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
Q

what is low dose dexamethasone test

A

diagnosis of cushings syndrome
dose given is sufficient of insufficient to suppres the cortisol production - not in Cushings

26
Q

what is seen with pituitary adenoma

A

high dose Dex
low ACTH
Low Cotisol

27
Q

what is seen with adrenal tumor

A

high dose Dex
Low ACTH
High Cortisol

28
Q

what is seen with Pananeoplastic (ACTH tumor)

A

High dose Dex
High ACTH
High Cortisol

29
Q

what is seen with Cushings syndrome

A

low dose Dex
normal or high cortisol

30
Q

what is seen with normal HPA-Anxis

A

low dose Dex
low ACTH
low/normal Cortisol

31
Q

What are the AE of glucocorticoids

A

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
Q

what pre-existing conditions have increased risk of complication with glucocortioids

A

DM
HTN
HF and peripheral edema
cataracts
glaucoma
PUD
infection
Low bone density/osteoporosis

33
Q

what is the naturally occuring mineralocorticoids

A

aldosterone

34
Q

what is the action of aldosterone

A

regulate salt and water metabolism
- increase salt reabsorption
-increase potassium excretion
- increase hydrogen ion excretion

35
Q

what is Fludrocortisone

A

synthetic mineralocorticoid
-mineralocoriticoid activity - salt and water retainin properties
- some glucocorticoid activity

36
Q

what are the indication for Fludrocortisone

A

Addison’s disease treatment and associated mineralocoritocid deficiency