Barcelona Laura, Marín Marcelo, Stamboulian Daniel
Fundación Centro de Estudios Infectológicos (FUNCEI), Buenos Aires.
Medicina (B Aires). 2008;68(1):65-74.
Betalactamases production is one of the main bacterial resistance mechanisms to betalactam antibiotics. The use of bectalactamases inhibitors combined with betalactam antibiotics allows the inactivation of certain betalactamases produced by Gram positive, Gram negative and anaerobic organisms, and even by mycobacteria. Betalactamases inhibitors are an improved therapeutic alternative compared with the other betalactam since, in most cases, they cover a wider antimicrobial spectrum than their analogues. Betalactamases enzimatic activity is specifically directed to the betalactam ring hydrolisis, producing a compound without antibacterial activity. According to their genomic position within microorganisms, betalactamases can be either chromosomic or plasmidic. Currently there are three betalactamases inhibitors locally available: clavulanic acid, sulbactam and tazobactam. Of them, only sulbactam has an intrinsic antimicrobial activity against penicillin binding proteins. The clinical experience from over 20 years confirms that the combination of betalactam antibiotics is effective in the empirical initial treatment of respiratory, intraabdominal, urinary tract and gynecologic infections, including those of polymicrobial origin. In the specific case of amoxicillin-sulbactam, experiences have shown the effectiveness of the combination in the treatment of peritonsillar abscess, otitis media, sinusitis, community acquired pneumonia, acute exacerbation of chronic obstructive pulmonar disease (COPD), urinary tract infection and obstetric/gynecologic infections. The spectrum and pharmacologic properties of this combination makes it also an excellent option for the treatment of skin/soft tissue and intraabdominal infections.
β-内酰胺酶的产生是细菌对β-内酰胺类抗生素产生耐药的主要机制之一。将β-内酰胺酶抑制剂与β-内酰胺类抗生素联合使用,可使革兰氏阳性菌、革兰氏阴性菌、厌氧菌甚至分枝杆菌产生的某些β-内酰胺酶失活。与其他β-内酰胺类药物相比,β-内酰胺酶抑制剂是一种更好的治疗选择,因为在大多数情况下,它们比同类药物具有更广泛的抗菌谱。β-内酰胺酶的酶活性专门针对β-内酰胺环水解,产生一种无抗菌活性的化合物。根据其在微生物基因组中的位置,β-内酰胺酶可分为染色体型或质粒型。目前有三种β-内酰胺酶抑制剂在当地可以买到:克拉维酸、舒巴坦和他唑巴坦。其中,只有舒巴坦对青霉素结合蛋白具有内在抗菌活性。20多年的临床经验证实,β-内酰胺类抗生素联合使用在呼吸道、腹腔内、泌尿道和妇科感染(包括多微生物来源的感染)的经验性初始治疗中是有效的。在阿莫西林-舒巴坦的具体案例中,经验表明该联合用药在治疗扁桃体周围脓肿、中耳炎、鼻窦炎、社区获得性肺炎、慢性阻塞性肺疾病(COPD)急性加重、泌尿道感染和妇产科感染方面是有效的。这种联合用药的抗菌谱和药理特性使其也是治疗皮肤/软组织和腹腔内感染的极佳选择。