Glucocorticoids Flashcards

1
Q

How/when are glucocorticoids released?

A

Diurnal rhythm in response to sleep/wake cycles

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2
Q

How is glucocorticoid release regulated?

A

negative feedback

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3
Q

______ use of ______ can suppress the HPA axis and result in adrenal atrophy and insufficient adrenal response to environmental stressors (adrenal crisis).

A

Chronic; pharmacologic doses of glucocorticoids

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4
Q

Chronic use of pharmacologic doses of glucocorticoids can suppress the _____ and result in adrenal atrophy and insufficient adrenal response to environmental stressors (adrenal crisis).

A

HPA axis

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5
Q

Chronic use of pharmacologic doses of glucocorticoids can suppress the HPA axis and result in _____ and insufficient adrenal response to environmental stressors (_____).

A

adrenal atrophy; adrenal crisis

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6
Q

_____ is present in plasma bound to cortisol-binding globulin (CBG).

A

Cortisol

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7
Q

Cortisol is present in plasma bound to _____.

A

cortisol-binding globulin (CBG)

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8
Q

What is the normal half life of cortisol?

A

60-90 mins

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9
Q

What organ eliminates cortisol?

A

the liver via reduction, then the kidney via conjugation

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10
Q

How can mineralcorticoid activity be separated from glucocorticoid activity?

A

by synthesizing structural changes

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11
Q

What is the overall metabolic goal of glucocorticoids?

A

maintain glucose supply to the brain

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12
Q

Why can excessive glucocorticoid use lead to a diabetes-like state?

A

bc it stimulates gluconeogenesis

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13
Q

Why can excessive glucocorticoid use lead to muscle wasting and atrophy?

A

bc protein synthesis is decreased- can lead to catabolism

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14
Q

Why can excessive glucocorticoid use lead to centripetal obesity?

A

bc it stimulates lipogenesis in the central tissues

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15
Q

What are the permissive effects of glucocorticoids?

A

vasoconstriction, bronchodilation with catecholamines; lipolysis

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16
Q

What are the mineralocorticoid effects?

A

aldosterone-like actions

17
Q

Why can excessive glucocorticoid use lead to increased sodium and fluid retention?

A

bc it induces Na+ reabsorption from renal distal tubules and increased secretion of H+ and K+

18
Q

What are the major glucocorticoid effects?

A

anti-inflammatory, suppress the immune system, reduced vasodilation, decrease cell activation

19
Q

How do glucocorticoids reduce inflammation?

A

reduce leukotrienes by inhibiting phospholipase A2; decrease prostaglandins by blocking COX-2

20
Q

When using these agents in _____ replacement regimens (e.g., Addison’s disease), it is necessary to use an agent with both glucocorticoid and mineralocorticoid activity such as cortisol.

A

physiologic

21
Q

When using these agents in physiologic replacement regimens (e.g., _____), it is necessary to use an agent with both glucocorticoid and mineralocorticoid activity such as _____.

A

Addison’s disease; cortisol

22
Q

When using these agents in physiologic replacement regimens (e.g., Addison’s disease), it is necessary to use an agent with both _____ and ______ activity such as cortisol.

A

glucocorticoid; mineralocorticoid

23
Q

When using these agents in _____ doses for their anti-inflammatory or immunosuppressive actions, it is desirable to select an agent with minimal or no mineralocorticoid activity (e.g., dexamethasone).

A

pharmacologic

24
Q

When using these agents in pharmacologic doses for their _____ or _____ actions, it is desirable to select an agent with minimal or no mineralocorticoid activity (e.g., dexamethasone).

A

anti-inflammatory; immunosuppressive

25
Q

When using these agents in pharmacologic doses for their anti-inflammatory or immunosuppressive actions, it is desirable to select an agent with _____ (e.g., _____).

A

minimal or no mineralocorticoid activity; dexamethasone

26
Q

Mineralocorticoid activity refers to _____ at the kidney.

A

salt (Na+)-retaining actions

27
Q

______ activity refers to salt (Na+)-retaining actions at the kidney.

A

Mineralocorticoid

28
Q

Glucocorticoid activity refers to _____ effects as well as _____ actions.

A

metabolic; anti-inflammatory

29
Q

______ activity refers to metabolic effects as well as anti-inflammatory actions.

A

Glucocorticoid

30
Q

What is the natural glucocorticoid molecule?

A

cortisol

31
Q

What is the natural mineralocorticoid molecule?

A

aldosterone

32
Q

11-hydroxy glucocorticoids are _____.

A

physiologically active

33
Q

_____ are physiologically active.

A

11-hydroxy glucocorticoids

34
Q

11-keto glucocorticoids are prodrugs that must be ____.

A

activated

35
Q

What does 11β hydroxysteroid dehydrogenase I do?

A

activates 11-keto glucocorticoids

36
Q

_____ are prodrugs that must be activated.

A

11-keto glucocorticoids