Corticosteroids Flashcards
Are Hydrocortisone, Prednisone, and Methylprednisolone short to mediate, intermediate, or long-lasting glucocorticoids?
short to medium
Which drug is the only intermediate acting glucocorticoid?
Triamcinolone
Which drug is the only long-acting glucocorticoid?
Dexamethasone
What two drugs are
glucorticoid synthesis inhibitors and antagonists?
Ketoconazole and Metyrapone
What drug has both glucocorticoid and mineralcorticoid activity?
(note: this drug is also a mineralcorticoid agonist)
Fludrocortisone
Which drug is a mineralocorticoid antagonist?
Spironolactone
What is the precursor of ACTH?
POMC
In what region of the adrenal cortex is aldosterone, a mineralcorticoid, made in?
Zona glomerulosa
Glucosteroids, such as cortisol, are secreted from which part of the adrenal cortex?
Zona fasiculata
ACTH interacts with MCR (melanocortin receptor 2) in the _____
adrenal cortex
What is the rate-limiting step of cortisol biosynthesis?
Cholesterol to pregnenolone
Cholesterol converted to pregnenolone, from here ___ can be made (glucocorticoid pathway) and ___ can be made (mineralcorticoid pathway)
cortisol; aldosterone
What molecule can be used to measure cortisol metabolites in urine?
17-OH
Both ACTH and cortisol follow a ____ rhythm
diurnal (peak in the early morning)
Why do the effects of corticosteroids take some time to become visible?
Because they work via a ligand-bind receptor entering into the nucleus and causes gene transcription
Besides glucocorticoid receptor elements, the coricosteroid-bound complex influences the function of other transcription factors (AP1, NF-kB) which regulate: ____, ___, ____, and ____
GF’s, cytokines, anti-growth, anti-inflammatory, and immunosuppresive effects of glucosteroids
The glucocorticoid receptor can either make ____ proteins or inhibit the translation of inflammatory proteins
anti-inflammatory
In general, glucosteroids enhance production of ___ (and therefore gluconeogenesis) and release of ____
glucose; insulin
How do glucocorticoids affect proteins/amino acids?
More proteolysis/release of amino acids
How do glucocorticoids affect fat/fatty acids?
Enhance fatty acid mobilization and lipolysis
How does aldosterone affect water and electrolyte balance?
1) Reabsorption of sodium in renal tubules
2) Enhances renal excretion of K/H
How do glucocorticoids affect the heart?
-Vasoconstrict
-Decrease capillary permeability (reduce histamine release by mast/basophils)
What elements of the blood do glucocorticosteroids elevate?
Elevate: Hb, RBC’s/WBC, neutrophils
Glucocorticoids inhibit prostaglandins and ____ by inducing production of annexins, which inhibit ____
leukotriene
phospholipase A2
How do glucocorticosteroids reduce manifestations of inflammation?
Suppress release of inflammatory cytokines and chemokines
Why can glucocorticosteroids cause mood, sleep patterns, changes in mood, and adrenal insufficiency?
They are able to enter the CNS
How do glucocorticoids affect skeletal muscle?
Muscle weakness, pain, protelysis
What drug is most effective for treating vasogenic edema or brain abscess?
Prednisone