Summary
The pharmacokinetics of intravenous (IV) dezocine, and bioavailability of intramuscular (IM) and subcutaneous (SQ) dezocine, were evaluated in healthy male volunteers. Elimination half-life following 5, 10, and 20 mg IV doses averaged 2.6–2.8 h, and was independent of dose. Clearance decreased slightly, although significantly, with dose. After Deltoid IM injection, dezocine was rapidly absorbed (peak level: 0.6 h after dose), with bioavailability 97%. Thus dezocine has extensive distribution, high clearance and short half-life over a range of IV doses. It is rapidly and completely absorbed following IM or SQ administration.
This is a preview of subscription content, log in via an institution to check access.
References
Wuest HP, Bellville JW (1979) The respiratory effects of dezocine and pentazocine in man. J Clin Pharmacol 4: 205–210
Downing JW, Brock-Utne JG, Barclay A, Schwegmann IL (1981) Wy 16225 (Dezocine), a new synthetic opiate agonist-antagonist and potent analgesic: Comparison with morphine for relief of pain after lower abdominal surgery. Br J Anaesth 53: 59–63
Oosterlink W, Verbaeys A (1980) Preliminary clinical experience with dezocine, a new potent analgesic. Curr Med Res Opin 6: 472–474
Sisenwine SF, Tio CO, Liu AL, Ruelius HW (1982) Pharmacokinetics of parenteral dezocine in rhesus monkeys and dogs. Drug Metab Dispos 10: 366–370
Locniskar A, Greenblatt DL (1986) Determination of ciramadol and dezocine, two new analgesics, by HPLC using electrochemical detection. J Chromatogr (in press)
Greenblatt DJ, Shader RI, Franke K, MacLaughlin DS, Harmatz JS, Allen MD, Werner A, Woo E (1979) Pharmacokinetics and bioavailability of intravenous, intramuscular and oral lorazepam in humans. J Pharm Sci 68: 57–63
Evans EF, Proctor JD, Fratkin MJ, Velandia J, Wasserman AJ (1978) Blood flow in muscle groups and drug absorption. Clin Pharmacol Ther 17: 44–47
Greenblatt DJ, Koch-Weser J (1976) Intramuscular injection of drugs. N Engl J Med 295: 542–546
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Locniskar, A., Greenblatt, D.J. & Zinny, M.A. Pharmacokinetics of dezocine, a new analgesic: Effect of dose and route of administration. Eur J Clin Pharmacol 30, 121–123 (1986). https://doi.org/10.1007/BF00614208
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00614208