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Pharm - corticosteroids
pharm
31
Veterinary Medicine
Undergraduate 3
05/25/2012

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Term
8 corticosteroid effects =
Definition
1. antinflam
2. immunosupressant
3. inhibit PLA2 and COX2
4. decr C' in plasma
5. decr NO
6. decr histamine release from basophils
7. derc IgG
8. decr cytokines
Term
give 3 examples of corticosteroids
Definition
hydrocortisone
prednisolone
dexamethasone
Term
natural corticosteroids in the body =
Definition
steroids secreted by the adrenal cortex
Term
2 main steroids =
Definition
mineralocorticoids
glucocorticoids
Term
mineralocorticoids =
Definition
effect water and electrolyte balance (eg aldosterone)
Term
glucocorticoids =
Definition
effect CHO and protein metab (eg hydrocortisone & corticosterone)
Term
glucocorticoids released is activated by...
Definition
...ACTH secreted in anterior pituitary
Term
ACTH secretion is regulated by...
Definition
CRF from the hypothalamus and the levels of glucocorticoids in the blood (-feedback)
Term
[corticosteroids] in blood in
a) the morning
b) midnight
Definition
a) high
b) low
Term
hydrocortisones used for...
Definition
...skin disorders
Term
prednisolone potency =
Definition
4x more potent than hyrdrocortisone
Term
prednisolone used for...
Definition
...chronic dz, in a lot of pain
long term use
eg RA
Term
potency of dexamethasone =
Definition
30x more potent than hydrocortisone
Term
uses of dexamethasone =
Definition
chronic dz, in alot of pain eg RA
long lasting
selective - no affinity for mineralocorticoid Rs = no effect on water balance :)

BUT side effects due to sich high potnecy!
Term
caffeine causes glucocorticoid levels to...
Definition
...incr
Term
early inflam =
Definition
redness
heat
swelling
pain
swelling
Term
late inflam =
Definition
wound healing and repair
proliferative actions of chronic inflam
Term
glucocorticoids effect early and late inflam therefor what should you give with glucocortocoids?
Definition
Adr to counteract inhibiton of healing and repair by glucocrticoids affecting late inflam
Term
glucocorticoids mech of action =
Definition
lipophilic = readily cross cell mb, moves to nucleus and either represses or induces gene transcription (most commonly supresses transcriptiion of genes for cytokines)
Term
glucocorticoids inhibit what in Tcells?
Definition
IL4 release IFNgamma release production of IL2 release of macro activating cytokines
Term
calcineurin inhibitors are used in conjunction with glucocorticosteroids. NAme 2
Definition
cyclosporin
tacrolimus (FK-506)
Term
cyclopsporin mech =
Definition
binds to R in cell cytoplasm called cyclophilin = inhibit calcineurin enzyme = inhibit IL2 production = no cell prolif and no cytokine release
Term
side effects of cyclosporin =
Definition
nephrotoxicity
Term
to prevent transplant rejection use...
Definition
....glucocorticoids and cyclosporin
Term
how do glucocorticoids inhibit PLA2?
Definition
they activate lipocortin which inhibits PLA2
Term
how does glucocorticoids inhibit cox2?
Definition
directly
Term
NO induces...
Definition
...inflam response
Term
clinical uses of glucocrticoids =
Definition
1. oral prednisolone to tx feline asthma
2. fluticasone to tx RAO
3. eczema, rhinitis - allergic conditions
4. hypersensitivity state - give high dose dexamethasone or hydrocortisone
5. supress graft rejection with cyclosporin (a calcineurin inhibitor)
6. acute s.c. injury (methylprednisolone up to 24-48hrs fter injury)
7. Autoimmune dz - high dos prednisolone long term
8. adrenal insufficiency (not producing hydrocortisone) -tx with hydrocortisone
Term
signs of adrenal insufficiency =
Definition
chronic fatigue mm weakness decr appetite weight loss hyperpigmentation
Term
admin of glucocorticosteroids =
Definition
oral
topical
parenteral
inhalers (local admin= less side effects :))
Term
side effects of glucocorticoids with high dose chronic tx =
Definition
1. immunosupression
2. supress endogenous glucocorticoid syth
3. metabolic actions
4. osteoporosis (bones brittle and fragile)
5. cushings dz
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