Endogenous Cushing Syndrome Medication

Updated: May 09, 2017
  • Author: Ha Cam Thuy Nguyen, MD; Chief Editor: Romesh Khardori, MD, PhD, FACP  more...
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Medication

Medication Summary

The goal of pharmacotherapy is to reduce morbidity and prevent complications.

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Somatostatin Analogs

Class Summary

Somatostatin analogs bind and activate human somatostatin receptors resulting in inhibition of ACTH secretion, which leads to decreased cortisol secretion.

Pasireotide (Signifor)

Pasireotide is a cyclohexapeptide somatostatin analog that binds to human somatostatin receptors (HSSTs) 1, 2, 3, 4 and 5. This action results in the inhibition of ACTH secretion, which in turn leads to decreased cortisol secretion. It is indicated for treatment of adults with Cushing disease in whom pituitary surgery is not an option or has not been curative.

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Adrenal steroid inhibitors

Class Summary

These agents inhibit key steps in the synthesis of adrenal glucocorticoids.

Metyrapone (Metopirone)

Inhibitor of endogenous adrenal corticosteroid synthesis. Inhibits 11-B-hydroxylation reaction in the adrenal cortex.

Ketoconazole

Ketoconazole is an imidazole broad-spectrum antifungal agent that inhibits cytochrome P450 enzyme system and 17,20-lyase. These enzymes are involved in the synthesis and catabolism of steroids. Ketoconazole may also inhibit the pituitary corticotroph function, which in turn inhibits ACTH secretion.

Etomidate (Amidate)

Etomidate, an imidazole-derivative anesthetic agent, decreases corticosteroid synthesis in the adrenal cortex by reversibly inhibiting 17-20 yase and 11-beta-hydroxylase at non-hypnotic doses. It is used intravenously at 0.3 mg/kg/h. Its use is limited by the requirement for administration by intravenous route. However, it rapidly decreases cortisol concentration and may be used as an adjunct to impending surgical procedure.

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Antineoplastic agents, other

Class Summary

Agents in this class that decrease cortisol production and alter the peripheral metabolism of steroids may reduce morbidity.

Mitotane (Lysodren)

Mitotane is an adrenolytic agent that acts by inhibiting 11-beta hydroxylase and several cholesterol side-chain cleavage enzymes. This drug also leads to mitochondrial destruction and necrosis of adrenocortical cells in the zona fasciculata and reticularis.

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Cortisol Receptor Blockers

Class Summary

Cortisol receptor blockers inhibit the effect of cortisol at the glucocorticoid receptor.

Mifepristone (Korlym, Mifeprex, Ru486)

Mifepristone is an antiprogestational agent, which, at low doses competitively binds to the intracellular progesterone receptor while, at high doses, competitively binds to the glucocorticoid receptor. It helps to control hyperglycemia secondary to hypercortisolism in adult patients with endogenous Cushing syndrome who have type 2 diabetes mellitus or glucose intolerance and have failed surgery, or are not candidates for surgery.

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