The constraints of intensive multifactorial management of type 2 diabetes dictate a need for effective, well-tolerated agents with simple administration regimens. Sulfonylureas remain the most frequently used agents, and represent a rational approach when consideration is given to the pathophysiology of this common condition. Trials of gliclazide modified release in varied populations have yielded very acceptable clinical results that support its first-line use in type 2 diabetes, including obese, elderly, and mild-to-moderate renal insufficient patients. The simplicity of its dose regimen and its efficacy and tolerance profile may significantly contribute to improving compliance.