Steroid Synthesis Inhibitors

Question 1

Aminoglutethimide MOA

Answer 1

Blocks conversion of cholesterol to pregnelone

Reduces prod of all steroid hormone

Question 2

Aminoglutethimide indications

Answer 2

Breast CA b4 tamoxifen and aromatase inhibitors

Adrenocortocal CA

Question 3

Aminoglutethimide side effects

Answer 3

Drowsiness

GI upset

Question 4

Ketoconazole MOA

Answer 4

P450 inhibition

Reduces synthesis of adrenal and sex hormones

Question 5

Ketoconazole indications

Answer 5

Antifungal drug

Cushing’s syndrome

Suppresses androgenic hair loss

Prostate CA

Question 6

Ketoconazole side effects

Answer 6

Hepatotoxicity

Gynecomastia in males

Question 7

Metyrapone MOA

Answer 7

Inhibition of steroid 11-hydroxylation

Relatively selectively suppresses formation of cortisol and corticosterone

Question 8

Metyrapone indications

Answer 8

Cushing’s syndrome

Pregos***** (only Drug for Cushing safe for them)

Question 9

Metyrapone side effects

Answer 9

Accumulation of 11-deoxycortisol —> increased aldosterone -> Na+ and H2O retention

Accumulation of 11-deoxycortisol -> increased androgens -> hirsutism in women

GI upset

Dizziness

Question 10

Mitotane MOA

Answer 10

Na+ ionofore, Ca2+ ionofore

Protein kinase C and adenylyl cyclase inhibitor

Non-selective cytotoxic action on adrenal cortex

Question 11

Mitotane indications

Answer 11

Adrenal carcinoma

Question 12

Mitotane side effects

Answer 12

Depression, somnolence

GI upset

Rashes