Abstract:The pathogenesis of hyperthyroidism is relatively complicated. In clinical practice, diffuse toxic goiter accompanied with hyperthyroidism (as known as Graves¢ disease) is more common. The pharmaceutical treatment of Graves¢ disease includes antithyroid drugs (ATD), iodine, β-blocker, glucocorticoids and lithium carbonate. ATD are the main treatment for hyperthyroidism, and Methimazole (MMI) and propylthiouracil (PTU) are the two drugs which are most commonly used currently. Generally, ATD are safe and effective, though their clinical adverse reactions are also relatively common. These reactions are usually reversible and disappeared spontaneously when the drug is discontinued. However, the serious rare side effects also occur sometimes. MMI is usually preferred over PTU because it has significantly fewer adverse reactions in a dose-dependent fashion. MMI is the first choice for treating mild and moderate hyperthyroidism. Iodine is mainly used in hyperthyroidism crisis and before operation. Glucocorticoids are mainly used for Graves¢ ophthalmopathy and hyperthyroidism crisis. β-blocker is used to control the symptoms at initial treatment. Lithium carbonate is not commonly used, and only suitable for short-term treatment. The clinicians should evaluate comprehensively and individually to choose appropriate agents for better outcome, and closely monitor their efficiency and side effects.