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20 Cards in this Set
- Front
- Back
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What is the hypothalamic axis?
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the hypothalamus produces CRH which acts on the pituitary to produce ACTH which acts on the adrenal gland to produce cortisol. Each product can negatively feedback on the previous step.
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what is the signalling pathway activated by cortisol?
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glucocorticoid receptor is complexed with other proteins in the cytosol, it binds cortisol and discociates and then dimerizes with another receptor. The dimer enters the nucleus to bind to glucocrticoid response elements which will turn txn on or off depending upon the gene.
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what is an example of the anti-inflamatory process of GC's?
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increase lipocortin txn which inhibits phospholipase A2 which decreases arachodonc acid and eicosanoids
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what are some effects of GC's?
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increase blood glucose, fat redistribution, and lipolysis
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what structures on the steroid are necessary for function?
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ketone at position 3 and 4:5 double bond
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small modifications in the basic corticosteroid structure alter what?
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potencies of carb effect, sodium retention, and anti-inflammatory. drug half life and transcortin (plama protein that binds GC and keeps plasma reserve)
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Adding fluoride to the steroid will have what effect? methyl group?
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F will increase potency while CH3 will increase anti-inflammatory effects and decrease sodium retention.
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these three drugs have very high GC potencies.
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dexamethasone, betamethasone, triamcinolone
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these drugs have high GC potencies...
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prednisolone, methylprenisolone
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this drug has very low GC potency..
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fludrocortisone
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what is the metabolism pathway of corticosteroids?
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in the liver, the 4, 5 double bond is reduced to inactive metabolite, then it is conjugated and excreted
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prednisone is a prodrug of what?
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prednisolone
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what is the most single long term side effect of GC's?
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osteoporosis
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what GC has causes weight loss instead of weight gain?
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triamcinolone
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what type of dosing schedule has minimized side effects?
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alternate day therapy
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what are withdrawal symptoms of GC's?
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acute adrenal insufficiency, physical dependance, psychological dependence, and exacerbation of underlying disease
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what are drugs that decrease steroid effectiveness?
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hepatic enzyme inducers and cholestyramine
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what are drugs that increase steroid effectiveness?
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certain antibiotics (erythromycin), oral contraceptives, ketoconazole
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what drugs will need to be increased if pt. starts taking steroids?
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anticoagulants, antihypertensives, and hypoglycemics
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what drugs will need to be decreased if the patient begins GC treatment?
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sympathomimetics
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