| Summary: | Selective ß<sub>2</sub>-agonists have been imputed as potential cause of <span style="font-variant: small-caps;">l</span>-hyperlactatemia since the 1970s. To document the prevalence of hyperlactatemia associated with selective ß<sub>2</sub>-agonists and to investigate the predisposing factors, we searched for published articles until April 2019 pertaining to the interplay of administration of selective ß<sub>2</sub>-agonists and circulating <span style="font-variant: small-caps;">l</span>-lactic acid in the Excerpta Medica, Web of Science, and the U.S. National Library of Medicine databases. Out of the 1834 initially retrieved records, 56 articles were included: 42 papers reporting individual cases, 2 observational studies, and 12 clinical trials. Forty-seven individual patients receiving a selective ß<sub>2</sub>-agonist were found to have <span style="font-variant: small-caps;">l</span>-lactatemia ≥5.0 mmol/L, which decreased by ≥3.0 mmol/L or to ≤2.5 mmol/L after discontinuing (N = 24), reducing (N = 17) or without modifying the dosage of the selective ß<sub>2</sub>-agonist (N = 6). Clinical trials found that <span style="font-variant: small-caps;">l</span>-lactic acid significantly increased in healthy volunteers administered a ß<sub>2</sub>-agonist. <span style="font-variant: small-caps;">l</span>-lactatemia ≥5.0 mmol/L was observed in 103 (24%) out of 426 patients with asthma or preterm labor managed with a selective ß<sub>2</sub>-agonist and was more common in patients with asthma (30%) than in premature labor (5.9%). A significant relationship was also noted between <span style="font-variant: small-caps;">l</span>-lactate level and intravenous albuterol dose or its circulating level. In conclusion, relevant <span style="font-variant: small-caps;">l</span>-hyperlactatemia is common on high dose treatment with a selective ß<sub>2</sub>-agonist.
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