Wallace R J, Niefield S L, Waters S, Waters B, Awe R J, Wiss K, Martin R R, Greenberg S B
Antimicrob Agents Chemother. 1982 Feb;21(2):231-5. doi: 10.1128/AAC.21.2.231.
Cefonicid (Smith Kline & French Laboratories; D-75073) is a new parenteral cephalosporin with a markedly long half-life, high serum levels, and good in vitro activity against Haemophilus influenzae. Patients with community-acquired pneumonia were randomized 2:1 to receive cefonicid, 1 g daily (21 cases) or cefamandole, 1 g every 6 h (12 cases). The two groups were similar, except that the cefonicid patients were older (mean 42 versus 31 years). Peak serum levels of cefonicid averaged 133 microgram/ml after intravenous and 83 microgram/ml after intramuscular administration compared with 55 microgram/ml with intravenous cefamandole. All 9 patients on intramuscular cefonicid and 8 or 12 patients on intravenous cefonicid had trough serum levels of greater than 2.0 microgram/ml at 24 h. Sputum levels of cefonicid were usually between 2.0 and 4.0 microgram/ml and did not correlate with serum levels. Cefonicid was well tolerated, and all cefonicid patients responded clinically. Sputum cultures for H. influenzae or Streptococcus pneumoniae became negative in 6 of 7 cefamandole patients and 13 or 15 cefonicid patients. In in vitro studies, cefonicid inhibited 90% of beta-lactamase-negative h. influenzae at 0.5 microgram/ml and beta-lactamase-positive strains at 2.0 microgram/ml. Cefonicid inhibited 50% of S. pneumoniae at 1.6 microgram/ml, but required 6.4 microgram/ml to inhibit 90%. Cefonicid once a day appears to be as safe and as effective as cefamandole four times a day for therapy of community-acquired pneumonia.
头孢尼西(史克必成公司;D - 75073)是一种新型胃肠外给药头孢菌素,其半衰期明显较长,血清浓度较高,对流感嗜血杆菌具有良好的体外活性。社区获得性肺炎患者按2:1随机分组,分别接受每日1克头孢尼西治疗(21例)或每6小时1克头孢孟多治疗(12例)。两组患者情况相似,只是接受头孢尼西治疗的患者年龄较大(平均年龄42岁,而头孢孟多组为31岁)。静脉注射头孢尼西后血清峰值浓度平均为133微克/毫升,肌肉注射后为83微克/毫升,相比之下,静脉注射头孢孟多的血清峰值浓度为55微克/毫升。所有9例接受肌肉注射头孢尼西的患者以及8或12例接受静脉注射头孢尼西的患者在24小时时的血清谷浓度均大于2.0微克/毫升。头孢尼西在痰液中的浓度通常在2.0至4.0微克/毫升之间,与血清浓度无关。头孢尼西耐受性良好,所有接受头孢尼西治疗的患者临床症状均有改善。7例接受头孢孟多治疗的患者中有6例以及15例接受头孢尼西治疗的患者中有13例,其痰液中流感嗜血杆菌或肺炎链球菌培养结果转为阴性。在体外研究中,头孢尼西在浓度为0.5微克/毫升时可抑制90%的β - 内酰胺酶阴性流感嗜血杆菌,在浓度为2.0微克/毫升时可抑制β - 内酰胺酶阳性菌株。头孢尼西在浓度为1.6微克/毫升时可抑制50%的肺炎链球菌,但抑制90%的肺炎链球菌则需要6.4微克/毫升。对于社区获得性肺炎的治疗,每日一次的头孢尼西似乎与每日四次的头孢孟多一样安全有效。