ABBREVIATED KINETIC PROFILES IN AREA-UNDER-THE-CURVE MONITORING OF CYCLOSPORINE THERAPY - TECHNICAL NOTE

Background. The new microemulsion formulation of cyclosporine (CsA-ME) displays more consistent pharmacokinetic properties than the original formulation and may allow successful implementation of an abbreviated area-under-the-curve (AUC) strategy. Methods. Here we compared two Li mited sampling strategies in order to define the one that best predict s AUC after CsA-ME in 51 renal transplant recipients with stable renal function. Pharmacokinetics were based on analysis of blood samples co llected over 12 hours after drug administration by high-performance li quid chromatography (HPLC). Predicted AUC was estimated by using a thr ee-point (0, 1 and 3 hr) or a two-paint (2 and 6 hr or 0 and 2 hr) sam pling strategy. Results. A simplified strategy with three time points of blood collection at 0, 1, and 3 hours after CsA-ME allowed adequate and accurate prediction of the daily exposure to CsA. AUC prediction with two-point sampling at 2 and 6 hours was less good with a very lar ge error in prediction (only 59% of the estimated AUC were within the accepted range). This limitation was even more evident when the 0 and 2 hour time points were examined, in which only 51% of AUC estimates w ere included in the accepted range of variation (-10 to 10%). Conclusi ons. A limited strategy of three-point sampling taken early after dosi ng allows an excellent and perfectly reliable prediction of the actual AUG.