OBJECTIVES: The objective was to evaluate the safety and tolerability of bisoprolol compared to atenolol in patients with essential mild to moderate hypertension. METHODS:  Studies were retrieved from Embase, Pubmed, and Cochrane databases using relevant search strategies. Randomised controlled trials which compared bisoprolol with atenolol were included according to pre-specified inclusion/exclusion criteria. The outcomes of interest were total withdrawals from study, withdrawals due to adverse events (AE), withdrawals due to lack of efficacy, any adverse events, bradycardia, fatigue, oedema and vertigo. Two reviewers independently extracted data from the included studies. Data was meta-analysed using RevMan (5). RESULTS:  Of the 1056 studies identified, 11 studies met the inclusion criteria. In total, 624 patients were randomised to bisoprolol, and 683 were randomised to atenolol. Seven of the included studies were double-blind, three were single-blind and one was open-label study. The Jadad score of eight studies was ≥3 and were of good quality. The study duration of included studies ranged from 8-weeks to 52-weeks.  Results of meta-analysis showed that with bisoprolol there was lower risk of study withdrawals [RR: 0.95 (0.79, 1.16)] and withdrawals due to lack of efficacy [RR: 0.58 (0.14, 2.37)] as compared to atenolol. Withdrawals due to AE were more in the bisoprolol group compared to atenolol. The risk of AE (any) was lower with atenolol compared to atenolol [RR: 0.94 (0.73, 1.21)]. The risk of bradycardia was higher with bisoprolol compared to atenolol (p=0.3). Lower risk of oedema (p=0.3) and vertigo (p=0.6) was reported with bisoprolol as compared to atenolol. CONCLUSIONS:  This review has included the evidence to date with regards to safety and tolerability of bisoprolol compared to atenolol. This review concludes that availability of bisoprolol provides the patients with a safe and efficacious first-line therapy option in hypertension.