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氟喹诺酮类药物。

The fluoroquinolones.

作者信息

Walker R C, Wright A J

机构信息

Division of Infectious Diseases and Internal Medicine, Mayo Clinic, Rochester, MN 55905.

出版信息

Mayo Clin Proc. 1991 Dec;66(12):1249-59. doi: 10.1016/s0025-6196(12)62477-x.

Abstract

The fluoroquinolone class of antibiotics promises to become as diverse and as important as beta-lactam agents. The fluoroquinolones inhibit bacterial DNA gyrase and are bactericidal. All fluoroquinolones have potent activity against most gram-negative bacteria; ciprofloxacin is the most active against Pseudomonas aeruginosa. Activity against gram-positive organisms is variable; methicillin-resistant Staphylococcus aureus has acquired resistance to the fluoroquinolones at an alarming rate. Currently available quinolones do not have, but new quinolone agents likely will have, substantial activity against anaerobic bacteria. Some quinolones are also active against Mycobacterium, Chlamydia, and Mycoplasma organisms. All fluoroquinolones have excellent absorption after oral administration; however, this process can be impaired by the presence of aluminum- or magnesium-containing antacids and by zinc, iron, or calcium supplements. Ciprofloxacin is also available for intravenous use. Although most fluoroquinolones do not achieve adequate cerebrospinal fluid levels, penetration into other tissues is excellent. Dosage adjustments for renal and hepatic dysfunction vary among the quinolones. Although side effects are rare, concomitant use of caffeine or theophylline with some quinolones may cause toxicity to the central nervous system. Because they may affect the development of cartilage, all fluoroquinolones are contraindicated in children, adolescents, and pregnant or breast-feeding women.

摘要

氟喹诺酮类抗生素有望变得像β-内酰胺类药物一样多样且重要。氟喹诺酮类药物抑制细菌DNA回旋酶,具有杀菌作用。所有氟喹诺酮类药物对大多数革兰氏阴性菌都有强效活性;环丙沙星对铜绿假单胞菌的活性最强。对革兰氏阳性菌的活性各不相同;耐甲氧西林金黄色葡萄球菌对氟喹诺酮类药物产生耐药性的速度惊人。目前可用的喹诺酮类药物对厌氧菌没有显著活性,但新的喹诺酮类药物可能会有。一些喹诺酮类药物对分枝杆菌、衣原体和支原体也有活性。所有氟喹诺酮类药物口服后吸收良好;然而,含铝或镁的抗酸剂以及锌、铁或钙补充剂的存在会损害这一过程。环丙沙星也有静脉注射剂型。尽管大多数氟喹诺酮类药物在脑脊液中达不到足够的浓度,但它们在其他组织中的渗透良好。不同喹诺酮类药物对肾功能和肝功能不全的剂量调整有所不同。虽然副作用很少见,但某些喹诺酮类药物与咖啡因或茶碱同时使用可能会导致中枢神经系统毒性。由于它们可能影响软骨发育,所有氟喹诺酮类药物都禁止用于儿童、青少年以及孕妇或哺乳期妇女。

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