Literature DB >> 8018462

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

G Geisslinger1, J Lötsch, S Menzel, G Kobal, K Brune.   

Abstract

Plasma concentrations of the enantiomers of flurbiprofen were measured following oral administration of (S)-flurbiprofen 50 mg and (R)-flurbiprofen 50 mg and 100 mg to sixteen healthy subjects. Chiral inversion did not occur to a measurable extent. Significantly higher values of AUC (55.2 +/- 17.0 vs 44.6 +/- 11.2 micrograms ml-1h) elimination half-life (5.6 +/- 1.4 vs 4.0 +/- 1.0 h) and mean residence time (7.5 +/- 1.6 vs 5.7 +/- 1.2 h) were observed after 50 mg (S)-flurbiprofen as compared with 50 mg (R)-flurbiprofen. With the exception of Cmax and AUC values pharmacokinetic data for the 50 mg and the 100 mg dose of (R)-flurbiprofen did not differ significantly. The data are of clinical relevance if (R)-flurbiprofen also has analgesic activity in humans and is to be developed as an analgesic.

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Year:  1994        PMID: 8018462      PMCID: PMC1364742          DOI: 10.1111/j.1365-2125.1994.tb04295.x

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


  10 in total

1.  Stereoselective high-performance liquid chromatographic determination of flurbiprofen in human plasma.

Authors:  G Geisslinger; S Menzel-Soglowek; O Schuster; K Brune
Journal:  J Chromatogr       Date:  1992-01-03

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

3.  Stereoselective disposition of flurbiprofen in normal volunteers.

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

4.  Stereoselective arylpropionyl-CoA thioester formation in vitro.

Authors:  M P Knadler; S D Hall
Journal:  Chirality       Date:  1990       Impact factor: 2.437

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

Authors:  M A Young; L Aarons; S Toon
Journal:  Br J Clin Pharmacol       Date:  1991-01       Impact factor: 4.335

6.  Aspirin-like drugs may block pain independently of prostaglandin synthesis inhibition.

Authors:  K Brune; W S Beck; G Geisslinger; S Menzel-Soglowek; B M Peskar; B A Peskar
Journal:  Experientia       Date:  1991-03-15

7.  Stereoselective disposition of ibuprofen and flurbiprofen in rats.

Authors:  R D Knihinicki; R O Day; G G Graham; K M Williams
Journal:  Chirality       Date:  1990       Impact factor: 2.437

8.  Chiral inversion of 2-arylpropionic acid non-steroidal anti-inflammatory drugs--1. In vitro studies of ibuprofen and flurbiprofen.

Authors:  R D Knihinicki; K M Williams; R O Day
Journal:  Biochem Pharmacol       Date:  1989-12-15       Impact factor: 5.858

9.  Variability of inversion of (R)-flurbiprofen in different species.

Authors:  S Menzel-Soglowek; G Geisslinger; W S Beck; K Brune
Journal:  J Pharm Sci       Date:  1992-09       Impact factor: 3.534

10.  Stereoselective pharmacokinetics of flurbiprofen in humans and rats.

Authors:  F Jamali; B W Berry; M R Tehrani; A S Russell
Journal:  J Pharm Sci       Date:  1988-08       Impact factor: 3.534

  10 in total
  15 in total

1.  Pharmacokinetic parameters of (R)-(-) and (S)-(+)-flurbiprofen in dairy bovines.

Authors:  L Igarza; A Soraci; N Auza; H Zeballos
Journal:  Vet Res Commun       Date:  2006-07       Impact factor: 2.459

2.  Combination therapy in a transgenic model of Alzheimer's disease.

Authors:  Bruce G Jenkins; Alpaslan Dedeoglu; Nurgul Aytan; Ji-Kyung Choi; Isabel Carreras; Neil W Kowall
Journal:  Exp Neurol       Date:  2013-10-10       Impact factor: 5.330

3.  Flurbiprofen enantiomers inhibit inducible nitric oxide synthase expression in RAW 264.7 macrophages.

Authors:  B Hinz; K Brune; T Rau; A Pahl
Journal:  Pharm Res       Date:  2001-02       Impact factor: 4.200

4.  Evaluation of flurbiprofen urinary ratios as in vivo indices for CYP2C9 activity.

Authors:  N K Zgheib; R F Frye; T S Tracy; M Romkes; R A Branch
Journal:  Br J Clin Pharmacol       Date:  2006-10-19       Impact factor: 4.335

5.  Flurbiprofen concentration in soft tissues is higher after topical application than after oral administration.

Authors:  Shuken Kai; Eiji Kondo; Yasuyuki Kawaguchi; Nobuto Kitamura; Kazunori Yasuda
Journal:  Br J Clin Pharmacol       Date:  2013-03       Impact factor: 4.335

6.  Use of a robust dehydrogenase from an archael hyperthermophile in asymmetric catalysis-dynamic reductive kinetic resolution entry into (S)-profens.

Authors:  Jacob A Friest; Yukari Maezato; Sylvain Broussy; Paul Blum; David B Berkowitz
Journal:  J Am Chem Soc       Date:  2010-05-05       Impact factor: 15.419

7.  NSAIDs and enantiomers of flurbiprofen target gamma-secretase and lower Abeta 42 in vivo.

Authors:  Jason L Eriksen; Sarah A Sagi; Tawnya E Smith; Sascha Weggen; Pritam Das; D C McLendon; Victor V Ozols; Kevin W Jessing; Kenton H Zavitz; Edward H Koo; Todd E Golde
Journal:  J Clin Invest       Date:  2003-08       Impact factor: 14.808

8.  Effects of flurbiprofen enantiomers on pain-related chemo-somatosensory evoked potentials in human subjects.

Authors:  J Lötsch; G Geisslinger; P Mohammadian; K Brune; G Kobal
Journal:  Br J Clin Pharmacol       Date:  1995-10       Impact factor: 4.335

Review 9.  Clinical pharmacokinetics of flurbiprofen and its enantiomers.

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

10.  R-flurbiprofen improves tau, but not Aß pathology in a triple transgenic model of Alzheimer's disease.

Authors:  Bruce G Jenkins; Alpaslan Dedeoglu; Isabel Carreras; Ann C McKee; Ji-Kyung Choi; Nurgul Aytan; Neil W Kowall
Journal:  Brain Res       Date:  2013-10-22       Impact factor: 3.252

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