European Journal of Clinical Pharmacology

, Volume 17, Issue 5, pp 385–391 | Cite as

The pharmacokinetics of intravenous and oral sulpiride in healthy human subjects

  • F. -A. Wiesel
  • G. Alfredsson
  • M. Ehrnebo
  • G. Sedvall
Originals

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.

Key words

sulpiride pharmacokinetics serum clearance renal clearance bioavailability healthy volunteers 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. 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: 187–193Google Scholar
  2. Bellomo LE, Fernandez H (1972) Double-blind study of sulpiride in psychotic patients. Psychiatric and psychological-clinical evaluation. Minerva Psiq Argentina 1: 29–50Google Scholar
  3. Boxenbaum HG, Riegelman S, Elashoff RM (1974) Statistical estimation in pharmacokinetics. J Pharmacol Biopharm 2: 123–248Google Scholar
  4. Dixon WJ (1975) BMDP-Biomedical Computers Programs. University of California Press, Berkeley, pp 541–572Google Scholar
  5. 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: 329–337Google Scholar
  6. Gibaldi M, Perrier D (1975) Pharmacokinetics. Marcel Dekker, New York, pp 48–96Google Scholar
  7. Imondi AR, Alam AS, Brennan JJ, Hagerman LM (1978) Metabolism of sulpiride in man and rhesus monkeys. Arch Int Pharmacodyn Ther 232: 79–91Google Scholar
  8. 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: 104–110Google Scholar
  9. 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: 2126–2131Google Scholar
  10. Nishiura M (1976) Clinical-pharmacological studies of sulpiride. Current Ther Res 20: 164–172Google Scholar
  11. Pinto CAC (1972) Sulpiride in schizophrenia. Double-blind study. Bol Psyquiatr 5: 103–142Google Scholar
  12. 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: 235–248Google Scholar
  13. 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: 221–229Google Scholar

Copyright information

© Springer-Verlag 1980

Authors and Affiliations

  • F. -A. Wiesel
    • 1
  • G. Alfredsson
    • 1
  • M. Ehrnebo
    • 2
  • G. Sedvall
    • 1
  1. 1.Laboratory of Experimental Psychiatry, Department of PsychiatryKarolinska InstituteStockholmSweden
  2. 2.Karolinska PharmacyKarolinska HospitalStockholmSweden

Personalised recommendations