Abstract
Serum protein binding of propylthiouracil (PTU) was measured by ultrafiltration in healthy and hyperthyroid patients. The serum protein binding in 12 euthyroid subjects was 76.2 +/- 1.2% (mean +/- s.d.), not significantly different from the values in 10 hyperthyroid patients: 76.6 +/- 1.3% Binding was unaffected by incubation time and temperatures between 25 and 37 degrees C, but increased from 76.5 to 79.1% when pH changed from 7.4 to 7.9. PTU is predominantly bound to albumin with two classes of binding groups with different number of binding sites and affinity. Displacement experiments showed interaction with acetylsalicylic acid, warfarin and phenylbutazone, but not with antipyrine and nortriptyline or other basic drugs.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Borgå O., Azarnoff D. L., Forshell G. P., Sjöqvist F. Plasma protein binding of tricyclic anti-depressants in man. Biochem Pharmacol. 1969 Sep;18(9):2135–2143. doi: 10.1016/0006-2952(69)90318-9. [DOI] [PubMed] [Google Scholar]
- Cooper D. S., Saxe V. C., Maloof F., Ridgway E. C. Studies of propylthiouracil using a newly developed radioimmunoassay. J Clin Endocrinol Metab. 1981 Feb;52(2):204–213. doi: 10.1210/jcem-52-2-204. [DOI] [PubMed] [Google Scholar]
- Feely J., Stevenson I. H., Crooks J. Altered plasma protein binding of drugs in thyroid disease. Clin Pharmacokinet. 1981 Jul-Aug;6(4):298–305. doi: 10.2165/00003088-198106040-00004. [DOI] [PubMed] [Google Scholar]
- Jansen J. A. Kinetics of the binding of salicylazosulfapyridine to human serum albumin. Acta Pharmacol Toxicol (Copenh) 1977 Nov;41(5):401–416. doi: 10.1111/j.1600-0773.1977.tb02151.x. [DOI] [PubMed] [Google Scholar]
- Johansen K., Andersen A. N., Kampmann J. P., Mølholm Hansen J. M., Mortensen H. B. Excretion of methimazole in human milk. Eur J Clin Pharmacol. 1982 Oct;23(4):339–341. doi: 10.1007/BF00613617. [DOI] [PubMed] [Google Scholar]
- Kampmann J. P., Johansen K., Hansen J. M., Helweg J. Propylthiouracil in human milk. Revision of a dogma. Lancet. 1980 Apr 5;1(8171):736–737. doi: 10.1016/s0140-6736(80)91233-7. [DOI] [PubMed] [Google Scholar]
- Kelly J. G., McDevitt D. G. Plasma protein binding of propranolol and isoprenaline in hyperthyroidism and hypothyroidism. Br J Clin Pharmacol. 1978 Aug;6(2):123–127. doi: 10.1111/j.1365-2125.1978.tb00836.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kurz H., Trunk H., Weitz B. Evaluation of methods to determine protein-binding of drugs. Equilibrium dialysis, ultrafiltration, ultracentrifugation, gel filtration. Arzneimittelforschung. 1977 Jul;27(7):1373–1380. [PubMed] [Google Scholar]
- Rosenthal H. E. A graphic method for the determination and presentation of binding parameters in a complex system. Anal Biochem. 1967 Sep;20(3):525–532. doi: 10.1016/0003-2697(67)90297-7. [DOI] [PubMed] [Google Scholar]
- Sakurai T., Tsuchiya S., Matsumaru H. Characteristics of protein binding of Thiobarbiturates and 6-n-propyl-2-thiouracil. Chem Pharm Bull (Tokyo) 1980 Feb;28(2):508–513. doi: 10.1248/cpb.28.508. [DOI] [PubMed] [Google Scholar]
- Storstein L. Protein binding of cardiac glycosides in disease states. Clin Pharmacokinet. 1977 May-Jun;2(3):220–233. doi: 10.2165/00003088-197702030-00006. [DOI] [PubMed] [Google Scholar]
- Sudlow G., Birkett D. J., Wade D. N. Further characterization of specific drug binding sites on human serum albumin. Mol Pharmacol. 1976 Nov;12(6):1052–1061. [PubMed] [Google Scholar]