Corticosteroids Flashcards
Actions of Cortisol
carbohydrate metabolism (gluconeogenesis)
increases protein catabolism
inhibits insulin from shuttling into cells
mobilized free fatty acids
suppression of pro inflammatory cytokines
suppress immune system
normal mg cortisol production per day
15-30, highest at 0800.
cortisol levels based on procedure
minor: up to 50mg/day. returns to baseline in 24h
moderate: up to 75-100mg/day. returns to baseline in 5d
major: up to 200mg/day. returns to baseline by day 5
Addisons Disease
primary adrenocortical insufficiency. destruction of all cortical zones
secondary adrenal insufficiency
after 2wks suppression of HPA axis, chronic glucocorticoid tx (3-4w), topical admin of aerosols for asthma, TBI.
adrenal crisis sx and causes
hypotension (hallmark), acute abdominal sx, n/v, AMS, fatigue, fever, hyponatremia, hyperkalemia, hypocalcemia.
caused by interruption of glucocorticoid intake, infx, surgery, gastroenteritis stress
adrenal crisis management
NS 1L over 6-12h, hydrocortisone 100mg. then 50mg q6h.
Corticosteroids MOA
stimulate changes in transcription of 456 DNA. target cells contain enzyme 11 beta hydroxysteroid dehydrogenase
PK of corticosteroids
antacids interfere with oral absorption
highly protein bound (90%) to corticosteroid binding globulin
readily crosses placenta
elimination half time of cortisol 1.5-3h
70% metabolized in liver to inactive or poorly active metabolites
clinical uses of corticosteroids
antiemetic (preop), analgesia (postop), immunosuppression, laryngeal edema, regional blocks (prolongs them), asthma (not rescue), cerebral edema, adrenal insufficiency
Prednisolone use
sole replacement therapy in adrenocortical insufficiency
prednisone conversion
rapidly converted to prednisolone after absorption from GI tract
methylprednisolone use
used to produce intense glucocorticoid effect
dexamethasone use
multiple uses
drug interactions: enzyme inhibition
antifungals (ketoconazole, fluconazole). 11b hydroxylation inhibitors (etomidate, metapyrone)