Literature DB >> 3910385

Imipenem/cilastatin: the first carbapenem antibiotic.

J A Lyon.   

Abstract

Imipenem/cilastatin is the first of a new class of beta-lactam antibiotics called carbapenems. The antibacterial spectrum of imipenem exceeds any antibiotic investigated to date and includes gram-positive, gram-negative, and anaerobic organisms. Only methicillin-resistant organisms, Strep. faecium, Pseudomonas cepacia, and Pseudomonas maltophilia have been shown to be resistant. Imipenem is administered in a 1:1 ratio with cilastatin, which inhibits a renal enzyme (dehydropeptidase) and improves urinary recovery of imipenem. The elimination half-life of both compounds is 1.0 hours and recommended doses are 0.25-0.5 g iv q6h. Adverse events are similar in nature and incidence to beta-lactam antibiotics, with phlebitis/thrombophlebitis, diarrhea, nausea, skin rash, and elevations of hepatic enzymes most common. Clinical studies in phase II and III trials have shown imipenem/cilastatin to be effective in soft tissue infections, endocarditis, obstetrics and gynecology, complicated urinary tract infections, mixed anaerobic-aerobic infections, osteomyelitis, bacteremias, and pneumonias. Several comparative clinical trials have shown imipenem/cilastatin to be equal in efficacy to combination therapy. Imipenem/cilastatin may prove to be an alternative to combination antibiotic therapy because of its extremely broad spectrum of activity.

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Year:  1985        PMID: 3910385

Source DB:  PubMed          Journal:  Drug Intell Clin Pharm        ISSN: 0012-6578


  11 in total

1.  Single-Center Pharmacokinetic Study and Simulation of a Low Meropenem Concentration in Brain-Dead Organ Donors.

Authors:  Jae-Myeong Lee; Joo Won Lee; Tae Seok Jeong; Eun Sook Bang; So Hee Kim
Journal:  Antimicrob Agents Chemother       Date:  2018-09-24       Impact factor: 5.191

2.  JBP485, A Dual Inhibitor of Organic Anion Transporters (OATs) and Renal Dehydropeptidase-I (DHP-I), Protects Against Imipenem-Induced Nephrotoxicity.

Authors:  Chong Wang; Changyuan Wang; Jingjing Wu; Qiang Meng; Huan Jin; Huijun Sun; Taiichi Kaku; Jing Chen; Xiaokui Huo; Kexin Liu
Journal:  Front Pharmacol       Date:  2022-06-08       Impact factor: 5.988

Review 3.  Imipenem/cilastatin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy.

Authors:  S P Clissold; P A Todd; D M Campoli-Richards
Journal:  Drugs       Date:  1987-03       Impact factor: 9.546

4.  Active-Site Plasticity Is Essential to Carbapenem Hydrolysis by OXA-58 Class D β-Lactamase of Acinetobacter baumannii.

Authors:  Shivendra Pratap; Madhusudhanarao Katiki; Preet Gill; Pravindra Kumar; Dasantila Golemi-Kotra
Journal:  Antimicrob Agents Chemother       Date:  2015-10-12       Impact factor: 5.191

Review 5.  OXA β-lactamases.

Authors:  Benjamin A Evans; Sebastian G B Amyes
Journal:  Clin Microbiol Rev       Date:  2014-04       Impact factor: 26.132

Review 6.  Structural basis for carbapenem-hydrolyzing mechanisms of carbapenemases conferring antibiotic resistance.

Authors:  Jeong Ho Jeon; Jung Hun Lee; Jae Jin Lee; Kwang Seung Park; Asad Mustafa Karim; Chang-Ro Lee; Byeong Chul Jeong; Sang Hee Lee
Journal:  Int J Mol Sci       Date:  2015-04-29       Impact factor: 5.923

Review 7.  A Clinical Review and Critical Evaluation of Imipenem-Relebactam: Evidence to Date.

Authors:  Toni A Campanella; Jason C Gallagher
Journal:  Infect Drug Resist       Date:  2020-11-25       Impact factor: 4.003

8.  Competing off-loading mechanisms of meropenem from an l,d-transpeptidase reduce antibiotic effectiveness.

Authors:  Trevor A Zandi; Craig A Townsend
Journal:  Proc Natl Acad Sci U S A       Date:  2021-07-06       Impact factor: 11.205

Review 9.  Antibiotic Resistance Profiles, Molecular Mechanisms and Innovative Treatment Strategies of Acinetobacter baumannii.

Authors:  Corneliu Ovidiu Vrancianu; Irina Gheorghe; Ilda Barbu Czobor; Mariana Carmen Chifiriuc
Journal:  Microorganisms       Date:  2020-06-21

Review 10.  Emerging Strategies to Combat β-Lactamase Producing ESKAPE Pathogens.

Authors:  Corneliu Ovidiu Vrancianu; Irina Gheorghe; Elena-Georgiana Dobre; Ilda Czobor Barbu; Roxana Elena Cristian; Marcela Popa; Sang Hee Lee; Carmen Limban; Ilinca Margareta Vlad; Mariana Carmen Chifiriuc
Journal:  Int J Mol Sci       Date:  2020-11-12       Impact factor: 6.208

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