We compared the effects of melatonin, an antioxidant and sleep inducer in humans, and rilmazafone hydrochloride, a hypnotic, in elderly patients with nocturia. Patients received either melatonin (2 mg/day; n = 20) or rilmazafone (2 mg/day; n = 22) for 4 weeks. There were no significant differences in the mean age, the quality of life (QoL) score and the serum melatonin levels between the two groups at baseline. After 4 weeks' treatment, the number of nocturnal urinations was significantly decreased and the QoL score was significantly improved in both groups. There was no significant difference between the patient-reported effectiveness ratings between the two groups. The serum melatonin level was significantly increased in the melatonin-treated group, but it remained unchanged in the rilmazafone-treated group. Melatonin and rilmazafone were equally effective for nocturia in the elderly. We recommend that the problems of sleep disturbance should be considered when choosing a therapy for nocturia.