Pharmacokinetic and pharmacodynamic properties of a long-acting formulation of the new somatostatin analogue, lanreotide, in normal healthy volunteers

Br J Clin Pharmacol. 1994 Sep;38(3):213-9. doi: 10.1111/j.1365-2125.1994.tb04344.x.

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+ '

Publication types

  • Clinical Trial
  • Comparative Study

MeSH terms

  • Abdominal Pain / chemically induced
  • Amino Acid Sequence
  • Analysis of Variance
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacokinetics*
  • Delayed-Action Preparations
  • Diarrhea / chemically induced
  • Glucagon / blood
  • Growth Hormone / blood
  • Humans
  • Injections, Intramuscular
  • Insulin / blood
  • Insulin-Like Growth Factor I / metabolism
  • Male
  • Molecular Sequence Data
  • Peptides, Cyclic / administration & dosage
  • Peptides, Cyclic / adverse effects
  • Peptides, Cyclic / chemistry
  • Peptides, Cyclic / pharmacokinetics*
  • Prolactin / blood
  • Radioimmunoassay
  • Somatostatin / administration & dosage
  • Somatostatin / adverse effects
  • Somatostatin / analogs & derivatives*
  • Somatostatin / chemistry
  • Somatostatin / pharmacokinetics
  • Thyroxine / blood

Substances

  • Antineoplastic Agents
  • Delayed-Action Preparations
  • Insulin
  • Peptides, Cyclic
  • lanreotide
  • Somatostatin
  • Insulin-Like Growth Factor I
  • Prolactin
  • Growth Hormone
  • Glucagon
  • Thyroxine