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Single dose pharmacokinetics of fenspiride hydrochloride: phase I clinical trial

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Summary

The absolute bioavailability of fenspiride has been studied in twelve healthy volunteers. It was administered IV and orally in single doses of 80 mg fenspiride hydrochloride according to a randomised crossover pattern.

Following IV administration, the plasma clearance of fenspiride was about 184 ml·min−1, and its apparent volume of distribution was moderately large (2151).

When given orally as a tablet, fenspiride exhibited fairly slow ab- sorption; the maximum plasma concentration (206 ng·ml−1) was achieved 6 h after administration. The absolute bioavailability was almost complete (90%). The tablet had slow release characteristics. The elimination half-life obtained from the plasma data was 14 to 16 h independent of the route of administration.

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References

  1. Carre P, Pipy B, Pinelli E, Forgue MF, Beraud M, Didier A, Leophonte P (1991) In vitro effects of fenspiride on the production of free oxygen radicals, prostaglandins and leukotrienes by guinea-pig alveolar macrophages. Eur Respir Rev 1: 79–85

    Google Scholar 

  2. Chapelain B, Neliat G, Bodinier MC, Jean T, Evrard Y, Gargouil YM (1991) Role of the epithelium in the action of fenspiride on the isolated guinea-pig and rat trachea. Eur Respir Rev 1: 86–92

    Google Scholar 

  3. Evrard Y, Kato G, Bodinier MC, Chapelain B (1991) Fenspiride and inflammation in experimental pharmacology. Eur Respir Rev 1: 93–100

    Google Scholar 

  4. Giacchero G, Taranger J (1982) Pneumorel retard au long cours dans le traitement des bronchites chroniques. Vie Méd 63: 791–794

    Google Scholar 

  5. Kafe H (1984) Intérêt du Pneumorel 80 mg dans le traitement de l'insuffisance respiratoire chronique. Vie Méd 65: 200–203

    Google Scholar 

  6. Turrisi E, Mea A, Bruno G, Vitagliano A (1984) Studio controllato del fenspiride ritardo in ambito pneumologico. Clin Ther 111: 339–346

    Google Scholar 

  7. Olivieri D, Del Donno M (1987) Etude de l'action du fenspiride sur la clairance mucociliaire chez le bronchitique chronique. JIM 96: 395–398

    Google Scholar 

  8. Leophonte P, Thack KS, Voigt JJ, Rouquet RM, Didier A (1986) Le fenspiride (Pneumorel 80 mg) dans le traitement des bronchopneumopathies chroniques obstructives. Vie Méd 23–24: 1047–1051

    Google Scholar 

  9. Akoun G, Arnaud F, Blanchon F, Botto JM, Cerf C, Clavier J, Derenne JP, Leophonte P, Nouvet G, Paramelle B, Patron P, Prefaut C, Verlardocchio JM (1991) Effects of fenspiride on airway function and blood gases in stable COPD patients. Eur Respir Rev 1: 111–125

    Google Scholar 

  10. Evrard Y, Lhoste F, Advenier C, Duhault J (1986) Le fenspiride et le système broncho-pulmonaire: nouvelle approche pharmacologique. Semaine Hôp 62: 1375–1381

    Google Scholar 

  11. Megel H, Holmes P, Zalipsky J, Schemano I, Beiler JM (1973) Fenspiride 14C: its distribution, excretion and metabolism in the rat. Arch Int Pharmacodyn Ther 201: 90–99

    Google Scholar 

  12. Jeanniot JP, Chezaubernard C (1991) Pharmacokinetic properties of fenspiride: an update. Eur Resp Rev 1: 101–104

    Google Scholar 

  13. Sauveur C, Baune A, Vergnes N, Jeanniot JP (1989) Quantitative determination of fenspiride in human plasma and urine by liquid chromatography with electrochemical or ultraviolet detection J Pharm Biomed Anal 7: 1799–1804

    Google Scholar 

  14. Weiner DL (1986) NONLIN 84/PC NONLIN: software for the statistical analysis of nonlinear models. Methods Find Exp Clin Pharmacol 8: 625–628

    Google Scholar 

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Montes, B., Catalan, M., Roces, A. et al. Single dose pharmacokinetics of fenspiride hydrochloride: phase I clinical trial. Eur J Clin Pharmacol 45, 169–172 (1993). https://doi.org/10.1007/BF00315501

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