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氯碳头孢。对其抗菌活性、药代动力学特性及治疗效果的综述。

Loracarbef. A review of its antimicrobial activity, pharmacokinetic properties and therapeutic efficacy.

作者信息

Brogden R N, McTavish D

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1993 May;45(5):716-36. doi: 10.2165/00003495-199345050-00008.

Abstract

Loracarbef is an orally administered member of a new synthetic class of beta-lactam antibiotics, the carbacephems, which is characterised by enhanced chemical stability. At low concentrations (< 2 mg/L) in vitro, it inhibits Streptococcus pneumoniae, S. pyogenes, beta-haemolytic streptococci groups B, C and G. Proteus mirabilis and Moraxella catarrhalis, including beta-lactamase-producing strains. At therapeutic plasma concentrations it is also active in vitro against most strains of Staphylococcus aureus, S. saprophyticus, Escherichia coli and beta-lactamase-positive and -negative strains of Haemophilus influenzae. Like other beta-lactams, loracarbef is inactive against methicillin-resistant strains of S. aureus. When administered at dosages of 200 to 400 mg twice daily, the clinical and bacteriological efficacy of loracarbef is comparable with that of amoxicillin and amoxicillin/clavulanic acid in patients with upper or lower respiratory tract infections, and comparable with that of cefaclor in treating infections of the lower respiratory tract, skin and skin structures and urinary tract. Loracarbef and phenoxymethylpenicillin (penicillin V) were equally effective in treating streptococcal pharyngitis and tonsillitis. Loracarbef is generally well tolerated by all age groups and causes less diarrhoea than amoxicillin/clavulanic acid. It is administered twice daily. It offers a suitable alternative to other orally administered antibiotics for the treatment of mild to moderate infections caused by susceptible organisms.

摘要

氯碳头孢是新型合成β-内酰胺类抗生素(碳头孢烯类)中的口服制剂,其特点是化学稳定性增强。在体外低浓度(<2mg/L)时,它可抑制肺炎链球菌、化脓性链球菌、B、C和G组β溶血性链球菌、奇异变形杆菌和卡他莫拉菌,包括产β-内酰胺酶菌株。在治疗性血浆浓度时,它在体外对大多数金黄色葡萄球菌、腐生葡萄球菌、大肠杆菌以及流感嗜血杆菌的β-内酰胺酶阳性和阴性菌株也有活性。与其他β-内酰胺类药物一样,氯碳头孢对耐甲氧西林金黄色葡萄球菌菌株无活性。当每日两次给予200至400mg剂量时,氯碳头孢在治疗上、下呼吸道感染患者时的临床和细菌学疗效与阿莫西林及阿莫西林/克拉维酸相当,在治疗下呼吸道、皮肤及皮肤结构和泌尿系统感染时与头孢克洛相当。氯碳头孢和苯氧甲基青霉素(青霉素V)在治疗链球菌性咽炎和扁桃体炎方面同样有效。氯碳头孢一般所有年龄组都能很好耐受,且引起的腹泻比阿莫西林/克拉维酸少。它每日给药两次。对于治疗由易感菌引起的轻至中度感染,它是其他口服抗生素的合适替代药物。

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