Owing to marked fluctuations in plasma concentrations, circadian CNS toxicity (maximum in the early afternoon) occurred in a 69-year-old female patient being treated with an instant-release formulation of carbamazepine (CBZ). The neurologic syndrome was reversible after administration of the same daily dose as sustained-release formulation. This case illustrates the importance of correct timing of blood sampling to detect drug-induced toxicity and of use of sustained-release formulations in antiepileptic therapy with CBZ.