On the 'micro'-pharmacodynamic and pharmacokinetic mechanisms that contribute to long-lasting drug action.

Introduction: Optimal drug therapy often requires continuing high levels of target occupancy. Besides the traditional pharmacokinetic (PK) contribution thereto, drug-target interactions that comprise successive 'microscopic' steps as well as the intervention of the cell membrane and other 'micro'-anatomical structures nearby may help attaining this objective.

Areas Covered: This article reviews the 'micro'-pharmacodynamic (PD) and PK mechanisms that may increase a drug's residence time.