Frampton J E, Brogden R N, Langtry H D, Buckley M M
Adis International Limited, Auckland, New Zealand.
Drugs. 1992 Nov;44(5):889-917. doi: 10.2165/00003495-199244050-00011.
Cefpodoxime proxetil is an orally administered prodrug which is absorbed and de-esterified by the intestinal mucosa to release the third generation cephalosporin, cefpodoxime. Cefpodoxime is stable towards the most commonly found plasmid-mediated beta-lactamases and the drug has a broad spectrum of antibacterial activity encompassing both Gram-negative and Gram-positive bacteria, rendering it a possible option for empirical use in a wide range of community acquired infections in both adult and paediatric patients. The extended plasma half-life of cefpodoxime (1.9 to 3.7 h) permits twice daily administration. In comparative trials, twice daily cefpodoxime proxetil (dose equivalent cefpodoxime 100 to 400 mg) was as effective as a 3- to 4-times daily regimen of phenoxymethylpenicillin in pharyngotonsillitis, as well as thrice daily amoxicillin (with or without clavulanic acid) or cefaclor against infections of the ear, the upper and lower respiratory tract, the urinary tract and those of the skin and soft tissues. The latter reflects the enhanced antistaphylococcal activity of cefpodoxime, which distinguishes it from other orally active third generation cephalosporins such as cefixime. Most notably, an oral regimen of cefpodoxime proxetil was as efficacious as parenterally administered ceftriaxone for the treatment of bronchopneumonia in hospitalised patients at risk due to the presence of underlying diseases, addictions or advancing age. A single oral dose of cefpodoxime was also as efficacious as ceftriaxone in uncomplicated anogenital gonococcal infections. Cefpodoxime proxetil is generally well tolerated, with mild to moderate gastrointestinal disturbances occurring in 4 to 15% of patients treated with therapeutic doses. Thus, a convenient twice daily oral regimen of cefpodoxime proxetil can be prescribed as an effective alternative to established beta-lactam therapies in the empirical outpatient treatment of infections of the respiratory and urinary tracts as well as those of the skin and soft tissues.
头孢泊肟酯是一种口服前体药物,经肠道黏膜吸收并去酯化后释放出第三代头孢菌素头孢泊肟。头孢泊肟对最常见的质粒介导的β-内酰胺酶稳定,该药物具有广泛的抗菌活性,涵盖革兰氏阴性菌和革兰氏阳性菌,使其成为成人和儿童患者多种社区获得性感染经验性用药的一个可能选择。头孢泊肟的血浆半衰期延长(1.9至3.7小时),允许每日给药两次。在比较试验中,每日两次服用头孢泊肟酯(剂量相当于头孢泊肟100至400毫克)在治疗咽炎和扁桃体炎方面与每日3至4次服用苯氧甲基青霉素的方案效果相当,在治疗耳部、上呼吸道和下呼吸道、泌尿道以及皮肤和软组织感染方面与每日三次服用阿莫西林(有无克拉维酸)或头孢克洛效果相当。后者反映了头孢泊肟增强的抗葡萄球菌活性,这使其有别于其他口服活性第三代头孢菌素如头孢克肟。最值得注意的是,对于因存在基础疾病、成瘾或年龄增长而有风险的住院患者,口服头孢泊肟酯方案在治疗支气管肺炎方面与静脉注射头孢曲松同样有效。在单纯性肛门生殖器淋球菌感染中,单次口服头孢泊肟的疗效也与头孢曲松相当。头孢泊肟酯一般耐受性良好,治疗剂量下4%至15%的患者会出现轻度至中度胃肠道不适。因此,在呼吸道、泌尿道以及皮肤和软组织感染的经验性门诊治疗中,可开具方便的每日两次口服头孢泊肟酯方案,作为已确立的β-内酰胺疗法的有效替代方案。