Department of Clinical Pharmacy, St Antonius Hospital, Nieuwegein, the Netherlands.
Clin Pharmacokinet. 2010 Apr;49(4):269-75. doi: 10.2165/11319350-000000000-00000.
For propofol clearance, allometric scaling has been applied successfully for extrapolations between species (rats and humans) and within the human bodyweight range (children and adults). In this analysis, the human bodyweight range is explored to determine for which range an allometric model with a fixed or estimated exponent can be used to predict propofol clearance, without correction for maturation. The predictive value of the allometric equation, clearance (CL) is equal to 0.071 x bodyweight in kg0.78, which was developed from rats, children and adults, and the predictive value of a fixed exponent allometric model derived from the basal metabolic rate, CL is equal to CL standardized to a 70 kg adult x (bodyweight in kg standardized to a 70 kg adult)0.75, were evaluated across five independent patient groups including (i) 25 (pre)term neonates with a postmenstrual age of 27-43 weeks; (ii) 22 postoperative infants aged 4-18 months; (iii) 12 toddlers aged 1-3 years; (iv) 14 adolescents aged 10-20 years; and (v) 26 critically ill adults sedated long term. The median percentage error of the predictions was calculated using the equation %error = (CL(allometric) - CL(i))/CL(i) x 100, where CL(allometric) is the predicted propofol clearance from the allometric equations for each individual and CL(i) is the individual-predicted (post hoc) propofol clearance value derived from published population pharmacokinetic models. In neonates, the allometric model developed from rats, children and adults, and the fixed-exponent allometric model, systematically overpredicted individual propofol clearance, with median percentage errors of 288% and 216%, respectively, whereas in infants, both models systematically underpredicted individual propofol clearance, with median percentage errors of -43% and -55%, respectively. In toddlers, adolescents and adults, both models performed reasonably well, with median percentage errors of -12% and -32%, respectively, in toddlers, 16% and -14%, respectively, in adolescents, and 12% and -18%, respectively, in adults. Both allometric models based on bodyweight alone may be of use to predict propofol clearance in individuals older than 2 years. Approaches that also incorporate maturation are required to predict clearance under the age of 2 years.
对于丙泊酚清除率,已成功应用了种间(大鼠和人类)和人体体重范围内(儿童和成人)的比例缩放法进行外推。在本分析中,探索了人体体重范围,以确定对于哪种范围,可以使用具有固定或估计指数的比例模型来预测丙泊酚清除率,而无需进行成熟度校正。从大鼠、儿童和成人中开发的丙泊酚清除率的比例方程预测值为 CL 等于 0.071 x 体重(kg)0.78,以及从基础代谢率推导出来的固定指数比例模型的预测值 CL 标准化至 70kg 成人 x(体重标准化至 70kg 成人)0.75,在包括以下五个独立患者组的研究中进行了评估:(i)胎龄 27-43 周的 25 例(早产)新生儿;(ii)4-18 个月的 22 例术后婴儿;(iii)1-3 岁的 12 例幼儿;(iv)10-20 岁的 14 例青少年;和(v)长期镇静的 26 例危重症成人。使用方程 %error = (CL(allometric) - CL(i))/CL(i) x 100 计算预测的中位数百分比误差,其中 CL(allometric) 是每个个体的比例方程预测的丙泊酚清除率,而 CL(i) 是从已发表的群体药代动力学模型中推导出的个体预测(事后)丙泊酚清除率值。在新生儿中,源自大鼠、儿童和成人的比例模型和固定指数比例模型系统地高估了个体丙泊酚清除率,中位数百分比误差分别为 288%和 216%,而在婴儿中,两个模型系统地低估了个体丙泊酚清除率,中位数百分比误差分别为-43%和-55%。在幼儿、青少年和成年人中,两个模型的表现都相当不错,幼儿的中位数百分比误差分别为-12%和-32%,青少年的中位数百分比误差分别为 16%和-14%,成年人的中位数百分比误差分别为 12%和-18%。仅基于体重的两个比例模型都可用于预测 2 岁以上个体的丙泊酚清除率。需要采用也包含成熟度的方法来预测 2 岁以下个体的清除率。