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The pharmacokinetics of intravenous and oral sulpiride in healthy human subjects

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Summary

The pharmacokinetics of sulpiride was studied in 6 healthy volunteers after intravenous and oral (tablets) administration of 100 mg. An open two- and in two subjects a three-compartment model was applied following intravenous administration. The average total distribution volume during the terminal slope was 2.72±0.66 l/kg and total systemic clearance was 415±84 ml/min. The serum half-life of the terminal slope following intravenous administration averaged 5.3 h (range 3.7–7.1 h) according to the two-compartment model. In two subjects the half-lives were 11.0 and 13.9 h when the three-compartment model was applied. Determination of urinary excretion rates of unchanged sulpiride indicated a half-life of 7.15 h. Following intravenous administration, 70±9% of the dose was recovered unchanged in urine within 36 h; the mean renal clearance was 310±91 ml/min. Sulpiride was absorbed slowly, with peak concentrations appearing between 3 and 6 h after oral administration. The recovery of unchanged drug in urine following oral administration was 15±5% of the dose, with a mean renal clearance of 223±47 ml/min. The bioavailability determined from combined plasma and urine data was only 27±9%. The low bioavailability was probably due to incomplete absorption.

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References

  • Alfredsson G, Sedvall G, Wiesel F-A (1979) Quantitative analysis of sulpiride in body fluids by high performance liquid chromatography with fluorescence detection. J Chromatogr 164: 187–193

    Google Scholar 

  • Bellomo LE, Fernandez H (1972) Double-blind study of sulpiride in psychotic patients. Psychiatric and psychological-clinical evaluation. Minerva Psiq Argentina 1: 29–50

    Google Scholar 

  • Boxenbaum HG, Riegelman S, Elashoff RM (1974) Statistical estimation in pharmacokinetics. J Pharmacol Biopharm 2: 123–248

    Google Scholar 

  • Dixon WJ (1975) BMDP-Biomedical Computers Programs. University of California Press, Berkeley, pp 541–572

    Google Scholar 

  • Ekstrand J, Ehrnebo M, Boréus LO (1978) Fluoride bioavailability after intravenous and oral administration: Importance of renal clearance and urine flow. Clin Pharmacol Ther 23: 329–337

    Google Scholar 

  • Gibaldi M, Perrier D (1975) Pharmacokinetics. Marcel Dekker, New York, pp 48–96

    Google Scholar 

  • Imondi AR, Alam AS, Brennan JJ, Hagerman LM (1978) Metabolism of sulpiride in man and rhesus monkeys. Arch Int Pharmacodyn Ther 232: 79–91

    Google Scholar 

  • Kleimola T, Leppänen O, Kanto J, Mäntylä R, Syvälahti F (1976) Spectrophotofluorometric method for quantitative determination of sulpiride in human plasma and urine. Ann Clin Res 8: 104–110

    Google Scholar 

  • Loo TL, Tanner BB, Housholder GE, Shepard BJ (1968) Some pharmacokinetic aspects of 5-(Demethyltriazeno)-imidazole-4-carboxamide in the dog. J Pharm Sci 57: 2126–2131

    Google Scholar 

  • Nishiura M (1976) Clinical-pharmacological studies of sulpiride. Current Ther Res 20: 164–172

    Google Scholar 

  • Pinto CAC (1972) Sulpiride in schizophrenia. Double-blind study. Bol Psyquiatr 5: 103–142

    Google Scholar 

  • Sugnaux FR, Benakis A (1978) Metabolism of sulpiride: Determination of the chemical structure of its metabolites in rat, dog and man. Eur J Drug Metab Pharmacokinet 4: 235–248

    Google Scholar 

  • Toru M, Shimazono Y, Miyasaka M, Kokubo T, Mori Y, Nasu T (1972) A double-blind comparison of sulpiride with chlorpromazine in chronic schizophrenia. J Clin Pharmacol 12: 221–229

    Google Scholar 

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Wiesel, F.A., Alfredsson, G., Ehrnebo, M. et al. The pharmacokinetics of intravenous and oral sulpiride in healthy human subjects. Eur J Clin Pharmacol 17, 385–391 (1980). https://doi.org/10.1007/BF00558453

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  • DOI: https://doi.org/10.1007/BF00558453

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