The pharmacokinetics of oral itraconazole in AIDS patients
The pharmacokinetics of oral itraconazole in AIDS patients
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艾滋病患者口服伊曲康唑的药代动力学
DOI：
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发表时间：
1992
期刊：
影响因子：
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通讯作者：
B. Gazzard
中科院分区：
文献类型：
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作者：
D. Smith;V. Velde;R. Woestenborghs;B. Gazzard
翻译后摘要-为了测试的假设，口服伊曲康唑的吸收可能会减少患者的获得性免疫缺陷综合征（AIDS），8例艾滋病患者给予两个100毫克的伊曲康唑胶囊15天。在摄入后的前8小时，然后在第1、8和15天的24、48、72和96小时，每小时通过HPLC测量血浆水平。约4 h后出现血浆峰水平。第8天和第15天的平均血浆峰浓度分别为446 ± 196和530 ± 214 ng mL−1。第1、8和15天的24 h曲线下面积（AUC 0 -24）分别为2105 ± 1241、7679 ± 3838和8748 ± 4385 ng mL−1 h。给药1周后达到稳态。无肝毒性证据，1例患者因皮疹停用伊曲康唑。可以得出结论，与正常志愿者相比，艾滋病患者口服伊曲康唑胶囊的吸收减少了约50%。艾滋病患者可能需要比非艾滋病患者更高剂量的伊曲康唑，以达到相当的血浆水平。
Abstract— To test the hypothesis that absorption of orally administered itraconazole may be reduced in patients with the Acquired Immunodeficiency Syndrome (AIDS), 8 patients with AIDS were given two 100 mg capsules of itraconazole for 15 days. Plasma levels were measured by HPLC hourly for the first 8 h following ingestion, then at 24, 48, 72 and 96 h on days 1, 8 and 15. Peak plasma levels occurred after approximately 4 h. Mean peak plasma concentrations were 446 ± 196 and 530 ± 214 ng mL−1 at days 8 and 15. The area under the curve over 24 h (AUC0–24) was 2105 ± 1241, 7679 ± 3838 and 8748 ± 4385 ng mL−1 h for days 1, 8 and 15, respectively. Steady‐state was achieved after one week of dosing. There was no evidence of hepatotoxicity and one patient stopped itraconazole due to a rash. It may be concluded that the absorption of oral itraconazole capsules is reduced in AIDS patients, by a factor of approximately 50%, when compared with normal volunteers. AIDS patients may require higher doses of itraconazole than used in non‐AIDS patients to achieve comparable plasma levels.
影响因子：
158.5
作者：
KLEIN, RS;HARRIS, CA;FRIEDLAND, GH
通讯作者：
FRIEDLAND, GH