S2 Glucocorticoids & Cyclosporine Flashcards
Glucocorticoids
Biological molecule = cortisol
Some molecules may bind to mineralocorticoid receptors
Mineralocorticoids
Biological molecule = aldosterone
Some molecules may bind to glucocorticoid receptors
Mifepristone
RU-486
Glucocorticoid antagonist
Also acts as a progesterone antagonist
Prednisolone
Intermediate potency and duration
Similar to Triamcinolone
Much higher oral bio-availability
Best choice for cats
Prednisone
Lower GI absorption
Inactive form
Requires hepatic metabolism
Conversion to active prednisolone
Cortisone
Inactive form
Requires hepatic metabolism
Conversion to active cortisol (hydrocortisone)
Weakest corticosteroid drug
Hydrocortisone (cortisol)
Low potency and short duration
Some mineralocorticoid activity
Triamcinolone
Intermediate potency and duration
Similar to prednisolone
Dexamethasone
Glucocorticoid full agonist
High potency and long duration (> 48 hrs)
Cyclosporin
Immunosupressive drug
Calcineurin inhibitor = T-cell suppressant
No effect on immunoglobulins
Similar but weaker than Tacrolimus
Tacrolimus
Immunosupressive drug Calcineurin inhibitor = T-cell suppressant No effect on immunoglobulins 500X more potent than Cyclosporin! Dermatological use only
Cortisol, dexamethasone, & corticosterone
Glucocorticoid full agonists
Deoxycorticosterone
Glucocorticoid partial agonist
Effects of glucocorticoids
- Inhibition of eicosanoids
- Reduction in proinflammatory cytokines
- Decreased IgE induced release of histamine and leukotrienes
- Decreased leukocyte adhesion molecules
- Inhibition of growth factors
a. Inhibits wound healing= negative effect
PALLIATIVE DRUGS ONLY!
= does not treat underlying cause
