Flashcards in Adrenocorticosteroids 2.1 Deck (16):
Glucocorticoid Agonists (6)
Mineralocorticoid Agonists (2)
Glucocorticoids peak release time at?
Hyrodrocortisone also known as?
MOA of Glucocorticoid agonist?
Binds a cytoplastmic receptor forming a complex that enters the nucleus and alters gene regulation (GRE) producing a specific tissue response
Metabolic effects of Cortisol (3)
1) Gluconeogenesis and glycogen synthesis which leads to increase serum glucose levels (leading to stimulation of insulin release & inhibiting uptake by muscle cells)
2) Stimulates lipolysis ( leading to fat deposition and redistribution... Cushings)
3) Stimulates protein catabolism
Net result: maintain adequate glucose supply to brain.
Catabolic effects of Cortisol (3)
1) In addition to protein catabolism, cortisol also has effects in lymphoid and connective tissue, muscle, peripheral fat and skin (wasting occurs at high concentrations)
3) Children -> growth retardation
Immunosuppressive effects of Cortisol on Leukocytes (3)
1) Increased neutrophils (increased influx into blood & decrease migration from blood vessels)
2) Decreased lymphocytes (T & B cells), monocytes, eosinophils and basophils (movement from vascular bed to lymphoid tissue)
3) Vasoconstriction due possibly to suppression of mast cell degranulation (decrease histamine release and capillary permeability)
Anti-inflammatory effects of Cortisol (3)
1) Inhibition of phospholipase A2 (through induction and activation of annexin I) which blocks arachidonic acid release
2) Cyclooxygenase-2 synthesis is reduced (through inhibition of NF-kB)
3) Induction of MAPK phosphatase I (inhibits proinflammatory signaling pathways)
"Other" effects of Cortisol (7)
1) CNS - behavioral changes (insomnia -> depression)
2) Increased intracranial pressure
3) Supression of release of ACTH, GH, TSH, LH
4) Peptic ulcers
5) Increase platelets & RBC's
6) Renal function
7) Development of Fetal Lungs
Prednisone is a prodrug which is rapidly converted to what?
What is important to know regarding the PK of Beclomethasone?
Short 1/2 life & penetrates airway mucosa (low systemic toxicity)
Synthetic Glucocorticoids which are aerosols