JOURNAL HOME CME HOME THIS MONTH PAST ISSUES ETOC COLLECTIONS
AUTHORS REVIEWERS EDITORIAL BOARD FEEDBACK RSS HELP
A&A International Anesthesia Research Society
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a colleague
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Liu, K.-S.
Right arrow Articles by Wang, J.-J.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Liu, K.-S.
Right arrow Articles by Wang, J.-J.
Related Collections
Right arrow Pain
Right arrow Pharmacology

Anesth Analg 2006;102:1445-1451
© 2006 International Anesthesia Research Society
doi: 10.1213/01.ane.0000205747.05693.30

ANESTHETIC PHARMACOLOGY

Novel Depots of Buprenorphine Prodrugs Have a Long-Acting Antinociceptive Effect

Kuo-Sheng Liu, MS* {dagger}, Jann-Inn Tzeng, MD, MS*, Yu-Wen Chen, MS*, Kuo-Lun Huang, MS*, Chun-Hsiung Kuei, PhD{dagger}, and Jhi-Joung Wang, MD, PhD*

*Departments of Anesthesiology and Medical Research, Chi-Mei Medical Center; {dagger}Department of Chemistry, National Cheng-Kung University, Tainan, Taiwan

Address correspondence and reprint requests to Jhi-Joung Wang, MD, PhD, Departments of Anesthesiology and Medical Research, Chi-Mei Medical Center, or Chun-Hsiung Kuei, PhD, Department of Chemistry, National Cheng-Kung University, Tainan, Taiwan. Address e-mail to 400002{at}mail.chimei.org.tw or kuei{at}mail.ncku.edu.tw

An analgesic with a prolonged duration may be desirable in patients with long-lasting pain. In this study, we evaluated the antinociceptive effects and durations of action of three novel depots of buprenorphine esters buprenorphine propionate, enanthate, and decanoate given by IM injection, in rats. The pharmacokinetic profiles of buprenorphine in blood after IM injection of these depots were also evaluated. Antinociception was evaluated using the plantar test. Buprenorphine concentrations in blood were assayed using high-performance liquid chromatography. We found that the traditional form of buprenorphine HCl (in saline) produced a dose-related antinociceptive effect. A dose of 0.6 µmol/kg buprenorphine HCl (in saline) produced a significant antinociceptive effect lasting 5 h. The same dose of buprenorphine base, propionate, enanthate, and decanoate (in oil) also produced a significant antinociceptive effect with longer durations of action of 26, 28, 52, and 70 h, respectively. The pharmacokinetic studies demonstrated that all the buprenorphine esters were prodrugs of buprenorphine. We conclude that the novel depots of buprenorphine prodrugs: buprenorphine propionate, enanthate, and decanoate produced a long-acting antinociceptive effect after IM injection in rats.






Lippincott, Williams & Wilkins Anesthesia & Analgesia® is published for the International Anesthesia Research Society® by Lippincott Williams & Wilkins with the assistance of Stanford University Libraries' HighWire Press®. Copyright 2006 by the International Anesthesia Research Society. Online ISSN: 1526-7598   Print ISSN: 0003-2999 HighWire Press
Copyright © 2006 by the International Anesthesia Research Society.