Parenti M A, Hatfield S M, Leyden J J
Department of Pharmacy, Thomas Jefferson University Hospital, Philadelphia, PA 19107.
Clin Pharm. 1987 Oct;6(10):761-70.
The chemistry, mechanism of action, antimicrobial activity, pharmacokinetics, clinical efficacy, adverse effects, dosage, and administration of mupirocin are reviewed. Mupirocin, formerly termed pseudomonic acid A, is a topical antibiotic under investigation for the treatment of impetigo and other superficial primary and secondary skin infections. Mupirocin (Bactroban, Beecham Laboratories) is currently formulated as a 2% ointment in a water-miscible polyethylene glycol base. The drug is a unique antimicrobial agent because of its structure and mechanism of action. Mupirocin apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis. Mupirocin has excellent in vitro activity against staphylococci and most streptococci but less activity against other gram-positive and gram-negative bacteria. The drug will only be used topically because of its rapid and extensive systemic metabolism. Several controlled clinical trials documented that mupirocin was significantly better than the polyethylene glycol vehicle alone or ampicillin and as effective as cloxacillin, dicloxacillin, or erythromycin in producing clinical and bacteriological cures in patients with impetigo and wound infections caused by gram-positive pathogens. Limited studies suggest that mupirocin may also have a role in eradicating nasal carriage of staphylococci. Reported adverse effects are local and may be related to the polyethylene glycol vehicle base. Mupirocin should be useful for treating patients with impetigo and wound infections caused by Staphylococcus aureus. However, additional controlled, comparative clinical studies are needed to identify the role of mupirocin in treating other primary and secondary skin infections and for eliminating nasal carriage of staphylococci.
本文综述了莫匹罗星的化学性质、作用机制、抗菌活性、药代动力学、临床疗效、不良反应、剂量及用法。莫匹罗星，以前称为假单胞菌酸A，是一种正在研究用于治疗脓疱病及其他浅表原发性和继发性皮肤感染的外用抗生素。莫匹罗星（百多邦，比彻姆实验室）目前配制成2%软膏，以水溶性聚乙二醇为基质。由于其结构和作用机制，该药物是一种独特的抗菌剂。莫匹罗星显然通过可逆性抑制异亮氨酰转运RNA发挥其抗菌活性，从而抑制细菌蛋白质和RNA合成。莫匹罗星对葡萄球菌和大多数链球菌具有优异的体外活性，但对其他革兰氏阳性和革兰氏阴性菌活性较低。由于其快速且广泛的全身代谢，该药物仅用于局部给药。多项对照临床试验证明，在治疗由革兰氏阳性病原体引起的脓疱病和伤口感染患者时，莫匹罗星明显优于单独使用聚乙二醇载体或氨苄西林，且与氯唑西林、双氯西林或红霉素疗效相当。有限的研究表明，莫匹罗星在根除鼻腔葡萄球菌携带方面可能也有作用。报道的不良反应为局部性，可能与聚乙二醇载体基质有关。莫匹罗星应可用于治疗由金黄色葡萄球菌引起的脓疱病和伤口感染患者。然而，需要更多对照、比较性临床研究来确定莫匹罗星在治疗其他原发性和继发性皮肤感染以及消除鼻腔葡萄球菌携带方面的作用。
