Pharmacokinetics of L-671,329 in rhesus monkeys and DBA/2 mice.

Abstract:

:The time course of plasma drug levels and urinary recovery for two lipopeptide antifungal antibiotics, L-671,329 and cilofungin, were measured in male rhesus monkeys (Macaca mulatta) and in female DBA/2 mice. The antibiotics were administered intravenously at 10 mg/kg of body weight in phosphate-buffered saline-26% polyethylene glycol for the rhesus monkeys and in 5% dimethyl sulfoxide for the mice. Plasma and urine drug concentrations were determined by high-pressure liquid chromatography and/or a microbiological assay versus Aspergillus niger, and pharmacokinetic parameters were determined for both species. In each of the two rhesus crossover tests as well as in the mouse studies, the pharmacokinetics of the two compounds were similar; however, a marked difference was evident between species. The half-lives of L-671,329 and cilofungin in plasma were 39 and 34 min in the mice and averaged 1.8 and 2 h in the rhesus monkeys, respectively. In mice and rhesus monkeys, urinary recovery was less than 4% for both compounds.

authors

Sundelof JG,Hajdu R,Cleare WJ,Onishi J,Kropp H

doi

10.1128/aac.36.3.607

subject

Has Abstract

pub_date

1992-03-01 00:00:00

pages

607-10

issue

3

eissn

0066-4804

issn

1098-6596

journal_volume

36

pub_type

杂志文章
  • Correlation between mutations in liaFSR of Enterococcus faecium and MIC of daptomycin: revisiting daptomycin breakpoints.

    abstract::Mutations in liaFSR, a three-component regulatory system controlling cell-envelope stress response, were recently linked with the emergence of daptomycin (DAP) resistance in enterococci. Our previous work showed that a liaF mutation increased the DAP MIC of a vancomycin-resistant Enterococcus faecalis strain from 1 to...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00509-12

    authors: Munita JM,Panesso D,Diaz L,Tran TT,Reyes J,Wanger A,Murray BE,Arias CA

    更新日期:2012-08-01 00:00:00

  • In vitro activities of aminomethyl-substituted analogs of novel tetrahydrofuranyl carbapenems.

    abstract::CL 188,624, CL 190,294, and CL 191,121 are novel aminomethyl tetrahydrofuranyl (THF)-1 beta-methylcarbapenems. The in vitro antibacterial activities of these THF carbapenems were evaluated and compared with those of biapenem, imipenem, and meropenem against 554 recent clinical isolates obtained from geographically dis...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.43.3.454

    authors: Weiss WJ,Petersen PJ,Jacobus NV,Lin YI,Bitha P,Testa RT

    更新日期:1999-03-01 00:00:00

  • Antileishmanial and antitrypanosomal activities of the 8-aminoquinoline tafenoquine.

    abstract::The 8-aminoquinoline tafenoquine showed significant in vitro activity against Leishmania species, including L. donovani amastigotes in macrophages, with 50% inhibitory concentrations (IC(50)s) between 0.1 and 4.0 μM for both pentavalent antimony (SbV)-sensitive and SbV-resistant strains and by oral administration in B...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00985-10

    authors: Yardley V,Gamarro F,Croft SL

    更新日期:2010-12-01 00:00:00

  • Correlation of resistance to proflavine and penicillin in Escherichia coli.

    abstract::A number of proflavine (PF)-resistant mutants of Escherichia coli B were also resistant to penicillin and cephalothin. Mutants resistant to 1.0 mM PF were 10 times more penicillin resistant than were the PF-susceptible, wild-type cells. Single-step mutants selected for resistance to either PF or penicillin were also r...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.10.4.765

    authors: McKellar RC,McKenzie CN,Kushner KJ

    更新日期:1976-10-01 00:00:00

  • Treatment of anaerobic infections with metronidazole.

    abstract::The results of treatment of 10 patients with anaerobic infections with metronidazole are presented. Six patients were cured, three showed initial good response but circumstances required a change to another drug, and one patient did not respond. The unique spectrum of the drug, its pharmacology, and limitations are di...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 临床试验,杂志文章

    doi:10.1128/aac.7.5.672

    authors: Tally FP,Sutter VL,Finegold SM

    更新日期:1975-05-01 00:00:00

  • Phase I, single-dose, dose-escalating study of inhaled dry powder capreomycin: a new approach to therapy of drug-resistant tuberculosis.

    abstract::Multidrug-resistant tuberculosis (MDR-TB) threatens global TB control. The lengthy treatment includes one of the injectable drugs kanamycin, amikacin, and capreomycin, usually for the first 6 months. These drugs have potentially serious toxicities, and when given as intramuscular injections, dosing can be painful. Adv...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02346-12

    authors: Dharmadhikari AS,Kabadi M,Gerety B,Hickey AJ,Fourie PB,Nardell E

    更新日期:2013-06-01 00:00:00

  • Molecular characterization of multidrug-resistant Mycobacterium tuberculosis isolated in Nepal.

    abstract::Despite the fact that Nepal is one of the first countries globally to introduce multidrug-resistant tuberculosis (MDR-TB) case management, the number of MDR-TB cases is continuing to rise in Nepal. Rapid molecular tests applicable in this setting to identify resistant organisms would be an effective tool in reversing ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.06418-11

    authors: Poudel A,Nakajima C,Fukushima Y,Suzuki H,Pandey BD,Maharjan B,Suzuki Y

    更新日期:2012-06-01 00:00:00

  • Isoxyl activation is required for bacteriostatic activity against Mycobacterium tuberculosis.

    abstract::Isoxyl (ISO), a thiourea derivative that was successfully used for the clinical treatment of tuberculosis during the 1960s, is an inhibitor of the synthesis of oleic and mycolic acids in Mycobacterium tuberculosis. Its effect on oleic acid synthesis has been shown to be attributable to its inhibitory activity on the s...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00433-07

    authors: Korduláková J,Janin YL,Liav A,Barilone N,Dos Vultos T,Rauzier J,Brennan PJ,Gicquel B,Jackson M

    更新日期:2007-11-01 00:00:00

  • Sulfide Protects Staphylococcus aureus from Aminoglycoside Antibiotics but Cannot Be Regarded as a General Defense Mechanism against Antibiotics.

    abstract::Sulfide production has been proposed to be a universal defense mechanism against antibiotics in bacteria (K. Shatalin, E. Shatalina, A. Mironov, and E. Nudler, Science 334:986-990, 2011, doi:10.1126/science.1209855). To gain insight into the mechanism underlying sulfide protection, we systematically and comparatively ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00602-18

    authors: Weikum J,Ritzmann N,Jelden N,Klöckner A,Herkersdorf S,Josten M,Sahl HG,Grein F

    更新日期:2018-09-24 00:00:00

  • Levofloxacin Population Pharmacokinetics in South African Children Treated for Multidrug-Resistant Tuberculosis.

    abstract::Levofloxacin is increasingly used in the treatment of multidrug-resistant tuberculosis (MDR-TB). There are limited pediatric pharmacokinetic data to inform dose selection for children. Children routinely receiving levofloxacin (250-mg adult tablets) for MDR-TB prophylaxis or disease in Cape Town, South Africa, underwe...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01521-17

    authors: Denti P,Garcia-Prats AJ,Draper HR,Wiesner L,Winckler J,Thee S,Dooley KE,Savic RM,McIlleron HM,Schaaf HS,Hesseling AC

    更新日期:2018-01-25 00:00:00

  • Lack of association between hypermutation and antibiotic resistance development in Pseudomonas aeruginosa isolates from intensive care unit patients.

    abstract::Hypermutation is a common feature of Pseudomonas aeruginosa isolates from chronically infected cystic fibrosis patients that is linked with antibiotic resistance development. In this work, using a large collection of sequential P. aeruginosa isolates from ICU patients, we found that despite the fact that mutational an...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.48.9.3573-3575.2004

    authors: Gutiérrez O,Juan C,Pérez JL,Oliver A

    更新日期:2004-09-01 00:00:00

  • Antibiotic Prophylaxis Is Associated with Subsequent Resistant Infections in Children with an Initial Extended-Spectrum-Cephalosporin-Resistant Enterobacteriaceae Infection.

    abstract::The objective of this study was to assess the association between previous antibiotic use, particularly long-term prophylaxis, and the occurrence of subsequent resistant infections in children with index infections due to extended-spectrum-cephalosporin-resistant Enterobacteriaceae We also investigated the concordance...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02656-16

    authors: Das S,Adler AL,Miles-Jay A,Kronman MP,Qin X,Weissman SJ,Burnham CA,Elward A,Newland JG,Selvarangan R,Sullivan KV,Zaoutis T,Zerr DM

    更新日期:2017-04-24 00:00:00

  • A zidovudine-resistant simian immunodeficiency virus mutant with a Q151M mutation in reverse transcriptase causes AIDS in newborn macaques.

    abstract::The simian immunodeficiency virus (SIV)-newborn rhesus macaque model of AIDS can be used to study directly the virulence of viral mutants which are resistant to antiviral drugs. A viral mutant called SIVmac79A6.1, isolated from an SIV-infected macaque after prolonged zidovudine treatment, was found to have a double-ba...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.41.2.278

    authors: Van Rompay KK,Greenier JL,Marthas ML,Otsyula MG,Tarara RP,Miller CJ,Pedersen NC

    更新日期:1997-02-01 00:00:00

  • Susceptibility of recent clinical isolates of herpes simplex virus to 5-ethyl-2'-deoxyuridine: preferential inhibition of herpes simplex virus type 2.

    abstract::We examined the in vitro susceptibilities of three reference strains and 41 recent clinical isolates of herpes simplex virus types 1 and 2 to 5-ethyl-2'-deoxyuridine. This thymidine analog exerts a type 2-preferential but not a type 2-specific antiviral effect. Utilizing a microtiter assay with BHK-21 cells, we found ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.23.5.637

    authors: Teh CZ,Sacks SL

    更新日期:1983-05-01 00:00:00

  • Antimicrobial prophylaxis for major head and neck surgery in cancer patients.

    abstract::A total of 113 patients were randomly allocated to receive either ticarcillin plus clavulanic acid (total dose, 20.8 g) or clindamycin (total dose, 2.4 g) plus amikacin (total dose, 1 g) as perioperative antimicrobial prophylaxis for major head and neck surgery. The two groups were similar in age, prior antineoplastic...

    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.32.10.1557

    authors: Gerard M,Meunier F,Dor P,Andry G,Chantrain G,Van der Auwera P,Daneau D,Klastersky J

    更新日期:1988-10-01 00:00:00

  • Mechanism of fluconazole resistance in Candida krusei.

    abstract::The mechanisms of fluconazole resistance in three clinical isolates of Candida krusei were investigated. Analysis of sterols of organisms grown in the absence and presence of fluconazole demonstrated that the predominant sterol of C. krusei is ergosterol and that fluconazole inhibits 14alpha-demethylase in this organi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.42.10.2645

    authors: Orozco AS,Higginbotham LM,Hitchcock CA,Parkinson T,Falconer D,Ibrahim AS,Ghannoum MA,Filler SG

    更新日期:1998-10-01 00:00:00

  • Efflux unbalance in Pseudomonas aeruginosa isolates from cystic fibrosis patients.

    abstract::Retrospective analysis of 189 nonredundant strains of Pseudomonas aeruginosa sequentially recovered from the sputum samples of 46 cystic fibrosis (CF) patients over a 10-year period (1998 to 2007) revealed that 53 out of 189 (28%) samples were hypersusceptible to the beta-lactam antibiotic ticarcillin (MIC < or = 4 mi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01024-08

    authors: Vettoretti L,Plésiat P,Muller C,El Garch F,Phan G,Attrée I,Ducruix A,Llanes C

    更新日期:2009-05-01 00:00:00

  • The polyaminoisoprenyl potentiator NV716 revives old disused antibiotics against intracellular forms of infection by Pseudomonas aeruginosa.

    abstract::Active efflux confers intrinsic resistance to multiple antibiotics in Pseudomonas aeruginosa, including old disused molecules. Beside resistance, intracellular survival is another reason for failure to eradicate bacteria with antibiotics. We evaluated the capacity of polyaminoisoprenyl potentiators (designed as efflux...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02028-20

    authors: Wang GW,Brunel JM,Bolla JM,Van Bambeke F

    更新日期:2020-12-14 00:00:00

  • Role of beta-lactamase in in vivo development of ceftazidime resistance in experimental Pseudomonas aeruginosa endocarditis.

    abstract::Two ceftazidime-resistant variants of Pseudomonas aeruginosa (PA-48, PA-60), obtained from cardiac vegetations of rabbits with endocarditis receiving ceftazidime therapy, were studied for mechanisms of resistance. Both resistant variants were stably derepressed for the type Id beta-lactamase, which was ceftazidime ind...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.31.2.253

    authors: Bayer AS,Peters J,Parr TR Jr,Chan L,Hancock RE

    更新日期:1987-02-01 00:00:00

  • Variants of the Klebsiella pneumoniae OKP chromosomal beta-lactamase are divided into two main groups, OKP-A and OKP-B.

    abstract::Two bla(OKP) subgroups were found, diverging by 4.2%. Subgroups bla(OKP-A) (10 enzyme variants, pIs from 7.1 to 8.3) and bla(OKP-B) (11 variants, pI 7.1) showed similar antibiotic susceptibilities. Sequencing of rpoB, gyrA, and mdh demonstrated a concordant subdivision of Klebsiella pneumoniae phylogenetic group KpII ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.49.12.5149-5152.2005

    authors: Fevre C,Passet V,Weill FX,Grimont PA,Brisse S

    更新日期:2005-12-01 00:00:00

  • In vitro antimicrobial susceptibilities of penicillinase-producing and non-penicillinase-producing strains of Neisseria gonorrhoeae isolated in Durban, South Africa.

    abstract::The in vitro susceptibilities of 22 penicillinase-producing and 32 non-penicillinase-producing strains of Neisseria gonorrhoeae to 13 antimicrobial agents, including the new semisynthetic penicillins and cephalosporins, are reported. Ceftriaxone, ceftazidime, and cefotaxime were the most active agents tested; none of ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.26.5.770

    authors: Coovadia YM,Ramsaroop U

    更新日期:1984-11-01 00:00:00

  • Malaria treatment with atovaquone-proguanil in malaria-immune adults: implications for malaria intervention trials and for pre-exposure prophylaxis of malaria.

    abstract::Eighty adults in areas of Kenya where malaria is holoendemic received presumptive treatment with atovaquone-proguanil and were followed closely. The time to the first Plasmodium falciparum parasitemia was 32 days. This prolonged prophylaxis period has implications for study design when used in malaria intervention tri...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,随机对照试验

    doi:10.1128/AAC.01367-07

    authors: Polhemus ME,Remich S,Ogutu B,Waitumbi J,Lievens M,Ballou WR,Heppner DG Jr

    更新日期:2008-04-01 00:00:00

  • Comparison of Septic Shock Due to Multidrug-Resistant Acinetobacter baumannii or Klebsiella pneumoniae Carbapenemase-Producing K. pneumoniae in Intensive Care Unit Patients.

    abstract::A significant cause of mortality in the intensive care unit (ICU) is multidrug-resistant (MDR) Gram-negative bacteria, such as MDR Acinetobacter baumannii (MDR-AB) and Klebsiella pneumoniae carbapenemase-producing K. pneumoniae (KPC-Kp). The aim of the present study was to compare the clinical features, therapy, and o...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02562-17

    authors: Russo A,Giuliano S,Ceccarelli G,Alessandri F,Giordano A,Brunetti G,Venditti M

    更新日期:2018-05-25 00:00:00

  • Characterization of high-level daptomycin resistance in Viridans group Streptococci developed upon in vitro exposure to daptomycin.

    abstract::Viridans group streptococci (VGS) are part of the normal flora that may cause bacteremia, often leading to endocarditis. We evaluated daptomycin against four clinical strains of VGS (MICs = 1 or 2 μg/ml) using an in vitro-simulated endocardial vegetation model, a simulated bacteremia model, and kill curves. Daptomycin...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.04219-14

    authors: Akins RL,Katz BD,Monahan C,Alexander D

    更新日期:2015-04-01 00:00:00

  • Treatment of Candida glabrata infection in immunosuppressed mice by using a combination of liposomal amphotericin B with caspofungin or micafungin.

    abstract::While Candida albicans remains the most common Candida isolate, Candida glabrata accounts for approximately 15 to 20% of all Candida infections in the United States. In this study we used immunosuppressed mice infected with C. glabrata to investigate the efficacy of liposomal amphotericin B alone or in combination wit...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.49.12.4895-4902.2005

    authors: Olson JA,Adler-Moore JP,Smith PJ,Proffitt RT

    更新日期:2005-12-01 00:00:00

  • Efficacy of sparfloxacin and autoradiographic diffusion pattern of [14C]Sparfloxacin in experimental Staphylococcus aureus joint prosthesis infection.

    abstract::Using a new rabbit model of methicillin-susceptible Staphylococcus aureus knee prosthesis infection, we compared the efficacies of sparfloxacin (50 mg/kg of body weight subcutaneously, twice a day) and pefloxacin (50 mg/kg subcutaneously, twice a day). A partial knee replacement was performed with a silicone implant f...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.40.9.2111

    authors: Crémieux AC,Mghir AS,Bleton R,Manteau M,Belmatoug N,Massias L,Garry L,Sales N,Mazière B,Carbon C

    更新日期:1996-09-01 00:00:00

  • Novel pharmacokinetic-pharmacodynamic model for prediction of outcomes with an extended-release formulation of ciprofloxacin.

    abstract::The pharmacokinetics of an extended-release (XR) formulation of ciprofloxacin has been compared to that of the immediate-release (IR) product in healthy volunteers. The only significant difference in pharmacokinetic parameters between the two formulations was seen in the rate constant of absorption, which was approxim...

    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.48.6.2061-2068.2004

    authors: Meagher AK,Forrest A,Dalhoff A,Stass H,Schentag JJ

    更新日期:2004-06-01 00:00:00

  • [Combination of bacteriostatic and bactericidal drugs: lack of significant in vitro antagonism between penicillin, cephalothin, and rolitetracycline].

    abstract::Although it is generally believed that bactericidal and bacteriostatic drugs should not be combined in vivo, in vitro experiments using the checkerboard dilution technique revealed no antagonism between penicillin/cephalothin and rolitetracycline but rather additive or synergistic activity of either drug combination i...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.10.5.802

    authors: Daschner FD

    更新日期:1976-11-01 00:00:00

  • In Vitro Activity of Ceftazidime-Avibactam against Contemporary Pseudomonas aeruginosa Isolates from U.S. Medical Centers by Census Region, 2014.

    abstract::Thein vitroantibacterial activities of ceftazidime-avibactam and comparator agents were evaluated using reference broth microdilution methods against 1,743Pseudomonas aeruginosaisolates collected in 2014 from 69 U.S. medical centers, representing each of the nine census regions. Ceftazidime-avibactam demonstrated pote...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.03056-15

    authors: Huband MD,Castanheira M,Flamm RK,Farrell DJ,Jones RN,Sader HS

    更新日期:2016-03-25 00:00:00

  • Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of the β-Lactamase Inhibitor Vaborbactam (RPX7009) in Healthy Adult Subjects.

    abstract::Vaborbactam (formerly RPX7009) is a member of a new class of β-lactamase inhibitor with pharmacokinetic properties similar to those of many β-lactams, including carbapenems. The pharmacokinetics and safety of vaborbactam were evaluated in 80 healthy adult subjects in a first-in-human randomized, placebo-controlled, do...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,随机对照试验

    doi:10.1128/AAC.00568-16

    authors: Griffith DC,Loutit JS,Morgan EE,Durso S,Dudley MN

    更新日期:2016-09-23 00:00:00