Objective To assess the effectiveness and safety of salbutamol in the treatment of preterm labor. Methods We searched MEDLINE (1966-Jan. 2007), EMBASE (1966-Jan. 2007), Cochrane Central Register of Controlled Trials (Issue 4, 2006), CBMdisc (1978-Jan. 2007) and CNKI (1979-Jan. 2007). Randomized controlled trials (RCTs) or quasi-randomized controlled trials (quasi-RCT) involving salbutamol for preterm labor were collected. The quality of the retrieved trials was assessed using the Jadad Scale. Meta-analyses were conducted with The Cochrane Collaboration’s RevMan 4.2 software. Results A total of 19 RCTs and quasi-RCTs were included, of which 16 were published in Chinese and 3 in English. The quality of the 16 Chinese studies was low, scored less than 3 by the Jadad Scale. None of the 16 RCTs mentioned the method of randomization, allocation concealment, double-blinding or the long-term effect. The quality of the 3 English studies was high. Compared with basic treatment, salbutamol was more effective in prolonging pregnancy over 48 hours (RR=6.30, 95%CI 3.23 to 14.32), and preventing neonatal asphyxia (RR=0.44, 95%CI 0.33 to 0.59), but the incidence of adverse events in pregnant women was higher in the salbutamol group (RR=4.57, 95%CI 1.34 to 15.54). Salbutamol was as effective as magnesium sulfate in prolonging pregnancy over 48 hours (OR=1.60, 95%CI 0.92 to 2.76), but more effective in preventing neonatal asphyxia (OR=0.29, 95%CI 0.14 to 0.61). Salbutamol was similar to atosiban in terms of prolonging pregnancy over 48 hours (OR=1.18, 95%CI 0.42 to 3.37) and preventing neonatal asphyxia (OR=1.13, 95%CI 0.30 to 4.31). Conclusion Salbutamol is effective in prolonging pregnancy over 48 hours and preventing neonatal asphyxia, but may cause more adverse events in pregnant women. Salbutamol has similar effects to other commonly-used drugs in regard to prolonging pregnancy over 48 hours, but is better than magnesium sulfate in decreasing the incidence of neonatal asphyxia. Salbutamol may lead to more adverse events compared with atosiban, but fewer adverse events than magnesium sulfate.