ER II Exam 2 copy > Adrenal Corticosteroids > Flashcards

Adrenal Corticosteroids Flashcards

(48 cards)

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1
Q

How does the 11β-hydroxysteroid-dehydrogenase type 1 vs. type 2 isoenzyme differ in their action on steroids?

A
  • Type 2 converts active steroids –> inert forms
  • Type 1 converts inert steroids –> active forms
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2
Q

What are the active forms of cortisone, 11-dehydrocorticosterone, and prednisone; which enzyme activates them?

A
  • Cortisone —> cortisol (active)
  • 11-dehydrocorticosterone –> corticosterone (active)
  • Prednisone —> prednisolone (active)

*All due to 11β-hydroxysteroid-dehydrogenase type 1*

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3
Q

What are known inhibitors of 11β-hydroxysteroid-dehydrogenase type 2?

A
  • Glycyrrhizin (licorice root extract)
  • Carbenoxolone (UK approved for Rx-esophageal ulcers)
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4
Q

What is the downstream effect following inhibition of 11β-hydroxysteroid-dehydrogenase type 2 by substances such as glycyrrhizin (licorice root extract)?

A

↑ activity cortisol 2 MR –> ↑ Na+ and H2O retention, ↑ K+ loss –> ↑ BP

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5
Q

List 5 ways that glucocorticoids effect the immune system and inlammation

A
  • ↓ production of prostaglandins and leukotrienes
  • ↓ production and ↑ apoptosis of immune cell types
  • ↓ production of cytokines + their receptors
  • ↓ transmigration of neutrophils and macrophages from blood –> tissue
  • ↓ expression of cell adhesion molecules
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6
Q

Which combination of corticosteroids can be given for primary adrenal insufficiency and congenital adrenal hyperplasia?

A

Hydrocortisone + Fludrocortisone

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7
Q

List the 5 short to medium acting glucocorticoids (<12 hours)?

A
  • Hydrocortisone (cortisol)
  • Cortisone
  • Prednisone
  • Prednisolone
  • Methylprednisolone
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8
Q

What is the intermediate-acting (12-36 hour) glucocorticoid?

A

Triamcinolone

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9
Q

List the 2 long-acting (>36 hours) glucocorticoids.

A
  • Betamethasone
  • Dexamethasone
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10
Q

What are AE’s associated with prednisolone use.

A
  • Adrenal suppression
  • Growth inhibition
  • Muscle wasting
  • Osteoporosis
  • Salt retention
  • Glucose intolerance
  • Behavioral changes
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11
Q

Which drug is a glucocorticoid receptor antagonist and which receptors does it act on?

A
  • Mifepristone
  • Antagonist of glucocorticoid and progesterone receptors
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12
Q

What are the clinical uses of Mifepristone?

A
  • Medical abortion
  • Very rarely for Cushing’s Syndrome
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13
Q

Which 2 short to medium acting corticosteroids have the most potent anti-inflammatory activity and are available in a topical formula?

A
  • Prednisolone
  • Methylprednisolone
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14
Q

Of the long-acting corticosteroids which is the most potent anti-inflammatory drug?

A

Dexamethasone

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15
Q

What is the name of the mineralocorticoid agonist used clincially and what is its anti-inflammatory vs. salt-retaining potency like?

A
  • Fludrocortisone
  • Mild anti-inflammatory potency w/ ↑↑↑ salt-retaining activity
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16
Q

List the AE’s associated with mifepristone.

A
  • Vaginal bleeding in women
  • Abdominal pain + GI upset
  • Diarrhea
  • HA
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17
Q

What is the clinical application for Fludrocortisone?

A

Adrenal insufficiency (Addison’s disease)

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18
Q

What is the duration of action like for Fludrocortisone?

A

Long

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19
Q

What are 3 AE’s associated with Fludrocortisone?

A
  • Salt and fluid retention
  • CHF
  • Signs and sx’s of glucocorticoid excess
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20
Q

What is the name of the mineralocorticoid receptor antagonist?

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A

Spironolactone and Eplerenone

21
Q

What are the clinical applications of Spironolactone?

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A
  • Hyperaldosteronism from any cause
  • Hypokalemia due to diuretic effect
  • Post-MI
22
Q

What is the onset of action and duration like for Spironolactone?

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A

Slow onset and offset; duration = 24-48 hrs

23
Q

What are the AE’s and drug-interactions associated with Spironolactone?

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A
  • HYPERkalemia
  • Gynecomastia
  • Additive interaction w/ other K+ retaining drugs
24
Q

In endocrine practice, corticosteroids are given only to establish the diagnosis and cause of

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A

Cushing’s Syndrome

25
In endocrine practice, corticosteroids are given for the treatment of
adrenal insufficiency using physiologic replacement doses
26
TheCorticosteroid agonists are
Glucocorticoids (predinosone) and Mineral corticoids (fludrocortisone)
27
Pharmacologic doses of corticosteroids are used to treat patients with
inflammatory, allergic and immunological disorders
28
corticosteroids recetpor antagonists are
receptor antagonists, which are Glucocorticoid Receptor Antagonists (Mifepristone) and Mineralcorticoid antagonists, (spironolactone and Eplerenone)
29
Corticosterioid Synthesis Inhibitors are
Ketaconazole
30
Adrenal Corticosteroids Belong To The Receptor Superfamily, they are ..... that modulate gene expression
Ligand-activated transcription factors that modulate gene expression
31
ALDOSTERONE (Mineralocorticoid) -Daily Production Rate ??? g/day CORTISOL (Glucocorticoid) - Daily Production Rate~0 ??? mg/day Binds to MR with equal affinity
ALDOSTERONE (Mineralocorticoid) -Daily Production Rate~10mg/day CORTISOL (Glucocorticoid) - Daily Production Rate~0.125mg/day
32
The big things to know about adrenal glucocorticoids is that they are used for
immunosuppresion and antiinflammatory
33
In medical emergencies, consider these three things
High doses can be administered for a few days with little risk. ◦ Should not be given for more than a few days for these conditions. ◦ Use must never replace or delay more specific primary therapies (i.e. Antibiotics for septic shock; EPI or antihistamines in anaphylaxis)
34
Guidelines for Pharmacologic Corticosteroid Therapy use only after what?
• Use only after other specific therapies fail
35
Metabolic Effects of Glucocorticoids for carbohydrate metabolism
◦ ^Gluconeogenesis ◦ ^Glucose Output ◦ ^Glycogen Synthesis ◦ Decreased Glucose Uptake\>\>Development of **Hyperglycemia** think sugar overload, fat overload.
36
Glucocorticoid relation to insulin
anti insulin action, gluconeogensis, decreased glucose intake lypolysis
37
who shouldn't you give corticoseroids to?
Immunocompromised patients (HIV/AIDS) Diabetics Patients with infections Patients with peptic ulcers Patients with cardiovascular conditions HPTN CHF Angina Children
38
Pharmacokinetics of Prednisolone
Duration of Activity is longer than pharmacokinetic t1/2 of drug owing to gene transcription effects
39
Mineralocorticoids are a class of steroid hormones that influence
salt and water balance.
40
Mineralocorticoids primarily act on the kidney, where they cause
sodium and water retention and active excretion of potassium and protons.
41
Eplerenone Clinical Applications
Indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular (CV) events, primarily strokes and MI.
42
Eplerenone is cleared predominantly by ......................, with an elimination halflife of 3 to 6 hours. Steady state is reached within 2 days
cytochrome P450 (CYP) 3A4 metabolism
43
Eplerenone AE's
Most common adverse reactions were hyperkalemia and increased creatinine.
44
Ketaconazole is a
Synthesis Inhibitor
45
Ketaconazole Clinical Applications
Inhibits mammalian steroid hormone synthesis and fungal ergosterol synthesis
46
Ketaconazole AE's
Hepatic dysfunction, many drug-drug CYP450 interactions
47
metyrapone is a medication which is used for
the diagnosis of adrenal insufficeincy and occasionaly in the treatment of cushings sydrome.
48
mirotane is used to
treat cancer of adrenal glands (adrenal cortical carcinoma
ER II Exam 2 copy
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