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PHAR 253 > Corticosteroids > Flashcards

Corticosteroids Flashcards

1
Q

where is steroid production?

A

adrenal glands

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2
Q

what do the adrenal glands do?

A

secrete mineralocorticoids, glucocorticoids, and sex hormones

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3
Q

what are the three zones of the adrenal gland cortex?

A

zona glomerulosa
zona fasciculata
zona reticularis

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4
Q

what hormones are produced in each zone of the cortex?

A

glomerulosa - aldosterone
fasciulata - cortisol
reticularis - testosterone

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5
Q

what are the primary functions of cortisol?

A

mediate the stress response
help regulate metabolism
help regulate the inflammatory response
help regulate the immune system

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6
Q

when is cortisol released?

A

in response to stress and it helps restore hormone levels when stress resolves

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7
Q

what regulates the production and secretion of cortisol?

A

hypothalamus pituitary adrenal(HPA) axis

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8
Q

what hormones are involved in the production and secretion of cortisol?

A

ACTH, CRH, and vasopressin

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9
Q

T or F: the production of cortisol is considered negative inhibition

A

True

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10
Q

what is the action of glucocorticoids?

A

suppress inflammatory and immunological responses

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11
Q

what is the MOA of an anti-inflammatory?

A

(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

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12
Q

what is the immunosuppressive MOA?

A

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

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13
Q

what are some of the other corticosteroid actions?

A

anti-mitotic activity
anti-tumour effects
anti-emetic effects

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14
Q

corticosteroid dosage forms

A

local - otic, ophthalmic, inhaled, topical
systemic agents - injectables, oral

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15
Q

how are otic/ophthalmic corticosteroids available?

A

drops, ointments, emulsions, intravitreal implants

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16
Q

what are ophthalmic/otic corticosteroids used for?

A

redness, itching, swelling, pain

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17
Q

what are some potential issues with ophthalmic/otic drops?

A

correct delivery technique
not getting drop into eye

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18
Q

uses for nasal inhaled corticosteroids

A

rhinitis, polyps, sinusitis

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19
Q

issues with topical nasal inhaled corticosteroids

A

installation technique

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20
Q

what are the metered dose inhalers?

A

fluticasone
beclomethasone
triamcinolone
ciclesonide
fluticasone propionate

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21
Q

what are the dry powders for inhalation?

A

budesonide
fluticasone
mometasone

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22
Q

pros of dry powders for inhalation

A

actuation, portable, show remaining doses

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23
Q

cons of dry powders for inhalation

A

powder deposition in mouth
requires good lung function

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24
Q

what are the types of inhaled corticosteroids?

A

nasal
metered-dose inhalers
dry powders for inhalation
combo products
solutions for inhalation (nebulizers)

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25
Q

what is the drug for nebulizers?

A

budesonide

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26
Q

pros of nebulizers

A

reasonable lung delivery when cannot generate sufficient flow rate
easy for infants and young children

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27
Q

cons of nebulizers

A

time consuming
expensive
non-portable equipment
false-sense of superiority

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28
Q

what are the topical corticosteroid dosage forms?

A

lotions
creams
gels
ointments
enemas
rectal ointments
suppositories
rectal foams

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29
Q

what is the effectiveness of topical corticosteroids based on?

A

potency
dosage form
concentration
formulation
application technique
site
skin condition

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30
Q

what are the injectable corticosteroids?

A

intravenous
intramuscular
intralesional
intra-articular

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31
Q

intravenous drugs

A

hydrocortisone
methylprednisolone

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32
Q

intramuscular drugs

A

betamethasone acetate/sodium phosphate
dexamethasone sodium phosphate
methylprednisolone
triamcinolone

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33
Q

intralesional drugs

A

triamcinolone acetonide

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34
Q

intra-articular drugs

A

triamcinolone
betamethasone
methylprednisolone

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35
Q

when is IV used

A

when a faster onset or high dose is required

36
Q

what is the usual site for intra-articular?

A

hip, knee, ankle, shoulder, elbow, wrist

37
Q

how often can a joint be injected?

A

no more then 3-4x per year

38
Q

how are oral corticosteroids absorbed?

A

rapidly and completely from the gut

39
Q

what are the oral corticosteroid tablet drugs?

A

betamethasone
cortisone
dexamethasone
hydrocortisone
methylprednisolone
prednisone
triamcinolone

40
Q

what drug is the oral solution corticosteroid?

A

prednisolone

41
Q

what are physiologic doses used for?

A

to replace deficiencies
ie. the amount of cortisol excreted by the adrenal cortex/day

42
Q

what does of prednisone is equivalent to the amount of cortisol we produce in a day?

A

~5mg

43
Q

how much cortisol do we produce per day?

A

10-20mg

44
Q

what are pharmacologic doses used for?

A

to treat disease states and provide supportive therapy

45
Q

what is the dosing for prednisone?

A

usually 0.5-1mg/day
moderate dose: 0.5mg/kg/day
high dose: 1-3mg/kg/day
massive dose: 15-30mg/kg/day

46
Q

REVIEW CORTICOSTEROID COMPARISONS - SLIDE 35

A
47
Q

what are the short acting oral corticosteroids?

A

cortisone
hydrocortisone
8-12 hours

48
Q

what are the intermediate acting oral corticosteroids?

A

prednisone
prednisolone
methylprednisolone
triamcinolone
12-36 hours

49
Q

what are the long acting oral cotricosteroids?

A

dexamethasone
betamethasone
36-72 hours

50
Q

what are the AE’s of ophthalmic corticosteroids?

A

stinging
redness
tears
burning
secondary infection
catarax
glaucoma

51
Q

what are the AE’s of oral inhalation corticosteroids?

A

thrush
hoarseness
dry mouth
dysphoria
difficulty swallowing

52
Q

what are the AE’s of nasal corticosteroids?

A

rhinorrhea
burning
sneezing
bloody nose

53
Q

what are the AE’s of topical corticosteroids?

A

pretty well tolerated but..
burning
irritation
skin atrophy
tachyphylaxis
telangiectasia

54
Q

what are some systemic complications of corticosteroids?

A

insomnia
thinning of skin
increased abdominal fat
poor wound healing
redistribution of fat
nausea
moon face

55
Q

are CNS effects of corticosteroids dose related?

A

yes

56
Q

what are the CNS effects of corticosteroids?

A

euphoria
insomnia
restlessness
memory impairment
can later become:
- depression
- mania
- psychosis

57
Q

what can increase when using ophthalmic corticosteroids?

A

IOP

58
Q

what are risk factors for cataracts?

A

daily dose
cumulative dose
duration
age
increased risk with oral prednisone >15mg/d x 1 year

59
Q

risk factors of glaucoma

A

pre-existing primary open angle glaucoma (POAG)
diabetes
fanilt history
rheumatoid arthritis

60
Q

gastrointestinal AE’s of corticosteroids

A

GI upset - take with food
dyspepsia
increased risk of peptic ulcer disease when used in conjunction with NSAIDs

61
Q

endocrine AE’s of corticosteroids

A

increase blood glucose - normally mild
sodium/water retention
increased appetite
growth retardation

62
Q

what will corticosteroids with greater mineralocorticoid activity do?

A

more likely to cause fluid retention and elevate BP

63
Q

why do CS’s cause growth retardation?

A

decrease osteoblasts and GH secretion
competitively inhibiting insulin receptors
more pronounced with oral therapy

64
Q

what is the HPA-axis?

A

a connection between the brain and adrenal glands
the body’s main stress system
it releases cortisol to activate a response to stress

65
Q

what is the diurnal cycle?

A

the release of cortisol throughout the day. endogenous levels of cortisol highest at 7-8am and decreases throughout the day

66
Q

when will cortisol release be increased?

A

during periods of stress
- illness, stress, surgery

67
Q

what kind of “control” is the HPA-axis under?

A

negative feedback control by endogenous cortisol

68
Q

what happens when exogenous corticosteroids are administered?

A

they cause negative feedback of CRH and ACTH resulting in suppression of the HPA-axis

69
Q

if HPA axis suppression is present, what will happen is the steroids are abruptly stopped or if the patient becomes severely ill?

A

hypotension
hypoglycaemia
flu-like symptoms
weight loss
confusion

70
Q

what factors may predict the occurrence of HPA-axis suppression?

A

dose
type of steroid
interval
route
duration
time of administration

71
Q

when is screening for HPA-axis suppression recommended?

A

taking oral CS’s for >2 consecutive weeks or > 3 cumulative weeks in previous 6 months

72
Q

what test is performed to determine HPA-axis suppression/recovery?

A

a blood test: SST (short synacthen test)

73
Q

which dosage form has the highest risk of adrenal insufficiency?

A

oral > intra-articular > nasal

74
Q

why do CS’s impair wound healing?

A

they can impair antibodies and phagocytosis

75
Q

what effects do corticosteroids have on bone?

A

protein catabolism
osteoblast inhibition
GH inhibition
decrease Ca absorption
decrease renal calcium reabsorption
30-50% will develop osteoporosis with chronic tx

76
Q

what are the long term SE’s in kids?

A

weight gain
growth retardation
cushingoid features
infection - most serious

77
Q

short course uses of CS’s in kids

A

croup
acute asthma

78
Q

short course SE’s of CS’s in kids

A

vomiting
behavioural changes
sleep disturbances

79
Q

when were CS’s used in COVID and what drug?

A

for hospitalized patients requiring oxygen
dexamethasone 6mg OD for up to 10 days

80
Q

what are the dosing guidelines for corticosteroids?

A

NO SET GUIDELINES
initial dosing: OD or BID
maintenance dosing: OD

81
Q

how do you taper lower then 5mg or prednisone?

A

may see conversion to 20mg HC and then taper further

82
Q

when might you see EOD dosing?

A

chronic administration necessary
children requiring maintenance dosing

83
Q

how can you change to EOD dosing?

A
  1. determine MED
  2. EOD dose is 2.5-3x the MED
  3. alternate the new calculated dose with MED
  4. taper the MED by 5mg/week until removed
  5. taper current dose by 5mg/week to the MED
84
Q

what is steroid pulse therapy?

A

administration of short term, high dose, IV or PO steroids in various situations where rapid remission of serious conditions is desired

85
Q

advantages to steroid pulse therapy

A

more rapid control of condition
help avoid AE’s by avoiding prolonged steroid therapy

86
Q

disadvantages to steroid pulse therapy

A

certain adverse effects may be more likely and significant
- hypertension
- infection
- seizure
- psychosis

PHAR 253 (8 decks)

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