It has been reported that losartan, an angiotensin II receptor blocker, alters the circadian rhythm of melatonin secretion and significantly reduces melatonin production. However, this finding has been confirmed at the animal experiment level only, and there are no reports of studies in humans. Therefore, we performed this study to confirm the reproducibility of the aforementioned findings of animal experiments in humans. Ten male subjects who were in good general health and free from any medical condition were recruited for this study. After a preliminary observation period of 7 days, the subjects received oral losartan treatment, 50 mg daily for 7 days. Blood samplings for measurement of the plasma melatonin concentrations were performed on day 7 of the preliminary observation period and day 7 of the losartan treatment period. The circadian rhythm of melatonin secretion after the 7-day treatment with losartan showed no significant difference from that recorded before the losartan administration. The significant decrease of the home blood pressure was observed on the afternoons. The blood samples showed significant decrease of the serum sodium and uric acid levels, along with a significant increase of the serum potassium level. The pharmacological actions of losartan at the ordinarily used clinical dose level were confirmed in humans, however, no significant inhibitory effect of the drug on melatonin secretion could be confirmed. These results are expected to be useful for guiding the proper use of angiotensin II receptor blockers.