title: Pharmacokinetic and pharmacodynamic properties of a long-acting formulation of the new somatostatin analogue, lanreotide, in normal healthy volunteers.
abstract: 1. The aims of the study were to assess the pharmacokinetic parameters and the hormonal effects of the slow-release formulation of the somatostatin analogue (SR-L) in normal male volunteers. 2. Eight healthy males were studied. For the determination of basal values blood was sampled before the injection of vehicle and then every other hour for 8 h in order to measure plasma GH, prolactin (PRL), TSH, free thyroxin (fT4), insulin and glucagon levels. Plasma insulin-like growth factor 1 (IGF-1) levels were measured on a single sample. On day 1 of the study, 30 mg SR-L was administered intramuscularly. Blood was drawn just before injection and then every other hour for a period of 8 h. Thereafter, blood was sampled three times a week for 3 weeks in order to measure lanreotide, IGF-1, TSH, fT4 and PRL concentrations. Plasma GH was determined on days 6 and 11 of the study. 3. Plasma lanreotide concentrations rose to 38.3 +/- 4.1 ng ml-1 2 h following injection. The levels then progressively decreased, remaining above 1.5 ng ml-1 until day 11 and reaching 0.92 +/- 0.28 ng ml-1 2 weeks after injection. The apparent plasma half-life and mean residence time were 4.52 +/- 0.50 and 5.48 +/- 0.51 days respectively. 4. By comparison with the control day, plasma insulin concentrations only decreased 2 h following injection, whereas plasma glucagon did not change at any time. 5. Plasma TSH concentrations were significantly (P < 0.01) reduced from 2 h to day 4 following SR-L injection.2+ '
authors: Department of Endocrinology, University of Rouen, France.
authors: J M
authors: JM
authors: Kuhn
authors: A
authors: A
authors: Legrand
authors: J M
authors: JM
authors: Ruiz
authors: R
authors: R
authors: Obach
authors: J
authors: J
authors: De Ronzan
authors: F
authors: F
authors: Thomas
mesh_terms: D015746:Abdominal Pain / Q000139:chemically induced; D000595:Amino Acid Sequence; D000704:Analysis of Variance; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations; D003967:Diarrhea / Q000139:chemically induced; D005934:Glucagon / Q000097:blood; D013006:Growth Hormone / Q000097:blood; D006801:Humans; D007273:Injections, Intramuscular; D007328:Insulin / Q000097:blood; D007334:Insulin-Like Growth Factor I / Q000378:metabolism; D008297:Male; D008969:Molecular Sequence Data; D010456:Peptides, Cyclic / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics*; D011388:Prolactin / Q000097:blood; D011863:Radioimmunoassay; D013004:Somatostatin / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D013974:Thyroxine / Q000097:blood
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D007328:Insulin; D010456:Peptides, Cyclic; C060347:lanreotide; D013004:Somatostatin; D007334:Insulin-Like Growth Factor I; D011388:Prolactin; D013006:Growth Hormone; D005934:Glucagon; D013974:Thyroxine