Objective To assess the efficacy and safety of levoamlodipine besylate for essential hypertension. Methods We searched MEDLINE (1999 to October 2007), EMBASE (1999 to October 2007), The Cochrane Library (Issue 3, 2007), CNKI (1999 to 2007), Wanfang (1999 to 2007), VIP (1999 to 2007) and CBM (1999 to October 2007). The quality of included studies was critically evaluated. Data analyses were performed with The Cochrane Collaboration’ s RevMan 4.2 software. Results A total of 345 articles were retrieved, but only 17 were finally included. Meta-analyses showed that the effective rate in patients receiving levoamlodipine besylate was significantly higher than that in patients receiving indapamide (RD 0.14, 95%CI 0.06 to 0.22, P=0.0004), while no significant differences were noted between the levoamlodipine besylate group and other control groups. The incidence of adverse effects was significantly lower in the levoamlodipine besylate group compared to the indapamide group (RD –0.12, 95%CI –0.21 to –0.03, P=0.01), the amlodipine group (RD –0.06, 95%CI –0.11 to –0.01, P=0.02) and the nitrendipine group (RD –0.27, 95%CI –0.46 to –?0.08, P=0.006). No significant differences were observed between the levoamlodipine besylate group and other control groups. Conclusion Levoamlodipine besylate tends to have better efficacy and safety profiles compared with other antihypertensive drugs. However, most trials included in the review were of poor quality and, so, multi-center large-scale randomized controlled trials of higher quality are needed to confirm this.