Reeves D S, Bullock D W
Infection. 1979;7 Suppl 5:S425-33. doi: 10.1007/BF01659764.
In this review we have compared and contrasted the antibacterial and pharmacological properties of the aminopenicillins currently available. It is apparent that there is little hard evidence (except in the case of thphoid fever) that either amoxycillin or the pro-drug esters of ampicillin are significantly more effective than ampicillin itself, despite their better absorption and higher serum levels. However, amoxycillin and the ampicillin pro-drug esters do cause fewer bowel side-effects than ampicillin, which may justify their use despite the extra cost involved. The problem of susceptibility to penicillinases is unlikely to be solved by modification of the aminopenicillin molecule. A more likely solution is administration of these substances with beta-lactamase inhibitors such as clavulanic acid. Trials with such combinations are already under way.
在本综述中,我们对目前可用的氨基青霉素的抗菌和药理学特性进行了比较和对比。显而易见,几乎没有确凿证据(伤寒热情况除外)表明阿莫西林或氨苄西林的前体药物酯比氨苄西林本身显著更有效,尽管它们吸收更好且血清水平更高。然而,阿莫西林和氨苄西林前体药物酯引起的肠道副作用比氨苄西林少,这可能证明尽管成本更高但仍可使用它们是合理的。对氨基青霉素分子进行修饰不太可能解决对青霉素酶敏感的问题。更有可能的解决办法是将这些物质与β-内酰胺酶抑制剂(如克拉维酸)联合使用。此类联合用药的试验已经在进行中。