Medical therapy to control hypercortisolism in adrenal Cushing's syndrome is currently not the first-line therapy. However, in many clinical scenarios like pre-surgical treatment, in patients who are not suitable candidates for surgery or in patients with bilateral hyperplasia, medical therapy can be important representing the only viable treatment option. Adrenal steroidogenesis inhibitors and glucocorticoid receptor blockers have been used for many years: metyrapone, ketoconazole and mifepristone are in current use and effective. Mitotane can be used as well but is considered second-line therapy because of its high toxicity. Etomidate has a special position as emergency medication in severe hypercortisolism. New drugs are tested in prospective trials (levoketoconazole, osilidrostat and relacorilant) and might become effective alternatives to common drugs. Oher drugs - adrenal steroidogenesis inhibitors as well as glucocorticoid receptor antagonists - are currently tested in vitro.

目前，控制肾上腺库欣综合征中皮质醇过多症的药物治疗不是一线治疗。但是，在许多临床情况下，如手术前治疗，对于不适合手术的患者或双侧增生的患者，药物治疗可能是唯一可行的治疗方法，非常重要。肾上腺类固醇生成抑制剂和糖皮质激素受体阻滞剂已经使用了很多年：甲吡酮，酮康唑和米非司酮目前正在使用并且有效。也可以使用线粒体，但由于其毒性高，因此被认为是二线治疗。依托咪酯在严重皮质醇过多症中作为急救药物具有特殊地位。新药在前瞻性试验中进行了测试（左旋酮康唑，osilidrostat和relacorilant），并可能成为普通药物的有效替代品。Oher药物-肾上腺类固醇生成抑制剂以及糖皮质激素受体拮抗剂-目前正在体外测试。