CORTILONE (Prednisolone) diffuses into the cell, and then binds noncovalently and with high affinity to the cytoplasmic glucocorticoid receptor (GR) and forms a complex. This activated steroid-receptor complex translocates to the nucleus, binds to specific DNA sequences called glucocorticoid-responsive elements (GREs), and alters the transcription rate of specific genes associated with the GRE. This increases the synthesis of phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. In addition, CORTILONE inhibits leukocyte infiltration at the site of inflammation, suppression of humoral immune responses, and reduction in edema or scar tissue.
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