Corticosteroids Flashcards
where is steroid production?
adrenal glands
what do the adrenal glands do?
secrete mineralocorticoids, glucocorticoids, and sex hormones
what are the three zones of the adrenal gland cortex?
zona glomerulosa
zona fasciculata
zona reticularis
what hormones are produced in each zone of the cortex?
glomerulosa - aldosterone
fasciulata - cortisol
reticularis - testosterone
what are the primary functions of cortisol?
mediate the stress response
help regulate metabolism
help regulate the inflammatory response
help regulate the immune system
when is cortisol released?
in response to stress and it helps restore hormone levels when stress resolves
what regulates the production and secretion of cortisol?
hypothalamus pituitary adrenal(HPA) axis
what hormones are involved in the production and secretion of cortisol?
ACTH, CRH, and vasopressin
T or F: the production of cortisol is considered negative inhibition
True
what is the action of glucocorticoids?
suppress inflammatory and immunological responses
what is the MOA of an anti-inflammatory?
(impeding each step of the inflammatory process)
altering cytokine release
blocking increased capillary permeability
causing less vasoactive substance release
inhibiting leukocyte and macrophage migration/adhesion
interfering with phagocytosis
what is the immunosuppressive MOA?
altering the cell function of specific genes
affecting the function of WBCs
inhibiting T-cell activation
inhibiting IL’s, cytokines, gamma-interferon, and TNF-alfa synthesis
what are some of the other corticosteroid actions?
anti-mitotic activity
anti-tumour effects
anti-emetic effects
corticosteroid dosage forms
local - otic, ophthalmic, inhaled, topical
systemic agents - injectables, oral
how are otic/ophthalmic corticosteroids available?
drops, ointments, emulsions, intravitreal implants
what are ophthalmic/otic corticosteroids used for?
redness, itching, swelling, pain
what are some potential issues with ophthalmic/otic drops?
correct delivery technique
not getting drop into eye
uses for nasal inhaled corticosteroids
rhinitis, polyps, sinusitis
issues with topical nasal inhaled corticosteroids
installation technique
what are the metered dose inhalers?
fluticasone
beclomethasone
triamcinolone
ciclesonide
fluticasone propionate
what are the dry powders for inhalation?
budesonide
fluticasone
mometasone
pros of dry powders for inhalation
actuation, portable, show remaining doses
cons of dry powders for inhalation
powder deposition in mouth
requires good lung function
what are the types of inhaled corticosteroids?
nasal
metered-dose inhalers
dry powders for inhalation
combo products
solutions for inhalation (nebulizers)
what is the drug for nebulizers?
budesonide
pros of nebulizers
reasonable lung delivery when cannot generate sufficient flow rate
easy for infants and young children
cons of nebulizers
time consuming
expensive
non-portable equipment
false-sense of superiority
what are the topical corticosteroid dosage forms?
lotions
creams
gels
ointments
enemas
rectal ointments
suppositories
rectal foams
what is the effectiveness of topical corticosteroids based on?
potency
dosage form
concentration
formulation
application technique
site
skin condition
what are the injectable corticosteroids?
intravenous
intramuscular
intralesional
intra-articular
intravenous drugs
hydrocortisone
methylprednisolone
intramuscular drugs
betamethasone acetate/sodium phosphate
dexamethasone sodium phosphate
methylprednisolone
triamcinolone
intralesional drugs
triamcinolone acetonide
intra-articular drugs
triamcinolone
betamethasone
methylprednisolone
when is IV used
when a faster onset or high dose is required
what is the usual site for intra-articular?
hip, knee, ankle, shoulder, elbow, wrist
how often can a joint be injected?
no more then 3-4x per year
how are oral corticosteroids absorbed?
rapidly and completely from the gut
what are the oral corticosteroid tablet drugs?
betamethasone
cortisone
dexamethasone
hydrocortisone
methylprednisolone
prednisone
triamcinolone
what drug is the oral solution corticosteroid?
prednisolone
what are physiologic doses used for?
to replace deficiencies
ie. the amount of cortisol excreted by the adrenal cortex/day
what does of prednisone is equivalent to the amount of cortisol we produce in a day?
~5mg
how much cortisol do we produce per day?
10-20mg
what are pharmacologic doses used for?
to treat disease states and provide supportive therapy
what is the dosing for prednisone?
usually 0.5-1mg/day
moderate dose: 0.5mg/kg/day
high dose: 1-3mg/kg/day
massive dose: 15-30mg/kg/day
REVIEW CORTICOSTEROID COMPARISONS - SLIDE 35
what are the short acting oral corticosteroids?
cortisone
hydrocortisone
8-12 hours
what are the intermediate acting oral corticosteroids?
prednisone
prednisolone
methylprednisolone
triamcinolone
12-36 hours
what are the long acting oral cotricosteroids?
dexamethasone
betamethasone
36-72 hours
what are the AE’s of ophthalmic corticosteroids?
stinging
redness
tears
burning
secondary infection
catarax
glaucoma
what are the AE’s of oral inhalation corticosteroids?
thrush
hoarseness
dry mouth
dysphoria
difficulty swallowing
what are the AE’s of nasal corticosteroids?
rhinorrhea
burning
sneezing
bloody nose
what are the AE’s of topical corticosteroids?
pretty well tolerated but..
burning
irritation
skin atrophy
tachyphylaxis
telangiectasia
what are some systemic complications of corticosteroids?
insomnia
thinning of skin
increased abdominal fat
poor wound healing
redistribution of fat
nausea
moon face
are CNS effects of corticosteroids dose related?
yes
what are the CNS effects of corticosteroids?
euphoria
insomnia
restlessness
memory impairment
can later become:
- depression
- mania
- psychosis
what can increase when using ophthalmic corticosteroids?
IOP
what are risk factors for cataracts?
daily dose
cumulative dose
duration
age
increased risk with oral prednisone >15mg/d x 1 year
risk factors of glaucoma
pre-existing primary open angle glaucoma (POAG)
diabetes
fanilt history
rheumatoid arthritis
gastrointestinal AE’s of corticosteroids
GI upset - take with food
dyspepsia
increased risk of peptic ulcer disease when used in conjunction with NSAIDs
endocrine AE’s of corticosteroids
increase blood glucose - normally mild
sodium/water retention
increased appetite
growth retardation
what will corticosteroids with greater mineralocorticoid activity do?
more likely to cause fluid retention and elevate BP
why do CS’s cause growth retardation?
decrease osteoblasts and GH secretion
competitively inhibiting insulin receptors
more pronounced with oral therapy
what is the HPA-axis?
a connection between the brain and adrenal glands
the body’s main stress system
it releases cortisol to activate a response to stress
what is the diurnal cycle?
the release of cortisol throughout the day. endogenous levels of cortisol highest at 7-8am and decreases throughout the day
when will cortisol release be increased?
during periods of stress
- illness, stress, surgery
what kind of “control” is the HPA-axis under?
negative feedback control by endogenous cortisol
what happens when exogenous corticosteroids are administered?
they cause negative feedback of CRH and ACTH resulting in suppression of the HPA-axis
if HPA axis suppression is present, what will happen is the steroids are abruptly stopped or if the patient becomes severely ill?
hypotension
hypoglycaemia
flu-like symptoms
weight loss
confusion
what factors may predict the occurrence of HPA-axis suppression?
dose
type of steroid
interval
route
duration
time of administration
when is screening for HPA-axis suppression recommended?
taking oral CS’s for >2 consecutive weeks or > 3 cumulative weeks in previous 6 months
what test is performed to determine HPA-axis suppression/recovery?
a blood test: SST (short synacthen test)
which dosage form has the highest risk of adrenal insufficiency?
oral > intra-articular > nasal
why do CS’s impair wound healing?
they can impair antibodies and phagocytosis
what effects do corticosteroids have on bone?
protein catabolism
osteoblast inhibition
GH inhibition
decrease Ca absorption
decrease renal calcium reabsorption
30-50% will develop osteoporosis with chronic tx
what are the long term SE’s in kids?
weight gain
growth retardation
cushingoid features
infection - most serious
short course uses of CS’s in kids
croup
acute asthma
short course SE’s of CS’s in kids
vomiting
behavioural changes
sleep disturbances
when were CS’s used in COVID and what drug?
for hospitalized patients requiring oxygen
dexamethasone 6mg OD for up to 10 days
what are the dosing guidelines for corticosteroids?
NO SET GUIDELINES
initial dosing: OD or BID
maintenance dosing: OD
how do you taper lower then 5mg or prednisone?
may see conversion to 20mg HC and then taper further
when might you see EOD dosing?
chronic administration necessary
children requiring maintenance dosing
how can you change to EOD dosing?
- determine MED
- EOD dose is 2.5-3x the MED
- alternate the new calculated dose with MED
- taper the MED by 5mg/week until removed
- taper current dose by 5mg/week to the MED
what is steroid pulse therapy?
administration of short term, high dose, IV or PO steroids in various situations where rapid remission of serious conditions is desired
advantages to steroid pulse therapy
more rapid control of condition
help avoid AE’s by avoiding prolonged steroid therapy
disadvantages to steroid pulse therapy
certain adverse effects may be more likely and significant
- hypertension
- infection
- seizure
- psychosis
