Adrenal Corticoid Drugs Flashcards
glucocorticoid agonist
prednisone
mineralocorticoid agonist
fludrocortison
Glucocorticoid receptor antagonist
mifepristone
mineralocorticoid receptor antagonist
spironolactone
corticosteroid synthesis inhibitor
ketoconazole
two therapeutic effects of corticosteroids
immunosuppression
anti-inflammatory
Problems with chronic corticosteroid use
cannot be given chronically without the risk of adverse events (infection, osteoporosis, weight gain, cushingoid appearance, etc)
Carbohydrate metabolism effects of glucocorticoids
- increased gluconeogenesis
- increased glucose output
- increased glycogen synthesis
- decreased glucose uptake –> development of hyperglycemia
Problem with diabetics and glucocorticoid use
hyperglycemia! (maybe fix with pramlintide?)
inhibitors of 11beta-HSD2 (2)
1) glycyrrhin (licorice root extract)
2) carbenoxolone
11beta-HSD2 action
converts active steroids to inactive steroids
result of inhibition of 11beta-HSD2
elevated blood pressure
Mitotane use
can treat cancer of the adrenal glands (adrenal cortical carcinoma)
short acting glucocorticoids (2) and duration of action
1) hydrocortisone (cortisol)
2) cortisone acetate
8 -12 hours
intermediate acting glucocorticoids (4) and duration of action
1) prednisone
2) prednisolone
3) methylprednisolone
4) triamcinolone
12 - 36 hours
long acting glucocorticoids (2) and duration of action
1) dexamethasone
2) betamethasone
36 to 72 hours
pharmacokinetics of prednisolone
duration of activity is longer than pharmacokinetic 1/2 of drug owing to gene transcription effects
Toxicities of prednisolone
adrenal suppression
mifepristone clinical applications
medical abortion
adverse effect mifepristone
vaginal bleeding in women
clinical use fludrocortisone
adrenal insufficiency (addison’s disease)
pharmacokinetics fludrocortisone
long duration of action
spironolactone pharmacoinetics
slow onset and offset (duration 24-28 hours)
adverse effects spironolactone
- hyperkalemia
- gynecomastia
- additive interaction with other K+ retaining drugs