Pedersen M, Støvring S, Mørkassel E, Koch C, Høiby N
Scand J Infect Dis. 1986;18(3):245-54. doi: 10.3109/00365548609032334.
A double-blind cross-over study was undertaken to compare the efficacy of amoxycillin and pivampicillin on Haemophilus influenzae infection of the lower respiratory tract in children. 20 patients with cystic fibrosis (CF) or chronic obstructive pulmonary disease (COPD) due to other causes were included in the study. All patients had a history of regularly harbouring H. influenzae in sputum and repeated treatment failures with pivampicillin. 18 completed two 14-day courses in random order with equimolar doses of pivampicillin (80 mg/kg/day) and amoxycillin (62 mg/kg/day). Both drugs were well tolerated with no serious side effects, but pivampicillin was associated with more pronounced nausea. In steady state the mean serum concentrations of antibiotics 2 and 4 h after medication were 9.7 and 3.7 micrograms/ml for pivampicillin and 19.1 and 7.9 micrograms/ml for amoxycillin (p less than 0.01). Eradication of H. influenzae and clinical improvement was seen in one-third of the courses with both drugs. Betalactamase producing ampicillin-resistant strains emerged during 58% of the amoxycillin courses, but only in 16% of the pivampicillin courses (p less than 0.001). The high number of treatment failures and the development of resistant strains indicate that betalactamase inhibitors may possibly improve the efficacy of these drugs, especially of amoxycillin, in these patients.
开展了一项双盲交叉研究,以比较阿莫西林和匹氨西林对儿童下呼吸道流感嗜血杆菌感染的疗效。该研究纳入了20例因囊性纤维化(CF)或其他原因导致的慢性阻塞性肺疾病(COPD)患者。所有患者均有痰中经常携带流感嗜血杆菌的病史,且使用匹氨西林反复治疗失败。18例患者以随机顺序完成了两个14天疗程,分别使用等摩尔剂量的匹氨西林(80mg/kg/天)和阿莫西林(62mg/kg/天)。两种药物耐受性良好,均无严重副作用,但匹氨西林导致的恶心更为明显。在稳态时,用药后2小时和4小时的抗生素平均血清浓度,匹氨西林分别为9.7和3.7μg/ml,阿莫西林分别为19.1和7.9μg/ml(p<0.01)。两种药物治疗的疗程中均有三分之一出现流感嗜血杆菌清除及临床改善。在58%的阿莫西林疗程中出现了产β-内酰胺酶的氨苄西林耐药菌株,但在匹氨西林疗程中仅为16%(p<0.001)。大量的治疗失败以及耐药菌株的出现表明,β-内酰胺酶抑制剂可能会提高这些药物,尤其是阿莫西林,对这些患者的疗效。