Pimecrolimus
- IUPAC: (3S, 4R, 5S, 8R, 9E, 12S, 14S, 15R, 16S, 18R, 19R, 26aS ) -3 - { (E) -2 - [( 1R, 3R, 4S) - 4-chloro- 3- methoxycyclohexyl ]-1- methyl- vinyl } - 8- ethyl-5, 6,8,11,12,13,14,15,16,17,18,19,24,25,26,26 a - hexadecahydro -5, 19.dihhydroxy -14 ,16- dimethoxy 4,10,12,18 -tetramethyl- 15 ,19 -epoxy -3H -pyrido [2,1- c] [ 1,4] - 1,7,20,21 oxazacyclotricosin (4H, 23H ) - tetrone
- SDZ ASM 981
D11AX15
Immunosuppressants
Template: Infobox chemical / molecular formula search available
Pimecrolimus ( Elidel ® trade name, manufactured by Novartis) is a drug (approval in EU: October 2002), used for the treatment of atopic dermatitis ( " eczema " ) is employed. As such, it is expected the group of topical immunomodulators, to which we also include tacrolimus. Pimecrolimus was initially treated as a very good alternative to, due to various side effects disrepute of glucocorticoids in the treatment of skin diseases. Now, however, there are growing fears that pimecrolimus in turn produces similar side effects, which is why a health warning was issued in March 2005 by the FDA.
Structure
It is a very lipophilic compound of the type of the macrolide. They found was the structure in a ferment Ascomycetenart ( ascomycete ).
Mechanism of Action
Similar to the mechanism of action of cyclosporine binds to an intracellular immunophilin pimecrolimus ( macrophilin -12). Characterized calcineurin is inhibited and decreased the activity of the T cells in the row. This now synthesize less cytokines and other inflammatory mediators. The release of inflammatory mediators from mast cells is suppressed, resulting in a decreased immune response.
Use
Pimecrolimus is used as a cream for various forms of atopic eczema to be applied on the affected skin. It is used both to short-term as well as used for long-term treatment, in which case the interval therapy is recommended. Because of the better tolerated than the glucocorticoids the possibility of a large-scale treatment and prophylactic use is granted.
Side effects
There are very commonly observed skin reactions in the form of burning, redness and itching especially at the beginning of treatment. There is also an increased risk of bacterial infections and viral diseases due to the immunosuppressive effect. An increased risk of cancer is discussed. Studies to evaluate this risk were given in USA and Europe in order. From the health authorities recommendations were initially made for use of topical immunomodulators provide, inter alia, a restriction for children up to 2 years and in immunocompromised individuals.