Corticosteroids Flashcards
Corticosteroid are steroid hormones produced by the —————
adrenal cortex
The 2 major physiologic and pharamcologic groups of corticosteroids
1) Glucocorticoids –> important effects on Inflammation
–> causes profoundinhibition of inflammatory responses and cause immunosuppression.
2) Mineralocorticoids –> regulate sodium and potassium reabsorption in the kidney
category of Aldosterone
Mineralcorticoids
MoA of Aldosterone
Regulate Sodium and potassium reabsorption in the Kidney.
Category of Cortisol
Natural Glucocorticoids
indication of cortisol/Hydrocorticone/ Prednisone/Betamethasone/Dexamethasone
1.Inflammatory or immunologic conditions.
–> Asthma, Organ transplant rejection, RA.
2. Adrenal cortical insufficiency’s (aka Addison’s disease)
3. Congenital adrenal hyperplasia.
4. For maturation of fetal lungs –>
Betamethasone is administered for
women in labor or having premature
contraction.
MoA of Cortisol/Hydrocortisone/Dexamethasone/Prednisone/Betamethasone
- Glucocorticoids enter the cell and bind to cytosolic receptors.
-Steroid-receptor complex is transported
into the nucleus.
- This causes alteration in gene expression by binding to glucocorticoid response elements (GREs)
toxcities of Dexamethasone/Cortisol/Hydrocotisol/
Predisone/Betamethasone
Toxicities;
1) Osteoporosis, growth inhibition, diabetes, muscle wasting, salt retention, psychosis (behavioral changes).
–> to minimize side effects –>Local application
(e.g. aerosols for asthma)
2) Alternate-day therapy.
Slow withdrawal after
continuous use–> to allow recovery of normal adrenal function.
Category of Hydrocortisone
Natural Glucocorticoid
Category of Prednidone
Synthetic Glucocorticoids
category of betamethasone
Synthetic Glucocorticoids
Category of Dexamethasone
Synthetic Glucocorticoids
PK/PD of cortisol/ Hydrocortisone
- 95% bound to CBG in plasma.
- Well absorbed when given orally, metabolized by the liver.
- Has a short duration of action compared with its synthetic analogs.
- Small but significant salt retaining effect
PK/PD dexamethasone/ Betamethasone/ Prednisone
- **Longer half-life and duration of action
- Reduced salt-retaining effect.**
- Special glucocorticoids have been developed for use in asthma and topical use.
–> Good surface activity on mucous membranes or skin is needed.
–> Systemic effects avoided.