Corticosteroids Flashcards

1
Q

What are the 2 main categories of Corticosteroids?

A
  1. Glucocorticoids- effect on carbohydrate metabolism

2. Mineralocorticoids- effect on electrolyte balance

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2
Q

Basic Cortisol Physiology:

A
  • Synthetic glucocorticoids are all derived from cortisol.
  • Cortisol is generated via the HPA axis.
  • -The hypothalamus release CRH, which acts on the anterior pituitary to release ACTH, which then acts on the Adrenal Gland to release Cortisol.
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3
Q

Main benefits effects of glucocorticoids?

A
  • Anti- inflammatory
  • Immunomodulating
  • Anti- proliferative
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4
Q

Glucocorticoid Mechanism of Action:

A

Glucocorticoids reduce the expression of Phospholipase 2 (PLA2) , inhibiting both the LOX (produces leukotrienes) and COX (produces PG’s and Thromboxane A2) pathway

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5
Q

LT Receptor Antagonists:

A

-Used as anti- inflammatories in the management of asthma.

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6
Q

Main Adverse Effects of Glucocorticoids:

A
  • Osteoporosis
  • Psychiatric (euphoria, depression, ect.)
  • Peptic Ulcer
  • -MANY metabolic effects (glucocorticoids oppose the effects of insulin)
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7
Q

Cushing’s Disease:

A

Cortisol in Excess
-Can be caused by Adenoma (Pituitary or Adrenal Tumour) causing excess ACTH secretion, as well as Iatrogenic causes (use of glucocorticoids)

  • Signs and symptoms of Cushing’s Disease:
  • Enhanced Fat Distribution (Moon facies & buffalo hump)
  • Enhanced proteolysis (muscle wasting)
  • Increased glucose levels (can lead to diabetes mellitus)
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8
Q

Effects of GC Withdrawal:

A

Administering glucocorticoids for long periods of time reduces cortisol secretion.
–Can lead to GC withdrawal when discontinued (also known as acute adrenal insufficiency)

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9
Q

Addisonian Crisis:

A

-Addison’s Disease- Cortisol Insufficiency
-Extreme reduction in cortisol levels.
–>Exogenous glucocorticoids inhibit ACTH production & reduce endogenous cortisol secretion.
(Life threatening and patients are left in shock)

Primary Causes: Impairment of the adrenal cortex due to serious illness.

Secondary Causes: Iatrogenic (administration of exogenous GC)

*Manage with oral or IV glucocorticoids.

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10
Q

True or False: Exogenous glucocorticoids suppress endogenous glucocorticoid secretion.

A

True.
(Occurs within 2 weeks of glucocorticoid administration/ year)
–Can take up to a full year to recover.

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11
Q

How is Addison’s Disease Managed?

A

Daily oral glucocorticoids

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12
Q

True or False: Tapering helps reduce risk / impact of GC withdrawal.

A

True.

*Mainly eliminated via hepatic metabolism.

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13
Q

Glucocorticoid effects vs. Mineralocorticoid effects:

A
  • Most glucocorticoids lack mineralocorticoid effects.
  • Cortisol has a very low anti- inflammatory effect when compared to a glucocorticoid such as Dexamethasone (30x higher anti-inflammatory)
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14
Q

Dexamethasone:

A
  • High potency glucocorticoid/ long lasting
  • -Systemic Drug
  • Used to treat nausea/ vomiting (can also be used to raise ICP)
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15
Q

Prednisone:

A
  • Intermediate acting glucocorticoid
  • Most commonly prescribed
  • Used to treat IBD, asthma/ COPD, ect.
  • Significant side effects, so use wisely.
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16
Q

Oral/ Local Applications for glucocorticoids?

A

-Inflammatory Bowel Disease
–>Budesonide has very low oral bioavailability so it is useful for local anti- inflammatory effects in IBD.
(Fewer side effects due to low oral bioavailability)

17
Q

Hydrocortisone (Cortate):

A
  • Topical corticosteroid
  • Topically used to treat rash and pruritus.

Key Side Effects:

  • Topical: Thinning of the Skin
  • Minimal systemic effects
18
Q

Flutisacone:

A
  • Inhaled corticosteroid
  • Used to treat asthma and COPD
  • -Used to treat Allergic Rhinitis (inhaled route to avoid systemic side effects)
  • Inhaled route to avoid systemic side effects.
  • Used primarily for their anti- inflammatory effects.

Key Side Effects:

  • Opportunistic Infections
  • Oral Thrush (Candida) due to local immune suppression effect.
19
Q

Metyrapone:

A
  • Corticosteroid Inhibitor

- Inhibits 11-B hydrolase

20
Q

Ketoconazole:

A
  • Corticosteroid Inhibitor

- Inhibits CYP450 enzymes (multiple steps)

21
Q

Mifepristone (RU486):

A
  • Progesterone Antagonist
  • An abortifacient
  • Very controversial drug
  • Also used to treat Cushing’s Syndrome (excess cortisol)