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Therapeutics I > Glucocorticoids > Flashcards

Glucocorticoids Flashcards

1
Q

What is the structural difference between Cortisol and aldosterone?

A

Cortisol has a 17-para-OH group

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2
Q

Where are corticoids released from?

A

Adrenal Cortex

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3
Q

What is the hypothalamic-pituitary-adrenal axis?

A

Stress signals release of CRH from hypothalamus, which signals release of ACTH from adrenal gland, which signals release of Cortisol from the adrenal gland
Cortisol is in a negative feedback loop on ACTH and CRH

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4
Q

What are the major functions of mineralocorticoids?

A

Regulate Na/K levels and blood pressure

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5
Q

What are the major functions of glucocorticoids?

A

Release stress homes, increase glucose concentration, anti-inflammator

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6
Q

What type of receptor is glucocorticoid receptor?

A

Nuclear–leads to gene activation

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7
Q

What effects does glucocorticoid have in the liver?

A

Gluconeogenesis and glycogen storage

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8
Q

What effects does glucocorticoid have in the muscle?

A

Protein degradation, decreased protein synthsis, decreases insulin sensitivity

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9
Q

What effects does glucocorticoid have on adipose tissue?

A

Lipolysis, decreased sensitivity to insulin

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10
Q

What effects does glucocorticoid have on the immune system?

A

Anti-inflammation (blocks eicosonaid synthesis)

Immunosuppression (blocks cytokine synthesis)

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11
Q

Why are glucocorticoids therapeutically useful?

A

For their anti-inflammatory action

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12
Q

What is a hormone response element (HRE)

A

The exact DNA sequence upstream of genes to be regulated by a nuclear receptor dimer

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13
Q

What are the two ways that glucocorticoids stop inflammation?

A

Up-regulate anti-inflammatory proteins like lipocortin

Down-regulate inflammatory proteins like cytokines

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14
Q

What does lipocortin I do?

A

Suppresses the production of phospholipase A2, which is used in eicosonoid production

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15
Q

How do glucocorticoids effect cytokine synthesis?

A

Activated glucocorticoid receptors bind to NFKB, so that it cannot bind to an HRE and cause cytokine production

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16
Q

What does NFKB do?

A

It acts as a transcription factor for cytokine synthesis

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17
Q

What normally inhibits NFKB?

A

IKB

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18
Q

What is Addisonian?

A

Too little glucocorticoid–causes severe weakness and can be fatal

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19
Q

What can cause Addisonian crisis?

A

Suddenly stopping glucocorticoids because of the negative feedback loop

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20
Q

What is Cushing’s syndrome?

A

Too much glucocorticoid–causes hyperglycemia, hypocalcemia, redistribution of fat, CNS effects)

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21
Q

What structural features are necessary for glucocorticoid and mineralocorticoid function?

A

C3 ketone

C3-4 double bond

22
Q

What structure features are necessary only for glucocorticoid function?

A

17-alhpa-hydroxyl

11-para-hydroxyl

23
Q

What is fludrocortisone?

A

A potent mineralocorticoid activator with a 9-alpha-F

24
Q

What is the structural difference between prednisolone and cortisol?

A

C1-2 double bond

25
Q

What is the structural difference between prednisone and prednisolone?

A

Prednisone has a ketone on 11-C that needs to be hydrolyzed before active (prodrug)

26
Q

What is the structural difference between methylprednisolone and prednisolone?

A

Methylprednisolone has a 6-alpha-methyl group

27
Q

What is the functional difference between methylprednisolone and prednisolone?

A

Methylprednisolone has a similar glucocorticoid potency with reduced mineralocorticoid activity

28
Q

What is the structural difference between triamcinolone and prednisolone?/

A

9-alpha F

16-alpha-OH

29
Q

What is the functional difference between triamcinolone and prednisolone?

A

Same glucocorticoid activity

Increased solubility, so poor absoroption/bioavailability

30
Q

What is the structural difference between dexamethasone and prednisolone?

A

9-alpha-F

16-alpha-methasone

31
Q

How does dexamethasone compare to prednisolone?

A

Stronger glucocorticoid activity with reduced mineralocorticoid
Better bioavailability than triamcinolone

32
Q

How does betamethasone compare to prednisolone structurally?

A

9-alpha-F
16-para-methasone
(like dexamethasone but with an opposite methyl group)

33
Q

What drug is betamethasone comparable to functionally?

A

Dexamethasone

34
Q

What is the benefit of a 21-ester?

A

They are activated by hydrolysis so you can control their delivery

35
Q

Which type of ester has the fastest hydrolysis?

A

Phosphate

36
Q

Which type of ester has the slowest hydrolysis?

A

Succinate

37
Q

When is phosphate ester used?

A

In emergency settings

38
Q

What does adding a 1,2 double bond do to drug activity?

A

Increase GR/MR

39
Q

What does adding a 6-alpha-CH3 or F do to activity?

A

Increase GR/MR

40
Q

What does adding a 9-alpha or Cl do to activity?

A

Increase GR and MR potency

41
Q

What does adding a 11-Beta-OH do?

A

Required for any activity

42
Q

What does adding a 16 alpha or Beta-CH3 or O do?

A

Decrease MR activity

43
Q

What does adding a 17-alpha-O do?

A

Required for GR activity

44
Q

What does adding a 21-OH or F or Cl do?

A

Required for Gr/MR activity

45
Q

What are the adverse effects of glucocorticoids?

A

Mineralocorticoid activity, metabolic effects, Cushing’s, impaired glucose tolerance, suppression of immune system, gastrointestinal, CNS, or cataracts, or Addisonian crisis

46
Q

What are the metabolic effects of glucocorticoids?

A

Steroid myopathy (muscle wasting), reduced lung bone growth in children, osteoporosis

47
Q

How can osteoporosis be prevented?

A

Bisphosphonate

48
Q

What Gastrointestinal problems can glucocorticoids cause?

A

Peptic ulcer

49
Q

What are effects can glucocorticoids have on the CNS?

A

Euphoria, depression

50
Q

What properties are desired for inhaled glucocorticoids?

A

High lipophilicty, low oral bioavailability, rapid clearance from body

Therapeutics I (9 decks)

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