Pharmacokinetics (PK), pharmacodynamics (PD), and PK-PD integration of danofloxacin in sheep biological fluids.

Abstract:

:The fluoroquinolone antimicrobial drug danofloxacin was administered to sheep intravenously (i.v.) and intramuscularly (i.m.) at a dose of 1.25 mg/kg of body weight in a two-period crossover study. The pharmacokinetic properties of danofloxacin in serum, inflamed tissue cage fluid (exudate), and noninflamed tissue cage fluid (transudate) were established by using a tissue cage model. The in vitro and ex vivo activities of danofloxacin in serum, exudate, and transudate against a pathogenic strain of Mannheimia haemolytica were established. Integration of in vivo pharmacokinetic data with the in vitro MIC provided mean values for the area under the curve (AUC)/MIC for serum, exudate, and transudate of 60.5, 85.6, and 45.7 h, respectively, after i.v. dosing and 55.9, 77.9, and 49.1 h, respectively, after i.m. dosing. After i.m. dosing, the maximum concentration/MIC ratios for serum, exudate, and transudate were 10.8, 3.0, and 1.6, respectively. The ex vivo growth inhibition data after i.m. dosing were fitted to the inhibitory sigmoid E(max) equation to provide the values of AUC/MIC required to produce bacteriostasis, bactericidal activity, and elimination of bacteria. The respective values for serum were 17.8, 20.2, and 28.7 h, and slightly higher values were obtained for transudate and exudate. It is proposed that use of these data might provide a novel approach to the rational design of dosage schedules.

authors

Aliabadi FS,Landoni MF,Lees P

doi

10.1128/aac.47.2.626-635.2003

subject

Has Abstract

pub_date

2003-02-01 00:00:00

pages

626-35

issue

2

eissn

0066-4804

issn

1098-6596

journal_volume

47

pub_type

杂志文章
  • Activity of methacycline, related tetracyclines, and other antibiotics against various L-forms and their parent bacteria in vitro.

    abstract::The activity of methacycline against microbial L-forms and their parent bacteria was compared with that of oxytetracycline, chlortetracycline, tetracycline, and demethylchlortetracycline, as well as with that of 22 other antibiotics which included examples of major groups of antibiotics. The L-forms and bacteria used ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.2.4.276

    authors: Hubert EG,Kalmanson GM,Montgomerie JZ,Guze LB

    更新日期:1972-10-01 00:00:00

  • β-Lactam Antibiotics with a High Affinity for PBP2 Act Synergistically with the FtsZ-Targeting Agent TXA707 against Methicillin-Resistant Staphylococcus aureus.

    abstract::Methicillin-resistant Staphylococcus aureus (MRSA) is a multidrug-resistant pathogen that poses a significant risk to global health today. We have developed a promising new FtsZ-targeting agent (TXA707) with potent activity against MRSA isolates resistant to current standard-of-care antibiotics. We present here result...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00863-17

    authors: Ferrer-González E,Kaul M,Parhi AK,LaVoie EJ,Pilch DS

    更新日期:2017-08-24 00:00:00

  • Molecular epidemiology, sequence types, and plasmid analyses of KPC-producing Klebsiella pneumoniae strains in Israel.

    abstract::Sporadic isolates of carbapenem-resistant KPC-2-producing Klebsiella pneumoniae were isolated in Tel Aviv Medical Center during 2005 and 2006, parallel to the emergence of the KPC-3-producing K. pneumoniae sequence type 258 (ST 258). We aimed to study the molecular epidemiology of these isolates and to characterize th...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01818-09

    authors: Leavitt A,Carmeli Y,Chmelnitsky I,Goren MG,Ofek I,Navon-Venezia S

    更新日期:2010-07-01 00:00:00

  • Efficacy of repeated intravenous injection of peramivir against influenza A (H1N1) 2009 virus infection in immunosuppressed mice.

    abstract::The efficacy of intravenous peramivir against influenza A (H1N1) 2009 virus infection was evaluated in mice in which the immune system was suppressed by cyclophosphamide (CP) treatment. The mortality rate of the vehicle control group was 100%, and the mice lost 20% of their body weight on average by day 13 postinfecti...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02324-12

    authors: Kitano M,Kodama M,Itoh Y,Kanazu T,Kobayashi M,Yoshida R,Sato A

    更新日期:2013-05-01 00:00:00

  • In vitro antiviral activity and single-dose pharmacokinetics in humans of a novel, orally bioavailable inhibitor of human rhinovirus 3C protease.

    abstract::(E)-(S)-4-((S)-2-{3-[(5-methyl-isoxazole-3-carbonyl)-amino]-2-oxo-2H-pyridin-1-yl}-pent-4-ynoylamino)-5-((S)-2-oxo-pyrrolidin-3-yl)-pent-2-enoic acid ethyl ester (Compound 1) is a novel, irreversible inhibitor of human rhinovirus (HRV) 3C protease {inactivation rate constant (Kobs/[I]) of 223,000 M-1s-1}. In cell-base...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 临床试验,杂志文章

    doi:10.1128/AAC.49.6.2267-2275.2005

    authors: Patick AK,Brothers MA,Maldonado F,Binford S,Maldonado O,Fuhrman S,Petersen A,Smith GJ 3rd,Zalman LS,Burns-Naas LA,Tran JQ

    更新日期:2005-06-01 00:00:00

  • Different genetic supports for the tet(S) gene in Enterococci.

    abstract::The diversity of tet(S) genetic contexts of 13 enterococci from human, animal, and environmental samples from different geographical areas is reported. The tet(S) gene was linked to either CTn6000 variants of chromosomal location or composite platforms flanked by IS1216 located on plasmids (∼40 to 115 kb). The compara...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00758-12

    authors: Novais C,Freitas AR,Silveira E,Baquero F,Peixe L,Roberts AP,Coque TM

    更新日期:2012-11-01 00:00:00

  • Bioavailability of oral trimetrexate in patients with acquired immunodeficiency syndrome.

    abstract::The combination of the lipophilic antifolate trimetrexate and the rescue agent leucovorin has shown promise in the treatment of Pneumocystis carinii pneumonia in patients with acquired immunodeficiency syndrome. The pharmacokinetic behavior of trimetrexate administered either by intravenous bolus or orally was studied...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.32.3.324

    authors: Rogers P,Allegra CJ,Murphy RF,Drake JC,Masur H,Poplack DG,Chabner BA,Parrillo JE,Lane HC,Balis FM

    更新日期:1988-03-01 00:00:00

  • In Vitro Characterization of Human Cytomegalovirus-Targeting Therapeutic Monoclonal Antibodies LJP538 and LJP539.

    abstract::Human cytomegalovirus (HCMV) infection is usually benign in healthy individuals but can cause life-threatening disease in those with compromised immune systems. Approved drugs available to treat HCMV disease, including ganciclovir, cidofovir, and foscarnet, have significant toxicities that limit their use in certain p...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00382-16

    authors: Patel HD,Nikitin P,Gesner T,Lin JJ,Barkan DT,Ciferri C,Carfi A,Akbarnejad Yazdi T,Skewes-Cox P,Wiedmann B,Jarousse N,Zhong W,Feire A,Hebner CM

    更新日期:2016-07-22 00:00:00

  • Interaction of azthreonam and related monobactams with beta-lactamases from gram-negative bacteria.

    abstract::Monobactams containing 3 beta-aminothiazolyl oxime side chains (SQ 81,377, SQ 81,402, azthreonam, and SQ 26,917) have poor affinities for the broad-spectrum beta-lactamases TEM-2 and K1. Addition of a 4-methyl substituent significantly increased stability to hydrolysis by these enzymes. P99 cephalosporinase from Enter...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.22.3.414

    authors: Bush K,Freudenberger JS,Sykes RB

    更新日期:1982-09-01 00:00:00

  • Mechanism of enhanced activity of liposome-entrapped aminoglycosides against resistant strains of Pseudomonas aeruginosa.

    abstract::Pseudomonas aeruginosa is inherently resistant to most conventional antibiotics. The mechanism of resistance of this bacterium is mainly associated with the low permeability of its outer membrane to these agents. We sought to assess the bactericidal efficacy of liposome-entrapped aminoglycosides against resistant clin...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01547-05

    authors: Mugabe C,Halwani M,Azghani AO,Lafrenie RM,Omri A

    更新日期:2006-06-01 00:00:00

  • Pharmacokinetics of lomefloxacin in healthy volunteers: comparison of 400 milligrams once daily and 200 milligrams twice daily given orally for 5 days.

    abstract::We evaluated the effect of repeated oral doses (5 days of treatment) on the kinetics of lomefloxacin in volunteers and compared the kinetics after two different regimens, i.e., 400 mg once daily and 200 mg twice daily. After 400 mg of lomefloxacin was given once daily, no significant modification in the pharmacokineti...

    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.34.1.150

    authors: Gros I,Carbon C

    更新日期:1990-01-01 00:00:00

  • Action of uracil analogs on human immunodeficiency virus type 1 and its reverse transcriptase.

    abstract::Three structural analogs of 5-ethyl-1-benzyloxymethyl-6-(phenylthio)uracil (E-BPU) inhibited human immunodeficiency virus type 1 (HIV-1) replication without cytotoxicity in vitro and were more potent than azidothymidine and were as potent as E-BPU. The target of these compounds is HIV-1 reverse transcriptase. Reverse ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.39.2.539

    authors: Piras G,Dutschman GE,Im GJ,Pan BC,Chu SH,Cheng YC

    更新日期:1995-02-01 00:00:00

  • Effects of ionenes on interferon induction by poly(inosinic acid) . poly(cytidylic acid).

    abstract::Depending on the spacing of their positive charges, ionenes, a class of quaternary ammonium polymers, increased the interferon-inducing activity of poly(inosinic acid).poly(cytidylic acid) in mouse L-929 cells, whereas they did not enhance poly(inosinic acid).poly(cytidylic acid) induced interferon production in prima...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.11.4.756

    authors: Clercq ED,Janik B,Sommer RG

    更新日期:1977-04-01 00:00:00

  • Streptococcus pneumoniae transposon Tn1545/Tn6003 changes to Tn6002 due to spontaneous excision in circular form of the erm(B)- and aphA3-containing macrolide-aminoglycoside-streptothricin (MAS) element.

    abstract::The macrolide-aminoglycoside-streptothricin (MAS) element, an ∼4.2-kb insertion containing erm(B) and aphA3 resistance determinants, distinguishes Streptococcus pneumoniae transposon Tn1545/Tn6003 from Tn6002. Here, it is shown to be an unstable genetic element that, although it lacks recombinase genes, can exploit lo...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01487-12

    authors: Palmieri C,Mingoia M,Massidda O,Giovanetti E,Varaldo PE

    更新日期:2012-11-01 00:00:00

  • Developing New Drugs for Mycobacterium tuberculosis Therapy: What Information Do We Get from Preclinical Animal Models?

    abstract::Preclinical animal models of infection are employed to develop new agents but also to screen among molecules to rank them. There are often major differences between human pharmacokinetic (PK) profiles and those developed by animal models of infection, and these may lead to substantial differences in efficacy relative ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01376-20

    authors: Drusano GL,Duncanson B,Scanga CA,Kim S,Schmidt S,Neely MN,Yamada WM,Vicchiarelli M,Peloquin CA,Louie A

    更新日期:2020-11-17 00:00:00

  • A tight-binding mode of inhibition is essential for anti-human immunodeficiency virus type 1 virucidal activity of nonnucleoside reverse transcriptase inhibitors.

    abstract::It was previously found that certain nonnucleoside reverse transcriptase inhibitors (NNRTI) possess virucidal activity against human immunodeficiency virus type 1 (HIV-1), and it was suggested that the tight-binding mode of inhibition of reverse transcriptase might be important for this virucidal activity (Borkow et a...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.46.6.1851-1856.2002

    authors: Motakis D,Parniak MA

    更新日期:2002-06-01 00:00:00

  • In Vitro and In Vivo Trypanosomicidal Action of Novel Arylimidamides against Trypanosoma cruzi.

    abstract::Arylimidamides (AIAs) have been shown to have considerable biological activity against intracellular pathogens, includingTrypanosoma cruzi, which causes Chagas disease. In the present study, the activities of 12 novel bis-AIAs and 2 mono-AIAs against different strains ofT. cruziin vitroandin vivowere analyzed. The mos...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01667-15

    authors: Guedes-da-Silva FH,Batista DG,Meuser MB,Demarque KC,Fulco TO,Araújo JS,Da Silva PB,Da Silva CF,Patrick DA,Bakunova SM,Bakunov SA,Tidwell RR,Oliveira GM,Britto C,Moreira OC,Soeiro MN

    更新日期:2016-03-25 00:00:00

  • Explaining the bias in the 23S rRNA gene mutations associated with clarithromycin resistance in clinical isolates of Helicobacter pylori.

    abstract::A single point mutation in the 23S rRNA gene of Helicobacter pylori is known to confer resistance to clarithromycin. Most prevalent among clarithromycin-resistant clinical H. pylori isolates are the mutations from A-2142 to G and A-2143 to G in the 23S rRNA gene. The bias in the 23S rRNA gene mutations conferring clar...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.42.10.2749

    authors: Debets-Ossenkopp YJ,Brinkman AB,Kuipers EJ,Vandenbroucke-Grauls CM,Kusters JG

    更新日期:1998-10-01 00:00:00

  • Pharmacodynamic parameters and toxicity of netilmicin (6 milligrams/kilogram/day) given once daily or in three divided doses to cancer patients with urinary tract infection.

    abstract::The pharmacologic parameters and toxicity of netilmicin (6 mg/kg/day) given once daily (qd) or thrice daily (tid) for the treatment of urinary tract infections were studied in a randomized prospective study of 60 cancer patients. The overall efficacy was 96%. Nephrotoxicity, assessed by the measure of urinary excretio...

    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.35.4.640

    authors: Van der Auwera P,Meunier F,Ibrahim S,Kaufman L,Derde MP,Tulkens PM

    更新日期:1991-04-01 00:00:00

  • Controlled Release of Plectasin NZ2114 from a Hybrid Silicone-Hydrogel Material for Inhibition of Staphylococcus aureus Biofilm.

    abstract::Staphylococcus aureus is a major human pathogen in catheter-related infections. Modifying catheter material with interpenetrating polymer networks is a novel material technology that allows for impregnation with drugs and subsequent controlled release. Here, we evaluated the potential for combining this system with pl...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00604-17

    authors: Klein K,Grønnemose RB,Alm M,Brinch KS,Kolmos HJ,Andersen TE

    更新日期:2017-06-27 00:00:00

  • Impact of Vancomycin MIC on Treatment Outcomes in Invasive Staphylococcus aureus Infections.

    abstract::There are conflicting data on the association of vancomycin MIC (VAN-MIC) with treatment outcomes in Staphylococcus aureus infections. We investigated the relationship between high VAN-MIC and 30-day mortality and identified the risk factors for mortality in a large cohort of patients with invasive S. aureus (ISA) inf...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,多中心研究

    doi:10.1128/AAC.01845-16

    authors: Song KH,Kim M,Kim CJ,Cho JE,Choi YJ,Park JS,Ahn S,Jang HC,Park KH,Jung SI,Yoon N,Kim DM,Hwang JH,Lee CS,Lee JH,Kwak YG,Kim ES,Park SY,Park Y,Lee KS,Lee YS,Kim HB

    更新日期:2017-02-23 00:00:00

  • Third type of plasmid conferring gentamicin resistance in Pseudomonas aeruginosa.

    abstract::R1033 is a plasmid of compatibility group P (= P1) transferred from a wild strain of Pseudomonas aeruginosa. It confers resistance to gentamicin by gentamicin acetyl-transferase 1 and to kanamycin and neomycin by neomycin phosphotransferase 1. ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.8.3.227

    authors: Smith DI,Lus RG,Rubio Calvo MC,Datta N,Jacob AE,Hedges RW

    更新日期:1975-09-01 00:00:00

  • Microbiological assay for estimating concentrations of DL-alanosine in mouse tissue.

    abstract::A sensitive, precise microbiological assay was developed for the determination of tissue distribution of dl-alanosine, a new antitumor agent. ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.3.6.739

    authors: Pittillo RF,Woolley C

    更新日期:1973-06-01 00:00:00

  • Impact of alpha interferon and ribavirin on the function of maturing dendritic cells.

    abstract::Alpha interferon and ribavirin are required in combination to achieve a sustained virological response in the treatment of hepatitis C virus (HCV) infection. Alpha interferon has direct antiviral activity and also enhances HCV-specific T-cell responses. Ribavirin has little direct activity against HCV but reduces hepa...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.48.9.3382-3389.2004

    authors: Barnes E,Salio M,Cerundolo V,Medlin J,Murphy S,Dusheiko G,Klenerman P

    更新日期:2004-09-01 00:00:00

  • Biochemical characterization of PER-2 and genetic environment of blaPER-2.

    abstract::PER-2 was the first detected and the second most prevalent extended-spectrum beta-lactamase in clinical pathogens isolated in Argentina and was also reported only in other South American countries. Citrobacter freundii 33587 was isolated in 1999 in Buenos Aires and was resistant to all tested beta-lactams except cepha...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01395-06

    authors: Power P,Di Conza J,Rodríguez MM,Ghiglione B,Ayala JA,Casellas JM,Radice M,Gutkind G

    更新日期:2007-07-01 00:00:00

  • Identification of a Novel Gene Associated with High-Level β-Lactam Resistance in Heterogeneous Vancomycin-Intermediate Staphylococcus aureus Strain Mu3 and Methicillin-Resistant S. aureus Strain N315.

    abstract::β-Lactam resistance levels vary among methicillin-resistant Staphylococcus aureus (MRSA) clinical isolates, mediated by chromosomal mutations and exogenous resistance gene mecA However, MRSA resistance mechanisms are incompletely understood. A P440L mutation in the RNA polymerase β' subunit (RpoC) in slow-vancomycin-i...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00712-18

    authors: Matsuo M,Yamamoto N,Hishinuma T,Hiramatsu K

    更新日期:2019-01-29 00:00:00

  • Pharmacokinetic properties of artemether, dihydroartemisinin, lumefantrine, and quinine in pregnant women with uncomplicated plasmodium falciparum malaria in Uganda.

    abstract::Pregnancy alters the pharmacokinetic properties of many drugs used in the treatment of malaria, usually resulting in lower drug exposures. This increases the risks of treatment failure, adverse outcomes for the fetus, and the development of resistance. The pharmacokinetic properties of artemether and its principal met...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00683-13

    authors: Tarning J,Kloprogge F,Dhorda M,Jullien V,Nosten F,White NJ,Guerin PJ,Piola P

    更新日期:2013-10-01 00:00:00

  • Susceptibilities of Streptococcus pneumoniae and Haemophilus influenzae to 10 oral antimicrobial agents based on pharmacodynamic parameters: 1997 U.S. Surveillance study.

    abstract::The susceptibilities of Streptococcus pneumoniae (1,476 strains) and untypeable Haemophilus influenzae (1,676 strains) to various oral beta-lactam, macrolide-azalide, and fluoroquinolone antimicrobial agents were determined by broth microdilution. Organisms were isolated from specimens obtained from outpatients in six...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,多中心研究

    doi:10.1128/AAC.43.8.1901

    authors: Jacobs MR,Bajaksouzian S,Zilles A,Lin G,Pankuch GA,Appelbaum PC

    更新日期:1999-08-01 00:00:00

  • Entecavir for treatment of hepatitis B virus displays no in vitro mitochondrial toxicity or DNA polymerase gamma inhibition.

    abstract::Therapy with nucleoside reverse transcriptase inhibitors (NRTIs) can be associated with mitochondrial toxicity. In vitro studies have been used to predict the predisposition for and characterize the mechanisms causing mitochondrial toxicity. Entecavir (ETV) is an approved deoxyguanosine nucleoside for the treatment of...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01122-07

    authors: Mazzucco CE,Hamatake RK,Colonno RJ,Tenney DJ

    更新日期:2008-02-01 00:00:00

  • Chitosan augments photodynamic inactivation of gram-positive and gram-negative bacteria.

    abstract::Antimicrobial photodynamic inactivation (PDI) was shown to be a promising treatment modality for microbial infections. This study explores the effect of chitosan, a polycationic biopolymer, in increasing the PDI efficacy against Gram-positive bacteria, including Staphylococcus aureus, Staphylococcus epidermidis, Strep...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00550-10

    authors: Tsai T,Chien HF,Wang TH,Huang CT,Ker YB,Chen CT

    更新日期:2011-05-01 00:00:00