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木匹诺星(Mupirocin)——一种曾被称为假单胞菌酸的局用抗生素,最近已被美国食品和药物管理局批准用于脓疱病的治疗。它将作为2％的油膏仅凭处方销售。药理学木匹诺星是由假单胞菌发酵衍生而得。它通过结合细菌的异亮氨酰基tRNA合成酶并阻止异亮氨酸结合进蛋白链以干扰细菌的RNA及蛋白质的合成。示踪药量被吸收进入循环后很快被水解,血浆半衰期低于30分钟。抗菌活性木匹诺星与其他抗生素几乎没有交叉耐药性,这可能是由于它独特的作用机理所致。此药在酸性pH时的抗菌活性最强。一项研究表明,当pH为6时,其活性
Mupirocin, a topical antibiotic known as Pseudomonic acid, has recently been approved by the U.S. Food and Drug Administration for the treatment of impetigo. It will be sold on prescription only as a 2% ointment. Pharmacology Mupirocin is derived from the fermentation of Pseudomonas. It interferes with bacterial RNA and protein synthesis by binding the bacterial isoleucyl tRNA synthetase and blocking the incorporation of isoleucine into the protein chain. Tracer dose is absorbed into the circulation soon after hydrolysis, plasma half-life of less than 30 minutes. Antibacterial activity Mupirocin has little or no cross-resistance with other antibiotics, probably due to its unique mechanism of action. The drug has the highest antibacterial activity at acidic pH. One study showed that when the pH is 6, its activity