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. 1984 Apr;17(4):411–415. doi: 10.1111/j.1365-2125.1984.tb02365.x

Pethidine binding in plasma: effects of methodological variables.

C La Rosa, L E Mather, D J Morgan
PMCID: PMC1463402  PMID: 6721987

Abstract

Several methodological variables potentially influencing the plasma protein binding of [14C]-pethidine in vitro were investigated using equilibrium dialysis and rigorous pH control. Ionic strength of buffer, pethidine concentration and 21 days of plasma samples frozen to -8 degrees C did not affect the outcome of the binding experiments. Unbound fraction decreased with increasing temperatures between 25 degrees C and 37 degrees C. Unbound fraction decreased with increased pH between pH 7.0 and 8.0; the mean unbound fraction at an equilibrium pH of 7.4 and at 37 degrees C was 0.58 (s.d. 0.03, n = 58). It is likely that previous reports of pethidine unbound fraction as being between 0.2 and 0.4 represent artefacts caused by inadequate pH control during dialysis.

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Selected References

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  1. Bower S. Plasma protein binding of fentanyl. J Pharm Pharmacol. 1981 Aug;33(8):507–514. doi: 10.1111/j.2042-7158.1981.tb13849.x. [DOI] [PubMed] [Google Scholar]
  2. Brinkschulte M., Breyer-Pfaff U. Binding of tricyclic antidepressants and perazine to human plasma. Methodology and findings in normals. Naunyn Schmiedebergs Arch Pharmacol. 1979 Jul;308(1):1–7. doi: 10.1007/BF00499712. [DOI] [PubMed] [Google Scholar]
  3. Brock A. Binding of digoxin to human serum proteins: influence of pH on the binding of digoxin to human albumin. Acta Pharmacol Toxicol (Copenh) 1974 Apr;34(4):260–266. doi: 10.1111/j.1600-0773.1974.tb03522.x. [DOI] [PubMed] [Google Scholar]
  4. Burney R. G., DiFazio C. A., Foster J. A. Effects of pH on protein binding of lidocaine. Anesth Analg. 1978 Jul-Aug;57(4):478–480. doi: 10.1213/00000539-197807000-00019. [DOI] [PubMed] [Google Scholar]
  5. Holmberg L., Odar-Cederlöf I., Nilsson J. L., Ehrnebo M., Boréus L. O. Pethidine binding to blood cells and plasma proteins in old and young subjects. Eur J Clin Pharmacol. 1982;23(5):457–461. doi: 10.1007/BF00605998. [DOI] [PubMed] [Google Scholar]
  6. Jackson A. J. Determination of meperidine blood to plasma concentration ratio (lambda) - effect of temperature and pH. Res Commun Chem Pathol Pharmacol. 1981 May;32(2):365–368. [PubMed] [Google Scholar]
  7. Jackson A. J., Miller A. K., Narang P. K. Human blood preservation: effect on in vitro protein binding. J Pharm Sci. 1981 Oct;70(10):1168–1169. doi: 10.1002/jps.2600701023. [DOI] [PubMed] [Google Scholar]
  8. Klotz U., McHorse T. S., Wilkinson G. R., Schenker S. The effect of cirrhosis on the disposition and elimination of meperidine in man. Clin Pharmacol Ther. 1974 Oct;16(4):667–675. doi: 10.1002/cpt1974164667. [DOI] [PubMed] [Google Scholar]
  9. Kristensen C. B., Gram L. F. Equilibrium dialysis for determination of protein binding or imipramine--evaluation of a method. Acta Pharmacol Toxicol (Copenh) 1982 Feb;50(2):130–136. doi: 10.1111/j.1600-0773.1982.tb00954.x. [DOI] [PubMed] [Google Scholar]
  10. Mather L. E., Tucker G. T., Pflug A. E., Lindop M. J., Wilkerson C. Meperidine kinetics in man. Intravenous injection in surgical patients and volunteers. Clin Pharmacol Ther. 1975 Jan;17(1):21–30. doi: 10.1002/cpt197517121. [DOI] [PubMed] [Google Scholar]
  11. Morgan D. J., Koay B. B., Paull J. D. Plasma protein binding of etidocaine during pregnancy and labour. Eur J Clin Pharmacol. 1982;22(5):451–457. doi: 10.1007/BF00542552. [DOI] [PubMed] [Google Scholar]
  12. Nation R. L. Meperidine binding in maternal and fetal plasma. Clin Pharmacol Ther. 1981 Apr;29(4):472–479. doi: 10.1038/clpt.1981.65. [DOI] [PubMed] [Google Scholar]
  13. Pond S. M., Kretschzmar K. M. Effect of phenytoin on meperidine clearance and normeperidine formation. Clin Pharmacol Ther. 1981 Nov;30(5):680–686. doi: 10.1038/clpt.1981.220. [DOI] [PubMed] [Google Scholar]
  14. Rochester C. L., Gammon D. E., Shane E., Bilezikian J. P. A radioreceptor assay for propranolol and 4-hydroxypropranolol. Clin Pharmacol Ther. 1980 Jul;28(1):32–39. doi: 10.1038/clpt.1980.127. [DOI] [PubMed] [Google Scholar]
  15. Wilting J., van der Giesen W. F., Janssen L. H. The effect of chloride on the binding of warfarin to albumin as a function of pH. Biochem Pharmacol. 1981 May 15;30(10):1025–1031. doi: 10.1016/0006-2952(81)90437-8. [DOI] [PubMed] [Google Scholar]

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