Pharmacology of Endocrinology Flashcards
What is metyrapone used for?
- Control of Cushing’s syndrome prior to surgery
- Control of Cushing’s syndrome after radiotherapy
What is the primary drug target of metyrapone?
- 11β-hydroxylase
- 11-deoxycortisol
What is the drug target type of metyrapone?
- Enzyme antagonist
What is the location of action of metyrapone?
- Zona fasciculata of the adrenal glands
What is the mechanism of action of metyrapone?
- Inhibition of 11β-hydroxylase
- Inhibit cortisol
- Inhibit 11-deoxycortisol
- Inhibit corticosterone
What are the main adverse effects of ketoconazole (1)?
-
Liver toxicity
- Need to monitor liver function weekly
What is ketoconazole used for?
- Control of Cushing’s syndrome prior to surgery
What is the primary drug target of ketoconazole?
- 17α-hydroxylase
What is the drug target type of ketoconazole?
- Enzyme antagonist
What is the location of action of ketoconazole?
- Adrenal glands
What is the mechanism of action of ketoconazole?
- Inhibition of 17α-hydroxylase
- Inhibit cortisol
What are the main adverse effects of metyrapone (2)?
- Hypertension
- Hirsutism
What is spinolactone used for?
- Potassium sparing diuretic for primary hypoaldosteronism
What is the primary drug target of spinolactone?
- Mineralocorticoid Receptor (MR)
What is the drug target type of spinolactone?
- Receptor antagonist
What is the location of action of spinolactone?
- Distal convoluted tubule
What is the mechanism of action of spinolactone?
- Inhibit Mineralocorticoid Receptor (MR)
- Inhibit aldosterone dependent sodium potassium exchange channels
- Increase in Na+ retention
- Increase in K+ secretion
- Increase in water secretion
What are the main adverse effects of spinolactone (2)?
- Menstrual irregularities (+ve progesterone receptor)
- Gynaecomastia (-ve androgen receptor)
