Desgrandchamps D
Pädiatrische Klinik, Kinderspital Luzern.
Schweiz Med Wochenschr. 1992 Feb 22;122(8):247-56.
In recent years, many new substances have been synthesized in the domain of beta-lactam antibiotics (penicillins, cephalosporins, monobactams, carbapenems), macrolide antibiotics, and quinolones. Their purpose was to counter the development of resistance to older antibiotics, or to achieve pharmacokinetic ameliorations. However, resistance of clinical relevance has also been observed with these new antibiotics: the effect of all third generation cephalosporins is neutralized by the overproduction of chromosomally encoded cephalosporinases (induction or stable derepression), or by the occurrence of extended-spectrum beta-lactamases. They should be used only with caution against bacteria with possible inducibility. In macrolide antibiotics, poor bioavailability after oral administration can lead to therapeutic failure. The improved pharmacokinetic properties of the new macrolide antibiotics can correct this disadvantage. The generally highly active quinolone antibiotics show diminished activity against grampositive bacteria and Pseudomonas aeruginosa. Careful surveillance of resistance and critical use of the quinolones are essential for the prevention and control of resistance.
近年来,在β-内酰胺类抗生素(青霉素类、头孢菌素类、单环β-内酰胺类、碳青霉烯类)、大环内酯类抗生素和喹诺酮类药物领域合成了许多新物质。其目的是对抗对旧有抗生素耐药性的发展,或实现药代动力学的改善。然而,这些新型抗生素也出现了具有临床相关性的耐药性:所有第三代头孢菌素的作用都可因染色体编码的头孢菌素酶过量产生(诱导或稳定去阻遏),或因超广谱β-内酰胺酶的出现而被中和。仅在谨慎对待可能具有诱导性的细菌时才应使用它们。在大环内酯类抗生素中,口服后生物利用度差可能导致治疗失败。新型大环内酯类抗生素改善的药代动力学特性可纠正这一缺点。一般来说活性很高的喹诺酮类抗生素对革兰氏阳性菌和铜绿假单胞菌的活性降低。对耐药性进行仔细监测并严格使用喹诺酮类药物对于预防和控制耐药性至关重要。