Objectives To assess the efficacy and safety of misoprostol for intrauterine insemination (IUI). Methods The Cochrane Library, EMbase, MEDLINE, SCIENCE Direct Database, CBM, Wangfang Data and CNKI were searched for collecting randomized controlled trials or controlled clinical trials published before October, 2009. Statistical analysis was performed with RevMan 5.0 software. Results Five Randomized controlled trials (RCTs) were included according to the inclusion and exclusion criteria at last. Five RCTs involving 546 participants and 1 133 cycles are included. Meta-analysis showed that, compared with placebo group, 400 μg misoprostol could increase pregnancy rate of IUI (RR=1.95, 95%CI 1.19 to 3.19); compared with 200 μg misoprostol group, 400 μg misoprostol also has higher incidence rate of abdominal pain (RR=3.13, 95%CI 1.86 to 5.26) and vaginal bleeding (RR=5.25, 95%CI 2.08 to 13.21). Conclusions Because of the limited studies, recommendation of using misoprostol in IUI cycles is not fully convinced, which has to be further proved by more randomized controlled trials in large sample with high quality.