5-甲氧基补骨脂素对银屑病患者咖啡因代谢的抑制作用。
Inhibition of caffeine metabolism by 5-methoxypsoralen in patients with psoriasis.
作者信息
Bendriss E K, Bechtel Y, Bendriss A, Humbert P H, Paintaud G, Magnette J, Agache P, Bechtel P R
机构信息
Department of Clinical Pharmacology, Besançon University Hospital, France.
出版信息
Br J Clin Pharmacol. 1996 May;41(5):421-4. doi: 10.1046/j.1365-2125.1996.33311.x.
Eight patients with psoriasis were given 200 mg caffeine orally with or without 1.2 mg kg-1 of 5-methoxypsoralen. Blood and urine samples were collected over a 2-day period. During 5-methoxypsoralen coadministration, the apparent volume of distribution of caffeine remained unchanged, but oral clearance (CLp.o.) decreased from 9.5 +/- 3.8 (mean +/- s.d.) to 3.2 +/- 0.51 h-1 (P < 0.01). The area under the plasma concentration-time curve (AUC) increased from 24 +/- 9 to 73 +/- 29 mg 1(-1) h (P < 0.001). This decrease in CLp.o. with increased AUC was consistent with a CYP1A2-dependent inhibition of caffeine N-demethylation which was further supported by significant decreases in the (AFMU+1U+1X)/17U and (AFMU+1U+1X)/17X urinary metabolic ratios.
八名银屑病患者口服200毫克咖啡因，同时或不同时服用1.2毫克/千克的5-甲氧基补骨脂素。在两天时间内采集血液和尿液样本。在与5-甲氧基补骨脂素共同给药期间，咖啡因的表观分布容积保持不变，但口服清除率（CLp.o.）从9.5±3.8（平均值±标准差）降至3.2±0.51 h-1（P<0.01）。血浆浓度-时间曲线下面积（AUC）从24±9增加到73±29毫克·1(-1)·小时（P<0.001）。CLp.o.的降低与AUC的增加与细胞色素P450 1A2依赖性咖啡因N-去甲基化抑制作用一致，尿代谢比值（AFMU+1U+1X）/17U和（AFMU+1U+1X）/17X的显著降低进一步支持了这一点。
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