Lamb H M, Wiseman L R
Adis International Limited, Auckland, New Zealand.
Drugs. 1998 Dec;56(6):1047-52; discussion 1053-4. doi: 10.2165/00003495-199856060-00011.
Pexiganan acetate (MSI 78) is a synthetic cationic peptide (22 amino acids) with antibacterial activity. It is an analogue of magainin 2, which is a host defence peptide isolated from frog skin. The drug is thought to act by disturbing the permeability of the cell membrane or cell wall. Pexiganan acetate has good in vitro activity against Gram-positive and Gram-negative aerobes; 99% of strains were susceptible to the agent using a break-point of 64 mg/L. 89 to 97% of anaerobes were susceptible to pexiganan acetate using the same break-point. After 7 passages in vitro, there was no evidence of resistance to pexiganan acetate among 2 strains of Staphylococcus aureus. In 2 phase III multicentre randomised double-blind trials in diabetic patients with infected foot ulcers, both topical pexiganan acetate 1% and oral ofloxacin 800 mg/day achieved clinical cure or improvement in about 90% of patients. Eradication of pathogens in the 2 studies was achieved in 82% of ofloxacin recipients and 66% of pexiganan acetate recipients at the end of therapy. Limited data indicate that pexiganan acetate is well tolerated.
醋酸聚西加南（MSI 78）是一种具有抗菌活性的合成阳离子肽（含22个氨基酸）。它是蛙皮素2的类似物，蛙皮素2是一种从蛙皮中分离出的宿主防御肽。该药物被认为是通过干扰细胞膜或细胞壁的通透性来发挥作用。醋酸聚西加南对革兰氏阳性和革兰氏阴性需氧菌具有良好的体外活性；采用64mg/L的折点，99%的菌株对该药物敏感。采用相同折点时，89%至97%的厌氧菌对醋酸聚西加南敏感。在体外传代7次后，2株金黄色葡萄球菌中没有出现对醋酸聚西加南耐药的迹象。在两项针对患有感染性足部溃疡的糖尿病患者的III期多中心随机双盲试验中，局部使用1%醋酸聚西加南和口服800mg/天的氧氟沙星，在约90%的患者中均实现了临床治愈或病情改善。在两项研究中，治疗结束时，82%的氧氟沙星治疗患者和66%的醋酸聚西加南治疗患者实现了病原体清除。有限的数据表明，醋酸聚西加南耐受性良好。
