Sinnett M J, Groff G D, Raddatz D A, Franck W A, Bertino J S
Department of Pharmacy Services, Mary Imogene Bassen Hospital, Cooperstown, NY 13326.
J Rheumatol. 1989 Jun;16(6):745-8.
Few studies have evaluated the pharmacokinetics of low dose oral methotrexate (MTX) therapy. MTX pharmacokinetics were studied in 10 patients with classic rheumatoid arthritis (RA) after a single 7.5 mg oral dose. MTX was rapidly absorbed. Peak concentrations varied considerably, ranging from 0.31-0.72 microM. Measurable drug concentration was found in all patients at 24 h after the dose. CL/F-MTX = 145 +/- 52 ml/min/1.73 m2 and elimination half-life was 4.5 +/- 0.89 h. Oral MTX given as a single weekly dose has predictable pharmacokinetics. Further studies to examine what relationship exists, if any, with efficacy and toxicity of MTX in RA must be undertaken.
很少有研究评估低剂量口服甲氨蝶呤（MTX）治疗的药代动力学。对10例典型类风湿关节炎（RA）患者单次口服7.5 mg剂量后MTX的药代动力学进行了研究。MTX吸收迅速。峰值浓度差异很大，范围为0.31-0.72微摩尔。给药后24小时在所有患者中均检测到可测量的药物浓度。CL/F-MTX = 145±52毫升/分钟/1.73平方米，消除半衰期为4.5±0.89小时。每周单次口服MTX具有可预测的药代动力学。必须进行进一步研究以检查MTX在RA中的疗效和毒性之间是否存在任何关系。
