B / 12 : Glucocorticoids for oral and parenteral use

Question 1

What are common pharmacokinetic properties of glucocorticoids? (3)

Answer 1

• High bioavailability
• 80% hepatic and 20% renal metabolism
• Transported in blood 90% through CBG (corticosteroid-binding protein) and 5-10% free form

Question 2

What are the glucocorticoids for oral and parenteral use? (5)

Answer 2

• Hydrocortisone (cortisol)
• Prednisolone
• Methylprednisolone
• Dexamethasone
• Triamcinolone

(Highly Motivated People Dare Thrive)

Question 3

Hydrocortisone
- MOA
- Effect
- Indications (5)

Answer 3

• Synthetic corticosteroid
• Anti-inflammatory + increased blood glucose + increased osteoclast activity
• For replacement therapy (insufficiency, Addison’s) + topical use + pulmonary (asthma) + autoimmune diseases + leukemia

Question 3

Why are glucocorticoids well absorbed orally?

Answer 3

Because they are lipid soluble

Question 4

What are the main SE of glucocorticoids? (7)

Answer 4

• Glucose intolerance, diabetes
• Muscle wasting, skin thinning
• Impaired wound healing
• Osteoporosis
• Adrenocortical atrophy
• Salt and fluid retention
• Hypertension

Question 5

Prednisolone
- MOA
- Effect
- Indication
- ROA
- Extra

Answer 5

• Activation of glucocorticoid receptors
• Alter gene expression + systemic anti-inflammatory and immunosuppressive effect
• For severe persistent asthma and hyperthyroidism
• Oral, topical, IV
• Active version : prodrug is prednisone

Question 6

Methylprednisolone
- MOA
- Effect
- Indication
- Extra
- ROA

Answer 6

• Activation of glucocorticoid receptors
• Systemic antinflammatory and immunosuppressive effect
• For severe persistent asthma, anaphylactic shock (w/ epinephrine)
• Higher efficiency than prednisolone
• Oral, IV

Question 7

Dosage methylprednisolone

Answer 7

4-250mg

Question 8

Dexamethasone
- MOA
- Effect
- Indication (6)
- ROA

Answer 8

• Synthetic corticosteroid (glucocorticoid)
• Anti-inflammatory and immunosuppressive effect
• For cerebral edema due to brain tumors + anaphylactic shock (w/ epinephrine) + asthma + leukemia + lymphoma + diagnosis of Cushing’s
• Oral

(Highly Motivated People Dare Thrive)

Question 9

Effect of dexamethasone in cerebral edema?

Answer 9

Minimal Na retaining

Question 10

Triamcinolone
- MOA
- Indication
- Extra
- ROA

Answer 10

• Synthetic corticosteroid (glucocorticoid)
• For allergic rhinitis, dermatitis
• Mainly topical application due to higher toxicity
• Nasal spray, ointment, solution

Question 11

How do glucocorticoids act as anti-inflammatory and immunosuppressive? (6)

Answer 11

• Decrease leukocyte migration
• Lysosomal membrane stabilization : decreased phagocytosis
• Decrease capillary permeability
• Decreased COX-2 expression
• Decreased IL and platelet activation factor
• Inhibition of TNF, IL pathways