Mod 1 lecture 1: corticosteroids and antagonists Flashcards

1
Q

what are the naturally occuring glucocorticoids

A

cortisol (hydrocortisone)
cortisone

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2
Q

what is the primary action of cortisol and cortisone

A

‘stress hormone’

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3
Q

what does cortisol and cortisone cause in the body

A

gluconeogensis in the liver - increase serum glucose
protein catabolims in extrahepatic tissue
fat catabolims in extrahepatic tissue
inhibits glucose uptake in muscle and adipose

Energy

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4
Q

what are the inflammatory and immune function of cortisol and cortisone

A

anti-inflammatory effects
immune response suppression
increase catecholamine production and response - increase BP

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5
Q

what releases CRH

A

hypothalamus

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6
Q

what releases ACTH

A

anterior pituitary

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7
Q

what releases cortisol

A

adrenal cortex

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8
Q

what does cortisol inhibit

A

CRH and ACTH

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9
Q

where is cortisol metabolized

A

liver

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10
Q

what are the corticosteroids

A

betamethasone
cortisone
dexamethasone
hydrocortisone
prednisone
methyprednisolone
triamcinalone

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11
Q

what are the mineralocorticoid agnoists and antagonists

A

fludrocortisone
spironolactone
eplerenone

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12
Q

what are the PK of corticosteroids

A

bound to corticosteroid bidning protein or albumin. metabolized by the liver and excreted by the kidney.
in CKD - would expect lower plasma protein, increased clearance, decreased t1/2. exception: prednisolone

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13
Q

What are the short acting glucocorticoids

A

1-12 hours
hydrocortisone and cortisone
have mineralocorticoid activity
liver will convert cortisone to hydrocortisone
kidney will convert hydrocortisone to cortisone

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14
Q

what are the intermediate acting glucocorticoids

A

12-36 hours
prednisone
prednisiolone
methyprednisiolne
triamcinolone

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15
Q

what are the long acting glucocorticoids

A

36-55 hours
betamethasone
dexamethasone

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16
Q

what are the key points regarding intermediate acting glucocortioids

A

have significanly more affinity to glucocortioid receptors
triamicolone has NO mineralocorticoid effects
prednisone is a prodrug that is first convered by the liver to prednisolone which is then metabolized

17
Q

what are the key points regarding long acting glucocorticoids

A

only bind to glucocorticoid receptor
used for high dose injections and lung maturation
potency is important to keep in mind

18
Q

what are the adrenal use for glucocorticoids

A

replacement therapy (hydrocortisone)
diagnosis of cushings syndrome (dexamethasone)

19
Q

what are the non-adrenal uses of glucocorticoids

A

anti - inflammatory
anti-allergy
acceleration of lung maturation (antenatal)

20
Q

what are the oral glucocoritoids

A

cortisone
dexamethasone
methyprednisolone
prednisone

21
Q

what are the intra-articular glucocorticoids

A

methyprednisolone
tramcinolone

22
Q

what are the inhaled/nasal glucocorticoids

A

beclomethasone
budesonide
flunisolids
fluticasone
mometasone
triamcinolone

23
Q

what are the IV/IM drugs

A

betamethasone
dexamethasone
hydrocortisone
methyprednisonlone
prednsolone

24
Q

what is an IM glucocortioid

A

triamcinolone

25
what is low dose dexamethasone test
diagnosis of cushings syndrome dose given is sufficient of insufficient to suppres the cortisol production - not in Cushings
26
what is seen with pituitary adenoma
high dose Dex low ACTH Low Cotisol
27
what is seen with adrenal tumor
high dose Dex Low ACTH High Cortisol
28
what is seen with Pananeoplastic (ACTH tumor)
High dose Dex High ACTH High Cortisol
29
what is seen with Cushings syndrome
low dose Dex normal or high cortisol
30
what is seen with normal HPA-Anxis
low dose Dex low ACTH low/normal Cortisol
31
What are the AE of glucocorticoids
Derm: skin thinning, weight gain, acne, cushingoid appearance, hirsutism, facial erythema, striae Eyes: cataract, intraoc pressure/glaucoma, exophthalmos Heart: fluid rentention, HTN, arrhythmias GI: gastritis, peptic ulcer, visceral perforation MSK: osteopososis, AVN, myopathy CNS: euphornia, depression, insomnia, akathisia, mania metabolism: hyperglycemia immune: increased infection risk heme: leukocytosis
32
what pre-existing conditions have increased risk of complication with glucocortioids
DM HTN HF and peripheral edema cataracts glaucoma PUD infection Low bone density/osteoporosis
33
what is the naturally occuring mineralocorticoids
aldosterone
34
what is the action of aldosterone
regulate salt and water metabolism - increase salt reabsorption -increase potassium excretion - increase hydrogen ion excretion
35
what is Fludrocortisone
synthetic mineralocorticoid -mineralocoriticoid activity - salt and water retainin properties - some glucocorticoid activity
36
what are the indication for Fludrocortisone
Addison's disease treatment and associated mineralocoritocid deficiency