Dose-dependent gastrointestinal effects of the somatostatin analog lanreotide in healthy volunteers.
OBJECTIVE
To investigate the gastrointestinal effects of intravenous lanreotide.


METHODS
Twenty healthy male subjects participated in 2 subsequent placebo-controlled, double-blind crossover studies. The effects of 3 doses of lanreotide (50, 100, and 200 microg/h) were investigated on 24-hour intragastric acidity (study I), food-stimulated gallbladder contraction, and plasma cholecystokinin release (study II).


RESULTS
Lanreotide showed linear pharmacokinetics. It raised median intragastric pH significantly and in a dose-dependent manner: from 1.4+/-0.2 (placebo) to 2.5+/-0.8 (P < .002) during administration of 50 microg/h lanreotide, to 3.2+/-0.7 (P < .001) during 100 microg/h lanreotide, and to 4.3+/-0.7 (P < .001) during 200 microg/h lanreotide. However, no significant inhibition of gastrin secretion could be established. All doses completely inhibited postprandial gallbladder contraction.


CONCLUSIONS
Intravenous administration of lanreotide at rates applied in this study was able to significantly inhibit intragastric acid secretion and postprandial gallbladder contraction; under these conditions few untoward effects were noted.
Drewe
J
J
Department of Internal Medicine, University Hospital/Kantonsspital, Basel, Switzerland.
Sieber
C C
CC
Mottet
C
C
Wullschleger
C
C
Larsen
F
F
Beglinger
C
C
D000328:Adult; D019540:Area Under Curve; D002766:Cholecystokinin / Q000097:blood*; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D005704:Gallbladder / Q000187:drug effects*; D005744:Gastric Acid / Q000378:metabolism*; D005765:Gastrointestinal Agents / Q000494:pharmacology*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008297:Male; D010456:Peptides, Cyclic / Q000494:pharmacology*; D011863:Radioimmunoassay; D012016:Reference Values; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000494:pharmacology
D005765:Gastrointestinal Agents; D010456:Peptides, Cyclic; C060347:lanreotide; D013004:Somatostatin; D002766:Cholecystokinin