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Research ArticleArticle

Dose-Dependent Inhibition of Platelet Cyclooxygenase-1 and Monocyte Cyclooxygenase-2 by Meloxicam in Healthy Subjects

Maria R. Panara, Giulia Renda, Maria G. Sciulli, Giovanna Santini, Maria Di Giamberardino, Maria T. Rotondo, Stefania Tacconelli, Francesca Seta, Carlo Patrono and Paola Patrignani
Journal of Pharmacology and Experimental Therapeutics July 1999, 290 (1) 276-280;
Maria R. Panara
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Giulia Renda
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Maria G. Sciulli
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Giovanna Santini
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Maria Di Giamberardino
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Maria T. Rotondo
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Stefania Tacconelli
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Francesca Seta
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Carlo Patrono
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Paola Patrignani
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Abstract

We evaluated whether therapeutic blood levels of meloxicam are associated with selective inhibition of monocyte cyclooxygenase (COX)-2 in vitro and ex vivo. Concentration-response curves for the inhibition of monocyte COX-2 and platelet COX-1 were obtained in vitro after the incubation of meloxicam with whole blood samples. Moreover, 11 healthy volunteers received placebo or 7.5 or 15 mg/day meloxicam, each treatment for 7 consecutive days, according to a randomized, double-blind, crossover design. Before dosing and 24 h after the seventh dose of each regimen, heparinized whole blood samples were incubated with lipopolysaccharide (10 μg/ml) for 24 h at 37°C, and prostaglandin E2 was measured in plasma as an index of monocyte COX-2 activity. The production of thromboxane B2in whole blood allowed to clot at 37°C for 60 min was assessed as an index of platelet COX-1 activity. The administration of placebo did not significantly affect plasma prostaglandin E2 (21.3 ± 7.5 versus 19.1 ± 4 ng/ml, mean ± S.D.,n = 11) or serum thromboxane B2(426 ± 167 versus 425 ± 150 ng/ml) levels. In contrast, the administration of 7.5 and 15 mg of meloxicam caused dose-dependent reductions in monocyte COX-2 activity by 51% and 70%, respectively, and in platelet COX-1 activity by 25% and 35%, respectively. Although the IC50 value of meloxicam for inhibition of COX-1 was 10-fold higher than the IC50 value of COX-2 in vitro, this biochemical selectivity was inadequate to clearly separate the effects of meloxicam on the two isozymes after oral dosing as a function of the daily dose and interindividual variation in steady-state plasma levels.

Footnotes

  • Send reprint requests to: Paola Patrignani, Ph.D., Cattedra di Farmacologia I, Dipartimento di Medicina e Scienze dell’Invecchiamento, Università di Chieti “G. D’Annunzio,” Via dei Vestini, 31, 66013 Chieti, Italy. E-mail: ppatrignani{at}unich.it

  • ↵1 This work was supported by a grant from Boehringer Ingelheim Italia spa.

  • Abbreviations:
    PGHS
    prostaglandin endoperoxide synthase
    COX
    cyclooxygenase
    LPS
    lipopolysaccharide
    AA
    arachidonic acid
    PGE2
    prostaglandin E2
    TXB2
    thromboxane B2
    NSAID
    nonsteroidal anti-inflammatory drug
    • Received November 30, 1998.
    • Accepted March 5, 1999.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 290 (1)
Journal of Pharmacology and Experimental Therapeutics
Vol. 290, Issue 1
1 Jul 1999
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Research ArticleArticle

Dose-Dependent Inhibition of Platelet Cyclooxygenase-1 and Monocyte Cyclooxygenase-2 by Meloxicam in Healthy Subjects

Maria R. Panara, Giulia Renda, Maria G. Sciulli, Giovanna Santini, Maria Di Giamberardino, Maria T. Rotondo, Stefania Tacconelli, Francesca Seta, Carlo Patrono and Paola Patrignani
Journal of Pharmacology and Experimental Therapeutics July 1, 1999, 290 (1) 276-280;

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Research ArticleArticle

Dose-Dependent Inhibition of Platelet Cyclooxygenase-1 and Monocyte Cyclooxygenase-2 by Meloxicam in Healthy Subjects

Maria R. Panara, Giulia Renda, Maria G. Sciulli, Giovanna Santini, Maria Di Giamberardino, Maria T. Rotondo, Stefania Tacconelli, Francesca Seta, Carlo Patrono and Paola Patrignani
Journal of Pharmacology and Experimental Therapeutics July 1, 1999, 290 (1) 276-280;
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