Dose-response effects of oral loxiglumide on postprandial gall-bladder emptying in man

• Published in: Arzneimittel-Forschung Vol. 42; no. 11; p. 1359
• Main Authors: Malesci, A, De Fazio, C, Festorazzi, S, Bonato, C, Valentini, A, Tacconi, M, Bekkering, M, Giacovelli, G, D'Amato, M, Rovati, L C
• Format: Journal Article
• Language: English
• Published: Germany 01.11.1992
• Subjects: Adult; Cholecystokinin - antagonists & inhibitors; Dose-Response Relationship, Drug; Double-Blind Method; Food; Gallbladder - anatomy & histology; Gallbladder Emptying - drug effects; Humans; Male; Proglumide - analogs & derivatives; Proglumide - pharmacology
• ISSN: 0004-4172

The effect of two different single oral doses of loxiglumide (CR 1505, CAS 107097-80-3) on gall-bladder emptying induced by a 550-cal standard mixed meal in 6 healthy volunteers was studied. Following placebo, the maximal gall-bladder emptying occurred about 90 min after the meal (minimal residual gall-bladder volume 27.4% of basal volume). Loxiglumide 400 or 800 mg dose-dependently inhibited the physiologica gall-bladder emptying. Loxiglumide plasma levels dose-dependently increased. The inhibition of gall-bladder emptying and the kinetic of loxiglumide plasma levels were temporally related. The results of the present study confirm that oral loxiglumide is a potent orally active cholecystokinin (CCK) antagonist in man and that CCK is the major physiological mediator of gallbladder emptying in response to meal.