The chemistry, pharmacology, pharmacokinetics, bacterial spectrum, clinical use, dosage, adverse reactions, and dosage forms and cost of cefaclor are reviewed. Cefaclor, a congener of cephalexin monohydrate, is a new semisynthetic cephalosporin antibiotic. It is well absorbed when given orally on an empty stomach; absorption is delayed by the presence of food. Although metabolism may play a role in the disposition of cefaclor, elimination is primarily renal. Cefaclor's spectrum of activity is similar to that of cefalexin, including a wide range of gram-negative and gram-positive bacteria; in particular, Escherichia coli, Klebsiella spp., Proteus mirabilis, Salmonella spp., and Haemophilus influenzae are more susceptible to clinically achievable concentrations of cefaclor than cephalexin. Cefaclor has been demonstrated to be effective against beta-lactamase-producing H. influenzae resistant to ampicillin, but further studies are needed to establish the clinical significance of this activity. Efficacy of cefaclor has been demonstrated in urinary tract, upper and lower respiratory tract, and skin and soft tissue infections in adults and children as well as in pediatric otitis media. Adverse reactions, mostly gastrointestinal, are generally mild and occur in few patients. Usual doses are 250-500 mg every eight hours in adults and 20--40 mg/kg/day in children, although this pediatric dose may be two low for otitis media. Clinical superiority of cefaclor over less expensive antibiotics has not been demonstrated.
本文综述了头孢克洛的化学性质、药理学、药代动力学、抗菌谱、临床应用、剂量、不良反应、剂型及成本。头孢克洛是头孢氨苄一水合物的同类物,是一种新型半合成头孢菌素抗生素。空腹口服时吸收良好;食物的存在会延迟吸收。虽然代谢可能在头孢克洛的处置中起作用,但其消除主要通过肾脏。头孢克洛的活性谱与头孢氨苄相似,包括多种革兰氏阴性菌和革兰氏阳性菌;特别是,大肠杆菌、克雷伯菌属、奇异变形杆菌、沙门菌属和流感嗜血杆菌对临床可达到浓度的头孢克洛比头孢氨苄更敏感。已证明头孢克洛对产β-内酰胺酶的氨苄西林耐药流感嗜血杆菌有效,但需要进一步研究来确定该活性的临床意义。头孢克洛在成人和儿童的尿路感染、上呼吸道和下呼吸道感染、皮肤和软组织感染以及小儿中耳炎中已证明有效。不良反应大多为胃肠道反应,一般较轻,且很少有患者出现。成人常用剂量为每8小时250-500毫克,儿童为20-40毫克/千克/天,不过小儿中耳炎的这个剂量可能偏低。尚未证明头孢克洛比价格较低的抗生素具有临床优越性。