The Sound of Evolution
Prednisone
Mechanism of action:
Prednisone is a synthetic glucocorticoid. Prednisone is a prodrug that is converted in the liver by 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) into prednisolone. Prednisolone is a lipophilic molecule that freely crosses the cell membrane and binds to the glucocorticoid receptor in the cytoplasm. This forms a ligand-receptor complex that then translocates into the nucleus, where it upregulates the expression of anti-inflammatory genes such as annexin A1 and suppresses the expression of pro-inflammatory genes such as IL-1, IL-2, IL-6, and TNF-alpha.
Reference(s):
1. Czock D et al. (2005). Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet.
2. Frey BM et al. (1990). Clinical pharmacokinetics of prednisone and prednisolone. Clin Pharmacokinet.