Literature DB >> 2015160

The pharmacokinetics of the enantiomers of flurbiprofen in patients with rheumatoid arthritis.

M A Young1, L Aarons, S Toon.   

Abstract

Plasma and synovial fluid concentrations of the enantiomers of flurbiprofen were measured in 15 rheumatoid patients receiving 100 mg racemic flurbiprofen twice daily. Pharmacokinetic parameters showed considerable variability within the group of patients, although differences in S(+)/R(-) plasma concentration ratios were small. The average values (+/- s.d.) of oral plasma clearance, volume of distribution and elimination half-life for R(-)-flurbiprofen were 0.075 (+/- 0.066) l min-1, 12.47 (+/- 5.79) l and 138 (+/- 61) min, respectively. The average values (+/- s.d.) of oral plasma clearance, volume of distribution and elimination half-life for S(+)-flurbiprofen were 0.057 (+/- 0.035) l min-1, 12.81 (+/- 4.43) l and 155 (+/- 49) min, respectively. S(+)/R(-) ratios (+/- s.d.) rose from 1.06 (+/- 0.12) to 1.75 (+/- 0.61) at the end of the 12 h interval in plasma and from 1.18 (+/- 0.13) to 1.47 (+/- 0.24) over the measured time course in synovial fluid. Increases in S(+)/R(-) ratios may be clinically important as they demonstrate accumulation of the pharmacologically active species.

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Year:  1991        PMID: 2015160      PMCID: PMC1368420          DOI: 10.1111/j.1365-2125.1991.tb03865.x

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


  13 in total

1.  Pharmacological differences between the optical isomers of ibuprofen: evidence for metabolic inversion of the (-)-isomer.

Authors:  S S Adams; P Bresloff; C G Mason
Journal:  J Pharm Pharmacol       Date:  1976-03       Impact factor: 3.765

2.  The pharmacological and toxicological significance of the stereochemistry of drug disposition.

Authors:  J Caldwell; S M Winter; A J Hutt
Journal:  Xenobiotica       Date:  1988-01       Impact factor: 1.908

3.  Bias in pharmacokinetics and clinical pharmacology.

Authors:  E J Ariëns; E W Wuis
Journal:  Clin Pharmacol Ther       Date:  1987-10       Impact factor: 6.875

Review 4.  The metabolic chiral inversion of 2-arylpropionic acids--a novel route with pharmacological consequences.

Authors:  A J Hutt; J Caldwell
Journal:  J Pharm Pharmacol       Date:  1983-11       Impact factor: 3.765

5.  Stereochemistry, a basis for sophisticated nonsense in pharmacokinetics and clinical pharmacology.

Authors:  E J Ariëns
Journal:  Eur J Clin Pharmacol       Date:  1984       Impact factor: 2.953

Review 6.  The metabolic chiral inversion and dispositional enantioselectivity of the 2-arylpropionic acids and their biological consequences.

Authors:  J Caldwell; A J Hutt; S Fournel-Gigleux
Journal:  Biochem Pharmacol       Date:  1988-01-01       Impact factor: 5.858

7.  GLC determination of ibuprofen ((plus or minus)-2-(p-isobutylphenyl)propionic acid) in plasma.

Authors:  D G Kaiser; G J Vangiessen
Journal:  J Pharm Sci       Date:  1974-02       Impact factor: 3.534

8.  High-performance liquid chromatographic separation of the enantiomers of anti-inflammatory 2-arylpropionates: suitability of the method for in vitro metabolic studies.

Authors:  J M Maître; G Boss; B Testa
Journal:  J Chromatogr       Date:  1984-09-21

9.  Dose-response study with ibuprofen in rheumatoid arthritis: clinical and pharmacokinetic findings.

Authors:  D M Grennan; L Aarons; M Siddiqui; M Richards; R Thompson; C Higham
Journal:  Br J Clin Pharmacol       Date:  1983-03       Impact factor: 4.335

10.  Plasma and synovial fluid kinetics of flurbiprofen in rheumatoid arthritis.

Authors:  L Aarons; R Salisbury; M Alam-Siddiqi; L Taylor; D M Grennan
Journal:  Br J Clin Pharmacol       Date:  1986-02       Impact factor: 4.335

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  5 in total

Review 1.  Enantioselective pharmacodynamics and pharmacokinetics of chiral non-steroidal anti-inflammatory drugs.

Authors:  A M Evans
Journal:  Eur J Clin Pharmacol       Date:  1992       Impact factor: 2.953

2.  Stereoselective disposition of flurbiprofen in uraemic patients.

Authors:  M P Knadler; D C Brater; S D Hall
Journal:  Br J Clin Pharmacol       Date:  1992-04       Impact factor: 4.335

Review 3.  Protein binding and stereoselectivity of nonsteroidal anti-inflammatory drugs.

Authors:  F Lapicque; N Muller; E Payan; N Dubois; P Netter
Journal:  Clin Pharmacokinet       Date:  1993-08       Impact factor: 6.447

4.  Stereoselective disposition of flurbiprofen in healthy subjects following administration of the single enantiomers.

Authors:  G Geisslinger; J Lötsch; S Menzel; G Kobal; K Brune
Journal:  Br J Clin Pharmacol       Date:  1994-04       Impact factor: 4.335

Review 5.  Clinical pharmacokinetics of flurbiprofen and its enantiomers.

Authors:  N M Davies
Journal:  Clin Pharmacokinet       Date:  1995-02       Impact factor: 6.447

  5 in total

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