Topotecan lacks third space sequestration.

摘要: The objective of this study was to determine the influence of pleural and ascitic fluid on pharmacokinetics antitumor camptothecin derivative topotecan. Four patients with histological proof malignant solid tumor received topotecan (0.45 or 1.5 mg/m 2 ) p.o. on several occasions in both presence absence third space volumes. Serial plasma fluid samples were collected during each dosing analyzed by high-performance liquid chromatography for intact lactone form its ring-opened carboxylate form. apparent clearance demonstrated substantial interpatient variability but remained unchanged within same patient [110 ± 55.6 liters/h/m (mean SD eight courses)] absence of [118 31.1 liters/h/m (mean seven courses)]. Similarly, terminal half-lives and area under concentration-time curve ratios lactone:total drug were similar between courses patient. Topotecan penetration into demonstrated a mean lag time 1.61 h (range, 1.37–1.86 h), with plasma concentration increased after all patients. The mean ratio space total drug the concentration-time that 0.55 (range, 0.26–0.87). These data indicate can be safely administered effusions ascites that there is these spaces, which may prove beneficial local effects.