Adrenal Corticosteroid Drugs Flashcards
Corticosteroids are only given in endocrine practice for what? (2)
Establish the diagnosis and cause of Cushing’s syndrome
Treatment of congenital adrenal hyperplasia (CAH)
Which 2 corticosteroids bind to the MR with equal affinity? What are their daily production rates?
Aldosterone (mineralcorticoid) - 10 mg/day
Cortisol (glucocorticoid) - 0.125 mg/day
…both bind the mineralcorticoid receptor with equal affinity
Which 2 corticosteroids are considered agonists?
Glucocorticoids (prednisone)
Mineralcorticoids (fludrocortisone)
What are the 2 subclasses of corticosteroid antagonists?
Receptor antagonists: glucocorticoid antagonists (mifepristone) and mineralcorticoid antagonists (spironolactone)
Synthesis inhibitors (ketoconazole)
What 2 enzymes are responsible for the conversion of active steroids (cortisol, corticosterone, prednisolone) to inert steroids (cortisone, 11-dehydrocorticosterone, prednisone)?
Active to inert = 11b-HSD2, 11b-dehydrogenase
What 2 enzymes are responsible for the conversion of inert steroids (cortisone, 11-dehydrocorticosterone, prednisone) of active steroids (cortisol, corticosterone, prednisolone)?
Inert to active = 11b-HSD1, 11-ketoreductase
What is the criteria for initiating cortisol therapy in medical emergencies? (3)
High doses can be given for a few days with little risk
Should not be given for more than a few days
Use must never replace or delay more specific therapies (Abx for shock, EPI for anti-histamines in anaphylaxis, etc.)
What must be considered before initiating chronic cortisol therapy?
Dose, frequency, route of administration
Chronic use presents significant risk
Common clinical applications of adrenal corticosteroids in endocrine conditions include: (2)
What are the drug combos are given for both?
Replacement therapy
- Primary adrenal insufficiency (Addison’s dz): glucocorticoid (hydrocortisone) and mineralcorticoid (fludrocortisone)
- Congenital adrenal hyperplasia (CAH): hydrocortisone + fludrocortisone
What are 4 common clinical applications for the use of adrenal corticosteroids in non-endocrine conditions?
Immunosuppression
Inflammatory/Allergic conditions
Skin diseases
Hypersensitivity reactions
What are 3 consequences of glucocorticoid use on the immune system and inflammation?
Decreased inflammation and its manifestations
Immune suppression
Decreased allergic/hypersensitivity reactions
How does administration of glucocorticoids affect the following:
Carbohydrate metabolism
Lipid metabolism
Protein metabolism
Carbohydrate metabolism - increased glucose levels
Lipid metabolism - increased lipid production and fat deposition
Protein metabolism - decreased AA uptake and decreased AA synthesis
Impaired activity/inhibition of which enzyme results in excessive activation of MR mediated by cortisol?
What are 2 known inhibitors of this enzyme?
11b-HSD2
Glycyrrhizin (licorice root extract)
Carbenoxolone
How can excess black licorice cause an increase in BP?
Licorice leads to an increase in cortisol 2 MR.
This causes Na+/water retention, and K+ loss which leads to hypertension.
Patient populations in which systemic glucocorticoid administration is problematic include…
Immunocompromised patients Diabetics Infections Peptic ulcers Cardiovascular dz Psychiatric conditions Osteoporosis Children
