abstract |
The use of azelastin (I; 4-(p-chlorobenzyl) -2-(hexahydro-1-methyl- 1H-azepin-4-yl)-1(2H)- phthalazinone), or its pharmaceutically useful salts for treatment of inflammatory diseases and psoriasis is new. Compsns. also include an alkylglycerine of formula (II), opt. together with usual additives, carriers and/or diluents. One of R1 and R2 = 2-12C alkyl, the other is H. USE/ADVANTAGE - (I) is already known (DE 2164508) for preventing asthma and as an antiallergic agent. It is now found to be effective against inflammatory diseases, esp. ulcerative colitis, psoriasis and other inflammatory skin conditions. When applied topically, (I) normalises epidermal leukotriene concns., increases the prostaglandin concn. and also inhibits oedema induced by platelet-activating factor (PAF). Unlike steroids conventionally used, it has no significant side effects. (I) also has a cytoprotective action, e.g. against ethanol-induced damage to the gastric mucosa, and its acute oral LD50 in mice is 120-17- mg/kg. |