Steroids Flashcards
What effects do glucocorticoids have?
Primary effects on carbohydrate and protein metabolism
Anti-inflammatory effects
Aldosterone, Cortisol and Estradiol are synthesized from what?
Cholesterol
Prednisolone, Dexamethasone, Fludrocortisone and Hydrocortisone (Cortisol) are in what class of drugs?
Synthetic corticosteroids
Which synthetic corticosteroids are salt-retaining?
Mineralocorticoids (Fludrocortisone, Desoxycorticosterone acetate)
Which mineralocorticoid is choice for replacement therapy?
Fludrocortisone
Cortisol synthesis is stimulated by what?
ACTH
Aldosterone synthesis is stimulated by what?
Angiotensin II and K+
Where are cortisol and aldosterone synthesized?
Adrenal cortex
Where does glucocorticoid synthesis regulation occur?
Hypothalamic-Pituitary-Adrenal Axis
What controls ACTH release?
CRH (Corticotropin Releasing Hormone) released from hypothalamic neurons
Where is ACTH released from?
Anterior pituitary
What does ACTH simulate?
Cortisol synthesis and release
How is glucocorticoid synthesis regulated?
- episodic secretion and circadian rhythm of ACTH
- stress responsiveness of the HPA axis
- feedback inhibition by cortisol of ACTH secretion
What is the mechanism of action of ACTH on cortisol secreting cells in the adrenal cortex?
- ACTH binds to receptor, adenylyl cyclase activated via Gs
- Increased cAMP activates PKA
- PKA phosphorylates cholesteryl ester hydrolase
- more free cholesterol formed and converted to pregnenolone in mitochondria
- products are shuttled between mitochondria and smooth endoplastic reticulum
What are the physiological actions of glucocorticoids?
Carbohydrate/Protein/Lipid metabolism
Maintain blood glucose levels during fasting
Calcium homeostasis
Cardiovascular system: HTN with prolonged high levels
Skeletal muscle wasting with prolonged high levels
CNS: excss or insufficiency
Endocrine system: decrease of secretion of growth hormone, increase in epinephrine synthesis, decrease in major hormone binding proteins