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Term III: Pharmacology > Anti-Inflammatory Steroids > Flashcards

Anti-Inflammatory Steroids Flashcards

1
Q

Stimulates adrenal cortex to secrete glucocorticoids, mineralocorticoids, and weak androgens.

A

Corticotropin (ACTH)

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2
Q

What is the prototype for glucocorticoids?

A

Cortisol

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3
Q

What is the prototype for mineralocorticoids?

A

Aldosterone

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4
Q

Prednisone/Prednisolone

A

Steroid

Inhibits phospholipase A2, resulting in less prostaglandins, leukotrienes

Anti-inflammatory

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5
Q

Name 2 fluorinated steroids.

A

Dexamethasone and triamcinolone

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6
Q

Where are glucocorticoid receptors found? What do they bind?

A

Intracellularly - translocate to cell nucleus and dimerize after steroid binding. Bind to HREs.

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7
Q

What are HRE’s?

A

Hormone responsive elements. DNA targets involved in regulation of specific gene promoters

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8
Q

Glucocorticoids induce synthesis of _____ which suppress activation of _____. As a result, release of ______ and production of pro-inflammatory eicosanoids are decreased.

A

Lipocortins

Phospholipase A2

Arachidonic acid

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9
Q

Glucocorticoids suppress _______ induction in inflammatory cells that are usually induced by pro-inflam stimuli like _____.

A

PGHS-2 (prostaglandin H synthase-2)

PGE2

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10
Q

Reduction of cytoprotective prostaglandin levels will lead to ______ and _____.

A

GI ulcerations and bleeds.

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11
Q

Prostaglandin that modulates gastric mucosal acid secretion, mucus levels, and blood flow.

A

PGE2

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12
Q

Prostaglandin with vasodilator actions that has cytoprotective properties.

A

PGI2

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13
Q

Prostaglandins that cause erythema.

A

PGD2, PGE1

PGE2, PGI2

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14
Q

Prostaglandins that cause systemic fever, local heat, and pain.

A

PGE2, PGI2

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15
Q

Prostaglandin that causes edema.

A

PGE2

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16
Q

Betamethasone

A

Most potent steroid

Anti-inflammatory

17
Q

Hydrocortisone

A

Glucocorticoid

Increases plasma glucose/lipids/Na+

Anti-inflammatory

18
Q

What are the 4 determinants of increased glucocorticoid duration of action?

A
  1. Protein binding – larger bound fraction correlates with extended duration
  2. 11β-HSD II binding affinity – lower affinity correlates with extended duration
  3. Lipophilicity – greater promotes adipose storage and extends duration
  4. Glucocorticoid Receptor Affinity – stronger binding extends duration of action
19
Q

What is a disease of primary adrenal insufficiency? How do you treat it?

A

Addison’s Disease - hydrocortisone supplemented with a mineralocorticoid (fluorocortisone)

20
Q

What is the correct treatment for secondary adrenal insufficiency?

A

Hydrocortisone alone (RAAAs provides enough mineralocorticoid)

21
Q

Lympholytic effects of steroids have proven efficacious in treatment of _______ and _____.

A

Lymphocytic leukemia and multiple myeloma

22
Q

T or F. Corticosteroids are curative drugs.

A

False! They suppress symptoms, but do not cure.

23
Q

What syndrome involves adrenocorticotropin (ACTH) excess caused by pituitary or ectopic ACTH overproduction, adrenal tumors, or exogenous glucocorticoid administration?

A

Cushing’s syndrome

24
Q

What are the symptoms of Cushing’s syndrome?

A
  1. Muscle weakness - due to decreased muscle mass
  2. Central fat deposition
  3. Moon face
  4. Purple abdominal striae
  5. Glucose intolerance
  6. Neuropsychiatric disorders
25
Q

What are the effects of glucocorticoid therapy on gastric mucosa?

A

Peptic ulcers

26
Q

What are possible skeletal effects of glucocorticoid therapy?

A

Osteoperosis and osteonecrosis

27
Q

Name potential effects of glucocorticoid therapy on the following:

  1. Ophthalmic effects
  2. Fluid and electrolyte disturbances (fluorcortesol)
  3. Iatrogenic adrenal insufficiency
  4. Blood glucose levels
A
  1. Cataracts
  2. Na+ and water retention
  3. Suppression of hypothalamic and pituitary activity, leading to adrenal atrophy
  4. Hyperglycemia –> Diabetes
28
Q

What are strategies for mgmt of adverse effects of glucocorticoid therapy?

A
  • Intermittent dosing strategies
  • Topical or inhaled administration
  • Use lowest dose possible
29
Q

What are potential issues after withdrawal from therapy?

A
  • Flare-up of disease (most frequent)

- Acute adrenal insufficiency (most severe)

30
Q

**sone

A

Inactive ketone form of steroid

31
Q

***solone

A

Active hydroxyl form of steroid

Topical/inhaled steroids for rapid use

Term III: Pharmacology (19 decks)

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