Skip to main content
PMC home page
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1981 Mar;11(3):245–250. doi: 10.1111/j.1365-2125.1981.tb00528.x

Sex-related differences in the plasma protein binding of lignocaine and diazepam.

P A Routledge, W W Stargel, B B Kitchell, A Barchowsky, D G Shand
PMCID: PMC1401626  PMID: 7213526

Abstract

1 The percentage of lignocaine free in the plasma of ten females receiving oral contraceptive medication was significantly greater than in 17 males of similar age (18--42 years). 2 In the same subjects the percentage of diazepam free in plasma was significantly greater in the contraceptive treated group than in 11 contraceptive-free females and significantly greater in contraceptive-free females than in males. 3 The differences in lignocaine binding were almost completely attributable to changes in alpha 1-acid glycoprotein concentration, which is reduced by oestrogens. The binding of diazepam was significantly related to albumin, alpha 1-acid glycoprotein and non-esterified fatty acid concentrations which together were related to 55% of the variation in the binding of this basic compound.

Full text

PDF
246

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Abel J. G., Sellers E. M., Naranjo C. A., Shaw J., Kadar D., Romach M. K. Inter- and intrasubject variation in diazepam free fraction. Clin Pharmacol Ther. 1979 Aug;26(2):247–255. doi: 10.1002/cpt1979262247. [DOI] [PubMed] [Google Scholar]
  2. Giudicelli J. F., Tillement J. P. Influence of sex on drug kinetics in man. Clin Pharmacokinet. 1977 May-Jun;2(3):157–166. doi: 10.2165/00003088-197702030-00001. [DOI] [PubMed] [Google Scholar]
  3. Hao Y. L., Wickerhauser M. Development of large-scale fractionation methods. IV. A simple method for the large-scale preparation of alpha1-acid glycoprotein. Biochim Biophys Acta. 1973 Sep 21;322(1):99–108. doi: 10.1016/0005-2795(73)90180-3. [DOI] [PubMed] [Google Scholar]
  4. Kim H. J., Kalkhoff R. K. Sex steroid influence on triglyceride metabolism. J Clin Invest. 1975 Oct;56(4):888–896. doi: 10.1172/JCI108168. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Kissebah A. H., Harrigan P., Wynn V. Mechanism of hypertriglyceridaemia associated with contraceptive steroids. Horm Metab Res. 1973 May;5(3):184–190. doi: 10.1055/s-0028-1093969. [DOI] [PubMed] [Google Scholar]
  6. Laurell C. B., Kullander S., Thorell J. Plasma protein changes induced by sequential type of contraceptive steroid pills. Clin Chim Acta. 1969 Aug;25(2):294–296. doi: 10.1016/0009-8981(69)90270-8. [DOI] [PubMed] [Google Scholar]
  7. Nilsen O. G., Leren P., Aakesson I., Jacobsen S. Binding of quinidine in sera with different levels of triglycerides, cholesterol, and orosomucoid protein. Biochem Pharmacol. 1978 Mar 15;27(6):871–876. doi: 10.1016/0006-2952(78)90411-2. [DOI] [PubMed] [Google Scholar]
  8. Roberts R. K., Desmond P. V., Wilkinson G. R., Schenker S. Disposition of chlordiazepoxide: sex differences and effects of oral contraceptives. Clin Pharmacol Ther. 1979 Jun;25(6):826–831. doi: 10.1002/cpt1979256826. [DOI] [PubMed] [Google Scholar]
  9. Routledge P. A., Barchowsky A., Bjornsson T. D., Kitchell B. B., Shand D. G. Lidocaine plasma protein binding. Clin Pharmacol Ther. 1980 Mar;27(3):347–351. doi: 10.1038/clpt.1980.46. [DOI] [PubMed] [Google Scholar]
  10. Routledge P. A., Kitchell B. B., Bjornsson T. D., Skinner T., Linnoila M., Shand D. G. Diazepam and N-desmethyldiazepam redistribution after heparin. Clin Pharmacol Ther. 1980 Apr;27(4):528–532. doi: 10.1038/clpt.1980.74. [DOI] [PubMed] [Google Scholar]
  11. Sampson D., Hensley W. J. A rapid gas chromatographic method for the quantitation of underivatised individual free fatty acids in plasma. Clin Chim Acta. 1975 May 15;61(1):1–8. doi: 10.1016/0009-8981(75)90391-5. [DOI] [PubMed] [Google Scholar]
  12. Song C. S., Merkatz I. R., Rifkind A. B., Gillette P. N., Kappas A. The influence of pregnancy and oral contraceptive steroids on the concentration of plasma proteins. Studies with a quantitative immunodiffusion method. Am J Obstet Gynecol. 1970 Sep 15;108(2):227–231. doi: 10.1016/0002-9378(70)90301-7. [DOI] [PubMed] [Google Scholar]
  13. Spector A. A., Santos E. C., Ashbrook J. D., Fletcher J. E. Influence of free fatty acid concentration on drug binding to plasma albumin. Ann N Y Acad Sci. 1973 Nov 26;226:247–258. doi: 10.1111/j.1749-6632.1973.tb20486.x. [DOI] [PubMed] [Google Scholar]
  14. Tsutsumi E., Inaba T., Mahon W. A. The displacing effect of a fatty acid on the binding of diazepam to human serum albumin. Biochem Pharmacol. 1975 Jul 15;24(13-14):1361–1362. doi: 10.1016/0006-2952(75)90355-x. [DOI] [PubMed] [Google Scholar]
  15. Vermeulen A., Verdonck L. Studies on the binding of testosterone to human plasma. Steroids. 1968 May;11(5):609–635. [PubMed] [Google Scholar]
  16. Wong G. B., Sellers E. M. Intravascular factors affecting diazepam binding to human serum albumin. Biochem Pharmacol. 1979 Nov 15;28(22):3265–3270. doi: 10.1016/0006-2952(79)90120-5. [DOI] [PubMed] [Google Scholar]

Articles from British Journal of Clinical Pharmacology are provided here courtesy of British Pharmacological Society

RESOURCES