Seven-day antinociceptive effect of a sustained release vapreotide formulation.
This work studies the antinociceptive effect of a sustained (7 day) release dosage form of vapreotide, a peptidic analogue of somatostatin, in rats submitted to a nociceptive mechanical stimulus (paw pressure). One intramuscular injection (0.6 mg/animal) induced a significant antinociceptive effect for 7 complete days with a maximal increase in vocalization thresholds of 68 +/- 5% and a plateau of activity during the first 4 days. This action was totally inhibited by naloxone (1 mg kg-1, s.c.) injected 24 h or 6 days after vapreotide, suggesting an opioidergic involvement throughout the antinociceptive effect. These findings suggest potential interest in human therapy.
Betoin
F
F
Laboratoire de Pharmacologie Médicale, Equipe NPPA, Faculté de Médecine, Clermont-Ferrand, France.
Eschalier
A
A
Duchene-Marullaz
P
P
Lavarenne
J
J
D000700:Analgesics / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000818:Animals; D003692:Delayed-Action Preparations; D007273:Injections, Intramuscular; D008297:Male; D009270:Naloxone / Q000494:pharmacology; D010146:Pain / Q000188:drug therapy*; D010147:Pain Measurement; D051381:Rats; D017207:Rats, Sprague-Dawley; D011957:Receptors, Opioid / Q000187:drug effects / Q000502:physiology; D013004:Somatostatin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D013997:Time Factors
D000700:Analgesics; D003692:Delayed-Action Preparations; D011957:Receptors, Opioid; C051458:vapreotide; D009270:Naloxone; D013004:Somatostatin