PHARMACOKINETICS OF METHOTREXATE IN ERYTHROCYTES IN PSORIASIS
PHARMACOKINETICS OF METHOTREXATE IN ERYTHROCYTES IN PSORIASIS
复制标题
DOI：
10.1007/bf00556900
复制
发表时间：
1984-01-01
影响因子：
2.9
通讯作者：
NYFORS, A
中科院分区：
文献类型：
--
作者：
HENDEL, J;NYFORS, A
对25例长期接受甲氨蝶呤治疗的顽固性银屑病患者的红细胞内叶酸和甲氨蝶呤水平进行了测定。红细胞中甲氨蝶呤的平均稳态浓度为85 nmol/l，红细胞中叶酸的平均浓度为729 nmol/l。这些参数之间没有观察到线性相关，但在红细胞叶酸浓度范围最低的细胞中发现了最大的甲氨蝶呤积累。在5例开始接受甲氨蝶呤治疗的患者中，随访了6个月以上的甲氨蝶呤和叶酸的红细胞浓度。甲氨蝶呤在第一次给药后3-4天在红细胞中呈浓度梯度积累。甲氨蝶呤浓度稳定升高，4 ~ 6周后达到稳态水平。在6个月的观察期内，保持稳态水平。红细胞叶酸浓度在此期间没有变化。显然，循环红细胞内甲氨蝶呤聚谷氨酸的合成是这些细胞中甲氨蝶呤积累的主要原因。
The intraerythrocytic levels of folate and methotrexate were measured in 25 patients on long-term methotrexate therapy for recalcitrant psoriasis. The mean steady state concentration of methotrexate in erythrocytes was 85 nmol/l and the mean erythrocyte folate concentration was 729 nmol/l. A linear correlation was not observed between these parameters, but the greatest methotrexate accumulation was found in cells at the lowest end of the erythrocyte folate concentration range. In 5 patients started on methotrexate therapy the erythrocyte concentrations of methotrexate and folate were followed over 6 mo. Methotrexate had accumulated against a concentration gradient in the erythrocytes 3-4 days after the 1st dose. The methotrexate concentration increased steadily until the steady state level was reached after 4-6 wk. The steady state level was maintained during the 6 mo. observation period. The erythrocyte folate concentration did not change during this period. Evidently methotrexate polyglutamate synthesis within the circulating erythrocyte is a major cause of methotrexate accumulation in these cells.