Corticosteroids Flashcards

1
Q

glucocorticoids

A

stress hormones
increase glucose concentrations
anti-inflammatory effects

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2
Q

mineralocorticoids

A

Na+ retention
increase blood volume
increase blood pressure

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3
Q

cortisol (hydrocortisone)

A

binds glucocorticoid receptor
long term persistent response
inhibit inflammatory processes
increase energy levels

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4
Q

2 mechanisms of action glucocorticoids

A

anti inflammatory and immunosupression

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5
Q

glucocorticoid effect in liver

A

increase gluconeogenesis and glycogen storage

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6
Q

glucocorticoid effect in muscle

A

promote protein degradation
decrease protein synthesis
decrease sensitivity to insulin

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7
Q

glucocorticoid effect in adipose tissue

A

promote lipolysis, decrease sensitivity to insulin

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8
Q

glucocorticoid effect on immune system

A

block cytokine synthesis and inhibit production eicosanoids
immunosuppression and anti-inflammation

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9
Q

Addisons Disease

A

destruction of the cortex by tuberculosis or atrophy, decreased cortisol and aldosterone production, increased ACTH and CRH

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10
Q

addisons disease symptoms (adrenal insufficiency)

A

weakness, anorexia, low blood pressure, depression

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11
Q

cessation of long term glucocorticoid therapy can lead to ____

A

addisonian symptoms

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12
Q

Cushing’s Disease (hyperadrenalism)

A

tumors in adrenal cortex (adrenal)
pituitary carcinoma (increased ACTH)
non pituitary carcinoma (increased ectopic ACTH)

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13
Q

cushings disease symptoms

A

increased protein catabolism (brusing, delayed wound healing, muscle wasting)
osteoporosis
infections

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14
Q

long term use of glucocorticoids can lead to ___

A

cushings symptoms

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15
Q

use of corticosteroids

A

allerigic reactions, inflammation, autoimmune disease, asthma, immunosuppressive

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16
Q

cortisol active form structure and name

A

11 beta hydroxy , hydrocortisone

17
Q

fludrocortisone (structure and use)

A

mineralocorticoid therapy, 9 alpha F

18
Q

prednisone/prednisolone (strucutre, activity)

A

extra double bond 1,2, greater glucocorticoid activity and increased selectivity

19
Q

methylprednisolone (structure, activity)

A

6 alpha methyl group, greater glucocorticoid activity, reduced mineralocorticoid activity

20
Q

triamcinolone (structure, activity)

A

9 alpha F and 16 alpha OH, powerful glucocorticoid, OH reduces MR, F enhances GR potency

21
Q

dexamethasone (structure, activity)

A

16 alpha methyl group, increased lipophillicity, increased receptor binding, reduced MR activity

22
Q

betamethasone (strucutre and activity)

A

16 beta methyl, enantiomer dexamethasone

23
Q

21 esters modifications

A

acetate - COCH3, -COC3H7, lipophillic
succinate - -COCH2CH2COO, soluble
phosphate - PO2, increased solubility for emergencies

24
Q

triamcinolone acetonide

A

resistant to hydrolysis, 8 x more potent prednisolone

25
Q

beclomethasone dipropionate

A

converted rapidly during hydrolysis
14x more potent than dexamethasone

26
Q

flunisolide

A

rapid first pass metabolism by liver, minimal systemic adverse effects

27
Q

budesonide

A

low oral bioavailability, first pass metabolism

28
Q

mometasone furoate

A

highly potent, rapid metabolism

29
Q

fluticasone propionate

A

rapid first pass metabolism, lipophillic not soluble

30
Q

desired properties of inhaled glucocorticoids

A

high potency, minimal systemic effects, prolonged action

31
Q

glucocorticoids with ___ potency are safest for chronic application

A

low

32
Q
A

triamcinolone acetonide (topical, good lipophillicity, esters)

33
Q
A

fluocinonide (topical, good lipophilicity, esters)

34
Q
A

betamethasone valerate (medium potency, good lipophillicity, esters)

35
Q

what groups make topical glucocorticoids more potent

A

halogenated

36
Q

21 chlorocorticoids

A

enhanced topical anti inflammatory activity