Pharmacology Of Glucocorticoids Flashcards
What is the adrenal gland zone responsible for the secretion of glucocorticoid?
Adrenal cortical region known as Zona fasiculata
What are the major pharmacological effects of glucocorticoids ?
The pharmacological effects are dose dependent. They are mainly immunosuppressive, anti-inflammatory and anti-allergic.
What are the main drivers of Glucocorticoid side effects ?
Higher dose and longer duration of therapy.
What are the glucocorticoids with stronger anti-inflammatory and immunosuppressive activity and weak mineralocorticoid activity ?
prednisolone and methylprednisolone
What are the mineralocorticoid effects of glucocorticoids ?
Sodium and water retention and potassium excretion.
What are the most commonly used glucocorticoids ?
prednisone, prednisolone, methylprednisolone or dexamethasone
What is the effect of glucocorticoids on the number of circulating blood cells ?
It decreases the number of T-cells, monocytes/ macrophages, eosinophils, and basophils. Whereas, it increases the number of neutrophils.
What is the effect of GC on endothelial cells?
GC treatment affects endothelial cells through diminished vessel permeability, expression
of adhesion molecules, and fibroblast
proliferation.
What are the major immunological effects of GC?
- Inhibit leukocyte traffic and access
of leucocytes to the site of inflammation, - Interfere with functions of leucocytes, fibroblasts and endothelial
cells. - Suppress the production and actions of humoral factors involved in the inflammatory process.
What is the effect of GC induced inhibition of the Proinflammatory transcription factor NFκB ?
It inhibits the synthesis of the proinflammatory cytokines IL-1, IL-6 and TNF-alpha in a dose dependent manner.
What is the biological cause of GC adverse effects ?
The glucocorticoids causes transactivation of lipocortin
1, inhibitor of NFκB, and regulator proteins which are important
for metabolism this leads to many of the GC side effects.
What is the low dose of GC ?
Less than 7.5 mg / day,these oral doses result in a saturation of the GCR of less than 40–50% and are known to result in rather mild adverse effects.
What is the medium dose of GC ?
7.5–30 mg per day which causes > 50% GCR saturation.
What is the high dose of GC
30-100 mg which causes 100% saturation of GCR.
What are the effects of GC on immune cells ?
*Decrease activation and clonal proliferation of T-helper cells
*Decrease capillary permeability of neutrophils – reduced migration to sites of injury.
*Dramatic reduction in circulating eosinophils due to promotion of eosinophil apoptosis
*Reduced circulating dendritic cells (antigen presenting cells)
