Glucocorticoids Flashcards
Cortisol
- glucocorticoid activity
- mineralocorticoid activity
- duration
-1
-1
short
Prednisone
- glucocorticoid activity
- mineralocorticoid activity
- duration
- 4
- 0.3
- medium
Triamcinolone
- glucocorticoid activity
- mineralocorticoid activity
- duration
- 5
- 0
- intermediate
Betamethasone
- glucocorticoid activity
- mineralocorticoid activity
- duration
- 25
- 0
- long-acting
Dexamethasone
- glucocorticoid activity
- mineralocorticoid activity
- duration
- 30
- 0
- long-acting
What are the cellular effects of glucocorticoids? (3)
1) decrease leukocyte migration (decreased integrins)
2) increase lysosomal membrane stability (decreased phagocytosis)
3) decrease capillary permeability
What are the biochemical effects of glucocorticoids (4)
1) inhibit PLA2 via increased lipocortin expression > decreased PGs and LTs
2) decreased expression of COX2
3) Decreased platelet-activating factor
4) decreased interleukins (esp IL2)
use of glucocorticoids
anti-inflammatory, immunosuppression
Side effects of glucocorticoids
increased cortisol
Glucocorticoid effect on pituitary
Suppress ACTH release > could cause a shock like syndrome if stopped abruptly
Glucocorticoid effect on adrenal gland
iatrogenic cushingoid syndrome
Glucocorticoid effect on blood sugars
hyperglycemia due to increased gluconeogenesis from induced PEPCK > decreased wound healing and increased infection > increased risk glaucoma and cataracts due to sorbitol build up
Glucocorticoid effect on bone
Increased osteoclastic activity > osteoporosis and decreased skeletal growth in children
Glucocorticoid effect on GI system
increased gastric acid and pepsin release > ulcers
Glucocorticoid effect on kidneys
Increased ACTH > Increase RAAS > Na/H2O retention, edema, HTN
Which steroids are used to treat primary adrenal insufficiency? Which is the emergency treatment?
Hydrocortisone, dexamethasone***, fludrocortisone
What drug is used as the suppression test in Dx of cushing’s syndrome
dexamethasone
What steroids are used for primary aldosteronism? what is their mechanism of action?
spironolactone and eplerenone > aldo receptor antagonists
Aminoglutethide
- use
- mechanism
- treat Cushing’s
- blocks conversion of cholesterol to pregnenolone
Ketoconazole
- use
- mechanism
- treat Cushing’s
- potent, nonselective inhibitor of adrnal and gonadal steroid synthesis
Mitotane
- use
- mechanism
- treat Cushing’s but not really because it is DDT
- non-selective cytotoxin to adrenal cortex
Mifopristone
- use
- mechanism
- side effects
- Control in Cushing’s hyperglycemia
- progesterone receptor antagonist; GR antagonist at high concentrations
- fatigue, nausea, hypokalemia, arthralgia
Pasireotide
- use
- mechanism
- treat Cushing’s
- somatostatin analog, blocks release of ACTH
Metyrapone
- use
- mechanism
- treat Cushing’s
- Relatively selective inhibitor of 11-hydroxylation > interferes with cortisol and corticosterone synthesis
Which steroid is used as a mineralocorticoid replacement therapy with adrenal insufficiency
fludrocortisone
How do you combat the risk of glucocorticoid induced osteoporosis
give Ca, Vit D, and bisphosphonates
