Corticosteroids

Question 1

glucocorticoids

Answer 1

stress hormones
increase glucose concentrations
anti-inflammatory effects

Question 2

mineralocorticoids

Answer 2

Na+ retention
increase blood volume
increase blood pressure

Question 3

cortisol (hydrocortisone)

Answer 3

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

Question 4

2 mechanisms of action glucocorticoids

Answer 4

anti inflammatory and immunosupression

Question 5

glucocorticoid effect in liver

Answer 5

increase gluconeogenesis and glycogen storage

Question 6

glucocorticoid effect in muscle

Answer 6

promote protein degradation
decrease protein synthesis
decrease sensitivity to insulin

Question 7

glucocorticoid effect in adipose tissue

Answer 7

promote lipolysis, decrease sensitivity to insulin

Question 8

glucocorticoid effect on immune system

Answer 8

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

Question 9

Addisons Disease

Answer 9

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

Question 10

addisons disease symptoms (adrenal insufficiency)

Answer 10

weakness, anorexia, low blood pressure, depression

Question 11

cessation of long term glucocorticoid therapy can lead to ____

Answer 11

addisonian symptoms

Question 12

Cushing’s Disease (hyperadrenalism)

Answer 12

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

Question 13

cushings disease symptoms

Answer 13

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

Question 14

long term use of glucocorticoids can lead to ___

Answer 14

cushings symptoms

Question 15

use of corticosteroids

Answer 15

allerigic reactions, inflammation, autoimmune disease, asthma, immunosuppressive

Question 16

cortisol active form structure and name

Answer 16

11 beta hydroxy , hydrocortisone

Question 17

fludrocortisone (structure and use)

Answer 17

mineralocorticoid therapy, 9 alpha F

Question 18

prednisone/prednisolone (strucutre, activity)

Answer 18

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

Question 19

methylprednisolone (structure, activity)

Answer 19

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

Question 20

triamcinolone (structure, activity)

Answer 20

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

Question 21

dexamethasone (structure, activity)

Answer 21

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

Question 22

betamethasone (strucutre and activity)

Answer 22

16 beta methyl, enantiomer dexamethasone

Question 23

21 esters modifications

Answer 23

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

Question 24

triamcinolone acetonide

Answer 24

resistant to hydrolysis, 8 x more potent prednisolone

Question 25

beclomethasone dipropionate

Answer 25

converted rapidly during hydrolysis 14x more potent than dexamethasone

Question 26

flunisolide

Answer 26

rapid first pass metabolism by liver, minimal systemic adverse effects

Question 27

budesonide

Answer 27

low oral bioavailability, first pass metabolism

Question 28

mometasone furoate

Answer 28

highly potent, rapid metabolism

Question 29

fluticasone propionate

Answer 29

rapid first pass metabolism, lipophillic not soluble

Question 30

desired properties of inhaled glucocorticoids

Answer 30

high potency, minimal systemic effects, prolonged action

Question 31

glucocorticoids with ___ potency are safest for chronic application

Answer 31

low

Question 32

Answer 32

triamcinolone acetonide (topical, good lipophillicity, esters)

Question 33

Answer 33

fluocinonide (topical, good lipophilicity, esters)

Question 34

Answer 34

betamethasone valerate (medium potency, good lipophillicity, esters)

Question 35

what groups make topical glucocorticoids more potent

Answer 35

halogenated

Question 36

21 chlorocorticoids

Answer 36

enhanced topical anti inflammatory activity