A novel long-acting analgesic:
buprenorphine palmitate in rats
by
Que J, Lin LC, Liu SY, Chu CC,
Liu KS, Ho ST, Wang JJ.
Department of Radio-oncology,
Chi-Mei Medical Center,
Tainan, Taiwan, ROC.
Acta Anaesthesiol Taiwan. 2005 Mar;43(1):11-6

ABSTRACT

BACKGROUND: A long-acting analgesic may be particularly desirable in patients with long-lasting pain. In order to provide a long-acting analgesic effect, a novel buprenorphine ester, buprenorphine palmitate, was synthesized in our laboratory. The aim of the study was to evaluate whether the ester had a long-lasting effect. METHODS: The antinociceptive effects (dose-range studies) of buprenorphine HCl and buprenorphine palmitate were evaluated using the plantar test in Sprague-Dawley rats. RESULTS: We found that intramuscular injection of buprenorphine HCl 0.05, 0.1 and 1 micromol/kg in rats produced dose-related antinociceptive effects of 2, 3, and 4 h, respectively. Intramuscular injection of buprenorphine palmitate 1, 5, and 10 micromol/kg also produced dose-related antinociceptive effects of 72, 76 and 78 h, respectively. On an equimolar basis of 1 micromol/kg, the durations of action of intramuscular buprenorphine HCl and buprenorphine palmitate were 4 and 72 h, respectively. CONCLUSIONS: Intramuscular injection of buprenorphine palmitate in rats produced a long-lasting antinociceptive effect which was much longer (18-fold) than did intramuscular buprenorphine HCl.

Pain
LAAM
Arousal
Fentanyl
Tramadol
Tolerance
Methadone
Endomorphins
LAAM v methadone
Opiates in psychiatry
Subutex and Suboxone
Opioids and depression
Buprenorphine and reward
Buprenorphine and naltrexone
Buprenorphine: the standard wisdom
Buprenorphine : behavioral pharmacology
Buprenorphine versus methadone or placebo

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