This episode provides a comprehensive review of methimazole for clinical endocrinologists, focusing on its historical context, pharmacological profile, and practical management strategies. We examine its mechanism of action, specifically the inhibition of thyroid peroxidase to block iodine organification and coupling, alongside its distinct pharmacokinetics that allow for once-daily dosing. The discussion covers precise titration strategies for mild to severe hyperthyroidism, monitoring protocols using thyroid function tests, and methods for tapering. Finally, we analyze the drug safety profile, differentiating minor cutaneous reactions from major idiosyncratic toxicities like agranulocytosis and cholestatic hepatotoxicity, while addressing first-trimester teratogenicity risks and pregnancy transitions.