A phase 1 study of N-696, a new .BETA.-adrenoceptor blocking agent.

概要

論文の詳細を見る
A phase 1 study of N-696, a new β-adrenoceptor blocking agent, was performed in normal healthy volunteers to define its pharmacological characteristics and safety. Following a single oral administration of 10 and 20 mg of N-696 after a meal (n=4 for each), both Cmax and AUC0-24 were twice as high in the group receiving 20 mg as in the group receiving 10 mg. However, Tmax was 3.0 hours in the 10-mg group and 4.3 hours in the 20-mg group with no statistically significant difference between groups. Also, Te1/2was as much as 12 hours, and urinary recovery of N-696 during 48 hours was 48% on both dosage regimens. Following a repeated oral administration of 20 mg of N-696 for 14 days (n=6), plasma concentration reached its plateau in 3 days and remained stable during rest of the study. The effects on hemodynamics appeared in 2-3 days. There was a 15.7% decrease in heart rate, a 9. 4% decrease in systolic blood pressure, a 11.4% decrease in diastolic blood pressure, and a 23.0% decrease in double products. The AUC0-∞ on the 1st day coincided well with the AUC0-24 on the 14th day, indicating no accumulation of N-696 in the body during the study. Neither adverse effects nor significantly abnormal changes in laboratory tests were noted in any volunteer. We conclude that N-696 is a long-acting and potent β-A-adrenoceptor blocking agent and can be safely used in a clinical setting.
一般社団法人日本臨床薬理学会の論文