Rau R
Z Rheumatol. 1986 Nov-Dec;45(6):283-95.
The therapeutic effect of low-dose MTX-treatment (10-25 mg/week) in active rheumatoid arthritis can be demonstrated by an improvement in clinical and laboratory parameters of disease activity already after 4-6 weeks. The mode of action is not fully understood. Direct anti-inflammatory effects seem to be more important than the weak immunosuppressive properties. Methotrexate treatment is indicated in all very active cases of rheumatoid arthritis, which do not respond to, or do not tolerate, conventional slow-acting antirheumatic drugs. In severe, rapidly progressing diseases MTX can be given without waiting for the effect of other disease modifying drugs. MTX is administered once a week i.v., i.m. or in one oral dose before breakfast. Absorption is reduced by food. The initial weekly dose is 15-25 mg and can be reduced to a minimum of 10 mg (7.5 mg) according to the clinical effect. A combination with antimalarials or gold salts is possible. The prescription of MTX is contraindicated in cases of renal function disturbances, active liver disease, bone marrow disturbances, active infectious diseases, pregnancy and excessive alcohol consumption. The most common side-effects are nausea and vomiting, stomatitis, transient elevations of transaminases. Rare conditions are leucopenia, thrombocytopenia and lung infiltrations. The side-effects are dose-related and disappear with dose reduction. They can be avoided by administering leucovorin 12 hours after giving MTX. Before starting the treatment total blood count with differential count and platelet count, serum creatinine and liver enzymes should be done. These laboratory studies have to be repeated every week for the first month, every two weeks up to the third month and every 1-2 months thereafter. When contraindications are considered and regular controls are made methotrexate is better tolerated than other cytotoxic agents. The rate of withdrawals is lower than with gold-treatment. In low-dose MTX-treatment drug interactions do not play a major role with normal renal function. Concomitant application of nonsteroidal antirheumatic drugs can delay MTX elimination and increase toxicity. We therefore avoid giving these drugs on the day of MTX-administration as far as possible.
小剂量甲氨蝶呤（MTX）治疗（10 - 25毫克/周）对活动性类风湿关节炎的疗效，在4 - 6周后即可通过疾病活动度的临床和实验室参数改善得到证实。其作用方式尚未完全明确。直接抗炎作用似乎比微弱的免疫抑制特性更为重要。甲氨蝶呤治疗适用于所有对传统慢作用抗风湿药物无反应或不耐受的活动性类风湿关节炎病例。在严重、快速进展的疾病中，无需等待其他改善病情药物起效即可给予MTX。MTX每周静脉注射、肌肉注射一次，或早餐前口服一次。食物会降低其吸收。初始每周剂量为15 - 25毫克，可根据临床效果减至最低10毫克（7.5毫克）。可与抗疟药或金盐联合使用。肾功能障碍、活动性肝病、骨髓功能障碍、活动性传染病、妊娠及过量饮酒患者禁用MTX。最常见的副作用是恶心、呕吐、口腔炎、转氨酶短暂升高。罕见情况有白细胞减少、血小板减少和肺部浸润。副作用与剂量相关，减量后可消失。在给予MTX 12小时后给予亚叶酸钙可避免副作用。开始治疗前应进行全血细胞计数及分类计数、血小板计数、血清肌酐和肝酶检查。第一个月每周重复这些实验室检查，第三个月前每两周重复一次，此后每1 - 2个月重复一次。当考虑到禁忌证并进行定期监测时，甲氨蝶呤的耐受性优于其他细胞毒性药物。停药率低于金制剂治疗。在小剂量MTX治疗中，肾功能正常时药物相互作用不起主要作用。非甾体类抗风湿药物的联合应用可延迟MTX清除并增加毒性。因此，我们尽可能避免在给予MTX当天使用这些药物。
