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阿莫西林:对其抗菌、药代动力学特性及治疗用途的综述。

Amoxycillin: A review of its antibacterial and pharmacokinietic properties and therapeutic use.

作者信息

Brogeden R N, Speight T M, Avery G S

出版信息

Drugs. 1975;9(2):88-140. doi: 10.2165/00003495-197509020-00002.

DOI:10.2165/00003495-197509020-00002
PMID:1126306
Abstract

Amoxycillin2 is an acid stable semisynthetic penicillin closely related to ampicillin. Unlike pivampicillin and hetacillin, amoxycillin is not converted to ampicillin in the body. The antibacterial spectrum and level of activity of amoxycillin is essentially the same as for ampicillin, and there is complete cross-resistance between the two drugs. After oral administration, amoxycillin is better absorbed than ampicillin. Mean peak serum levels of amoxycillin are generally twice those of ampicillin after an equal dose. The better absorption and penetration into certain body tissues and fluids of amoxycillin and its greater activity against experimental infections in mice, suggest that it might be preferred to ampicillin in the treatment of some infections, but any clear superiority over ampicillin in clinical practice has yet to be demonstrated. However, these properties have enabled amoxycillin to be given at half the dose of ampicillin without loss of therapeutic efficacy, and the princpal side-effects of skin rashes and diarrhoea have tended to be less frequent with amoxycillin than with ampicillin. Other side-effects are essentially similar in nature to those reported with ampicillin.

摘要

阿莫西林2是一种酸稳定的半合成青霉素,与氨苄西林密切相关。与匹氨西林和海他西林不同,阿莫西林在体内不会转化为氨苄西林。阿莫西林的抗菌谱和活性水平与氨苄西林基本相同,两种药物之间存在完全交叉耐药性。口服后,阿莫西林比氨苄西林吸收更好。同等剂量后,阿莫西林的平均血清峰值水平通常是氨苄西林的两倍。阿莫西林更好的吸收和对某些身体组织及体液的渗透,以及其对小鼠实验性感染更强的活性,表明在治疗某些感染时它可能比氨苄西林更具优势,但在临床实践中相对于氨苄西林的任何明显优越性尚未得到证实。然而,这些特性使得阿莫西林可以以氨苄西林一半的剂量给药而不损失治疗效果,并且阿莫西林引起的皮疹和腹泻等主要副作用往往比氨苄西林更少。其他副作用在本质上与氨苄西林报道的副作用基本相似。

相似文献

1
Amoxycillin: A review of its antibacterial and pharmacokinietic properties and therapeutic use.阿莫西林:对其抗菌、药代动力学特性及治疗用途的综述。
Drugs. 1975;9(2):88-140. doi: 10.2165/00003495-197509020-00002.
2
[Amoxicillin: microbiological, pharmacokinetic and therapeutic aspects].[阿莫西林:微生物学、药代动力学及治疗学方面]
Farmaco Prat. 1975 Aug;30(8):357-73.
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Diagnosis and treatment: drugs five years later. Amoxicillin.诊断与治疗:五年后的药物。阿莫西林。
Ann Intern Med. 1979 Mar;90(3):356-60. doi: 10.7326/0003-4819-90-3-356.
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Amoxycillin/clavulanic acid: a review of its antibacterial activity, pharmacokinetics and therapeutic use.阿莫西林/克拉维酸:抗菌活性、药代动力学及治疗用途综述
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Amoxycillin injectable: a review of its antibacterial spectrum, pharmacokinetics and therapeutic use.注射用阿莫西林:抗菌谱、药代动力学及治疗用途综述
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Antibacterial activity and synergy, in vitro and in vivo, of a combination of amoxycillin and flucloxacillin.
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The oral absorption of ampicillin, pivampicillin and amoxycillin in infants and children.氨苄西林、匹氨西林和阿莫西林在婴幼儿及儿童中的口服吸收情况。
Acta Pharmacol Toxicol (Copenh). 1981 Jul;49(1):38-42. doi: 10.1111/j.1600-0773.1981.tb00867.x.
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Amoxycillin: a preliminary report of its pharmokinetic properties and therapeutic efficacy.阿莫西林:其药代动力学特性及治疗效果的初步报告。
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Parenteral amoxycillin treatment of severe infections in hospitalized patients.住院患者严重感染的阿莫西林肠外给药治疗
J Antimicrob Chemother. 1979 Jan;5(1):109-12. doi: 10.1093/jac/5.1.109.
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Oral pivampicillin and amoxycillin in newborn infants.
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Amoxillin- and pefloxacin-induced cholesterogenesis and phospholipidosis in rat tissues.阿莫西林和培氟沙星诱导大鼠组织中的胆固醇生成及磷脂质蓄积
Lipids Health Dis. 2015 Feb 21;14:13. doi: 10.1186/s12944-015-0011-8.
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Roxithromycin 150 mg b.i.d. versus amoxycillin 500 mg/clavulanic acid 125 mg t.i.d. for the treatment of lower respiratory tract infections in general practice.罗红霉素150毫克,每日两次,与阿莫西林500毫克/克拉维酸125毫克,每日三次,用于全科医疗中治疗下呼吸道感染。
Infection. 1995;23 Suppl 1:S15-20. doi: 10.1007/BF02464954.
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Absorption and disposition kinetics of amoxicillin in normal human subjects.

本文引用的文献

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Amoxycillin--pharmacology, bacteriology and clinical studies.
Br J Clin Pract. 1972 Jul;26(7):341-6.
2
Use of amoxycillin in chest infections in the elderly. A double-blind study.阿莫西林在老年人胸部感染中的应用。一项双盲研究。
Gerontol Clin (Basel). 1974;16(1):92-9. doi: 10.1159/000245490.
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Treatment of typhoid carriers with amoxycillin and in combination with probenecid.
Chemotherapy. 1974;20(1):29-38. doi: 10.1159/000221788.
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阿莫西林在正常人体受试者中的吸收与处置动力学
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Treatment of urinary tract infections with a combination of amoxicillin and clavulanic acid.阿莫西林与克拉维酸联合治疗尿路感染
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Bacterial kill rates of amoxycillin and ampicillin at exponentially diminishing concentrations simulating in vivo conditions.在模拟体内条件下,阿莫西林和氨苄西林在指数递减浓度时的细菌杀灭率。
Infection. 1980;Suppl 1:103-8. doi: 10.1007/BF01644943.
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Ampicillin and alternatives.氨苄西林及其替代药物。
Br Med J (Clin Res Ed). 1983 Feb 19;286(6365):583-5. doi: 10.1136/bmj.286.6365.583.
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Pharmacokinetic study of a paediatric formulation of amoxycillin and clavulanic acid in children.
Eur J Clin Pharmacol. 1985;29(2):235-9. doi: 10.1007/BF00547429.
9
Synergistic effects between amoxicillin, metronidazole, and the hydroxymetabolite of metronidazole against Actinobacillus actinomycetemcomitans.阿莫西林、甲硝唑及其羟基代谢物对伴放线放线杆菌的协同作用。
Antimicrob Agents Chemother. 1991 May;35(5):961-6. doi: 10.1128/AAC.35.5.961.
10
Antibacterial drugs today. I.当今的抗菌药物。I.
Drugs. 1975;10(1):1-55. doi: 10.2165/00003495-197510010-00001.
Treatment of enterococcal endocarditis with oral amoxicillin and intramuscular gentamicin.
口服阿莫西林和肌肉注射庆大霉素治疗肠球菌性心内膜炎。
J Infect Dis. 1974 Jun;129(0):suppl:S213-5. doi: 10.1093/infdis/129.supplement_2.s213.
5
Comparative clinical pharmacology of three ampicillins and amoxicillin administered orally.三种口服氨苄西林和阿莫西林的比较临床药理学
J Infect Dis. 1974 Jun;129(0):suppl:S156-68. doi: 10.1093/infdis/129.supplement_2.s156.
6
Pharmacokinetics of the new penicillins. Amoxycillin and flucloxacillin in patients with terminal renal failure undergoing haemodialysis.新型青霉素的药代动力学。接受血液透析的终末期肾衰竭患者体内的阿莫西林和氟氯西林。
Chemotherapy. 1973;19(5):279-88. doi: 10.1159/000221466.
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Amoxycillin: pilot study of its use in pneumonia and chronic bronchitis.阿莫西林:用于肺炎和慢性支气管炎的初步研究。
Br J Clin Pract. 1973 May;27(5):161-4.
8
Evaluation of amoxycillin--a new semisynthetic penicillin.阿莫西林——一种新型半合成青霉素的评估。
Med J Aust. 1973 Sep 15;2(11):537-41.
9
[Clinical and bacteriological evaluation of amoxicillin in infections not caused by enterobacteria].阿莫西林在非肠杆菌所致感染中的临床及细菌学评价
Chemotherapy. 1973;18:Suppl:81-90.
10
Amoxycillin (BRL 2333) in children. Serum concentrations and clinical report.阿莫西林(BRL 2333)用于儿童。血清浓度及临床报告。
Chemotherapy. 1973;18:Suppl:92-6.