Drugs

, Volume 68, Issue 1, pp 123–130 | Cite as

Diclofenac Sodium Injection (Dyloject®)

In Postoperative Pain
Adis Drug Profile

Abstract

  • ▲ A new formulation of the nonselective NSAID diclofenac sodium suitable for intravenous bolus injection has been developed using hydroxypropyl β-cyclodextrin as a solubility enhancer (HPβCD diclofenac).

  • ▲ HPβCD diclofenac intravenous bolus injection was shown to be bioequivalent to the existing parenteral formulation of diclofenac containing propylene glycol and benzyl alcohol as solubilizers (PG-BA diclofenac), which is relatively insoluble and requires slow intravenous infusion over 30 minutes.

  • ▲ Single-dose HPβCD diclofenac 3.75, 9.4, 18.75, 25, 37.5, 50 and 75 mg administered by intravenous bolus injection produced significantly greater responses than placebo for total pain relief (TOTPAR) over 6 hours or pain intensity at 4 hours in the treatment of moderate or severe postoperative dental pain in randomized, double-blind trials. HPβCD diclofenac 37.5 and 75 mg were similar in efficacy to intravenous bolus ketorolac 30 mg.

  • ▲ In a well controlled trial, single-dose HPβCD diclofenac 75 mg intravenous bolus injection was shown to be superior to PG-BA diclofenac 75 mg intravenous infusion with respect to TOTPAR over 4 hours, indicating faster onset of analgesia in the treatment of moderate or severe postoperative dental pain. Both HPβCD diclofenac and PG-BA diclofenac were superior to placebo.

  • ▲ HPβCD diclofenac was generally well tolerated during single-dose treatment of postoperative pain. The tolerability profile was similar to that of PG-BA diclofenac, but with a lower incidence of thrombophlebitis.

Keywords

Pain Intensity Ketorolac Thrombophlebitis Intramuscular Administration Intravenous Bolus Injection 

References

  1. 1.
    White PF. The role of non-opioid analgesic techniques in the management of pain after ambulatory surgery. Anesth Analg 2002; 94: 577–85PubMedCrossRefGoogle Scholar
  2. 2.
    Filos KS, Lehmann KA. Current concepts and practice in postoperative pain management: need for a change? Eur Surg Res 1999; 31(2): 97–107PubMedCrossRefGoogle Scholar
  3. 3.
    Wheeler M, Oderda GM, Ashburn MA, et al. Adverse events associated with postoperative opioid analgesia: a systematic review. J Pain 2002 Jun; 3(3): 159–80PubMedCrossRefGoogle Scholar
  4. 4.
    National Pharmaceutical Council. Pain: current understanding of assessment, management, and treatments [online]. Available from URL: http://www.npcnow.org/resources/PDFs/painmonograph.pdf [Accessed 2007 Jun 5]
  5. 5.
    Todd PA, Sorkin EM. Diclofenac sodium: a reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy. Drugs 1988 Mar; 35(3): 244–85PubMedCrossRefGoogle Scholar
  6. 6.
    Barden J, Edwards J, Moore RA, et al. Single dose oral diclofenac for postoperative pain. Cochrane Database Syst Rev 2004; (2): CD004768Google Scholar
  7. 7.
    Leeson RM, Harrison S, Ernst CC, et al. Dyloject, a novel injectable diclofenac formulation, offers greater safety and efficacy than Voltarol for postoperative dental pain. Reg Anesth Pain Med 2007 Jul–Aug; 32(4): 303–10PubMedGoogle Scholar
  8. 8.
    Brogden RN, Heel RC, Pakes GE, et al. Diclofenac sodium: a review of its pharmacological properties and therapeutic use in rheumatic diseases and pain of varying origin. Drugs 1980 Jul; 20(1): 24–48PubMedCrossRefGoogle Scholar
  9. 9.
    Maier R, Menasse R, Riesterer L, et al. The pharmacology of diclofenac sodium (Voltarol). Rheumatol Rehabil 1979; Suppl. 2: 11–21PubMedGoogle Scholar
  10. 10.
    Chandrasekharan NV, Dai H, Roos KLT, et al. COX-3, a cyclooxygenase-1 variant inhibited by acetaminophen and other analgesic/antipyretic drugs: cloning, structure, and expression. Proc Natl Acad Sci U S A 2002 Oct 15; 99(21): 13926–31PubMedCrossRefGoogle Scholar
  11. 11.
    Javelin Pharmaceuticals Inc. A phase 1, randomized, analytically blind, fasted, single-dose, four-way crossover study of the bioavailability of one dose level of parenteral DIC075V (diclofenac sodium 75 mg/2 ml), administered intramuscularly and intravenously, vs. parenteral Voltarol® (diclofenac sodium 75 mg/3 ml) administered intramuscularly and intravenously in healthy adult volunteers. New York: Javelin Pharmaceuticals Inc., 2004. (Data on file)Google Scholar
  12. 12.
    Christensen K, Daniels S, Bandy D, et al. Dyloject™, a novel injectable diclofenac: efficacy of unexpectedly low doses and faster onset than ketorolac [abstract no. 643]. Eur J Pain 2006; 10 Suppl. S1: S168CrossRefGoogle Scholar
  13. 13.
    Javelin Pharmaceuticals Inc. A randomized, double-blind, placebo- and comparator-controlled, single-dose, parallel-group comparison of the analgesic efficacy and safety of intravenous DIC075V (diclofenac sodium injection), ketorolac tromethamine and placebo following surgery. New York: Javelin Pharmaceuticals Inc., 2006. (Data on file)Google Scholar
  14. 14.
    Data on file, Javelin Pharmaceuticals Inc., 2007Google Scholar
  15. 15.
    Wallerstein K. A cost minimization analysis of IV bolus versus IV infusion diclofenac in post-operative pain [abstract and poster]. 10th Annual European Congress of the International Society for Pharmacoeconomics and Outcomes Research; 2007 Oct 20–23; DublinGoogle Scholar
  16. 16.
    Catalano MA. Worldwide safety experience with diclofenac. Am J Med 1986 Apr 28; 80(4B): 81–7PubMedCrossRefGoogle Scholar
  17. 17.
    Novartis Pharmaceuticals UK Ltd. Voltarol ampoules: summary of product characteristics [online]. Available from URL: http://emc.medicines.org.uk [Accessed 2007 May 30]
  18. 18.
    Javelin Pharmaceuticals Inc. Javelin Pharmaceuticals receives marketing authorization approval for Dyloject® in the United Kingdom [media release]. 2007 Oct 31Google Scholar

Copyright information

© Adis Data Information BV 2008

Authors and Affiliations

  1. 1.Wolters Kluwer Health ¦ AdisMairangi Bay, North Shore 0754, AucklandNew Zealand
  2. 2.Wolters Kluwer HealthConshohockenUSA

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