Drugs inflammatory and related disorder_ Glucocorticoids Flashcards
syntheic dervative of cortisol drugs, _________,______that have equal glucocorticoid and mineralocorticoid activity of 1 with short duration
Cortisol, Hydrocortisone
Glucocorticoid and Mineralocorticoid activity = 1; short duration
Cortisol, Hydrocortisone
medium duration drugs that have:
Glucocorticoid activity = 4
mineralocorticoid activity = 0.3
Prednisone
intermediate acting drug that have:
Glucocorticoid activity = 5 but
Mineralocorticoid activity = 0
Triamcinolone
Long-acting drug that has:
glucocorticoid activity = 25 but
mineralocorticoid activity = 0
Betamethasone
Long-acting drug that has:
glucocorticoid activity = 30 but
mineralocorticoid activity = 0
dexamethasone
glucocorticoids uses
anti-inflammatory and immunosuppressive
mechanism of actions of glucocorticoids
cellular effects: - decrease leukocyte migration - increase lysosomal membrane stability ----> decrease phagocytosis - decrease capillary permeability
biochemical actions: - inhibits PLA2 (via Lipocortin expressions) --> decrease PGs and decrease LTs - decrease platelet-activating factor - interleukins (eg; IL-2 )
Side effects of glucocorticoids
. suppression of ACTH: cortical atrophy; malaise; myalgia;
arthralgia; and fever
- may result in shock state with abrupt withdrawal
. Iatrogenic Cushingoid syndrome: fat deposition, muscle
weakness/ atrophy, bruising, acne
. Hyperglycemia: due to increase gluconeogenesis —————->increased insulin demand and other adverse effects
. Osteoporosis: vertebral fractures-aseptic hip necrosis
. Increase GI acid and pepsin release —> ulcer, GI
bleeding
. Electrolyte imbalance: Na+/H2O retention –>edema and
HTN, Hypokalemic alkalosis and hypo-Ca2+
. decrease skeletal growth in child
.decrease wound healing, increase infections (thrush)
. increase glaucome, cataracts (via sorbitol)
. increase mental dysfunction
How to minimize steroidal toxicity
- Alternate-day therapy; local application (aerosols)
- Dose-tapering to avoid cortical suppression