Bianchi Gerolamo, Caporali Roberto, Todoerti Monica, Mattana Paolo
Division of Rheumatology, ASL3 Genovese, Genoa, Italy.
Division of Rheumatology, IRCCS San Matteo, University of Pavia, Pavia, Italy.
Adv Ther. 2016 Mar;33(3):369-78. doi: 10.1007/s12325-016-0295-8. Epub 2016 Feb 4.
Methotrexate (MTX) is still considered the drug of choice in rheumatoid arthritis (RA) management. Comparing subcutaneous (MTX SC) and oral (MTX OR) routes of administration is important to optimize the everyday therapeutic strategy in the real-life setting. This review summarizes scientific evidence currently available on this topic. As shown by pharmacokinetic studies, at the same dose level, bioavailability of MTX SC is significantly higher and less variable than that of MTX OR. This difference is even more pronounced for medium-to-high dosages (i.e., >15 mg/week). With regard to clinical response (Disease Activity Score-28, American College of Rheumatology Criteria), randomized, double-blind studies and retrospective or longitudinal analyses in real-life settings showed that MTX SC is more effective than MTX OR. This is true both in MTX-naive patients with early RA, and in patients who switch from MTX OR to MTX SC due to previous treatment failure, lack of efficacy and/or adverse events. Finally, MTX SC has a better tolerability profile than MTX OR, with fewer gastroenterological side effects. Delaying the use of more expensive biological therapies by switching from MTX OR to MTX SC in non-responders might provide cost savings, with relevant implications in the management of patients with RA.
Alfa Wassermann.
甲氨蝶呤（MTX）仍是类风湿关节炎（RA）治疗的首选药物。比较皮下注射（MTX SC）和口服（MTX OR）给药途径对于优化现实生活中的日常治疗策略很重要。本综述总结了目前关于该主题的科学证据。药代动力学研究表明，在相同剂量水平下，MTX SC的生物利用度显著高于MTX OR，且变异性更小。这种差异在中高剂量（即>15毫克/周）时更为明显。关于临床反应（疾病活动评分-28，美国风湿病学会标准），随机双盲研究以及现实生活中的回顾性或纵向分析表明，MTX SC比MTX OR更有效。这在初治的早期RA患者以及因先前治疗失败、缺乏疗效和/或不良事件而从MTX OR转换为MTX SC的患者中均成立。最后，MTX SC的耐受性优于MTX OR，胃肠道副作用更少。对于无反应者，从MTX OR转换为MTX SC可延迟使用更昂贵的生物疗法，从而节省成本，这对RA患者的管理具有重要意义。
阿尔法·瓦塞尔曼公司。
