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Serum protein binding of propylthiouracil
British Journal of Clinical Pharmacology
|November 1, 1983
Summary
Propylthiouracil (PTU) serum protein binding is similar in healthy and hyperthyroid individuals. PTU primarily binds to albumin, with interactions observed with certain acidic drugs.
Area of Science:
- Pharmacokinetics
- Biochemistry
- Clinical Medicine
Background:
- Propylthiouracil (PTU) is a medication used to treat hyperthyroidism.
- Understanding drug-protein binding is crucial for determining drug efficacy and dosage.
- Limited data exists on PTU's specific binding characteristics in different thyroid states.
Purpose of the Study:
- To quantify and characterize serum protein binding of PTU in euthyroid and hyperthyroid subjects.
- To investigate factors influencing PTU binding, including pH and temperature.
- To identify potential drug interactions based on competitive binding to serum proteins.
Main Methods:
- Ultrafiltration technique used to measure PTU serum protein binding.
- Experiments conducted on serum from healthy and hyperthyroid patients.
- Binding assays performed under varying pH, temperature, and in the presence of other drugs.
Main Results:
- Serum protein binding of PTU was consistently high (approximately 76%) in both euthyroid and hyperthyroid subjects.
- Binding was stable across tested temperatures (25-37°C) and incubation times.
- PTU binding increased at higher pH (7.9) and showed competitive displacement with acidic drugs like warfarin and acetylsalicylic acid.
Conclusions:
- PTU exhibits significant and consistent serum protein binding, primarily to albumin.
- Thyroid status does not appear to significantly alter PTU's protein binding.
- Potential for drug interactions exists with co-administered acidic medications that bind to similar sites on albumin.