CLINICAL PHARMACOLOGY OF FLURBIPROFEN
Prof. Gian Maria Pacifici*
ABSTRACT
Flurbiprofen is a propionic acid derivative and is a nonselective cyclooxygenase inhibitor. Flurbiprofen is approved for the symptomatic treatment of rheumatoid arthritis, juvenile arthritis, pain, ankylosing spondylitis, acute gout arthritis, bursitis, postoperative dental pain, and primary dysmenorrhoea. In adults, the dose of flurbiprofen in 40 mg once-daily or twice-daily. Flurbiprofen is hydroxylated into 4’-hydroxy flurbiprofen by CYP2C9 and is conjugated with glucuronic acid by different glucuronosyl transferases and UGT2B7 catalyses the glucuronidation of flurbiprofen at the highest activity. The pharmacokinetics of flurbiprofen have been studied in CYP2C9 extensive and poor metabolizers and the elimination half-life of flurbiprofen is 5.1+0.3 and 6.1+0.6 hours (P-value = 0.0004) in extensive and poor metabolisers, respectively. The efficacy and safely of flurbiprofen, the prophylaxis with flurbiprofen, the treatment of patients with flurbiprofen, and the trials conducted with flurbiprofen have been reviewed. The concentration of flurbiprofen in different human tissues has been reviewed following topical and oral administration and the concentration of flurbiprofen in fat, tendon, periosteum, and muscle is higher following the topical than oral administration. The interaction of flurbiprofen with drugs and the toxicity induced by flurbiprofen have been reviewed. The aim of this study is to review the efficacy and safely of flurbiprofen, the prophylaxis with flurbiprofen, the treatment of patients with flurbiprofen, and the trials conducted with flurbiprofen. In addition, the metabolism of flurbiprofen, the tissue concentration of flurbiprofen, the interaction of flurbiprofen with drugs, and the toxicity induced by flurbiprofen have also been reviewed.
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