Objective To investigate the effect of penehyclidime hydrochloride as the preanesthetic medication for general anesthesia, and also to provide evidence for clinical practice. Methods We searched The Cochrane library (2007, Issue 3), MEDLINE (1966 to 2007), EMBASE (1988 to 2007), CBM (1978 to 2007), VIP (1989 to 2007) and CNKI (1994 to 2007). Randomised trials comparing penehyclidime hydrochloride with other drugs were collected. Quality assessment and data extraction were performed. Results A total of 23 trials were included, and the quality of all studies was low. Among them, 11 trials compared penehyclidime hydrochloride with atropine, of which only 2 measured the airway secretion volume and indicated that the airway secretion volume was smaller in the penehyclidime hydrochloride group than that in the atropine group (WMD –8.00, 95%CI –8.16 to –7.85, Plt;0.000 01). Twelve trials compared penehyclidime hydrochloride with scopolamine, of which only 2 measured the airway secretion volume and revealed no significant difference between the two groups (WMD –17.07, 95%CI –45.49 to 11.35, P=0.24). Three trials compared penehyclidime hydrochloride with placebo, which showed that the airway secretion volume was smaller in the penehyclidime hydrochloride group than that in the placebo group (WMD –10.60, 95%CI –13.64 to –7.56, Plt;0.000 01). No significant adverse drug reactions were found. Conclusion Current evidence suggested that penehyclidime hydrochloride was not inferior to other drugs in decreasing airway secretion and keeping heart rate stable.