Exam 4; Glucocorticoids Flashcards
The synthesis of steroids is essentially via which enzymes
P450s
What is the mechanism of action of steroids
enter the target cell and bind to a cytoplasmic receptor
The steroid dimerizes, then binds to a response element in the DNA, causing what to occur
either enhance gene transcription or suppress gene transcription
Regarding glucocorticouds, this is induced
lipocortin 1
What is the function of lipocortin 1
it is an extremely important regulator of the immune system; inhibits phospholipase A2 → decrease in arachniodonic acid → inhibiting the synthesis of prostaglandins and leukotrienes
Lipocortin inhibits the synthesis of may what
cytokines, leading to a profound suppression of the immune system
What is the immunosuppressive potency, relative mineralcorticoid, and duration of cortisone and hydrocortisone
immunosuppressive potency; 1
relative mineralcorticoid; 1
duration 8-12 hours
What is the immunosuppressive potency, relative mineralcorticoid, and duration of prednisone, triamcinolone, and predinisolone
immunosuppressive potency; 4
relative mineralcorticoid; 0.25
duration; 18-36 hours
What is the immunosuppressive potency, relative mineralcorticoid, and duration of dexamethasone and betamethasone
immunosuppressive potency; 25
relative mineralcorticoid; <0.01
duration; 36-54 hours
What type of drugs are the GCs
pro-drugs; must be metabolized by P450
Why are GCs not effective when used topically
topical use can lead to systemic effects
What can topical use of GCs be affected by
Dose Duration of exposure Potency Size of area covered Occlusive dressings Skin damage Thickness of the skin
What are the side effects of a deficiency of cortisol production
Weight loss
low BP
muscle weakness
Addison’s disease
What are the side effects of an excess production of cortisol (Cushing’s)
adrenal suppression; body is no longer making its of GCs; relying on exogenous GCs, which some from no where; leading to Addison’s like symptoms
What are the metabolic effects of GCs
Increased liver gluconeogenesis Decreased glucose uptake by muscle cells Increased protein breakdown Decreased protein synthesis Affects lipolysis; fat redistribution