Prentice A G, Warnock D W, Johnson S A, Phillips M J, Oliver D A
Department of Haematology, Derriford Hospital, Plymouth, UK.
J Antimicrob Chemother. 1994 Aug;34(2):247-52. doi: 10.1093/jac/34.2.247.
The pharmacokinetics of itraconazole oral solution were measured in seven patients receiving chemotherapy followed by autologous bone marrow transplantation for leukaemia or lymphoma. Patients received 5 mg/kg/day itraconazole either as a once or twice daily dose. Drug concentrations reached steady state by day 15, in both groups. The mean pre-dose itraconazole serum concentration at hour 0, day 8 was 385 ng/mL in the od group and 394 ng/mL in the bd group, rising to 762 and 845 ng/mL by day 15, respectively. The mean AUCs for 0-24 h on day 8, 15 and 22 were 17,310 and 13,302 ng/mL/h, 24,476 and 25,154 and 22,621 and 21,423, for the od and bd groups, respectively. Thus serum concentrations of itraconazole suitable for antifungal prophylaxis can be attained in neutropenic patients, with the administration of an oral solution in a dosage of 5 mg/kg as either an od or bd schedule, following pre-autograft high-dose cytotoxic chemotherapy.
在7例接受化疗后进行自体骨髓移植治疗白血病或淋巴瘤的患者中,测定了伊曲康唑口服溶液的药代动力学。患者接受5mg/kg/天的伊曲康唑,每日一次或两次给药。两组患者在第15天时药物浓度均达到稳态。第8天0小时时,od组伊曲康唑血清预给药浓度均值为385ng/mL,bd组为394ng/mL,到第15天时分别升至762和845ng/mL。od组和bd组在第8天、15天和22天0-24小时的平均AUC分别为17310和13302ng/mL/h、24476和25154、22621和21423。因此,在自体移植前大剂量细胞毒性化疗后,以5mg/kg的剂量每日一次或两次口服伊曲康唑溶液,可使中性粒细胞减少患者达到适合抗真菌预防的血清浓度。