A simple, specific and rapid radioimmunoassay (RIA) method for the assessment of non-protein bound ('free') phenytoin (DPH) concentrations in mixed saliva is described. Epileptic patients on maintenance phenytoin therapy have mixed saliva phenytoin concentrations similar to 'free' drug levels measured directly in serum or cerebrospinal fluid (CSF), Salivary phenytoin levels are approximately 10% of the total serum level in treated epileptic patients and in normal subjects after ingestion of a single oral dose. The half time of disappearance of phenytoin after 100 or 300 mg doses is 12.2 +/- 3.0 (SD) h in serum and 12.3 +/- 3.2 (SD) h in saliva. This method of assessing the biologically active fraction of the drug may be particularly valuable in situations where serum protein binding is abnormal or in drug interactions. It is also non-invasive and requires small sample volumes (20mul) and may therefore be valuable in paediatric practice and in pharmacokinetic studies in which multiple venepunctures would otherwise be required.

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