Macrolides: pharmacokinetics and pharmacodynamics.

Abstract:

:Three pharmacokinetic/pharmacodynamic parameters--(i) the peak concentration to the minimum inhibitory concentration ratio (C(max)/MIC); (ii) the area under the concentration-time curve to MIC ratio (AUC(24h)/MIC); and (iii) the time the concentration exceeds the MIC (T>MIC)--are important predictors of the clinical efficacy of antibiotics. For antibiotics with pronounced concentration-dependent killing, such as the fluoroquinolones or the aminoglycosides, C(max)/MIC and AUC(24)/MIC are the main factors that establish efficacy. Antibiotics with a weak, or no, concentration dependency generally have their efficacy linked to T>MIC, and these include the beta-lactams and the conventional macrolides. Antibiotics with weak concentration-dependent effects, but with prolonged persistent effects, such as tetracyclines and azithromycin, have their activity mostly related to the AUC(24)/MIC. By applying these concepts to current antibiotics, and also to the development of novel agents, it is possible to optimise their dosages and administration schedules. This will maximise therapeutic efficacy, may prevent or delay the emergence of bacterial resistance to antibiotics, and can certainly minimise side-effects.

authors

Van Bambeke F,Tulkens PM

doi

10.1016/s0924-8579(01)00406-x

subject

Has Abstract

pub_date

2001-01-01 00:00:00

pages

S17-23

eissn

0924-8579

issn

1872-7913

pii

S092485790100406X

journal_volume

18 Suppl 1

pub_type

杂志文章,评审
  • Trypanocidal activity of piperazine-linked bisbenzamidines and bisbenzamidoxime, an orally active prodrug.

    abstract::A series of 32 piperazine-linked bisbenzamidines (and related analogues) were analysed for their in vitro and in vivo trypanocidal activity against a drug-sensitive strain of Trypanosoma brucei brucei and a drug-resistant strain of Trypanosoma brucei rhodesiense. The compounds showed similar potencies against both str...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2007.07.021

    authors: Huang TL,Bacchi CJ,Kode NR,Zhang Q,Wang G,Yartlet N,Rattendi D,Londono I,Mazumder L,Vanden Eynde JJ,Mayence A,Donkor IO

    更新日期:2007-12-01 00:00:00

  • Setting interpretive breakpoints for antimicrobial susceptibility testing using disk diffusion.

    abstract::Antimicrobial susceptibility testing plays a key role in clinical microbiology. The disk diffusion test dates back to the 1940s and became standardised from the 1950s, with the International Collaborative Study (ICS) and National Committee for Clinical Laboratory Standards (NCCLS) as the two major standards. Interlabo...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijantimicag.2011.04.006

    authors: Kronvall G,Giske CG,Kahlmeter G

    更新日期:2011-10-01 00:00:00

  • Clinical outcomes and therapeutic options of bloodstream infections caused by extended-spectrum beta-lactamase-producing Escherichia coli.

    abstract::This study was conducted to assess the clinical outcomes of bloodstream infections caused by extended-spectrum beta-lactamase-producing Escherichia coli. A total of 53 patients were included in the study. Forty-five patients (84.9%) received appropriate antibiotic therapy. Initial empirical treatment was appropriate i...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2005.06.012

    authors: Metan G,Zarakolu P,Cakir B,Hascelik G,Uzun O

    更新日期:2005-09-01 00:00:00

  • Emergence of a novel multidrug-resistant Pseudomonas aeruginosa strain producing IMP-type metallo-β-lactamases and AAC(6')-Iae in Japan.

    abstract::The emergence of multidrug-resistant (MDR) Pseudomonas aeruginosa isolates producing IMP-type metallo-β-lactamases (MBLs) and aminoglycoside 6'-N-acetyltransferase [AAC(6')-Iae] has become a serious problem in medical settings in Japan. A total of 217 MDR P. aeruginosa isolates were obtained from August 2009 to April ...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2012.01.020

    authors: Kitao T,Tada T,Tanaka M,Narahara K,Shimojima M,Shimada K,Miyoshi-Akiyama T,Kirikae T

    更新日期:2012-06-01 00:00:00

  • Current and future approaches to antimycotic treatment in the era of resistant fungi and immunocompromised hosts.

    abstract::Due to the ever-increasing number of immunocompromised patients, both localised and life-threatening systemic fungal infections are on the increase. Conventional treatment is of limited help, not in the least due to a less optimum benefit-to-risk ratio. Moreover, emerging pathogens with reduced antimicrobial susceptib...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章,评审

    doi:10.1016/s0924-8579(00)00323-x

    authors: Bastert J,Schaller M,Korting HC,Evans EG

    更新日期:2001-02-01 00:00:00

  • In vitro activity of several antimicrobial agents against 1003 isolates of Streptococcus pyogenes collected from Western Canada.

    abstract::Streptococcus pyogenes is a common pathogen which may be associated with significant morbidity and mortality. Recent information is not readily available, in Canada, regarding the susceptibility of clinical isolates to penicillin, extended spectrum and/or newer agents. We collected and tested 1003 isolates of S. pyoge...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/s0924-8579(98)00105-8

    authors: Blondeau JM,Church D,Yaschuk Y,Bjarnason J

    更新日期:1999-06-01 00:00:00

  • Risk factors for polymyxin-resistant carbapenemase-producing Enterobacteriaceae in critically ill patients: An epidemiological and clinical study.

    abstract::This study aimed to assess the clinical impact and potential risk factors associated with polymyxin-resistant Enterobacteriaceae strains isolated from patients hospitalized in adult and neonatal intensive care units. A case-control study was conducted from September 2015 to January 2017. Antimicrobial susceptibility o...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2020.105882

    authors: da Silva KE,Baker S,Croda J,Nguyen TNT,Boinett CJ,Barbosa LS,Tetila A,Simionatto S

    更新日期:2020-03-01 00:00:00

  • Pharmacokinetics of the ketolide telithromycin after single and repeated doses in patients with hepatic impairment.

    abstract::The pharmacokinetic profiles of single and repeated oral doses of telithromycin 800 mg/day were compared in patients with hepatic impairment and healthy subjects in two open-label, non-randomized, parallel-group, multicentre studies. The maximal plasma concentrations (Cmax) and the area under the plasma concentration-...

    journal_title:International journal of antimicrobial agents

    pub_type: 临床试验,杂志文章,多中心研究

    doi:10.1016/s0924-8579(03)00128-6

    authors: Cantalloube C,Bhargava V,Sultan E,Vacheron F,Batista I,Montay G

    更新日期:2003-08-01 00:00:00

  • Comparative in vitro activity of gatifloxacin, grepafloxacin, levofloxacin, moxifloxacin and trovafloxacin against 4151 Gram-negative and Gram-positive organisms.

    abstract::Gatifloxacin, grepafloxacin, moxifloxacin and trovafloxacin are fluoroquinolones with enhanced Gram-positive activity while retaining broad-spectrum activity against Gram-negative pathogens. Levofloxacin and ciprofloxacin are older quinolones with broad activity against Gram-negative pathogens and borderline activity ...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/s0924-8579(99)00143-0

    authors: Blondeau JM,Laskowski R,Bjarnason J,Stewart C

    更新日期:2000-02-01 00:00:00

  • Mupirocin resistance among Malaysian isolates of methicillin-resistant Staphylococcus aureus.

    abstract::Four hundred methicillin-resistant Staphylococcus aureus strains (MRSA) from different geographical areas in Malaysia were tested for mupirocin susceptibility using minimum inhibitory concentration (MIC) determination. The majority of these strains (98.75%) were susceptible to mupirocin with MICs of < or = 4 mg/l. Fif...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/s0924-8579(01)00314-4

    authors: Norazah A,Koh YT,Ghani Kamel A,Alias R,Lim VK

    更新日期:2001-05-01 00:00:00

  • Antibacterial effects of theaflavin and synergy with epicatechin against clinical isolates of Acinetobacter baumannii and Stenotrophomonas maltophilia.

    abstract::Stenotrophomonas maltophilia and Acinetobacter baumannii are recognised as important nosocomial pathogens; however, due to their intrinsic resistance to multiple antibiotics, treatment options are limited. Polyphenols from black tea have been shown to possess antibacterial action. In this study, the antibacterial effe...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2011.07.006

    authors: Betts JW,Kelly SM,Haswell SJ

    更新日期:2011-11-01 00:00:00

  • Association between augmented renal clearance, antibiotic exposure and clinical outcome in critically ill septic patients receiving high doses of β-lactams administered by continuous infusion: a prospective observational study.

    abstract::This study assessed whether augmented renal clearance (ARC) impacts negatively on antibiotic concentrations and clinical outcomes in patients treated by high-dose β-lactams administered continuously. Over a 9-month period, all critically ill patients without renal impairment treated by one of the monitored β-lactams f...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2017.11.013

    authors: Carrié C,Petit L,d'Houdain N,Sauvage N,Cottenceau V,Lafitte M,Foumenteze C,Hisz Q,Menu D,Legeron R,Breilh D,Sztark F

    更新日期:2018-03-01 00:00:00

  • Legal framework of antimicrobial stewardship in hospitals (LEASH): a European Society of Clinical Microbiology and Infectious Diseases (ESCMID) cross-sectional international survey.

    abstract::Antimicrobial stewardship (AMS) is the cornerstone activity in the combat against antimicrobial resistance. In order to ensure sustainable deployment and development of AMS, a strategic and regulatory framework needs to be provided by national healthcare authorities. Experts from 32 European countries, Israel and Turk...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2018.07.019

    authors: Beović B,Pulcini C,Dumartin C,Béraud G,Nerat B,Maurel C,Doušak M,Čižman M,LEASH Study Group on behalf of ESCMID Study Group for Antimicrobial StewardshiP (ESGAP).

    更新日期:2018-11-01 00:00:00

  • Open-label, multicentre, emergency-use study of clinafloxacin (CI-960) in the treatment of patients with serious life-threatening infections.

    abstract::In an open-label emergency-use study, 23 patients with bacterial infections caused by multiply drug resistant pathogens were treated with clinafloxacin. Efficacy and safety were evaluated by tabulating investigators' assessments at the end of treatment, treatment discontinuations and adverse event data. Most of the pa...

    journal_title:International journal of antimicrobial agents

    pub_type: 临床试验,杂志文章,多中心研究

    doi:10.1016/s0924-8579(02)00006-7

    authors: Shah P,Trostmann U,Tack K

    更新日期:2002-03-01 00:00:00

  • Staphylococcus aureus bacteraemia with known sources.

    abstract::Meticillin-resistant Staphylococcus aureus (MRSA), both hospital-acquired and community-acquired MRSA (CA-MRSA) strains, have increased in frequency in the last few years, reaching epidemic dimensions. This review discusses several clinical forms of staphylococcal infection leading to bacteraemia in a high proportion ...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijantimicag.2008.06.006

    authors: Rubinstein E

    更新日期:2008-11-01 00:00:00

  • In vivo activity of amoxicillin/clavulanic acid and erythromycin in experimental otitis media caused by Streptococcus pneumoniae plus Haemophilus influenzae.

    abstract::A gerbil model of acute otitis media induced by Streptococcus pneumoniae plus Haemophilus influenzae was used to assess the efficacy of amoxicillin/clavulanic acid (A/C) (1.5/0.3, 2.5/0.5 and 10/2 mg/kg) and erythromycin (2.5, 10, 20 and 50 mg/kg) with or without acetaminophen. The amoxicillin/clavulanic acid MIC was ...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2003.05.016

    authors: Parra A,Ponte C,Cenjor C,García-Olmos M,Giménez MJ,Aguilar L,Soriano F

    更新日期:2004-01-01 00:00:00

  • SILA 421, an inhibitor of efflux pumps of cancer cells, enhances the killing of intracellular extensively drug-resistant tuberculosis (XDR-TB).

    abstract::Multidrug-resistant and extensively drug-resistant tuberculosis (MDR/XDR-TB) are problematic to manage, especially in patients with acquired immune deficiency syndrome (AIDS). There is therefore a dire need for effective anti-MDR/XDR-TB agents. We have previously shown that agents that inhibit the efflux pumps of MDR ...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2008.10.028

    authors: Martins M,Viveiros M,Ramos J,Couto I,Molnar J,Boeree M,Amaral L

    更新日期:2009-05-01 00:00:00

  • Composition of the outer membrane proteins of Escherichia coli strains in relation to serum susceptibility after exposure to subinhibitory concentrations of amikacin and ciprofloxacin.

    abstract::The effect of subinhibitory concentrations of amikacin and ciprofloxacin on the susceptibility of Escherichia coli strains to the bactericidal action of normal human serum, outer membrane protein (OMP) expression and cell morphology was investigated. Sub-minimal inhibitory concentrations (sub-MICs) of both antibiotics...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2008.12.006

    authors: Wojnicz D,Cisowska A

    更新日期:2009-06-01 00:00:00

  • Managing skin and soft-tissue infection and nosocomial pneumonia caused by MRSA: a 2014 follow-up survey.

    abstract::As a follow-up to our 2009 survey, in order to explore opinion and practice on the epidemiology and management of meticillin-resistant Staphylococcus aureus (MRSA) in Europe, we conducted a second survey to elicit current opinions on this topic, particularly around antibiotic choice, dose, duration and route of admini...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/S0924-8579(15)30002-9

    authors: Dryden M,Andrasevic AT,Bassetti M,Bouza E,Chastre J,Baguneid M,Esposito S,Giamarellou H,Gyssens I,Nathwani D,Unal S,Voss A,Wilcox M

    更新日期:2015-04-24 00:00:00

  • Antimicrobial activities of levofloxacin, clarithromycin, and KRM-1648 against Mycobacterium tuberculosis and Mycobacterium avium complex replicating within Mono Mac 6 human macrophage and A-549 type II alveolar cell lines.

    abstract::The antimicrobial activities of levofloxacin, clarithromycin and KRM-1648 against Mycobacterium tuberculosis (MTB) and Mycobacterium avium complex (MAC) residing in Mono Mac 6 human macrophage-like cells (MM6-Mphis) and A-549 human type II alveolar epithelial cells (A-549 cells) were studied. We measured the antimicro...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/s0924-8579(00)00163-1

    authors: Sato K,Tomioka H,Akaki T,Kawahara S

    更新日期:2000-09-01 00:00:00

  • High prevalence of CTX-M-15-producing Klebsiella pneumoniae isolates in Asian countries: diverse clones and clonal dissemination.

    abstract::The characteristics of 218 Klebsiella pneumoniae isolates from patients with hospital-acquired pneumonia in nine Asian countries were investigated. In total, 92 isolates (42.2%) produced extended-spectrum β-lactamases (ESBLs), amongst which 67 (72.8%) possessed CTX-M ESBL genes; CTX-M-15 was the major ESBL (55 isolate...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2011.03.020

    authors: Lee MY,Ko KS,Kang CI,Chung DR,Peck KR,Song JH

    更新日期:2011-08-01 00:00:00

  • Phenothiazinium-fluoroquinolone drug conjugates.

    abstract::Synthesis and antibacterial screening of a homologous series of 3-dialkylaminophenothiazinium-7-norfloxacin conjugates was carried out alongside a corresponding series of symmetrical methylene blue derivatives. The norfloxacin conjugates maintained typical methylene blue derivative photoproperties, such as long wavele...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2009.11.022

    authors: Wainwright M,Shah A,Meegan K,Loughran C,Smith A,Valli N,Dempster N

    更新日期:2010-04-01 00:00:00

  • The effect of Nepeta cataria extract on adherence and enzyme production of Staphylococcus aureus.

    abstract::Nepeta cataria L., commonly known as catnip, is a perennial herb with a considerable folkloric reputation. A diethyl ether extract of this plant has been shown to have antimicrobial activity against fungi and Gram-positive bacteria. The aim of this work was to study the activity of N. cataria extract on 44 Staphylococ...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/s0924-8579(01)00452-6

    authors: Nostro A,Cannatelli MA,Crisafi G,Alonzo V

    更新日期:2001-12-01 00:00:00

  • Combination effects of cephalexin and gentamicin on Edwardsiella tarda and Streptococcus iniae.

    abstract::The objective of this study was to determine the in vitro activity of cephalexin-gentamicin combination by a microbroth chequerboard technique against clinical isolates of Edwardsiella tarda and Streptococcus iniae. Gentamicin was shown more susceptible than cephalexin against both bacteria. The effect of cephalexin-g...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/s0924-8579(03)00086-4

    authors: Lim JH,Hwang YH,Park BK,Yun HI

    更新日期:2003-07-01 00:00:00

  • Daptomycin-containing regimens for treatment of Gram-positive endocarditis.

    abstract:PURPOSE:Infective endocarditis (IE) is a severe infection, and a leading cause of mortality and morbidity. Due to its favourable microbiological and pharmacological characteristics, daptomycin is routinely used in clinical practice for treating IE. METHODS:A prospective study was conducted at a large tertiary-care hos...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2019.08.011

    authors: Russo A,Peghin M,Givone F,Ingani M,Graziano E,Bassetti M

    更新日期:2019-10-01 00:00:00

  • Current challenges in the diagnosis and management of invasive fungal infections: report from the 15th International Symposium on Infections in the Immunocompromised Host: Thessaloniki, Greece, 22-25 June 2008.

    abstract::New, aggressive forms of immunosuppression and an increasing population of patients at risk provide fertile ground for opportunistic invasive fungal infections (IFIs). Particularly challenging is the changing epidemiology of IFIs: rare pathogens are now more common and resistant strains are emerging among species that...

    journal_title:International journal of antimicrobial agents

    pub_type:

    doi:10.1016/j.ijantimicag.2008.08.014

    authors: Groll AH,McNeil Grist L

    更新日期:2009-02-01 00:00:00

  • Identification and bioevaluation of SRI-12742 as an antimicrobial agent against multidrug-resistant Acinetobacter baumannii.

    abstract::Multidrug-resistant Acinetobacter baumannii (MDR-Ab) is one of the most significant nosocomial pathogens that is being increasingly isolated in healthcare settings worldwide. Owing to its inherent drug-resistant nature, coupled with its ability to readily acquire resistance to other antibiotic classes, there is a real...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2018.02.018

    authors: Shukla M,Soni I,Matsuyama K,Tran T,Tanga M,Gong L,Chopra S

    更新日期:2018-07-01 00:00:00

  • Novel cell-based in vitro screen to identify small-molecule inhibitors against intracellular replication of Cryptococcus neoformans in macrophages.

    abstract::The fungal pathogen Cryptococcus neoformans poses a major threat to immunocompromised patients and is a leading killer of human immunodeficiency virus (HIV)-infected patients worldwide. Cryptococci are known to manipulate host macrophages and can either remain latent or proliferate intracellularly within the host phag...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/j.ijantimicag.2016.04.018

    authors: Samantaray S,Correia JN,Garelnabi M,Voelz K,May RC,Hall RA

    更新日期:2016-07-01 00:00:00

  • Ofloxacin and fleroxacin enhance superoxide production in human polymorphonuclear leukocytes by increasing phosphorylation in the signal transduction pathway.

    abstract::Many antimicrobial agents including new quinolones (NQs) influence the cellular defense mechanisms such as polymorphonuclear leukocytes (PMNs), macrophages and lymphocytes. We examined the effects of NQs on superoxide (SO) production of PMNs following stimulation of phorbol myristate acetate (PMA). Ofloxacin (OFLX) an...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章

    doi:10.1016/0924-8579(95)00024-0

    authors: Matsumoto T,Nagafuji T,Takahashi K,Kubo S,Sakumoto M,Mizunoe Y,Kumazawa J

    更新日期:1995-12-01 00:00:00

  • Community-acquired pneumonia: new management strategies for evolving pathogens and antimicrobial susceptibilities.

    abstract::Community-acquired pneumonia (CAP) is still one of the leading causes of mortality and morbidity. The most common bacterial cause of CAP is Streptococcus pneumoniae. The increase in antimicrobial resistance has raised concerns about the efficacy of available therapies, and a call for the reassessment of both existing ...

    journal_title:International journal of antimicrobial agents

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijantimicag.2004.08.006

    authors: Klugman KP,Low DE,Metlay J,Pechere JC,Weiss K

    更新日期:2004-11-01 00:00:00