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头孢氨苄的药理学。

The pharmacology of cephalexin.

作者信息

Griffith R S

出版信息

Postgrad Med J. 1983;59 Suppl 5:16-27.

PMID:6364086
Abstract

Cephalexin has an antimicrobial spectrum that includes those pathogens most frequently encountered in clinical practice. It is useful in the treatment of infections of the upper and lower respiratory tract, skin and soft tissue, and the genitourinary tract. It can be administered in relatively high oral doses without gastrointestinal irritation, and because it is absorbed high in the intestinal tract, it does not disturb the lower bowel flora. Because of its stability and chemical configuration, it causes a very low incidence of allergy. Cephalexin is not absorbed from the stomach but is totally and rapidly absorbed in the upper intestine. Children, because of their greater body water turnover, may need higher doses per kilogram than those used in treating adults. Distribution to the tissues, other than the spinal fluid and aqueous humour, is rapidly achieved. Cephalexin does not penetrate into the host tissue cells, which probably accounts for its low incidence of side effects. Binding to human serum proteins is low, and there is no measurable destruction or metabolism of cephalexin during its sojourn in the body fluids. Cephalexin is rapidly cleared from the body by the kidneys. Seventy to 100% of the dose is found in the urine 6-8 hr after each dose. Concentrations of 500-1000 micrograms/ml of urine follow 250 to 500 mg oral doses of cephalexin, many times greater than the minimum inhibitory concentration for the usual urinary tract pathogens. Patients with creatinine clearances less than 30 ml/min require a reduction in cephalexin dosage. This reduction should be proportional to the reduced function which may be established by determination of creatinine clearance or serum creatinine.

摘要

头孢氨苄的抗菌谱包括临床实践中最常遇到的那些病原体。它可用于治疗上、下呼吸道感染、皮肤及软组织感染和泌尿生殖道感染。它可以相对较高的口服剂量给药而无胃肠道刺激,并且由于它在肠道上部被吸收,所以不会干扰下段肠道菌群。由于其稳定性和化学构型,其过敏发生率非常低。头孢氨苄不被胃吸收,但在上段肠道中被完全且快速地吸收。儿童由于其身体水分周转较快,每公斤体重可能需要比治疗成人更高的剂量。除脑脊液和房水外,它能迅速分布到组织中。头孢氨苄不渗透到宿主组织细胞中,这可能是其副作用发生率低的原因。与人类血清蛋白的结合率低,并且在其存在于体液期间没有可测量到的头孢氨苄的破坏或代谢。头孢氨苄通过肾脏迅速从体内清除。每次给药后6 - 8小时,70%至100%的剂量可在尿液中发现。口服250至500毫克头孢氨苄后,尿液浓度可达500 - 1000微克/毫升,比通常尿路病原体的最低抑菌浓度高许多倍。肌酐清除率低于30毫升/分钟的患者需要减少头孢氨苄的剂量。这种减少应与通过测定肌酐清除率或血清肌酐所确定的功能降低成比例。

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