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Phenytoin binding in healthy volunteers
M J Berg1, B E Ebert, R W Fincham
1College of Pharmacy, University of Iowa, Iowa City 52242.
Therapeutic Drug Monitoring
|December 1, 1987
Summary
Most individuals taking phenytoin have less than 10% unbound drug concentration in their serum. This finding is consistent across different doses, suggesting a common pharmacokinetic profile for this anti-seizure medication.
Area of Science:
- Pharmacology
- Clinical Pharmacokinetics
Background:
- The therapeutic efficacy of phenytoin, an anti-seizure medication, is primarily determined by its unbound concentration in serum.
- Previous literature suggests that approximately 10% of phenytoin in serum is unbound, a critical factor for its pharmacologic effect.
Purpose of the Study:
- To investigate the actual unbound serum concentration of phenytoin in healthy adult males.
- To compare the observed unbound phenytoin levels with the previously reported 10%.
Main Methods:
- A study involving 14 healthy male volunteers aged 20-35 years.
- Administration of two different doses of phenytoin to the participants.
- Measurement of unbound phenytoin concentrations in serum samples.
Main Results:
- In 13 out of 14 volunteers, the unbound phenytoin concentration was found to be less than 10%.
- This observation held true for the majority of subjects across the tested phenytoin doses.
- The results indicate a consistent pharmacokinetic profile in the study population.
Conclusions:
- The majority of healthy young males exhibit less than 10% unbound phenytoin in their serum.
- These findings support the established understanding of phenytoin's pharmacokinetics in this demographic.
- Further research may explore variations in unbound phenytoin levels in different patient populations or disease states.