Exam 3 Corticosteroids Flashcards
What steroid is this?
Cortisol or hydrocortisone, the body’s stress hormone. A glucocorticoid.
What steroid is this?
Aldosterone, the body’s sodium and water retention hormone. A mineralocorticoid.
What steroid is this?
Fludrocortisone, a steroid with higher glucocorticoid activity but MUCH higher mineralocorticoid activity. Used to replace aldosterone.
What steroid is this?
Prednisone, a steroid only effective when given orally. More potent glucocorticoid than cortisol but lower mineralocorticoid.
What steroid is this?
PrednisoLONE, an more potent corticosteroid than cortisol and lower aldosterone-like activity.
What steroid is this?
MethylprednisoLONE, a steroid similar to prednisoLONE but with lower aldosterone-like activity.
What steroid is this?
Triamcinolone, a steroid with similar potency to prednisone but lower aldosterone-like activity. Also more hydrophilic.
What steroid is this?
Dexamethasone, one of the strongest corticosteroids we have, due to increased lipophilicity. Lower mineralocorticoid activity.
What steroid is this?
Betamethasone, an enantiomer of dexamethasone and with similarly strong steroid potency.
What does an acetate or butyrate ester substituent on carbon 21 do to steroid activity?
Increases lipophilicity and prolongs action when given IM or intra-articular
What does a phosphate ester substituent on carbon 21 do to steroid activity?
Increases solubility but is hydrolyzed off quickly. Ideal for IV or IM injection.
What does a succinate ester substituent on carbon 21 do to steroid activity?
Increases solubility but is hydrolyzed off very slowly
What are the two strongest steroids?
Dexamethasone and betamethasone
What steroid is used for aldosterone replacement, not for glucocorticoid activity?
Flucrocortisone
What steroid can only be given orally?
Prednisone
What steroid is this? How is it given?
Triamcinolone acetonide (Azmacort or Nasocort), an ICS that is 8x more potent than prednisolone. Hydrolyzed slowly.
What steroid is this? How is it given?
Beclomethasone dipropionate (Vanceril or Qvar), an ICS that is 14x more potent than dexamethasone! Hydrolyzed rapidly
What steroid is this? How is it given?
Flunisolide (Aerobid), an ICS that is rapidly absorbed and metabolized by the liver, which minimizes systemic side effects.
What steroid is this? How is it given?
Budesonide (Pulmicort), an ICS that has low oral bioavailability due to extensive first pass metabolism but faster topical uptake.
What steroid is this? How is it given?
Mometasone furoate (Asmanex), a highly potent ICS with a rapid onset of action and negligible systemic availability due to rapid metabolism and low oral bioavailability.
What steroid is this? How is it given?
Fluticasone propionate (Flovent), an ICS that is highly lipophilic so highly potent but also has minimal systemic effects due to low oral bioavailability and rapid first pass metabolism. Rapid topical uptake.
Name the short-term side effects of corticosteroids
Sodium and water retention, myopathy, hyperglycemia, impaired glucose tolerance, suppressed immune system, mood changes
Name the long-term side effects of corticosteroids
Cataracts, osteoporosis, PUD, reduced growth, Cushing’s syndrome, Addison’s syndrome (on discontinuing drug)
What are the two main intracellular targets of glucocorticoids?
NFkB – prevents its binding therefore preventing cytokine gene transcription
Hormone receptors that increase transcription of anti-inflammatory proteins like lipocortin-1
