In vitro and in vivo evaluation of tiacumicins B and C against Clostridium difficile.

Abstract:

:Tiacumicins B and C are members of a novel group of 18-membered macrolide antibiotics with in vitro activity against Clostridium difficile. The MICs against 15 strains of C. difficile were 0.12 to 0.25 microgram/ml for tiacumicin B, 0.25 to 1 microgram/ml for tiacumicin C, and 0.5 to 1 microgram/ml for vancomycin. The resistance frequency for both compounds against C. difficile was less than 2.8 x 10(-8) at four and eight times the MIC. The in vivo activities of the tiacumicins against two strains of C. difficile were compared with that of vancomycin in a hamster model of antibiotic-associated colitis. Oral therapy with 0.2, 1, or 5 mg of tiacumicin B or C per kg of body weight protected 100% of clindamycin-treated hamsters exposed to C. difficile ATCC 9689. Oral treatment with identical doses of vancomycin produced a prolonged, dose-dependent survival of hamsters, but it did not prevent the development of fatal colitis at doses of up to 5 mg/kg. When clindamycin-treated animals were exposed to another strain of C. difficile, both tiacumicin B and vancomycin were protective at 5 mg/kg, but not at lower doses. Tiacumicin C was not tested in vivo against the second strain of C. difficile. No tiacumicin B or C was detected in the sera of hamsters treated with single oral doses of 25 mg/kg, while antibiotic levels in the ceca of these hamsters reached 248 micrograms/ml and 285 mg/ml for tiacumicins B and C, respectively. The tiacumicins demonstrated in vitro and in vivo potencies against C. difficile and achieved high concentrations in the cecum, but not the serum, of hamsters after oral administration.

authors

Swanson RN,Hardy DJ,Shipkowitz NL,Hanson CW,Ramer NC,Fernandes PB,Clement JJ

doi

10.1128/aac.35.6.1108

subject

Has Abstract

pub_date

1991-06-01 00:00:00

pages

1108-11

issue

6

eissn

0066-4804

issn

1098-6596

journal_volume

35

pub_type

杂志文章
  • Effect of porins and plasmid-mediated AmpC beta-lactamases on the efficacy of beta-lactams in rat pneumonia caused by Klebsiella pneumoniae.

    abstract::The in vivo activities of imipenem, meropenem, and cefepime were studied in a model of rat pneumonia caused by a plasmid-mediated AmpC beta-lactamase ACT-1-producing Klebsiella pneumoniae strain (K. pneumoniae strain 12) and a derivative porin-deficient mutant (K. pneumoniae strain 12dp). No differences between these ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01513-05

    authors: Padilla E,Alonso D,Doménech-Sánchez A,Gomez C,Pérez JL,Albertí S,Borrell N

    更新日期:2006-06-01 00:00:00

  • International interlaboratory quality control program for measurement of antiretroviral drugs in plasma.

    abstract::An international interlaboratory quality control program for measurement of antiretroviral drugs was initiated. The first round was confined to protease inhibitors and showed large variability in the performance of participating laboratories. The results demonstrate the need for and utility of an ongoing quality contr...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.46.3.884-886.2002

    authors: Aarnoutse RE,Verweij-van Wissen CP,van Ewijk-Beneken Kolmer EW,Wuis EW,Koopmans PP,Hekster YA,Burger DM

    更新日期:2002-03-01 00:00:00

  • In vitro and in vivo pharmacokinetics-pharmacodynamics of GV143253A, a novel trinem.

    abstract::The aim of the present study was to characterize the pharmacokinetic-pharmacodynamic relationship of GV143253A, a novel trinem anti-methicillin-resistant Staphylococcus aureus (MRSA) agent active against gram-positive cocci, including multidrug-resistant clinical isolates. An in vitro pharmacodynamic study with methic...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.2.770-776.2003

    authors: Ferrari L,Iavarone L,Braggio S,Di Modugno E

    更新日期:2003-02-01 00:00:00

  • CEM-101 activity against Gram-positive organisms.

    abstract::The in vitro activity of CEM-101, a new fluoroketolide, was determined against Gram-positive organisms with various macrolide susceptibility profiles. Experiments for determination of the MICs and minimum bactericidal concentrations (MBCs), timed killing, single-step and multistep mutation rates, the erythromycin indu...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01662-09

    authors: Woosley LN,Castanheira M,Jones RN

    更新日期:2010-05-01 00:00:00

  • International spread and persistence of TEM-24 is caused by the confluence of highly penetrating enterobacteriaceae clones and an IncA/C2 plasmid containing Tn1696::Tn1 and IS5075-Tn21.

    abstract::TEM-24 remains one of the most widespread TEM-type extended-spectrum beta-lactamases (ESBLs) among Enterobacteriaceae. To analyze the reasons influencing its spread and persistence, a multilevel population genetics study was carried out on 28 representative TEM-24 producers from Belgium, France, Portugal, and Spain (1...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00959-09

    authors: Novais A,Baquero F,Machado E,Cantón R,Peixe L,Coque TM

    更新日期:2010-02-01 00:00:00

  • Rifampin: inhibition of ribonucleic acid synthesis after potentiation by amphotericin B in Saccharomyces cerevisiae.

    abstract::The inhibition of Saccharomyces cerevisiae growth by amphotericin B and rifampin was studied. Rifampin alone had no effect on growth or macromolecular syntheses. Lethal amounts of amphotericin B produced a late inhibition of ribonucleic acid (RNA) synthesis simultaneous with the arrest of growth and protein synthesis....

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.5.4.371

    authors: Battaner E,Kumar BV

    更新日期:1974-04-01 00:00:00

  • Susceptibility of Haemophilus influenzae type b to ampicillin-sulbactam.

    abstract::Seventy-five strains of Haemophilus influenzae type b, including 45 beta-lactamase-positive strains, were tested by MIC and time kill studies for susceptibility to ampicillin-sulbactam at various ratios. beta-Lactamase-negative strains were inhibited by lower concentrations of ampicillin-sulbactam than beta-lactamase-...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.33.9.1620

    authors: Azimi PH,Dunphy MG

    更新日期:1989-09-01 00:00:00

  • A potent plant-derived antifungal acetylenic acid mediates its activity by interfering with fatty acid homeostasis.

    abstract::6-Nonadecynoic acid (6-NDA), a plant-derived acetylenic acid, exhibits strong inhibitory activity against the human fungal pathogens Candida albicans, Aspergillus fumigatus, and Trichophyton mentagrophytes. In the present study, transcriptional profiling coupled with mutant and biochemical analyses were conducted usin...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.05663-11

    authors: Xu T,Tripathi SK,Feng Q,Lorenz MC,Wright MA,Jacob MR,Mask MM,Baerson SR,Li XC,Clark AM,Agarwal AK

    更新日期:2012-06-01 00:00:00

  • Evernimicin (SCH27899) inhibits a novel ribosome target site: analysis of 23S ribosomal DNA mutants.

    abstract::Spontaneous mutants of susceptible clinical and laboratory isolates of Streptococcus pneumoniae exhibiting reduced susceptibility to evernimicin (SCH27899; MIC, 0.5 to 4.0 mg/liter) were selected on plates containing evernimicin. Four isolates that did not harbor mutations in rplP (which encodes ribosomal protein L16)...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.44.11.3101-3106.2000

    authors: Adrian PV,Mendrick C,Loebenberg D,McNicholas P,Shaw KJ,Klugman KP,Hare RS,Black TA

    更新日期:2000-11-01 00:00:00

  • Virulence factors of Escherichia coli isolates that produce CTX-M-type extended-spectrum beta-lactamases.

    abstract::This study determined the phylogenetic groups and virulence factors of 37 Escherichia coli isolates producing types of CTX-M compared with those of 19 isolates producing different types of extended-spectrum beta-lactamases (ESBLs) in a well-defined North American population. Most CTX-M-14 producers (97%) were from phy...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.49.11.4667-4670.2005

    authors: Pitout JD,Laupland KB,Church DL,Menard ML,Johnson JR

    更新日期:2005-11-01 00:00:00

  • In vitro susceptibilities of Mycoplasma pneumoniae, Mycoplasma hominis, and Ureaplasma urealyticum to sparfloxacin and PD 127391.

    abstract::The in vitro activities of two investigational quinolones, sparfloxacin (previously designated AT 4140) and PD 127391, were determined for 30 strains each of Mycoplasma pneumoniae, Mycoplasma hominis, and Ureaplasma urealyticum and compared with those of ciprofloxacin, tetracycline, clindamycin, and erythromycin. Eryt...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.35.6.1181

    authors: Waites KB,Duffy LB,Schmid T,Crabb D,Pate MS,Cassell GH

    更新日期:1991-06-01 00:00:00

  • Gardimycin, a new antibiotic inhibiting peptidoglycan synthesis.

    abstract::Gardimycin, a new antibiotic, at 100 mug/ml, specifically inhibited cell wall synthesis and induced accumulation of uridine 5'-diphosphate-N-acetylmur-amylpentapeptide in whole cells of Bacillus subtilis. The antibiotic was active in a particulate enzyme preparation from Bacillus stearothermophilus: 60 mug/ml caused 5...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.11.3.396

    authors: Somma S,Merati W,Parenti F

    更新日期:1977-03-01 00:00:00

  • UK-18892, a new aminoglycoside: an in vitro study.

    abstract::UK-18892 is a new aminoglycoside antibiotic, a derivative of kanamycin A structurally related to amikacin. It was found to be active against a wide range of pathogenic bacteria, including many gentamicin-resistant strains. The spectrum and degree of activity of UK-18892 were similar to those of amikacin, and differenc...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.14.2.228

    authors: Wise R,Andrews JM

    更新日期:1978-08-01 00:00:00

  • In vitro activities of benflumetol against 158 Senegalese isolates of Plasmodium falciparum in comparison with those of standard antimalarial drugs.

    abstract::The 50% inhibitory concentration (IC50s) of benflumetol (range, 12.5 to 240 nM; mean, 55.1 nM) for 158 Senegalese isolates were evaluated. Ten isolates (6%) showed decreased susceptibility to benflumetol. Benflumetol was slightly more potent against chloroquine-resistant isolates (P < 0.025). No correlation or weak co...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.43.2.418

    authors: Pradines B,Tall A,Fusai T,Spiegel A,Hienne R,Rogier C,Trape JF,Le Bras J,Parzy D

    更新日期:1999-02-01 00:00:00

  • Ciprofloxacin resistance in clinical isolates of Salmonella typhimurium obtained from two patients.

    abstract::Two patients (patients A and B) infected with Salmonella typhimurium failed ciprofloxacin therapy, and the posttherapy isolates had reduced susceptibilities to quinolones; 6 of 11 isolates from patient B were also cross-resistant to chemically unrelated agents. No transferable resistance, chloramphenicol-acetylating e...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.37.4.662

    authors: Piddock LJ,Griggs DJ,Hall MC,Jin YF

    更新日期:1993-04-01 00:00:00

  • Discovery of New Inhibitors of Toxoplasma gondii via the Pathogen Box.

    abstract::Toxoplasma gondii is a cosmopolitan protozoan parasite which affects approximately 30% of the population worldwide. The drugs currently used against toxoplasmosis are few in number and show several limitations, such as drug intolerance, poor bioavailability, or drug resistance mechanism developed by the parasite. Thus...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01640-17

    authors: Spalenka J,Escotte-Binet S,Bakiri A,Hubert J,Renault JH,Velard F,Duchateau S,Aubert D,Huguenin A,Villena I

    更新日期:2018-01-25 00:00:00

  • Fluoroquinolone and Third-Generation-Cephalosporin Resistance among Hospitalized Patients with Urinary Tract Infections Due to Escherichia coli: Do Rates Vary by Hospital Characteristics and Geographic Region?

    abstract::This analysis of nearly 10,000 hospital-associated urinary tract infection (UTI) episodes due to Escherichia coli showed that fluoroquinolone and third-generation-cephalosporin resistance rates were 34.5% and 8.6%, respectively; the rate of concurrent resistance to both agents was 7.3%. Fluoroquinolone resistance rate...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02505-15

    authors: Bidell MR,Palchak M,Mohr J,Lodise TP

    更新日期:2016-04-22 00:00:00

  • Effects of various media on the activity of NXL103 (formerly XRP 2868), a new oral streptogramin, against Haemophilus influenzae.

    abstract::The activity of NXL103 against 108 strains of Haemophilus influenzae was tested using Haemophilus test media (HTM) obtained from various sources. With the exception of those obtained with stored HTM, MICs did not differ significantly, with MIC(50) and MIC(90) values of 0.5 and 0.5 to 1 microg/ml, respectively, in each...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00587-06

    authors: Pankuch GA,Hoellman D,Bryskier A,Lowther J,Appelbaum PC

    更新日期:2006-11-01 00:00:00

  • Evaluation of a loop-mediated isothermal amplification-based methodology to detect carbapenemase carriage in Acinetobacter clinical isolates.

    abstract::Carbapenem-resistant Acinetobacter baumannii is a major source of nosocomial infections worldwide and is mainly associated with the acquisition of OXA-type carbapenemases and, to a lesser extent, metallo-β-lactamases (MBLs). In this study, 82 nonepidemiologically related Acinetobacter strains carrying different types ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.03870-14

    authors: Vergara A,Zboromyrska Y,Mosqueda N,Morosini MI,García-Fernández S,Roca I,Cantón R,Marco F,Vila J

    更新日期:2014-12-01 00:00:00

  • Advancing the Therapeutic Potential of Indoleamides for Tuberculosis.

    abstract::Indole-2-carboxamide derivatives are inhibitors of MmpL3, the cell wall-associated mycolic acid transporter of Mycobacterium tuberculosis In the present study, we characterized indoleamide effects on bacterial cell morphology and reevaluated pharmacokinetics and in vivo efficacy using an optimized oral formulation. Mo...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00343-19

    authors: Lun S,Tasneen R,Chaira T,Stec J,Onajole OK,Yang TJ,Cooper CB,Mdluli K,Converse PJ,Nuermberger EL,Raj VS,Kozikowski A,Bishai WR

    更新日期:2019-06-24 00:00:00

  • Pharmacokinetics of sulfobutylether-beta-cyclodextrin and voriconazole in patients with end-stage renal failure during treatment with two hemodialysis systems and hemodiafiltration.

    abstract::Sulfobutylether-beta-cyclodextrin (SBECD), a large cyclic oligosaccharide that is used to solubilize voriconazole (VRC) for intravenous administration, is eliminated mainly by renal excretion. The pharmacokinetics of SBECD and voriconazole in patients undergoing extracorporeal renal replacement therapies are not well ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,随机对照试验

    doi:10.1128/AAC.01540-09

    authors: Hafner V,Czock D,Burhenne J,Riedel KD,Bommer J,Mikus G,Machleidt C,Weinreich T,Haefeli WE

    更新日期:2010-06-01 00:00:00

  • Inhibition of herpes simplex virus DNA synthesis by pokeweed antiviral protein.

    abstract::Pokeweed antiviral protein at a concentration of 3 microM inhibited both the synthesis and release of infectious herpes simplex virus type 1 in cell culture by 90 and 99%, respectively. Addition of pokeweed antiviral protein to Vero cell monolayers before virus infection was 10 to 15% more effective in reducing virus ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.23.3.390

    authors: Teltow GJ,Irvin JD,Aron GM

    更新日期:1983-03-01 00:00:00

  • Synergistic activity of colistin and ceftazidime against multiantibiotic-resistant Pseudomonas aeruginosa in an in vitro pharmacodynamic model.

    abstract::Despite the marketing of a series of new antibiotics for antibiotic-resistant gram-positive bacteria, no new agents for multiple-antibiotic-resistant gram-negative infections will be available for quite some time. Clinicians will need to find more effective ways to utilize available agents. Colistin is an older but no...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.3.905-909.2003

    authors: Gunderson BW,Ibrahim KH,Hovde LB,Fromm TL,Reed MD,Rotschafer JC

    更新日期:2003-03-01 00:00:00

  • Role of the K101E substitution in HIV-1 reverse transcriptase in resistance to rilpivirine and other nonnucleoside reverse transcriptase inhibitors.

    abstract::Resistance to the recently approved nonnucleoside reverse transcriptase inhibitor (NNRTI) rilpivirine (RPV) commonly involves substitutions at positions E138K and K101E in HIV-1 reverse transcriptase (RT), together with an M184I substitution that is associated with resistance to coutilized emtricitabine (FTC). Previou...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01536-13

    authors: Xu HT,Colby-Germinario SP,Huang W,Oliveira M,Han Y,Quan Y,Petropoulos CJ,Wainberg MA

    更新日期:2013-11-01 00:00:00

  • In Vivo Characterization of the Activation and Interaction of the VanR-VanS Two-Component Regulatory System Controlling Glycopeptide Antibiotic Resistance in Two Related Streptomyces Species.

    abstract::The VanR-VanS two-component system is responsible for inducing resistance to glycopeptide antibiotics in various bacteria. We have performed a comparative study of the VanR-VanS systems from two streptomyces strains, Streptomyces coelicolor and Streptomyces toyocaensis, to characterize how the two proteins cooperate t...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01367-15

    authors: Novotna GB,Kwun MJ,Hong HJ

    更新日期:2015-12-28 00:00:00

  • Clinafloxacin for Treatment of Burkholderia cenocepacia Infection in a Cystic Fibrosis Patient.

    abstract::Respiratory infection with Burkholderia cenocepacia is associated with accelerated decline in lung function and increased mortality in cystic fibrosis (CF) patients (A. M. Jones, M. E. Dodd, J. R. W. Govan, V. Barcus, C. J. Doherty, J. Morris, and A. K. Webb, Thorax 59:948-951, 2004, http://dx.doi.org/10.1136/thx.2003...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01428-15

    authors: Balwan A,Nicolau DP,Wungwattana M,Zuckerman JB,Waters V

    更新日期:2015-12-31 00:00:00

  • Comparative pharmacokinetics of two prodrugs of zidovudine in rabbits: enhanced levels of zidovudine in brain tissue.

    abstract::The pharmacokinetics of two prodrugs of zidovudine (AZT), 1,4-dihydro-1-methyl-3-[(pyridylcarbonyl)oxy] ester and isoleucinyl ester (DPAZT and IAZT, respectively), were investigated in a rabbit model to determine their potential utility as drugs against human immunodeficiency virus. Drugs were administered by intraven...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.37.4.818

    authors: Lupia RH,Ferencz N,Lertora JJ,Aggarwal SK,George WJ,Agrawal KC

    更新日期:1993-04-01 00:00:00

  • Randomized, controlled trial of a 10-day course of amifloxacin versus trimethoprim-sulfamethoxazole in the treatment of acute, uncomplicated urinary tract infection. Amifloxacin Multi-Center Trial Group.

    abstract::We conducted a randomized controlled trial of orally administered amifloxacin versus trimethoprimsulfamethoxazole (TMP-SMX) as treatments of acute uncomplicated urinary tract infection in women. Amifloxacin at a dosage of 200 mg twice a day appeared as safe and effective as TMP-SMX, but amifloxacin at 400 mg twice a d...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1128/aac.34.4.665

    authors: Boyko EJ,Iravani A,Silverman MH,Schelling DJ,Wright RA

    更新日期:1990-04-01 00:00:00

  • Changes in superhelical density of closed circular deoxyribonucleic acid by intercalation of anti-R-plasmid drugs and primaquine.

    abstract::The following compounds, which possess anti-R-plasmid activity (Hahn and Ciak, 1976) in decreasing order, were shown by viscometric titration to change systematically the superhelical density of closed circular PM2 deoxyribonucleic acid in the manner of intercalators: ethidium bromide, quinacrine, acridine orange, qui...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.11.2.251

    authors: Allison RG,Hahn FE

    更新日期:1977-02-01 00:00:00

  • No findings of dental defects in children treated with minocycline.

    abstract::Forty-one children <8 years of age treated for brucellosis with oral minocycline (2.5 mg/kg) twice daily for 3 weeks were recalled and examined to check for dental staining and defects. Dental staining and defects were found in 14 of 41 exposed children (34.1%) and in 30 of 82 matched controls (36.6%), respectively (P...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.48.7.2739-2741.2004

    authors: Cascio A,Di Liberto C,D'Angelo M,Iaria C,Scarlata F,Titone L,Campisi G

    更新日期:2004-07-01 00:00:00