Perlík F, Pucelíková T, Slanar O
Oddĕlení klinické farmakologie a I. interní klinika 1. LF UK a VFN, Praha.
Cas Lek Cesk. 2001 Feb 1;140(2):51-3.
Caffeine elimination and monitoring of its metabolites after a single peroral administration in used to evaluate liver metabolic function. The aim of the study was to use the paraxanthine/caffeine ratio in saliva to evaluate liver function in patients with liver cirrhosis. Results were correlated with various procedures evaluating the elimination rate of caffeine.
The study group consisted of 7 patients with compensated liver cirrhosis and 10 healthy volunteers, all individuals were given a single 280 mg dose of caffeine perorally. Concentration of salivary caffeine was determined in each person with high performance liquid chromatography after 4, 6, 8 and 12 hours after application. The paraxanthine/caffeine ratio was evaluated at the 6-hour interval. Estimated clearance (CL), half-life (t1/2) and volume of distribution (Vd) were calculated from 2 or 4 concentrations of the drug. The metabolic ratio of the patients (x = 0.15 +/- 0.07) was significantly lower then the control group (x = 0.55 +/- 0.29). Using a four-point procedure we acquired the following values: patients--CL 2.39 +/- 2.36 l/h, t1/2 = 90.18 +/- 168.44 h; healthy volunteers--CL = 8.10 +/- 4.58 l/h, t1/2 = 8.60 +/- 4.12 h (p < 0.05). Statistically significant correlation was found between the metabolic ratio and CL value (rs = 0.83) or between half-life (rs = -0.72). Similar results were also obtained using the two-point method.
In patients with liver cirrhosis we found significantly lower paraxanthine/caffeine ratio which correlates with lowered elimination of caffeine. Its evaluation enables non-invasive assessment of liver metabolic function from a single sample of saliva.
单次口服咖啡因后其消除及代谢物监测用于评估肝脏代谢功能。本研究旨在利用唾液中副黄嘌呤/咖啡因比值评估肝硬化患者的肝功能。结果与评估咖啡因消除率的各种方法相关。
研究组包括7例代偿期肝硬化患者和10名健康志愿者,所有个体均口服280mg单剂量咖啡因。给药后4、6、8和12小时,用高效液相色谱法测定每个人唾液中咖啡因的浓度。每6小时间隔评估副黄嘌呤/咖啡因比值。根据药物的2个或4个浓度计算估计清除率(CL)、半衰期(t1/2)和分布容积(Vd)。患者的代谢比值(x = 0.15±0.07)显著低于对照组(x = 0.55±0.29)。采用四点法我们获得以下值:患者——CL 2.39±2.36l/h,t1/2 = 90.18±168.44h;健康志愿者——CL = 8.10±4.58l/h,t1/2 = 8.60±4.12h(p < 0.05)。代谢比值与CL值(rs = 0.83)或半衰期(rs = -0.72)之间存在统计学显著相关性。采用两点法也获得了类似结果。
在肝硬化患者中,我们发现副黄嘌呤/咖啡因比值显著降低,这与咖啡因消除降低相关。对其进行评估能够从单一唾液样本对肝脏代谢功能进行无创评估。