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SATURDAYOctober 16SESSION 210:45– 11:00Click here to return to Dermatology Update 2004 Schedule and Abstracts |
Kim Papp Retinoids are small molecule hormones that control the expression of numerous genes by interacting with multiple nuclear receptors. The effects of retinoids are mediated by 2 distinct classes of receptor with 3 pathways each: Retinoic Acid Receptors (RAR a , RAR b , RAR g ) and Retinoid X Receptors ( RXR a , RXR b , RXR g ). Current retinoids bind non-selectively to both RAR and RXR receptors which upon activation may give an array of positive therapeutic activities but which also can be negative in that they illicit a broad spectrum of unwanted side effects. Tazarotene is a prodrug which is rapidly converted into its active metabolite Tazarotenic acid. It is a locked molecule meaning that it can avoid isomerization, and hence, act specifically on target receptors. Tazarotene is highly selective for RAR b & RAR g and has less of an affinity for RAR g . It does not bind to the RXR subtype. RAR g are the only receptors expressed in the skin. This selective nature of receptor activation leads to a designer retinoid that avoids the typical retinoid class side effects. Oral Tazarotene has shown no known drug-drug interactions, it is not stored in fatty tissue and has a short half life of 7-12 hours.
Click here to return to Dermatology Update 2004 Schedule and Abstracts |