Anti-Inflammatory Corticosteroids Flashcards
Addison’s disease requires _________.
cortisol supplementation
Cushing’s disease results from _________.
excess endogenous cortisol
Once you administer glucocorticoids for a significant time, you need to __________.
continue administering it, because the exogenous glucocorticoids inhibits pituitary release of ACTH
ACTH (also called ________) is acts on the ________.
adrenocorticotropin hormone; adrenal glands to stimulate cortisol production
CRF (____________) is released by the ________ and acts on the ________.
corticotropin-releasing factor; hypothalamus; pituitary
ACTH inhibits _______.
CRF release from the hypothalamus
Pituitary release of ________ is inhibited by ________.
ACTH; glucocorticoids
What are the metabolic symptoms of Cushing’s disease/excess glucocorticoids?
Diabetes (due to increased gluconeogenesis), obesity, muscle wasting (due to AA shuttle to liver), skin atrophy,
What are the mineralocorticoid effects of aldosterone?
Sodium retention (and consequent increased water reabsorption from the kidneys resulting in increased BP); metabolic alkalosis; hypokalemia
Immunologically, glucocorticoids ______.
suppress the immune response by decreasing lymphocyte activation and restricting vasodilation
Cortisol has a ______ backbone.
cholesterol
Prednisone and cortisone have to __________.
be metabolized in the liver to the active prednisolone and cortisol
________ inhibits the mineralocorticoid action while _______ stimulates it.
Dexamethasone; fludrocortisone
Aldosterone ______ potassium levels.
lowers (if you don’t have enough aldosterone, such as in Addison’s, you will be hyperkalemic)
In the kidneys, ______ converts cortisol to cortisone, thus ensuring that aldosterone is the primary glucocorticoid regulator in the kidneys.
11Beta-HSD2
The most potent anti-inflammatory is ______.
dexamethasone (Decadron)
Which two glucocorticoids have to go through the liver?
Cortisone and prednisone
______________ are released in concert with cortisol, but not aldosterone.
Adrenal androgens (such as dihydroandostenedione and androstenedione)
Endogenous and exogenous glucocorticoids negatively affect the ___________.
hypothalamus and pituitary (production of CRF and ACTH, respectively)
In the plasma, cortisol is ________.
bound to cortisol-binding globulin (CBG)
Once in the cell, cortisol ___________.
dimerizes with R, forming R-S complex that binds the response element on DNA
The half-life of cortisol is roughly ______.
60 - 90 minutes
Aldosterone works by ________.
activating transcription factors (in the nucleus) that produce protein for sodium and potassium resorption–leading to increased water retention
What are the two ways glucocorticoids antagonize inflammation?
They (1) inhibit the synthesis of IL-1 to IL-6, IL-8, GM-CSF, and TNF, and they (2) inhibit the production of arachidonic acid metabolites
The inactivating enzyme is _______, while the activating enzyme is _______.
11Beta-HSD2; 11Beta-HSD1
The alternate-day schedule __________.
lessens adverse effects, because the anti-inflammatory effects outlast the HPA effects
What do mineralocorticoids do to potassium levels?
Decrease
Excess aldosterone can lead to _______.
hypertension, increased blood volume, hypokalemia, and metabolic alkalosis
The glucocorticoid with the best topical activity is ________.
triamcinolone
