Glaxosmithkline, Schering corp sub schering plough corp, Schering corp • 糖皮质激素类药。主要用于持续性哮喘的长期治疗。按照支气管哮喘严重程度分级标准,在轻度持续(2级以上)即可使用吸入糖皮质激素治疗;外用适用于对糖皮质激素外用有效的各种非感染性炎症性皮肤病,如亚急性和慢性湿疹、脂溢性皮炎、接触性皮炎、特应性皮炎、局限性神经性皮炎、寻常型银屑病、盘状红斑狼疮、扁平苔癣等。亦可用于常年性变应性鼻炎和季节性变应性鼻炎及血管收缩性鼻炎;亦用于鼻息肉切除术后,预防息肉的再生。
Beclomethasone dipropionate is an inhaled corticosteroid used as maintenance treatment in the prophylaxis of asthma attacks.
Beclomethasone dipropionate is a corticosteroid and prodrug that is rapidly activated by hydrolysis to the active monoester, 17 monopropionate (17-BMP), which mediates anti-inflammatory actions. 17-BMP has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor which is approximately 13 times that of dexamethasone and 25 times that of beclomethasone dipropionate. Upon binding of the ligand, the glucocorticoid receptors dimerize and translocate into the nucleus, where they subsequently bind to glucocorticoid response elements (GRE) on glucocorticoid-responsive genes, leading to changes in transcription. There are several proposed mechanisms for the anti-inflammatory action of corticosteroids. Corticosteroids may work by increasing the transcription of genes coding for anti-inflammatory proteins, including lipocortin-1 and interleukin-10. Corticosteroids were also shown to inhibit the expression of multiple genes that encode pro-inflammatory factors, such as cytokines, chemokines, and adhesion molecules, that are activated during the chronic inflammatory process. This is thought to be due to the direct inhibitory interaction between activated glucocorticoid receptors and activated pro-inflammatory transcription factors, such as nuclear factor-kappa B and activator protein-1. Chronic inflammation is often characterized by enhanced expression of these transcription factors that bind to and activate coactivator molecules, which then acetylate core histones to switch on gene transcription to further amplify the inflammatory process. Corticosteroids suppress the multiple inflammatory gene expression by promoting histone deacetylation, resulting in tighter coiling of DNA and reduced access of transcription factors to their binding sites.