title: Effects of ligand priming and multiple-dose injection on tissue uptake of 111In-pentetreotide in rats.
abstract: In patients undergoing somatostatin receptor scintigraphy, treatment with octreotide (Sandostatin) is usually discontinued 24-48 h before and after injection with the radioligand 111In-pentetreotide ([111In-DTPA(O)]octreotide) (Octreoscan) because octreotide competes with radioligand for the same receptors. However, Dörr et al. and Soresi et al. reported improved visualization of carcinoid and small cell lung cancer lesions, respectively, during continued octreotide treatment. We found that intravenous administration of unlabeled octreotide to rats inhibited the binding of an optimal dose (0.5 microg) of 111In-pentetreotide to somatostatin receptors in pancreas and adrenals in a mass- and time-dependent way. Pretreatment with unlabeled octreotide never increased receptor binding of 111In-pentetreotide. Administration of 100 microg of octreotide decreased receptor-bound radioactivity if given simultaneously with or 10 or 20 min after injection of the radioligand, but had no effect if given 30 min after the radioligand. These findings indicate rapid processing of receptor-bound octreotide and suggest that octreotide treatment of patients undergoing 111In-pentetreotide scintigraphy may be reinitiated as soon as 1 h after radioligand administration.
authors.affiliation: Department of Nuclear Medicine, University Hospital Dijkzigt, Rotterdam, The Netherlands. breeman@nuge.azr.nl
authors.forename: W A
authors.initials: WA
authors.lastname: Breeman
authors.forename: M
authors.initials: M
authors.lastname: de Jong
authors.forename: B F
authors.initials: BF
authors.lastname: Bernard
authors.forename: W H
authors.initials: WH
authors.lastname: Bakker
authors.forename: E J
authors.initials: EJ
authors.lastname: Rolleman
authors.forename: D J
authors.initials: DJ
authors.lastname: Kwekkeboom
authors.forename: T J
authors.initials: TJ
authors.lastname: Visser
authors.forename: E P
authors.initials: EP
authors.lastname: Krenning
mesh_terms: D000818:Animals; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D005947:Glucose / Q000494:pharmacology; D007205:Indium Radioisotopes; D008024:Ligands; D008297:Male; D010179:Pancreas / Q000378:metabolism; D011869:Radioligand Assay; D019275:Radiopharmaceuticals / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D017481:Receptors, Somatostatin / Q000032:analysis / Q000378:metabolism; D013004:Somatostatin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D014018:Tissue Distribution
chemical_list: D007205:Indium Radioisotopes; D008024:Ligands; D019275:Radiopharmaceuticals; D017481:Receptors, Somatostatin; D013004:Somatostatin; C081788:pentetreotide; D005947:Glucose