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亚胺培南/西司他丁。对其抗菌活性、药代动力学特性及治疗效果的综述。

Imipenem/cilastatin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy.

作者信息

Clissold S P, Todd P A, Campoli-Richards D M

出版信息

Drugs. 1987 Mar;33(3):183-241. doi: 10.2165/00003495-198733030-00001.

DOI:10.2165/00003495-198733030-00001
PMID:3552595
Abstract

Imipenem is the first available semisynthetic thienamycin and is administered intravenously in combination with cilastatin, a renal dipeptidase inhibitor that increases urinary excretion of active drug. In vitro studies have demonstrated that imipenem has an extremely wide spectrum of antibacterial activity against Gram-negative and Gram-positive aerobic and anaerobic bacteria, even against many multiresistant strains of bacteria. It is very potent against species which elaborate beta-lactamases. Imipenem in combination with equal doses of cilastatin has been shown to be generally well tolerated and an effective antimicrobial for the treatment of infections of various body systems. It is likely to be most valuable as empirical treatment of mixed aerobic and anaerobic infections, bacteraemia in non-neutropenic patients and serious hospital-acquired infections.

摘要

亚胺培南是首个可用的半合成硫霉素,需与西司他丁联合静脉给药,西司他丁是一种肾脏二肽酶抑制剂,可增加活性药物的尿排泄量。体外研究表明,亚胺培南对革兰氏阴性菌和革兰氏阳性需氧菌及厌氧菌具有极广的抗菌活性,甚至对许多多重耐药菌株也有效。它对产生β-内酰胺酶的菌种非常有效。亚胺培南与等量西司他丁联合使用已证明一般耐受性良好,是治疗各种身体系统感染的有效抗菌药物。作为需氧菌和厌氧菌混合感染、非中性粒细胞减少患者的菌血症以及严重医院获得性感染的经验性治疗,它可能最具价值。

相似文献

1
Imipenem/cilastatin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy.亚胺培南/西司他丁。对其抗菌活性、药代动力学特性及治疗效果的综述。
Drugs. 1987 Mar;33(3):183-241. doi: 10.2165/00003495-198733030-00001.
2
Imipenem/cilastatin: the first carbapenem antibiotic.亚胺培南/西司他丁:第一种碳青霉烯类抗生素。
Drug Intell Clin Pharm. 1985 Dec;19(12):895-9.
3
Thienamycin: development of imipenen-cilastatin.硫霉素:亚胺培南-西司他丁的研发
J Antimicrob Chemother. 1983 Dec;12 Suppl D:1-35. doi: 10.1093/jac/12.suppl_d.1.
4
Imipenem-cilastatin sodium, a broad-spectrum carbapenem antibiotic combination.亚胺培南西司他丁钠,一种广谱碳青霉烯类抗生素组合。
Clin Pharm. 1986 Sep;5(9):719-36.
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Carbapenems, a new class of beta-lactam antibiotics. Discovery and development of imipenem/cilastatin.碳青霉烯类,一类新型β-内酰胺抗生素。亚胺培南/西司他丁的发现与研发。
Am J Med. 1985 Jun 7;78(6A):3-21. doi: 10.1016/0002-9343(85)90097-x.
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[Imipenem/cilastatin: in vitro activity, concentrations in plasma and prostatic adenoma and therapeutic results in patients with complicated urinary tract infections].亚胺培南/西司他丁:体外活性、血浆和前列腺腺瘤中的浓度以及复杂性尿路感染患者的治疗结果
Infection. 1986;14 Suppl 2:S122-9. doi: 10.1007/BF01647496.
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Pharmacokinetic profile of imipenem/cilastatin in normal volunteers.
Am J Med. 1985 Jun 7;78(6A):47-53. doi: 10.1016/0002-9343(85)90101-9.
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Combined imipenem/cilastatin and tobramycin therapy of multiresistant Pseudomonas aeruginosa in cystic fibrosis.亚胺培南/西司他丁与妥布霉素联合治疗囊性纤维化患者多重耐药铜绿假单胞菌感染
J Antimicrob Chemother. 1987 Jan;19(1):101-7. doi: 10.1093/jac/19.1.101.
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Imipenem/cilastatin.亚胺培南/西司他丁
Eur J Clin Microbiol. 1984 Oct;3(5):453-5. doi: 10.1007/BF02017374.
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[Fundamental and clinical studies on imipenem/cilastatin sodium in the field of pediatrics].
Jpn J Antibiot. 1986 Jul;39(7):1828-46.

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本文引用的文献

1
Comparative in vitro activity of new beta-lactam antibiotics against anaerobic bacteria.新型β-内酰胺类抗生素对厌氧菌的体外活性比较
Antimicrob Agents Chemother. 1981 Nov;20(5):600-9. doi: 10.1128/AAC.20.5.600.
2
Susceptibility of multiply antibiotic-resistant pneumococci to the new beta-lactam drugs and rosaramicin.多重耐药肺炎球菌对新型β-内酰胺类药物和罗沙米星的敏感性
Antimicrob Agents Chemother. 1981 Apr;19(4):675-7. doi: 10.1128/AAC.19.4.675.
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In vitro activity of new beta-lactam antibiotics and other antimicrobial drugs against anaerobic isolates from obstetric and gynecological infections.
Indian J Ophthalmol. 2022 May;70(5):1696-1700. doi: 10.4103/ijo.IJO_2640_21.
4
Antibacterial Activity of Imipenem/Relebactam against Clinical Isolates in Japan.亚胺培南/雷巴他定对日本临床分离株的抗菌活性。
Microbiol Spectr. 2022 Apr 27;10(2):e0223521. doi: 10.1128/spectrum.02235-21. Epub 2022 Apr 13.
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A knowledge graph of clinical trials ([Formula: see text]).临床试验知识图谱 ([公式:见正文])。
Sci Rep. 2022 Mar 18;12(1):4724. doi: 10.1038/s41598-022-08454-z.
6
Significant increase in the secretion of extracellular vesicles and antibiotics resistance from methicillin-resistant Staphylococcus aureus induced by ampicillin stress.耐甲氧西林金黄色葡萄球菌在氨苄西林胁迫下,细胞外囊泡分泌显著增加,并导致抗生素耐药性增强。
Sci Rep. 2020 Dec 3;10(1):21066. doi: 10.1038/s41598-020-78121-8.
7
iTRAQ®-based quantitative proteomics reveals the proteomic profiling of methicillin-resistant Staphylococcus aureus-derived extracellular vesicles after exposure to imipenem.基于 iTRAQ®的定量蛋白质组学揭示了耐甲氧西林金黄色葡萄球菌来源的细胞外囊泡在暴露于亚胺培南后蛋白质组学特征。
Folia Microbiol (Praha). 2021 Apr;66(2):221-230. doi: 10.1007/s12223-020-00836-y. Epub 2020 Nov 9.
8
Protective effect of cilastatin against diclofenac-induced nephrotoxicity through interaction with diclofenac acyl glucuronide via organic anion transporters.西司他丁通过与双氯芬酸酰基葡萄糖醛酸经有机阴离子转运体相互作用对双氯芬酸诱导的肾毒性的保护作用。
Br J Pharmacol. 2020 May;177(9):1933-1948. doi: 10.1111/bph.14957. Epub 2020 Mar 5.
9
Impact of antibiotic treatment and host innate immune pressure on enterococcal adaptation in the human bloodstream.抗生素治疗和宿主固有免疫压力对肠球菌在人体血液中适应的影响。
Sci Transl Med. 2019 Apr 10;11(487). doi: 10.1126/scitranslmed.aat8418.
10
Asp305Gly mutation improved the activity and stability of the styrene monooxygenase for efficient epoxide production in Pseudomonas putida KT2440.Asp305Gly 突变提高了苯乙烯单加氧酶的活性和稳定性,有利于在恶臭假单胞菌 KT2440 中高效生产环氧化物。
Microb Cell Fact. 2019 Jan 24;18(1):12. doi: 10.1186/s12934-019-1065-5.
新型β-内酰胺类抗生素及其他抗菌药物对妇产科感染分离出的厌氧菌的体外活性
Antimicrob Agents Chemother. 1982 Oct;22(4):711-4. doi: 10.1128/AAC.22.4.711.
4
Sensitivity of 341 non-fermentative gram-negative bacteria to seven beta-lactam antibiotics.341株非发酵革兰阴性菌对七种β-内酰胺类抗生素的敏感性
Eur J Clin Microbiol. 1982 Jun;1(3):159-65. doi: 10.1007/BF02019617.
5
In-vitro susceptibility of Nocardia and Rhodococcus to fourteen beta-lactam antibiotics.
J Antimicrob Chemother. 1982 Dec;10(6):564-5. doi: 10.1093/jac/10.6.564.
6
The susceptibility of Yersinia to eleven antimicrobials.
J Antimicrob Chemother. 1982 Dec;10(6):543-7. doi: 10.1093/jac/10.6.543.
7
In vitro activities of thirteen beta-lactam antibiotics against Chlamydia trachomatis.13种β-内酰胺类抗生素对沙眼衣原体的体外活性
Antimicrob Agents Chemother. 1982 Sep;22(3):520-1. doi: 10.1128/AAC.22.3.520.
8
Metabolism of thienamycin and related carbapenem antibiotics by the renal dipeptidase, dehydropeptidase.硫霉素及相关碳青霉烯类抗生素在肾脏二肽酶即脱氢肽酶作用下的代谢
Antimicrob Agents Chemother. 1982 Jul;22(1):62-70. doi: 10.1128/AAC.22.1.62.
9
Comparative activities of 13 beta-lactam antibiotics.13种β-内酰胺类抗生素的比较活性
Antimicrob Agents Chemother. 1982 Jun;21(6):925-34. doi: 10.1128/AAC.21.6.925.
10
Susceptibility of Nocardia asteroides to various antibiotics, including newer beta-lactams, trimethoprim-sulfamethoxazole, amikacin, and N-formimidoyl thienamycin.星形诺卡菌对多种抗生素的敏感性,包括新型β-内酰胺类、甲氧苄啶-磺胺甲恶唑、阿米卡星和N-甲酰亚胺硫霉素。
Antimicrob Agents Chemother. 1982 Jun;21(6):1011-2. doi: 10.1128/AAC.21.6.1011.