Breimer

文献摘要

被引文献

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研究了7例(18-79岁)结核患者(同时接受异烟肼和吡嗪酰胺治疗)8天利福平(每日600 mg)治疗对安替比林血浆清除率和代谢物形成的影响。所有患者经利福平治疗后,安替比林的消除半衰期由12.9 +/- 5.0缩短至8.8 +/- 2.0 h (P < 0.05)。安替比林清除率由2.2 +/- 0.9升/小时增加至2.9 +/- 0.7升/小时(P < 0.05),而表观分布容积无变化。安替比林清除率的增加主要是由于诺替比林的形成率选择性地增加了80%,从6.9 +/- 3.4 ml/min增加到12.4 +/- 3.4 ml/min。利福平似乎优先诱导参与安替比林到去甲基化的细胞色素P-450(异)酶(s)。安替比林代谢的其他途径几乎不受影响。这为细胞色素P-450系统的不同同工酶参与人体安替比林代谢提供了进一步证据。
The influence of an 8-day therapy with rifampicin (600 mg daily) was studied on antipyrine plasma clearance and metabolite formation in seven patients with tuberculosis (age 18-79 years), who were also treated with isoniazid and pyrazinamide. After rifampicin treatment the elimination half-life of antipyrine had decreased in all patients from 12.9 +/- 5.0 to 8.8 +/- 2.0 h (P less than 0.05). Antipyrine clearance had increased from 2.2 +/- 0.9 to 2.9 +/- 0.7 l/h (P less than 0.05), while no change in apparent volume of distribution was observed. The increase in antipyrine clearance was primarily due to a selective increase in the rate of formation of norantipyrine by 80% from 6.9 +/- 3.4 to 12.4 +/- 3.4 ml/min. Rifampicin seems to induce preferentially the cytochrome P-450 (iso-) enzyme(s) involved in the demethylation of antipyrine to norantipyrine. Other pathways of antipyrine metabolism were hardly affected. This provides further evidence for the involvement of different iso-enzymes of the cytochrome P-450 system in antipyrine metabolism in man.