Glucocorticoids/Anti-Inflammatory Agents Flashcards
glucocorticoid drugs target the same receptor as endogenous cortisol, which is
GC-R
activation of GC-R receptor
is necessary for __
anti-inflammatory actions
what receptor is responsible for ADRs of glucocorticoids
GC-R
same as anti inflammatory
short to med acting glucocorticoids
hydrocortisone (cortisol)
prednisone
methylprednisone
intermediate-acting glucocorticoid to know
triamcinolone
long-acting glucocorticoid to know
dexamethasone
which 2 glucocorticoids have no topical use
cortisone
prednisone
major regulator of aldosterone synthesis
angiotensin II
effect of GC on the adrenal gland
suppression
t/f: endogenous AND exogenous GC also suppress ACTH release
T!
chronic use of pharmacologic doses of GCs can suppress __,
which leads to no ACTH and __
HPA axis
adrenal hypertrophy
if the adrenal gland is suppressed, the patient is reliant on
exogenous GCs
insufficient adrenal response to environmental stressors is called
adrenal crisis
tx for adrenal crisis
exogenous GCs
t/f: pharmacologic doses of GCs can cause iatrogenic Cushing’s
T!
excess GC use causes (7)
hyperglycemia
muscle wasting
central obesity
insomnia/dpn/euphoria
OP
ulcers
iatrogenic hyperaldosteronism → fluid retention, hypokalemia, metabolic alkalosis
bad AI/IS effects of GCs (3)
decrease healing
diminish immunoprotection
clinical value of GCs
suppress chronic inflammation
suppress AI rxns
GCs inhibit synthesis of both
PGs (prostaglandins)
LTs (leukotrienes)
which to GCs require activation in the liver
prednisone → prednisolone
cortisone → hydrocortisone
which form of GCs are inactive
11-keto
which functional group is required for activation of GCs
OH → hydroxyl
mc used oral GC used for steroid burst therapy
prednisone
which steroid has minimal MC action
methylprednisone
dexamethasone
IV form of methylprednisolone
solu-medrol
oral form of methylprednisolone
medrol
clinical use of cortisol (hydrocortisone)
replacement therapy → emergencies
how is cortisol administered (2)
oral
parenteral
which GC has no topical activity
prednisone
needs to be converted in the liver
most potent GC
dexamethasone (Decadron)
uses of dexamethasome
cerebral edema
chemo-induced vomiting
which GC has greatest suppression of ACTH secretion at pituitary
dexamethasone (decadron)
which GC has excellent systemic AND topical activity, but no MC action
triamcinolone
non-adrenal collagen-vascular disorder to know
RA
order of tx for RA (4)
- NSAIDs
- GCs as bridge
- MTX (DMARD)
- Etanercept and Infliximab
when are DMARDs added to RA tx
when dx is certain → suppress dz progression
how are GCs used for RA (2)
as a bridge until DMARDs take effect
adjunctive when dz persists
__ side effects vary w. agent
but __ side effects are unavoidable
MC
GC
list GC agents in order of least to most MC effect
cortisol
prednisone
methylprednisone/dexamethasone
how is dosage figured out w. GC
trial and error → re-evaluation
when should you reduce dose of GC
as soon as therapeutic dosages are obtained
if a larger initial dose is needed, what GC should you choose
one w. little MC action
how do you minimize adrenal suppression of GC
alternate day schedule
how do you minimize dz rebound and adrenal crisis (insufficiency)
terminate gradually
major consideration in deciding route of GC administration
minimize systemic actions
routes of administration for GC (7)
oral
topical
ophthalmic
intra-articular
enemas
inhalants
nasal sprays
mc rout of administration when systemic actions are desired
oral
also IV/IM
what 4 things can cause systemic effects of topical GCs
potent agent
long term use
occlusive dressings
large area of application
route of GC administration for OA/RA
intra-articular
why would you use a GC enema
UC
what determines adverse effects of GCs (2)
dose
duration
what s.e can you expect w. GC use >2-4 weeks
iatrogenic Cushing’s → DM like state
HPA axis suppression
mood disturbance
increased infxn risk
impaired wound healing/increased bruising
OP
cataracts
skin atrophy/collagen loss
growth retardation
peptic ulcers
moon facies
which 2 GC cause the most HPA suppression
dexamethasone
betamethasone
may also cause decrease in GH
what reduces peptic ulcer risk w. long term GC use
antacids
what decreases risk of OP w. long term GC use
bisposphanates
what s.e of GC are seen w. burst therapy
GI upset
insomnia
DPN
HTN
hyperglycemia
