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Pharm exam 4 > Adrenal agents > Flashcards

Adrenal agents Flashcards

1
Q

Drug targets

A

11B-hydroxylase (if inhibited –> no aldosterone)

17a-hydroxylase (if inhibited –> no cortisol)

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2
Q

Metabolism of cortisol:

Cortisol cortisone

  • high doses of cortisol can cause 1 to become saturated
  • Elevation of cortisol levels in kidney cells can activate 2 causing salt/water retention, 3 and 4.
A
  1. 11B-HSD2
  2. MR
  3. hypokalemia
  4. hypertension
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3
Q

what glucocorticoids are prodrugs

what enzyme activates them?

A

cortisone

prednisone

cortisone, prednision –1B-HSD1 (liver)–> cortisol, prednisolone

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4
Q

General adverse effects of glucocorticoid therapy

A
  1. decrease growth in children
  2. osteoporosis
  3. increased appetite
  4. glaucoma
  5. increased risk of infection/impaired wound healing
  6. emotional disturbances
  7. increased risk of diabetes
  8. hypokalemia
  9. HTN

**HPA axis suppression - function may not return to normal for up to 12 months

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5
Q

Glucocorticoid drug interactions:

  • can bind to MR in renal collecting duct and increase 1 retention and 2 secretion
  • coadministration of 3 with glucocorticoids can increase risk of stomach ulcers
  • can reduce the effects of 4, 5, and 6 medications
A
  1. Na
  2. K+
  3. NSAIDs
  4. hypoglycemic
  5. blood pressure
  6. glaucoma meds
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6
Q

Antiinflammatory effects of glucocorticoids

A
  • inhibit phospholipase A –> decrease eicosanoids
  • inhibit COX-2 synthesis –> decrease prostaglandin
  • inhibit cytokine production –> suppression of cell-mediated inflammation
  • reduce activity and number of mast cells –> decrease histamine and 5-HT, decrease capillary permeability
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7
Q

what is the 1st line tx for pts with persistent asthma

A

Fluticasone

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8
Q

____ should be used in pts who take B2-receptor agonists more than twice weekly

A

inhaled glucocorticoids - fluticasone

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9
Q

MOA of inhaled glucocorticoids

A

Reduce leakiness of vascular endothelial cells (caused by inflammation)

reduce grwowth of airway smooth muscles (proliferation and hypertrophy of ASM cell contribute to asthma pathology)

decrease adhesion molecules in airway epithelial cells

increase epithelial integrity

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10
Q

interaction b/w GC and long-acting B2-receptor agonists

A

corticosteroids:

  • increase B2-R expression
  • prevent desensitization of B2-R

B2 agonist effects:

  • Increase nuclear translocation of GR
  • Increase binding of GRs to GREs on genes
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11
Q

SE of inhaled GC

A

Local effects: dysphonia (hoarse voice)

oropharyngeal candidiasis

cough

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12
Q

how is primary adrenal insufficiency treated (Addison’s disease)

  • deficiency in cortisol, aldosterone, and androgens
  • ACTH and CRH elevated
  • Hypotension
A

Oral cortisol

Fludrocortisone

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13
Q

How would you treat secondary adrenal insufficiency?

Pituitary disease

  • decrease ACTH –> increase CRH
  • decrease in cortisol

Hypothalmic disease

  • decrease in CRH –> decrease in ACTH
  • decrease in cortisol
A

cortisol

no fludrocortisone

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14
Q

What would you use to determine the cause of Cushing’s syndrome?

A

Dexamethosone

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15
Q

High dose dexamthasone suppression test: what is the cause of cushings if:

  • decrease CRH
  • increase ACTH

50% reduction in cortisol

A

Pituitary hypersecretion of ACTH (Cushing’s disease)

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16
Q

High dose dexamthasone suppression test: what is the cause of cushings if:

  • decrease CRH
  • decrease ACTH
A

Adrenal adenoma

17
Q

High dose dexamthasone suppression test: what is the cause of cushings if:

decreased CRH

increase ACTH

A

Ectopic ACTH production

18
Q

what drugs are used for the tx of Cushing’s syndrome?

A

Metyrapone

Ketoconazole

19
Q

MOA of metyropone

A

inhibitor of 11B-hydroxylase

blocks aldosterone and cortisol secretion

20
Q

MOA of Ketoconzaole (antifungal)

A

inhibit 17a-hydroxylase (can inhibit 11B-hydroxylase at high levels)

blocks cortisol formation

21
Q

SE of ketoconazole

A

liver toxicity

22
Q

at high doses what drug is a glucocorticoid receptor antagonists that is used to treat inoperable pts with ectopic ACTH secretion or adrenal carcinoma

A

Mifepristone (also has anti-progestin effects used to terminate pregnancy)

23
Q

Cortisol, prednisone, triamcinolone, dexamethasone - compare the anti-inflammatory effects, salt retaining effects and duration of action

A

Cortisol = short acting, lowest anti-inflammatory effect, low salt retention

Prednisone = intermed. acting, intermed. anti-inflammatory, low salt retention

Triamcinolone = intermed acting, intermed antiinflammatory, 0 salt retention

Dexamethasone = long acting; highest anti-inflammatory effect, 0 salt retention

Pharm exam 4 (15 decks)

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