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Therapeutics Spring 2015 > Glucocorticoids > Flashcards

Glucocorticoids Flashcards

1
Q

What kind of activity does Fludrocortisone have?

A

good glucocorticoid activity

Strong mineralcorticoid activity

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2
Q

What kind of ADE does fludrocortisone have?

A

Strong mineralcortocoid activity causes strong Na+ retention leading to edema

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3
Q

What structural differences does fludrocortisone have compared to hydrocortisone?

A

It has a 9alpha-Fluorine

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4
Q

what kind of activity does prednisone have?

A

Strong glucocorticoid activity

reduced mineralcorticoid activity

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5
Q

What kind of activity does prednisolone have?

A

Strong glucocorticoid activity

reduced mineralcorticoid activity

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6
Q

What is the structural difference between prednisone and hydrocortisone?

A

Prednisone has a C1=C2 double bond

Prednisone has C11 double bond oxygen

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7
Q

What is the structural difference between prednisolone and hydrocortisone?

A

prednisolone has a C1=C2 double bond

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8
Q

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

A

Prednisone

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9
Q

Which has a rapid onset between prednisone and prednisolone?

A

Prednisolone

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10
Q

What is the activity of methylprednisolone?

A

very reduced mineralcorticoid activity

Strong glucocorticoid activity

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11
Q

how does methylprednisolone differ from hydrocortisone?

A

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

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12
Q

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

A

The -CH3 sterically clashes with the mineralcorticoid receptor

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13
Q

What kind of activity does triamcinolone have?

A

Strong glucocorticoid activity

reduced mineralcorticoid activity

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14
Q

What structure modifications does triamcinolone have?

A

9alpha-fluorine

16alpha-OH

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15
Q

How does the 16a-OH affect activity?

A

Reduces mineralcorticoid activity

Increases solubility –> decreases bioavailability

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16
Q

How does the 9a-F affect activity?

A

Enhances glucocorticoid activity

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17
Q

What structural alteration does dexamethasone have?

A

It has a 16a-methyl group

C1=C2

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18
Q

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

A

Increases lipophilicity –> increases receptor binding –> increases effects

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19
Q

What is the activity of dexamethasone?

A

Reduced mineralcorticoid activity

Strongest glucocorticoid activity

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20
Q

What is the structural modification of betamethasone?

A

16beta-methyl group

C1=C2

21
Q

What are 3 21-ester modifications?

A

Acetate/butyrate
phosphate
succinate

22
Q

How does a 21-ester modification affect the drug?

A

Makes it a prodrug that is activated by esterases

23
Q

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

A

Increases lipophilicity

Increases duration of action upon IM injection

24
Q

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

A

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

25
Q

How does a 21-ester succinate affect the drug?

A

Soluble

Slows hydrolysis

26
Q

What are ADE of corticoids?

A 
Crossover mineralcorticoid activity
metabolic effects
osteoporosis
Cushings-like
Impaired glucose tolerance
immunosupression
GI effects
CNS effects
Cataracts
27
Q

Triamcinolone Acetonide

A

Inhaled glucocorticoid

Azamacort, Nasocort

28
Q

What are some unique properties of triamcinolone acetonide?

A

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

29
Q

Beclomethasone dipropionate

A

Vanceril, Qvar

30
Q

What are some unique properties of Qvar?

A
  • rapidly converted hydrolyzed
  • 14x more potent than dexamethasone
  • Lipophillic
31
Q

What are some unique structural properties of Qvar?

A

9-Cl, 2 Ester-CH2CH3 groups

32
Q

Flunisolide

A

Aerobid

33
Q

What are some unique properties of flunisolide?

A
  • rapid absorption from nasal/lung tissue

- rapid liver metabolism

34
Q

What is a unique structural property of flunisolide?

A

-6Fluorine

35
Q

Budesonide

A

Pulmicort

36
Q

What is a unique structural property of budesonide?

A

1:1 mix of 16,17 butylacetal

37
Q

What are some unique properties of budesonide?

A

Faster topical uptake
low oral bioavailability
extensive first pass metabolism

38
Q

Mometasone furoate

A

Asmanex

39
Q

What are some unique structural features of mometasone furoate?

A

Aromatic group on carboxylic acid

Cl on right side

40
Q

fluticasone propionate

A

flovent, flonase

41
Q

What is a unique structural feature of fluticosone propionate?

A

S- - F group

thioester

42
Q

What are some properties of fluticasone?

A 
Inactivated by hydrolysis of thioester
very lipophilic and insoluble
very potent
poor GI absorption
Rapid topical uptake
43
Q

What are 2 types of adenocorticoids?

A

Glucocorticoids

mineralocorticoids

44
Q

What is an example of glucocorticoids?

A

cortisone (hydrocortisone)

45
Q

What is an example of mineralocorticoids?

A

aldosterone

46
Q

What is the function of glucocorticoids?

A
  • stress hormones
  • increase glucose concentrations
  • potent anti- inflammatory effects
47
Q

What is the function of mineralocorticoids?

A
  • Na reuptake in the kidney

- controls BP

48
Q

What part of the adrenal gland releases adrenal hormones–glucocorticoids, mineralocorticoids and androgens?

A

The adrenal cortex

49
Q

What is the HPA axis?

A

Stress–> brain–>hypothalamus–> Corticotropin releasing hormone–> pituitary gland–>releases adrenocorticotropic hormone–> stimulates the adrenal gland to release cortisol

Therapeutics Spring 2015 (12 decks)

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