Purpose Drug effects can be unpredictable during cardiac surgery due to factors that may influence drug concentration, such as extracorporeal oxygenation and hemodilution. The primary aim of the current investigation was to determine whether plasma gabapentin concentration is altered by cardiopulmonary bypass (CPB). Methods Following approval from the Research Ethics Board and written informed consent, we conducted this open-label prospective cohort investigation. A convenience sample of 16 patients, who were scheduled for coronary bypass surgery, received oral gabapentin 600 mg as follows: 90 min prior to induction of anesthesia, following tracheal extubation, and then every eight hours for a total of four doses. Plasma gabapentin concentration, as well as pain and sedation scores, were documented. Results Plasma gabapentin concentrations were unaltered during CPB (31.9 ± 12.7 lmolÁL -1 prior to CPB, 35.6 ± 12.9 to 37.2 ± 9.6 lmolÁL -1 during CPB). However, using the current protocol, drug accumulation (reflected by increased drug concentrations) was observed following the third (58.2 ± 19.5 lmolÁL -1 ) and the fourth (71.9 ± 34.3 lmolÁL -1 ) doses. Pain and sedation scores and opioid requirements were comparable with those found in other studies. Conclusion Plasma gabapentin concentration is unaltered during CPB following preoperative administration.