Ittel T H, Legler U F, Polak A, Glöckner W M, Sieberth H G
Chemotherapy. 1987;33(2):77-84. doi: 10.1159/000238478.
The pharmacokinetic disposition of 5-fluorocytosine (5-FC) was studied in 7 patients with acute renal failure undergoing continuous hemofiltration (CH). CH was performed with a high-flux membrane and the average filtration rate (FR) was 16.3 ml/min. Following an intravenous loading dose of 2,500 mg, 5-FC concentrations were measured in plasma and ultrafiltrate. The half-lives of 5-FC were markedly prolonged in all patients, ranging from 15.9 to 37.2 h and longer half-lives corresponded to lower FR. The clearance of 5-FC averaged 97.5% of the FR. Within 48 h, 29-35% of the administered dose was recovered in the ultrafiltrate of 3 patients. The volume of distribution ranged from 0.772 to 0.982 l/kg. We found a linear relationship between the elimination rate constant and the FR, and based on these data, a dosage schedule is proposed regarding the use of 5-FC in patients treated with CH.
对7例接受持续血液滤过(CH)的急性肾衰竭患者进行了5-氟胞嘧啶(5-FC)的药代动力学研究。采用高通量膜进行CH,平均滤过率(FR)为16.3 ml/min。静脉注射负荷剂量2500 mg后,测定血浆和超滤液中的5-FC浓度。所有患者的5-FC半衰期均显著延长,范围为15.9至37.2小时,半衰期越长,FR越低。5-FC的清除率平均为FR的97.5%。在48小时内,3例患者的超滤液中回收了29%-35%的给药剂量。分布容积为0.772至0.982 l/kg。我们发现消除速率常数与FR之间存在线性关系,并基于这些数据提出了关于CH治疗患者使用5-FC的给药方案。