Glucocorticoids Flashcards Preview

Therapeutics Spring 2015 > Glucocorticoids > Flashcards

Flashcards in Glucocorticoids Deck (49)
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1

What kind of activity does Fludrocortisone have?

good glucocorticoid activity
Strong mineralcorticoid activity

2

What kind of ADE does fludrocortisone have?

Strong mineralcortocoid activity causes strong Na+ retention leading to edema

3

What structural differences does fludrocortisone have compared to hydrocortisone?

It has a 9alpha-Fluorine

4

what kind of activity does prednisone have?

Strong glucocorticoid activity
reduced mineralcorticoid activity

5

What kind of activity does prednisolone have?

Strong glucocorticoid activity
reduced mineralcorticoid activity

6

What is the structural difference between prednisone and hydrocortisone?

Prednisone has a C1=C2 double bond
Prednisone has C11 double bond oxygen

7

What is the structural difference between prednisolone and hydrocortisone?

prednisolone has a C1=C2 double bond

8

Which is more selective for the glucocorticoid receptor, prednisone or prednisolone?

Prednisone

9

Which has a rapid onset between prednisone and prednisolone?

Prednisolone

10

What is the activity of methylprednisolone?

very reduced mineralcorticoid activity
Strong glucocorticoid activity

11

how does methylprednisolone differ from hydrocortisone?

It has a C1=C2 and a 6alpha-CH3 group

12

What effect does the -CH3 in methylprednisolone have on the mineralcorticoid receptor?

The -CH3 sterically clashes with the mineralcorticoid receptor

13

What kind of activity does triamcinolone have?

Strong glucocorticoid activity
reduced mineralcorticoid activity

14

What structure modifications does triamcinolone have?

9alpha-fluorine
16alpha-OH

15

How does the 16a-OH affect activity?

Reduces mineralcorticoid activity
Increases solubility --> decreases bioavailability

16

How does the 9a-F affect activity?

Enhances glucocorticoid activity

17

What structural alteration does dexamethasone have?

It has a 16a-methyl group
C1=C2

18

What affect does the 16a-methyl group have on activity?

Increases lipophilicity --> increases receptor binding --> increases effects

19

What is the activity of dexamethasone?

Reduced mineralcorticoid activity
Strongest glucocorticoid activity

20

What is the structural modification of betamethasone?

16beta-methyl group
C1=C2

21

What are 3 21-ester modifications?

Acetate/butyrate
phosphate
succinate

22

How does a 21-ester modification affect the drug?

Makes it a prodrug that is activated by esterases

23

How does a 21-ester acetate modification affect drug properties?

Increases lipophilicity
Increases duration of action upon IM injection

24

How does a 21-ester phosphate modification affect the drug?

increases solubility
Rapidly hydrolized--> decreases time to onset
optimal for IM/IV injection

25

How does a 21-ester succinate affect the drug?

Soluble
Slows hydrolysis

26

What are ADE of corticoids?

Crossover mineralcorticoid activity
metabolic effects
osteoporosis
Cushings-like
Impaired glucose tolerance
immunosupression
GI effects
CNS effects
Cataracts

27

Triamcinolone Acetonide

Inhaled glucocorticoid
Azamacort, Nasocort

28

What are some unique properties of triamcinolone acetonide?

8x more potent than prednisolone
Acetonide is resistant to hydrolysis
Highly soluable

29

Beclomethasone dipropionate

Vanceril, Qvar

30

What are some unique properties of Qvar?

-rapidly converted hydrolyzed
- 14x more potent than dexamethasone
-Lipophillic