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Pharmacokinetics of oxiracetam following intravenous and oral administration in healthy volunteers

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Summary

The kinetics of oxiracetam after single intravenous and oral doses (2000 mg) were investigated in four healthy volunteers. Following intravenous administration, the decline in serum levels showed a prolonged, rapid phase followed by a delayed terminal phase. Mean residence times ranged from 3.9 to 6.5 h. Volumes of distribution ranged from 0.9 to 1.81 · kg−1, whereas clearance values ranged from 100 to 119 ml·.h−1· kg -1 More than 90% of the intravenous dose was recovered unchanged in the urine within 48 h. Oral administration resulted in peak levels within 1–2 h; thereafter, the decline in serum levels showed a pattern similar to that observed after the intravenous dose — almost 50% of the oral dose was excreted in the urine within 6 h. The absolute availability of oral oxiracetam was 75 ± 7%.

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References

  1. Banfi S., Cornelli U. and Carpi C. (1977): Pharmacological study on learning and memory tests of a new compound : 4-hydroxy-2-oxo-l-pyrrolidinacetamide (ISF 2522). VI Int. Meeting Int. Society for Neurochemistry, Copenhagen, 21–26 August 1977. 274

  2. Banfi S., Semeraro C, Allievi E., Fonio W. and Dorigotti L. (1981): Impaired learning rate of SH rats with cerebrovascular lesions: effect of oxiracetam (ISF 2522), a new nootropic agent. Int. Symp. on Cerebrovascular Diseases, Gardone, 2–4 July 1981.

  3. Fratini F., Teza E., Gaiti A., Porcellati G. (1977): The effect on brain metabolism of 4-hydroxy-2-oxo-l-pyrro-Iidinacetamide. VI Int. Meeting Int. Society for Neuro-chemistry, Copenhagen, 21–26 August 1977.

  4. Pedata F., Moroni F., Banfi S. and Pepeu G. (1983): Effects of nootropic drugs on brain cholinergic mechansism: biochemical and behavioral investigations. Int. Conference on the Dynamics of Cholinergic Mechanisms, Ogleby, West Virginia, 30 October–4 November 1983.

  5. Itil T.M., Soldatos C, Bozak M., Ramadanoglu E., Dayican G., Morgan V. and Menon G.N. (1979): Curr. Ther. Res., CNS effects of ISF 2522, a new nootropic (a phase I safety and CNS-efficacy study with quantitative pharmaco-EEG and pharmaco-psychology),26, 525–538.

    Google Scholar 

  6. Itil T.M., Menon G.N., Bozak M. and Songar A. (1982): Drug Develop. Res., The effects of oxiracetam (ISF 2522) in patients with organic brain syndrome (a doubleblind controlled study with piracetam),2, 447–461.

    Article  Google Scholar 

  7. Perucca E. and Richens A. (1979): Br. J. Clin. Pharmacol., Reduction of oral bioavailability of lignocaine by induction of first-pass metabolism in epileptic patients,5, 21–31.

    Google Scholar 

  8. Wagner J.G. (1969): Pharmacokinetics, Richards Laboratories, Grosse Point.

  9. Benet L.Z. and Galeazzi R.L. (1979): J. Pharm. Sei., Noncompartmental determination of the steady-state volume of distribution,68, 1071–1074.

    Article  CAS  Google Scholar 

  10. Riggs D.S. (1963): The mathematical approach to physiological problems, Williams and Wilkins, Baltimore.

    Google Scholar 

  11. Assael B.M., Banfi G., Appiani A.C., Edefonti A. and Jusko W.J. (1982): Eur. J. Clin. Pharmacol., Disposition of pulse dose of methylprednisolone in adult and paediatric patients with the nephrotic syndrome,23, 429–433.

    Article  CAS  PubMed  Google Scholar 

  12. Oppenheimer J.H., Schwartz J.L. and Surks M.l. (1975): J. Clin. Endocrinol. Metab., Determination of common parameters of iodothyronine metabolism and distribution in man by noncompartmental analysis,41, 319–324.

    Article  CAS  PubMed  Google Scholar 

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Perucca, E., Albrici, A., Gatti, G. et al. Pharmacokinetics of oxiracetam following intravenous and oral administration in healthy volunteers. European Journal of Drug Metabolism and Pharmacokinetics 9, 267–274 (1984). https://doi.org/10.1007/BF03189650

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