Abstract
The kinetics at steady state of prednisone and its metabolite prednisolone were determined in nine nephrotic children during the active phase of the disease and in remission. There were no differences in serum prednisone levels between the two occasions. Prednisone levels were lower than prednisolone levels. Total serum prednisolone levels were significantly lower during the active phase than in remission (AUC: 2452 +/- 207 vs 3392 +/- 293 ng ml-1 h respectively). Half-life values were similar on both occasions. The binding of prednisolone to serum proteins was markedly impaired during the active phase as compared to the remission. Free fraction values correlated positively with total drug concentration. A negative correlation between free fraction and serum albumin level was found during the active phase. Free prednisolone levels during the active phase did not differ significantly from those observed during remission (AUC: 937 +/- 128 vs 847 +/- 81 ng ml-1 h respectively). These data indicate that pharmacokinetic changes are unlikely to be responsible for alterations in steroid responsiveness in nephrotic patients with hypoalbuminaemia.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Frey B. M., Frey F. J. Estimation of transcortin concentration by measurements of plasma protein-binding of prednisolone and by electroimmunodiffusion. Br J Clin Pharmacol. 1982 Feb;13(2):245–249. doi: 10.1111/j.1365-2125.1982.tb01370.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Frey F. J., Frey B. M. Altered prednisolone kinetics in patients with the nephrotic syndrome. Nephron. 1982;32(1):45–48. doi: 10.1159/000182800. [DOI] [PubMed] [Google Scholar]
- Jusko W. J., Rose J. Q. Monitoring prednisone and prednisolone. Ther Drug Monit. 1980;2(2):169–176. doi: 10.1097/00007691-198004000-00011. [DOI] [PubMed] [Google Scholar]
- Lewis G. P., Jusko W. J., Graves L., Burke C. W. Prednisone side-effects and serum-protein levels. A collaborative study. Lancet. 1971 Oct 9;2(7728):778–780. doi: 10.1016/s0140-6736(71)92738-3. [DOI] [PubMed] [Google Scholar]
- Pickup M. E. Clinical pharmacokinetics of prednisone and prednisolone. Clin Pharmacokinet. 1979 Mar-Apr;4(2):111–128. doi: 10.2165/00003088-197904020-00004. [DOI] [PubMed] [Google Scholar]
- Riva R., Albani F., Baruzzi A., Galvani I., Perucca E. Determination of unbound valproic acid concentration in plasma by equilibrium dialysis and gas--liquid chromatography: methodological aspects and observations in epileptic patients. Ther Drug Monit. 1982;4(4):341–352. doi: 10.1097/00007691-198212000-00003. [DOI] [PubMed] [Google Scholar]
- Rocci M. L., Jr, Assael B. M., Appiani A. C., Edefonti A., Jusko W. J. Effect on nephrotic syndrome on absorption and disposition of prednisolone in children. Int J Pediatr Nephrol. 1982 Sep;3(3):159–166. [PubMed] [Google Scholar]
- Rose J. Q., Jusko W. J. Corticosteroid analysis in biological fluids by high-performance liquid chromatography. J Chromatogr. 1979 Mar 1;162(3):273–280. doi: 10.1016/s0378-4347(00)81514-5. [DOI] [PubMed] [Google Scholar]
- SARETT L. H., PATCHETT A. A., STEELMAN S. L. THE EFFECTS OF STRUCTURAL ALTERATION ON THE ANTI-INFLAMMATORY PROPERTIES OF HYDROCORTISONE. Fortschr Arzneimittelforsch. 1963;5:11–153. doi: 10.1007/978-3-0348-7047-4_1. [DOI] [PubMed] [Google Scholar]
- Steele W. H., Hawksworth G. M., Barber H. E. The binding of prednisolone in human serum and to recrystallized human albumin in vitro. Br J Clin Pharmacol. 1982 Nov;14(5):667–672. doi: 10.1111/j.1365-2125.1982.tb04954.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Wagner J. G., Wexler D., Ağabeyoğlu I. T., Bergstrom R. F., Sakmar E., Kay D. R. Plasma protein-binding parameters of prednisolone in immune disease patients receiving long-term prednisone therapy. J Lab Clin Med. 1981 Apr;97(4):487–501. [PubMed] [Google Scholar]