药品详细
Pimecrolimus(吡美莫司)
化学结构式图
中文名
吡美莫司
英文名
Pimecrolimus
分子式
C43H68ClNO11
化学名
(1R,9S,12S,13S,14S,17R,21S,23S,24R,25S,27R)-12-[(1E)-1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0^{4,9}]octacos-18-ene-2,3,10,16-tetrone
分子量
Average: 810.453
Monoisotopic: 809.44808973
Monoisotopic: 809.44808973
CAS号
137071-32-0
ATC分类
D11A 未知
药物类型
small molecule
阶段
approved
商品名
Elidel;
同义名
ASM 981;pimecrolimus;SDZ ASM 981;
基本介绍
Pimecrolimus is an immunomodulating agent used in the treatment of atopic dermatitis (eczema). It is currently available as a topical cream, once marketed by Novartis, (however Galderma will be promoting the molecule in Canada in early 2007) under the trade name Elidel. [Wikipedia]
生产厂家
- Novartis pharmaceuticals corp
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference |
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剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
IMMUNOSUPPRESSIVE 免疫抑制;
药理
| Indication | For treatment of mild to moderate atopic dermatitis. |
| Pharmacodynamics | Pimecrolimus is a chemical that is used to treat atopic dermatitis (eczema). Atopic dermatitis is a skin condition characterized by redness, itching, scaling and inflammation of the skin. The cause of atopic dermatitis is not known; however, scientists believe that it may be due to activation of the immune system by various environmental or emotional triggers. Scientists do not know exactly how pimecrolimus reduces the manifestations of atopic dermatitis, but pimecrolimus reduces the action of T-cells and mast cells which are part of the immune system and contribute to responses of the immune system. Pimecrolimus prevents the activation of T-cells by blocking the effects of chemicals (cytokines) released by the body that stimulate T-cells. Pimecrolimus also reduces the ability of mast cells to release chemicals that promote inflammation. |
| Mechanism of action | Pimecrolimus binds with high affinity to macrophilin-12 (FKBP-12) and inhibits the calcium-dependent phosphatase, calcineurin. As a consequence, it inhibits T cell activation by blocking the transcription of early cytokines. In particular, pimecrolimus inhibits at nanomolar concentrations Interleukin-2 and interferon gamma (Th1-type) and Interleukin-4 and Interleukin-10 (Th2-type) cytokine synthesis in human T cells. Also, pimecrolimus prevents the release of inflammatory cytokines and mediators from mast cells in vitro after stimulation by antigen/lgE. |
| Absorption | Because of the low systemic absorption of pimecrolimus following topical application the calculation of standard pharmacokinetic measures such as AUC, Cmax, half-life, etc. cannot be reliably done. |
| Volume of distribution | Not Available |
| Protein binding | 74%-87% (in vitro, bound to plasma proteins) |
| Metabolism |
No drug metabolism was observed in human skin in vitro. Oral administration yielded metabolites produced from O-demethylation and oxygenation reactions.
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| Route of elimination | 80% of the drug is excreted in the feces. |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | Side effects include burning sensation, irritation, pruritus, erythema, and skin infections, at the application site. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| ado-trastuzumab emtansine | Avoid combination due to the increase in immunosuppressant side effects. |
| Bleomycin | Pimecrolimus may enhance the adverse/toxic effect of immunosuppressants like bleomycin. This combination is contraindicated |
| BRENTUXIMAB VEDOTIN | Avoid combination due to the potential enhancement of toxic effects of immunosuppressants |
| Canakinumab | Avoid combination due the potential increase in immunosuppressant adverse effects. |
| Carboplatin | Pimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as carboplatin. Avoid use of pimecrolimus cream in patients receiving immunosuppressants. |
| Carmustine | Pimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as carmustine. Avoid use of pimecrolimus cream in patients receiving immunosuppressants. |
| Chlorambucil | Pimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as chlorambucil. Avoid use of pimecrolimus cream in patients receiving immunosuppressants. |
| Cisplatin | Pimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as cisplatin. Avoid use of pimecrolimus cream in patients receiving immunosuppressants. |
| Cladribine | Pimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as cladribine. Avoid use of pimecrolimus cream in patients receiving immunosuppressants. |
| Clofarabine | Pimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as clofarabine. Avoid use of pimecrolimus cream in patients receiving immunosuppressants. |
| golimumab | Avoid combination due to enhancement of side effects from immunosuppressants. |
| Homoharringtonine | Avoid combination as there is potential to increase immunosuppressant adverse effects. |
| Paclitaxel | Avoid combination due to the enhancement of adverse effects of immunosuppressants. |
| Teriflunomide | Avoid combination due to the increased toxic effects of immunosuppressants. |
| Tofacitinib | Avoid combination due to the potential increase in immunosuppressant associated adverse effects. |
食物相互作用
Not Available
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