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Corticosteroids
N/A
99
Pharmacology
Professional
04/30/2011

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Cards

Term
prototype glucocorticosteroid agonist
Definition
prednisone
Term
prototype mineralocorticosteroid agonist
Definition
aldosterone
Term
prototype glucocorticoid antagonist
Definition
mifepristone
Term
prototype mineralocorticoid antagonist
Definition
spironolactone
Term
prototype corticosteroid antagonist (synthesis inhibitor)
Definition
ketoconazole
Term
duration of action for cortisol
Definition
short acting
Term
duration of action for cortisone
Definition
short acting
Term
duration of action for prednisone
Definition
intermediate acting
Term
duration of action for prednisolone
Definition
intermediate acting
Term
duration of action for methylprednisone
Definition
intermediate acting
Term
duration of action for triamcinolone
Definition
intermediate acting
Term
duration of action for betamethasone
Definition
long acting
Term
duration of action for dexamethasone
Definition
long acting
Term
What are the two mineralocorticoids?
Definition
corticosterone
fludrocortisone
Term
corticosteroid indications
Definition
rheumatoid arthritis
bronchial asthma
renal disease
lupus erythematosus
ocular disorders
organ transplants
Term
Corticosteroids controls _________; they do not stop __________ of a disease.
Definition
symptoms; progression (cure)
Term
What is needed to make all corticosteroids?
Definition
cholesterol
Term
Explain the H-P-A axis.
Definition
1. circadian regulation and stress cause release of CRH from hypothalamus
2. CRH acts on anterior pituitary to release ACTH
3. ACTH acts on adrenal cortex to release steroid hormone
4. both ACTH and steroid hormone act as negative feedback to turn off release of CRH from the hypothalamus
Term
What overrides the negative feedback mechanism in the H-P-A axis?
Definition
stress (more cortisol is kicked out of the adrenal cortex)
Term
When are glucocorticoid levels highest and lowest during the day?
Definition
highest in the early morning
lowest in the evening
Term
mineralocorticoid -->
Definition
aldosterone
Term
glucocorticoid -->
Definition
cortisol
Term
androgen -->
Definition
testosterone
Term
What metabolic effects do glucocorticoids have?
Definition
stimulate gluconeogenesis
Term
What catabolic effects do glucocorticoids have?
Definition
protein catabolism

wasting of lymph, connective tissue, fat, and skin
Term
What immunosuppressive effects do glucocorticoids have?
Definition
inhibit cell mediated actions (especially lymphocytes)
Term
What anti-inflammatory effects to glucocorticoids have?
Definition
inhibit T cell activation, eosinophils, and mast cells (histamine)
Term
Glucocorticoids are fat/water soluble.
Definition
fat soluble (cholesterol)
Term
absorption of glucocorticoids
Definition
rapid and comlete
DO cross BBB (because lipid soluble)
Term
primary site of glucocorticoid metabolism
Definition
liver (CYP450, CYP3A4)
Term
primary route of glucocorticoid excretion
Definition
renal clearance (urine)
Term
How long does a short acting corticosteroid last?
Definition
8-12 hrs
Term
duration of action for hydrocortisone
Definition
short acting
Term
duration of action for fludrocortisone
Definition
short acting
Term
special use for fludrocortisone
Definition
hypotension
Term
What type of corticosteroid is hydrocortisone?
Definition
glucocorticoid
Term
What type of corticosteroid is fludrocortisone?
Definition
mineralocorticoid
Term
prototype corticosteroid for anti-inflammatory activity
Definition
hydrocortisone
Term
hydrocortisone uses
Definition
localized inflammatory condtions
(ex: ulcerative colitis, dermatitis)
Term
relative anti-inflammatory potency of hydrocortisone
Definition
1
Term
hydrocortisone biological half life
Definition
8-12 hrs
Term
hydrocortisone contraindications
Definition
systemic fungal infection
recent ileocolostomy
intestinal anastomoses
abscess
Term
How long does an intermediate acting corticosteroid last?
Definition
18-36 hrs
Term
What type of corticosteroids are prednisone and triamcinolone?
Definition
glucocorticoids
Term
prednisone uses
Definition
adjunct for arthritis (short-term only)
asthma
COPD
ulcerative colitis/Crohn's disease
rheumatic disorders
dermatologic disorders
Term
relative anti-inflammatory potency of prednisone
Definition
4
Term
Prednisone is _________ on its own. It must be metabolized in the ________ to an active metabolite.
Definition
inactive; liver
Term
plasma half life of prednisone
Definition
60 min
Term
biological half life of prednisone
Definition
18-36 hrs
Term
administration of prednisone
Definition
oral only
Term
beclomethasone
Definition
inhaled glucocorticoid
Term
budesonide
Definition
inhaled glucocorticoid
Term
flunisolide
Definition
inhaled glucocorticoid
Term
fluticasone propionate
Definition
inhaled glucocorticoid
Term
tramcinolone acetodnide
Definition
inhaled glucocorticoid
Term
prednisone and prednisolone
Definition
oral glucocorticoids (quick relief of asthmatic symptoms)
Term
prednisolone uses
Definition
ophthalmic disorders
respiratory diseases
Term
plasma half life of prednisolone
Definition
60 min
Term
biological half life of prednisolone
Definition
18-36 hrs
Term
administration of prednisolone
Definition
oral and injectable
(systemic and local)
Term
methylprednisolone
Definition
intermediate acting glucocorticoid
Term
methylprednisolone uses
Definition
RA intra-articular injection
ulcerative colitis
severe alcoholic hepatitis
Term
plasma half life of methylprednisolone
Definition
60 min
Term
biological half life of methylprednisolone
Definition
18-36 hrs
Term
adverse effects of methylprednisolone
Definition
vertigo, headache, weight gain (fluid retention), sodium/water retention, impaired wound healing
Term
triamcinolone
Definition
intermediate acting glucocorticoid
Term
triamcinolone uses
Definition
ophthalmic disorders
respiratory diseases
Term
plasma half life of trimacinolone
Definition
60 min
Term
biological half life of trimacinolone
Definition
18-36 hrs
Term
administration of trimacinolone
Definition
oral and injectable
(systemic and local)
Term
administration of methylprednisolone
Definition
oral and injectable
(systemic and local)
Term
side effects of inhaled glucocorticoids
Definition
-oropharyngeal candidiasis (thrush)
-dysphonia (hoarseness)
-adrenal suppression
-bone loss
-retarded growth (in children)
Term
mechanisms of action for inhaled glucocorticoids
Definition
-reduce bronchial hyperreactivity
-decreased sythesis and release of inflammatory mediators
-decrease infiltration and activity of inflammatory cells
-decrease edema of the airway mucosa and mucus production
-increase responsiveness to beta-2 agonists
Term
How long do long acting corticosteroids last?
Definition
36-54 hrs
Term
betamethasone uses
Definition
respiratory diseases
respiratory distress syndrome
local inflammatory conditions
life-threatening/disabling conditions
Term
relative anti-inflammatory potency
Definition
25
Term
plasma half life for betamethasone
Definition
300+ min
Term
biological half life for betamethasone
Definition
36-54 hrs
Term
administration of betamethasone
Definition
oral, topical, and injectable
(systemic and local)
Term
dexamethasone uses
Definition
lupus
RA
life-threatening/disabling conditions
Term
relative anti-inflammatory potency
Definition
25
Term
plasma half life of dexamethasone
Definition
110-210 min
Term
biological half life of dexamethasone
Definition
36-54 hrs
Term
administration of dexamethasone
Definition
oral, topical, and injectable
(systemic and local)
Term
What drug is uses diagnostically in Cushing's?
Definition
dexamethasone
Term
Cushing's disease
Definition
pituitary releases too much ACTH which causes too much release of cortisol
Term
Cushing's sydrome
Definition
either adrenal releases too much cortisol or there is an ectopic release of ACTH or CRH that causes the adrenal to release too much cortisol

pituitary is NOT involved!
Term
cardinal signs of Cushing's
Definition
moon face
glaucoma/cataract formation
hirsutism/masculinization
cervicodorsal fat (buffalo hump)
extremity thinning/atrophy
abdominal striae (purplish)
protuberant abdomen
truncal obesity
swelling (fluid retention, edema)
brittle bones (osteoporosis)
Term
With the dexamethasone suppression test, no suppression means...
Definition
ectopic or adrenal problem
Term
With the dexamethasone suppression test, suppression means...
Definition
pituitary problem
Term
adverse effects of glucocorticoids
Definition
-adrenocortical insufficiency (HPA suppression)
-adrenocortical excess (Cushing's)
-CNS effects (psychological/behavioral changes, aggravation of pre-existing disorders)
-impaired wound healing
-MSS effects (osteoporosis, muscle weakness and atrophy)
-CV effects (fluid retention, edema, HTN)
Term
Glucocorticoid withdrawal...
Definition
should be performed SLOWLY
Term
symptoms of glucocorticoid withdrawal syndrome
Definition
hypotension
hypoglycemia
myalgia
fatigue
Term
With steroid withdrawal, the longer the duration of therapy, the ______________ the withdrawal.
Definition
slower
Term
HPA axis recover may take _______ or up to _______.
Definition
months; 2 years
Term
drugs that enhance corticosteroid effects
Definition
estrogens
OCPs
antifungals
antibiotics

*all of these inhibit CYP450 enzymes*
Term
drugs that reduce corticosteroid effects
Definition
antacids
cholestyramine
*these decrease absorption*

phenytoin
*inhibits CYP450 enzymes*
Term
corticosteroid contraindications
Definition
infections
hypertension
psychosis
peptic ulcer disease
diabetes mellitus
osteoporosis
glaucoma
pregnancy (prednisolone preferred)
Term
What exams should be done before, during, and after steroid therapy?
Definition
body weight
x-ray of spine
blood glucose
eye exam
blood pressure
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