Local anesthetics play a crucial role in aesthetic procedures, offering temporary pain relief while preserving recipient’s consciousness. They are widely used in procedures such as laser treatments, injectable therapies, chemical peels, and microneedling. This review explores the mechanisms of action, pharmacokinetics, formulations, and safety considerations of these agents, emphasizing their influence on procedural outcomes and patient comfort. Local anesthetics work by inhibiting sodium ion channels, preventing nerve signal transmission. Their efficacy depends on factors like chemical composition, lipid solubility, pKa, and the tissue environment. Common formulations include creams, gels, patches, and sprays, each tailored to specific applications and procedural needs. Safety concerns, including systemic toxicity and allergic reactions, highlight the importance of appropriate dosing and formulation choice. Recent advancements, such as nanotechnology and enhanced delivery systems, promise to improve anesthetic performance and safety. This review underscores the indispensable role of local anesthetics in modern aesthetic practice.