Brogden R N, Carmine A, Heel R C, Morley P A, Speight T M, Avery G S
Drugs. 1981 Nov;22(5):337-62. doi: 10.2165/00003495-198122050-00001.
Clavulanic acid is a beta-lactamase inhibitor produced from Streptomyces clavuligerus, which when combined with certain beta-lactam antibiotics extends their activity against bacteria which owe their resistance to the production of beta-lacatamases. In combination with amoxycillin it extends the antibacterial activity of amoxycillin to include beta-lactamase-producing strains, which are otherwise resistant, as well as amoxycillin-resistant species such as Bacteroides fragilis. The addition of clavulanic acid to amoxycillin occasionally extends (but does not decrease) the susceptibility of amoxycillin-sensitive bacteria. Clavulanic acid is adequately absorbed after oral administration and its basic pharmacokinetic characteristics are similar to those of amoxycillin. Preliminary therapeutic trials suggest that amoxycillin plus clavulanic acid is effective in urinary tract infections caused by amoxycillin-resistant organisms and in lower respiratory tract infections unresponsive to previous routine antibiotic therapy, in hospitalised patients. It is generally well tolerated; nausea, vomiting, diarrhoea and skin rash being the most frequently reported adverse effects.
克拉维酸是由棒状链霉菌产生的一种β-内酰胺酶抑制剂,它与某些β-内酰胺类抗生素联合使用时,可扩大其对因产生β-内酰胺酶而具有耐药性的细菌的活性。与阿莫西林联合使用时,它可扩大阿莫西林的抗菌活性,使其包括产β-内酰胺酶的菌株(否则这些菌株具有耐药性)以及对阿莫西林耐药的菌种,如脆弱拟杆菌。在阿莫西林中添加克拉维酸偶尔会扩大(但不会降低)对阿莫西林敏感细菌的敏感性。口服给药后,克拉维酸吸收良好,其基本药代动力学特征与阿莫西林相似。初步治疗试验表明,阿莫西林加克拉维酸对住院患者中由耐阿莫西林的微生物引起的尿路感染以及对先前常规抗生素治疗无反应的下呼吸道感染有效。它通常耐受性良好;恶心、呕吐、腹泻和皮疹是最常报告的不良反应。