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In the meantime, you can enjoy access to all the latest news, events and resources for different therapy areas on our website.Mechanism of action of topical corticosteroid therapy
Topical corticosteroids (TCSs) are available in a wide variety of preparations and strengths 1 and act as anti-inflammatory agents via multiple mechanisms to inhibit late phase allergic reactions. Such mechanisms include:
- Decreasing the density of mast cells
- Decreasing chemotaxis and activation of eosinophils
- Decreasing cytokine production by lymphocytes, monocytes, mast cells and eosinophils
- Inhibiting the metabolism of arachidonic acid 2
TCSs: From application to action 34
TCS action induces anti-inflammatory and immunosuppressive activity 4
Receptor binding specificity
TCSs bind GC receptors to elicit a response. 5Five types of naturally occurring/endogenous steroid receptors have been identified in vertebrates; each is associated with specific functions .6The basic structure of many steroid receptors is very similar, resulting in some overlap in the effects exerted by steroid ligands of different classes. 7,8GC receptors are the main target for mediating dermatological effects. 8High selectivity of TCSs for the GC receptor is important in order to minimise potentially harmful off-target effects of TCSs, such as fluid-electrolyte imbalance and hypertension. 9–11
Pharmacokinetics of TCS binding to GC receptors
Different TCSs can have different GC receptor affinities and binding half-lives, as demonstrated in receptor studies in the lung. 1213
High receptor affinity and a high retention in the target tissue may help to confer high local efficacy with low systemic exposure 12
Comparison of GC receptor affinity and receptor–complex half-lives of various inhaled corticosteroids in human lung 1213
References:
- Eichenfield LF, et al. J Am Acad Dermatol 2014;71:116–32
- Betnovate Cream SPC (eMC, September 2013). Available at: https://www.medicines.org.uk/emc/medicine/707 (Last accessed September 2015)
- Mehta R: InetCE (2004). Available at: www.inetce.com/articles/pdf/221-146-04-054-h01.pdf (Last accessed September 2015)
- Barnes PJ. Clinical Science 1998;94:557–72
- Ausiello DA, et al. Ausiello Ann Intern Med 2003;139:359–70
- Gao W, Bohl CE, Dalton JT. Chem Rev 2005;105:3352–70
- Fuller PJ, Lim-Tio SS, Brennan FE. Kidney Int 2000;57:1256–64
- Pérez P. Dermatoendocrinol 2011;3:166–74
- Burris TP, et al. Pharmacol Rev 2013;65:710–78
- Grossmann C, et al. Eur J Endocrinol 2004;151:397–406
- Schäcke H et al. Proc Natl Acad Sci USA 2004;101:227–32
- Valotis A, et al. J Pharm Sci 2004; 93:1337–50
- Johnson MJ. Allergy Clin Immunol 1998;101:S434–9
Cutivate, Betnovate, Dermovate and, Eumovate are registered trademarks of Stiefel, a GSK company.
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