中国临床药学杂志

目的探讨中、小剂量甲氨蝶呤(MTX)肌内注射治疗异位妊娠的药动学及临床疗效、不良反应。方法选择因早期异位妊娠住院患者40例,随机分为2组,均采用MTX保守治疗。A组:50 mg.m-2单次肌注,B组:0.4 mg.kg-1.d-1连续5 d肌注。采用荧光偏振免疫分析法测定用药后MTX血清浓度,比较2组药动学参数、疗效和不良反应。结果A组MTX达峰浓度为2.66×10-6mol.L-1,维持血药浓度在10-6mol.L-1水平6 h,10-8~10-7mol.L-1水平42 h;B组达峰浓度0.99×10-6mol.L-1,维持10-8~10-7mol.L-1水平5 d。2组平均cmax比较P<0.01。A、B组治疗有效率分别为80%和90%。结论MTX治疗异位妊娠疗效好、安全,治疗有效血药浓度在10-8~10-7mol.L-1水平,单次肌注具有疗程短、依从性好的特点。

AIM To explore the pharmacokinetics of intramuscular methotrexate(MTX)with low-medium doses in treatment of ectopic pregnancy and its adverse drug reaction.METHODS Forty cases of early ectopic pregnancy were divided into 2 groups with MTX intramuscular therapy.A single dose of MTX 50 mg·m^-2,im,in group A and MTX(0.4 mg·)kg^-1·d^-1,im,for 5 d in group B were given respectively.The blood MTX concentration was determined and the results of 2 groups were compared.RESULTS The peak concentration of MTX in group A can reach 2.66×10^-6mol·L^-1 and maintain at 10^-6mol·L^-1 for 6 h and 10^-8-10^-7mol·L^-1 for 42 h.The peak concentration of MTX in group B can reach(0.99)×10^-6mol·L^-1 and maintain at 10^-8-10^-7mol·L^-1 for 5 d.The average c_max between 2 groups showed significantly statistical difference(P<0.01).The effective rates of group A and B were 80% and 90% respectively.CONCLUSION MTX is an effective and safe drug in treatment of ectopic pregnancy and its effective concentration is 10^-8-10^-7mol·L^-1.The advantage of single dose of MTX is its shorter course of treatment and compliance.