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Flashcards in Corticosteroids Deck (11):
1

Glucocorticoids
-produced by
-endogenous hormone
-drugs

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

2

Non-genomic effects of Glucocorticoids

Glucocorticoid receptors in the membrane, rapid effects

3

Genomic effects of Glucocorticoids

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

4

Physiologic effects of Glucocorticoids

Increase calcium excretion
Reduce fever
Suppress immune response
Lymphotoxic

5

Adverse effects/contraindications of Glucocorticoids

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

6

Clinical uses of glucocorticoids

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

7

Pharmacokinetics of glucocorticoids

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

8

Hydrolyzed glucocorticoids

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

9

Duration differences in glucocorticoids

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

10

For injectable steroids, 2 kinds of recipients may be added

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

11

Mineralcorticoids
-produced by
-endogenous hormone
-drugs

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