Effects of lysine clonixinate and ketorolac tromethamine on prostanoid release from various rat organs incubated ex vivo

  • Pallapies D
  • Salinger A
  • zum Gottesberge A
 et al. 
  • 4

    Readers

    Mendeley users who have this article in their library.
  • 25

    Citations

    Citations of this article.

Abstract

The release of prostanoids from rat brain, gastric mucosa, lungs and kidneys incubated ex vivo has been investigated for up to 5 h after oral administration of 10 mg / kg lysine clonixinate or 1 mg / kg ketorolac tromethamine. Additionally, 60 min after drug administration, a time point of near-maximal inhibition of prostanoid release, the effects of 2.5, 10 and 30 mg / kg lysine clonixinate and of 0.0225, 0.15 and 1 mg / kg ketorolac tromethamine were compared. In all organs investigated both drugs inhibited fatty acid cyclooxygenase (COX) in a dose-dependent manner, but ketorolac tromethamine was more potent and had a longer-lasting effect than lysine clonixinate. While the ID50values for lysine clonixinate were in the same order of magnitude for all 4 organs investigated, ketorolac tromethamine exhibited some organ selectivity with a particularly high activity in the kidneys. This effect might be related to the renal toxicity of ketorolac tromethamine. On the other hand, the difference in potency was smallest in brain suggesting that inhibition of central prostanoid biosynthesis could contribute to the rapid and effective inhibition of pain by both drugs. IC50values for inhibition of purified COX-1 and COX-2 in vitro were slightly lower for lysine clonixinate (2.4 and 24.6 μg / ml, respectively) than for ketorolac tromethamine (3.7 and 25.6 μg / ml, respectively). © 1995.

Author-supplied keywords

  • cyclooxygenase
  • ketorolac tromethamine
  • lysine clonixinate
  • prostaglandin
  • thromboxane

Get free article suggestions today

Mendeley saves you time finding and organizing research

Sign up here
Already have an account ?Sign in

Find this document

Authors

  • D. Pallapies

  • A. Salinger

  • A. Meyer zum Gottesberge

  • D. J. Atkins

  • G. Rohleder

  • P. Nagyiványi

Cite this document

Choose a citation style from the tabs below

Save time finding and organizing research with Mendeley

Sign up for free