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巴卡西林治疗急性扁桃体炎的药理与临床研究——与氨苄西林的比较

Pharmacological and clinical study of bacampicillin in acute peritonsillitis--a comparison with ampicillin.

作者信息

Hallander H O, Flodström A, Sjövall J

出版信息

Antimicrob Agents Chemother. 1977 Feb;11(2):185-90. doi: 10.1128/AAC.11.2.185.

Abstract

The pharmacological and clinical properties of bacampicillin in three dosage groups were studied in 66 hospitalized patients with unilateral acute peritonsillitis in a comparison with ampicillin. Bacampicillin is a new semisynthetic aminopenicillin which is rapidly converted to ampicillin but is better absorbed. Both drugs were given orally. The mean individual peak serum levels achieved with 200, 400, and 800 mg of bacampicillin in the first morning dose were 4.9, 6.8, and 11.9 mg/liter, respectively, with an almost linear dose response. The peak level of 800 mg of bacampicillin was significantly higher than the 6.8 mg/liter noted after a nearly equimolar dose of 500 mg of ampicillin. A linear relationship was also seen between dose and area under the serum concentration-time curve. Preliminary antibiotic concentration studies in five patients indicated therapeutic levels in peritonsillar pus. Beta-streptococci alone or in combination with anaerobes were isolated from about half of the abscesses, whereas anaerobes were isolated from the other half. Treatment was supplemented by surgical procedures in the majority of cases. The clinical effect was good in all treatment groups, with only one relapse. All beta-streptococci were eliminated during therapy. The total number of gastrointestinal side effects was significantly lower in patients treated with bacampicillin, although the difference in frequency of diarrhea alone was not significant.

摘要

在66例单侧急性扁桃体炎住院患者中,研究了三个剂量组的巴卡西林与氨苄西林相比的药理和临床特性。巴卡西林是一种新型半合成氨基青霉素,可迅速转化为氨苄西林,但吸收更好。两种药物均口服给药。首次晨服200、400和800mg巴卡西林所达到的平均个体血清峰值水平分别为4.9、6.8和11.9mg/升,剂量反应几乎呈线性。800mg巴卡西林的峰值水平显著高于近等摩尔剂量500mg氨苄西林后测得的6.8mg/升。剂量与血清浓度-时间曲线下面积之间也呈线性关系。对5例患者进行的初步抗生素浓度研究表明,扁桃体周脓肿中有治疗水平的药物。约一半的脓肿中分离出单独的β-链球菌或与厌氧菌混合的菌株,而另一半则分离出厌氧菌。大多数病例通过外科手术辅助治疗。所有治疗组的临床效果良好,仅1例复发。治疗期间所有β-链球菌均被清除。接受巴卡西林治疗的患者胃肠道副作用总数显著较低,尽管仅腹泻频率的差异不显著。

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The pharmacokinetics of bacampicillin.巴氨西林的药代动力学。
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本文引用的文献

1
BRL.8988 (talampicillin), a well-absorbed oral form of ampicillin.
Antimicrob Agents Chemother. 1974 Jun;5(6):670-1. doi: 10.1128/AAC.5.6.670.
2
Acyloxymethyl esters of ampicillin.氨苄西林的酰氧基甲酯。
J Med Chem. 1970 Jul;13(4):607-12. doi: 10.1021/jm00298a005.
3
Anaerobic infections (third of three parts).厌氧感染(三部分之第三部分)
N Engl J Med. 1974 Jun 6;290(23):1289-94. doi: 10.1056/NEJM197406062902305.
10
Microbiological aspects on peritonsillar abscesses.扁桃体周围脓肿的微生物学方面
Scand J Infect Dis. 1976;8(3):157-60. doi: 10.3109/inf.1976.8.issue-3.06.

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