Corticosteroids

Question 1

Glucocorticoids

• produced by
• endogenous hormone
• drugs

Answer 1

Produced by the zona fasciculata
Cortisol is the endogenous hormone
Prednisone, Prednisolone, Dexamethasone, Triamcinolone, Methylprednisolone
Used for anti-inflammatory effects

Question 2

Non-genomic effects of Glucocorticoids

Answer 2

Glucocorticoid receptors in the membrane, rapid effects

Question 3

Genomic effects of Glucocorticoids

Answer 3

Nuclear type GCRs in the cytoplasm, after binding move into the nucleus to increase or decrease gene expression

Question 4

Physiologic effects of Glucocorticoids

Answer 4

Increase calcium excretion
Reduce fever
Suppress immune response
Lymphotoxic

Question 5

Adverse effects/contraindications of Glucocorticoids

Answer 5

Alter water metabolism - cause PU/PD
Generally catabolic
Antagonize insulin, avoid in diabetics
Important in parturition but inhibit fertility
Cause a 'stress' leukogram
Impair healing
Increase GI acid and decrease mucus
Increase fat absorption/disposition, increase liver enzymes

Question 6

Clinical uses of glucocorticoids

Answer 6

Diagnostic testing:
Low- and high-dose dexamethasone suppression test
Anti-inflammatory: allergies
Immunosuppressive: immune-mediated diseases

Question 7

Pharmacokinetics of glucocorticoids

Answer 7

Well absorbed orally or parenterally
Protein bound:
Specific transporter transcortin - high affinity, low capacity
Albumin secondary - low affinity, high capacity
Metabolites excreted in urine

Question 8

Hydrolyzed glucocorticoids

Answer 8

Some must be hydrolyzed to release the steroid base
Prednisone - Prednisolone
Cortisone - Cortisol
Methylprednisone - Methylprednisolone

Question 9

Duration differences in glucocorticoids

Answer 9

Short = hydrocortisone, prednisone/prednisolone, methylprednisolone
Intermediate = triamcinolone
Long = dexamethasone

Question 10

For injectable steroids, 2 kinds of recipients may be added

Answer 10

1. Salt Esters (Na succinate, Na phosphate)
   make the steroid soluble; suitable for IV administration; onset may be faster
2. Insoluble Esters (pivalate, acetate, acetonide)
   the less soluble the ester, the longer it will take to absorb =delayed onset, long duration
   opaque suspensions - not for IV use

Question 11

Mineralcorticoids

• produced by
• endogenous hormone
• drugs

Answer 11

Produced by the zona glomerulosa
Aldosterone is the endogenous hormone
Regulate Na+ retention/K+ excretion by the kidney
Fludrocortisone
DOCP