corticosteroids Flashcards
4 major classes of steroids?
- sex hormone
- bile acids
- vitamins
- adrenocorticoids
2 major classes of glucocorticoid secretion?
not pre stored - made and released on demand
levels maintained via feedback mechanism
feedback mechanism of glucocorticoid secretion?
1- levels low, hypothalamus secretes CRF causing ACTH release
2- stimulates adrenal cortex to release adrenocorticoids
3- levels become sufficiently high
4- inhibition of CRF secretion
how do corticosteroids have an anti-inflammatory effect?
affect protein synthesis, increases lipocortin, inhibits phospholipase A2
how do they inhibit cytokines?
inhibits IL-1 and stimulates T and B lymphocyte proliferation
what happens when they inhibit mast cells?
inhibits release of histamine and autocoid release
what loss of activity results from metabolism of functional groups?
ring a reduction
c-17 oxidation
c-11 keo-enol isomerisation
how do steroid hormones enter cells ?
lipophilic so enter by diffusion acoss plasma membrane
what happens when they combine with an intracellular receptor?
conformational change exposes DNA-binding domain
what happens to the receptor steroid complex?
moves to nucleus and binds to steroid response elements in DNA