Abstract
A Phase I study on cisapride (R 51 619), a new gastrointestinal prokinetic agent, was conducted in 12 healthy Japanese male volunteers. The safety and pharmacokinetics of the drug were studied in repeated oral doses of 15 mg/day and 30 mg/day.
The volunteers were randomly divided into two groups (group 1 and group 2). The six men of group 1 received 15 mg/day t.i.d. for 5 days and the remaining six individuals (group 2) were given 30 mg/day t.i.d. for 7 days.
No abnormalities were observed in the vital signs, ECGs or laboratory tests. Among subjective symptoms, one individual in each group complained of a slight feeling of heavyheadedness and headache on the first day of administration.
The measured plasma levels of unchanged cisapride in this study almost coincided with the simulation curves which were defined based on the parameters obtained in the single oral dosing study. Moreover, the plasma levels reached steady states on the 3 rd or 4 th day of administration.
The serum levels of prolactin rose temporarily within the normal range on the first day of administration and normalized after repeated dosing.
The above results confirmed the safety of cisapride in repeated oral dosing in healthy male volunteers.
