Glucocorticoids Flashcards
Glucocorticoid anti-inflammatory drugs
Drugs targe the same receptor as endogenous ___________ glucocorticoid.
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Mechanism of glucocorticoid action
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Cortisol is present in plasma bound to cortisol- binding globulin (CBG), enters cell as free molecule [S].
-Binding of cortisol to cytosolic receptor releases stabilizing proteins (Hsp90), allowing S-R complex to dimerize and enter the nucleus and bind the glucocorticoid response element on DNA – regulates transcription by RNA polymerase II, activating or inhibiting transcription of target genes
Resulting effects on protein synthesis bring about the final hormone response – delayed onset, occurring in hours or longer.
NOTE: Some actions of GCs occur within minutes (e.g., suppression of ACTH release) and can’t be explained by above pathway. Proposed mechanisms include interactions with membrane receptors.
Regulation of cortisol release:
What control the synthesis/secretion of cortisol from the adrenal cortex (zona fasciculata)?
What can chronic use of synthetic GCs do to adrenal gland?
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HPA Axis
In which zone of the adrenal cortex is cortisol produced?
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Pharmacology HPA axis
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Glucocorticoid metabolic effects
What are its effects on protein? Carbohydrate? Lipids?
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Mineralocorticoid effects:
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Pharmacology of glucocorticoids:
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On cellular events, at what points do clucocorticoids block immunity responses?
T cell activatin
Cytokine production by T cells
Eosinophil release of histamine, citokines
Mast cell mediator release
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Effects on inflammatory mediators:
At what points do GCs supress inflammatory reactions?
They block COX pathway and the production of arachidonic acid from phospholipids via phospholipase A2
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GC- Structure and relation to their activity:
Which drug allows separation of mineralocorticoid vs glucocorticoid actions?
Can you separata anti-inflammatory from immunosupressive actions?
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Dexamethasone
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Metabolism of glucocorticoids:
In the liver the enzyme_________ activates cortisone back to cortisol.
In the kidneys the enzyme_______ deactivates cortisol by coverting it back to cortisone.
11B-HSD1; 11B-HSD2
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Metabolism of Glucocorticoids
In the fetus, what enzyme is not present?
Can you treat mother without effect on fetus?
What would be the best option for treating fetus with GCs?
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Sample question:
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Why? See table
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Use of individual agents:
1- Which one is administered orally and parenterally, and has a ratio od GC:MC of 1:1?
2- Which one is the most commonly used GC for steroid burst therapy and has a ratio of GC:MC of 15:1, and has no topical activity?
3- Which one has minimal MC actions and can be given oraly or IV?
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