A.6- glucocorticoids for oral and parenteral use Flashcards
list glucocorticoids
"Hey Brother, Please Don't Tell ME CraP" Hydrocortisone (cortisol) Betamethasone Prednisone Dexamethasone Triamcinolone Methylprednisolone cortisone prednisolone
short duration (8-12h) of action GC
hydrocortisone, cortisone
intermediate duration (12-36h) of action GC
prednisolone, methylprednisolone, prednisone
triamcinolone
long duration(36-72h) of action GC
dexamethasone, betamethasone
which GC has the highest topical activity?
triamcinolone >100
which GC has the highest anti-inflammatory activity?
betamethasone 25-40
which GC is the drug of choice for replacement therapy (adrenocortical insufficiency)?
hydrocortisone (cortisol)
most important corticosteroid for Addison’s disease?
fludrocortisone (cause of it’s GC activity)
Aldosterone analogues for ADDISON’S DISEASE
Desoxycorticosterone, fludrocortisone
drug of choice for systemic anti-inflammatory and immunosuppressive effects
prednisolone, methylprednisolone
others less preferred: dexamethasone, betamethasone
topical application mainly GC
Triamcinolone
pharmacokinetics of GC
- high BA (good oral absorption)
- transport in blood- 90% CBG, 5-10% free form
- half life-60-90 min’
- metabolism: 80% hepatic, 20% renal or other
give 5 mechanisms of GC as anti-inflammatory and immunosuppressive drug
- ↓ leukocyte migration
- ↓ phagocytosis
- ↓ cox 2 expression
- ↓ interleukins (IL-2)
- inhibition of NF-KB pathway
clinical indications for GC
- allergic reactions
- collagen- vascular disorders
- eye diseases
- pulmonary diseases
- GI diseases
- hematologic disorders
- skin abnormalities
- neurologic disorders
systemic inflammation, sepsis, organ transplantation, autoimmune disorders, dexamethasone suppression test (diagnostics)
everything….
SE of GC
- growth inhibition
- diabetes
- central adiposity
- impaired wound healing
- osteoporosis
- hypertension
- psychosis
- hypokalemia
- glaucoma
- adrenal atrophy
