Dimethocaine is a synthetic cocaine-derived local anesthetic with stimulant properties. It acts primarily as a dopamine reuptake inhibitor and voltage-gated sodium channel blocker, producing cocaine-like but generally less intense effects. Despite being perceived as milder, it carries substantial cardiovascular and tissue toxicity risks. Metabolism is dominated by NAT2-mediated N-acetylation, with additional contributions from multiple cytochrome P450 enzymes, resulting in significant inter-individual variability and elevated risk for slow acetylators.