Effective Loading Dose of Teicoplanin for Hypoalbuminemic Patients Based on Evaluation of Serum Concentration of Unbound Drug

Abstract

  Teicoplanin (TEIC) is active against Gram positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and Enterococcus spp.. TDM studies have indicated that serum TEIC concentrations are important for determining efficacy in patients. TEIC is known to be extensively bound to serum proteins such as human serum albumin. Therefore, the clinical pharmacokinetics of TEIC are expected to be considerably affected by protein binding with albumin. This study evaluated protein binding of TEIC in human serum, and determined the albumin-dependent relationship between the unbound and total serum TEIC concentrations in hypoalbuminemic patients. Consequently, more accurate and effective trough concentration ranges of TEIC were established, with effective unbound concentration over the minimum inhibitory concentration against MRSA (MIC₉₀). The effective loading doses of TEIC are proposed, especially in hypoalbuminemic patients on the basis of the unbound serum concentrations.