Pharmacokinetics of temafloxacin in humans after multiple oral doses.

Abstract:

:The multiple-dose pharmacokinetics and tolerance of temafloxacin, a new fluoroquinolone antibacterial agent, were evaluated in healthy volunteers. Temafloxacin was found to be well tolerated when administered orally every 12 h for 7 days at doses of 100, 200, 300, 400, 600, and 800 mg. Steady-state maximum and minimum concentrations in plasma were proportional to dose, averaging slightly over 1.0 and 0.5 microgram/ml/100 mg administered. Analyses of variance found no significant differences among the dosage groups in total apparent clearances (CLT/F), renal clearances (CLR), or nonrenal clearances, which averaged 197, 119, and 78 ml/min, respectively. The half-life increased slightly with dose, averaging 8.4 h overall. The extent of absorption of temafloxacin was quite reproducible, with day-to-day intrasubject variability in minima averaging under 10%. Renal glomerular filtration of unbound drug was the dominant elimination process; however, tubular secretion and reabsorption also appear to occur. Secretion was estimated to account for about 12% of CLT/F during a regimen of 600 mg every 12 h. CLR was relatively constant for urine flow rates above 1 ml/min, but reabsorption appeared to occur under low-flow conditions, resulting in day-versus-night differences in CLR. Intersubject variability in CLT/F over the eightfold range in dosage was only 20%, and 60% of this variance was accounted for by differences in body surface area (or lean body mass), concentration in plasma, and urine flow rate. Overall, it appears that the pharmacokinetics of temafloxacin are essentially linear, reproducible within a subject, and predictable among subjects.

authors

Granneman GR,Carpentier P,Morrison PJ,Pernet AG

doi

10.1128/aac.36.2.378

subject

Has Abstract

pub_date

1992-02-01 00:00:00

pages

378-86

issue

2

eissn

0066-4804

issn

1098-6596

journal_volume

36

pub_type

杂志文章
  • Pharmacokinetics of the aminoglycoside antibiotic tobramycin in humans.

    abstract::The pharmacokinetics, distribution, and plasma and renal clearance of a new aminoglycoside antibiotic, tobramycin, was studied in the treatment of 18 elderly male patients (average age, 69 years) with urinary tract infections. Ten of these patients had normal renal function and eight had impaired renal function of var...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.3.4.469

    authors: Naber KG,Westenfelder SR,Madsen PO

    更新日期:1973-04-01 00:00:00

  • Characterization of Tn6238 with a new allele of aac(6')-Ib-cr.

    abstract::Here, we report that the genetic structure of Tn1331 remained conserved in Argentina from 1989 to 2013 (72 of 73 isolates), with the exception being the plasmid-borne Tn1331-like transposon Tn6238 containing a new aac(6')-Ib-cr allele recovered from a colistin-resistant Klebsiella pneumoniae clinical isolate. A bioinf...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.03213-14

    authors: Quiroga MP,Orman B,Errecalde L,Kaufman S,Centrón D

    更新日期:2015-05-01 00:00:00

  • DS86760016, a Leucyl-tRNA Synthetase Inhibitor with Activity against Pseudomonas aeruginosa.

    abstract::DS86760016 is a new leucyl-tRNA-synthetase inhibitor at the preclinical development stage. DS86760016 showed potent activity against extended-spectrum multidrug-resistant Pseudomonas aeruginosa isolated from clinical samples and in vitro biofilms. In a murine catheter-associated urinary tract infection model, DS867600...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02122-18

    authors: Kumar M,Rao M,Purnapatre KP,Barman TK,Joshi V,Kashyap A,Chaira T,Bambal RB,Pandya M,Khodor SA,Upadhyay DJ,Masuda N

    更新日期:2019-03-27 00:00:00

  • Mechanism of antimalarial action of the synthetic trioxolane RBX11160 (OZ277).

    abstract::RBX11160 (OZ277) is a fully synthetic peroxidic antimalarial in clinical development. To study the possible mechanisms of action of RBX11160, we have examined its ability to inhibit PfATP6, a sarcoplasmic reticulum calcium ATPase and proposed target for semisynthetic peroxidic artemisinin derivatives. RBX11160 inhibit...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01064-06

    authors: Uhlemann AC,Wittlin S,Matile H,Bustamante LY,Krishna S

    更新日期:2007-02-01 00:00:00

  • Cryptococcus neoformans resistance to echinocandins: (1,3)beta-glucan synthase activity is sensitive to echinocandins.

    abstract::(1,3)Beta-D-glucan synthase (EC 2.4.1.34. UDP-glucose: 1,3-beta-D-glucan 3-beta-glucosyltransferase) uses UDP-glucose as substrate and catalyzes the polymerization of glucose ([1,3]-beta-linkages) to form the major carbohydrate component of the fungal cell wall. We have optimized in vitro assay conditions for (1,3)bet...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.49.7.2851-2856.2005

    authors: Maligie MA,Selitrennikoff CP

    更新日期:2005-07-01 00:00:00

  • Identification of a plasmid-borne resistance gene cluster comprising the resistance genes erm(T), dfrK, and tet(L) in a porcine methicillin-resistant Staphylococcus aureus ST398 strain.

    abstract::A novel plasmid-borne resistance gene cluster comprising the genes erm(T) for macrolide-lincosamide-streptogramin B resistance, dfrK for trimethoprim resistance, and tet(L) for tetracycline resistance was identified in a porcine methicillin-resistant Staphylococcus aureus sequence type 398 (ST398) strain. This erm(T)-...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01091-09

    authors: Kadlec K,Schwarz S

    更新日期:2010-02-01 00:00:00

  • Ultrastructural alterations induced by two ergosterol biosynthesis inhibitors, ketoconazole and terbinafine, on epimastigotes and amastigotes of Trypanosoma (Schizotrypanum) cruzi.

    abstract::We report the ultrastructural alterations induced during the proliferative stages of Trypanosoma (Schizotrypanum) cruzi, the causative agent of Chagas' disease, by two ergosterol biosynthesis inhibitors, ketoconazole and terbinafine, which had previously been shown to be potent growth inhibitors whose effects are pote...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.34.11.2097

    authors: Lazardi K,Urbina JA,de Souza W

    更新日期:1990-11-01 00:00:00

  • In vitro activities of daptomycin, vancomycin, quinupristin- dalfopristin, linezolid, and five other antimicrobials against 307 gram-positive anaerobic and 31 Corynebacterium clinical isolates.

    abstract::The activities of daptomycin, a cyclic lipopeptide, and eight other agents were determined against 338 strains of gram-positive anaerobic bacteria and corynebacteria by the NCCLS reference agar dilution method with supplemented brucella agar for the anaerobes and Mueller-Hinton agar for the corynebacteria. The daptomy...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.1.337-341.2003

    authors: Goldstein EJ,Citron DM,Merriam CV,Warren YA,Tyrrell KL,Fernandez HT

    更新日期:2003-01-01 00:00:00

  • Transcriptional regulation of chitin synthases by calcineurin controls paradoxical growth of Aspergillus fumigatus in response to caspofungin.

    abstract::Attenuated activity of echinocandin antifungals at high concentrations, known as the "paradoxical effect," is a well-established phenomenon in Candida albicans and Aspergillus fumigatus. In the yeast C. albicans, upregulation of chitin biosynthesis via the protein kinase C (PKC), high-osmolarity glycerol response (HOG...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00854-09

    authors: Fortwendel JR,Juvvadi PR,Perfect BZ,Rogg LE,Perfect JR,Steinbach WJ

    更新日期:2010-04-01 00:00:00

  • Experimental prediction of the evolution of ceftazidime resistance in the CTX-M-2 extended-spectrum beta-lactamase.

    abstract::We applied in vitro evolution to an Escherichia coli strain containing bla(CTX-M-2) and obtained 10 independent mutant bla(CTX-M-2) alleles that confer elevated resistance to ceftazidime (MIC > or = 32 microg/ml) but lost the ability to confer resistance to cefepime. All alleles had a Pro-to-Ser substitution at positi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.49.3.1242-1244.2005

    authors: Welsh KJ,Barlow M,Tenover FC,Biddle JW,Rasheed JK,Clark LA,McGowan JE Jr

    更新日期:2005-03-01 00:00:00

  • Mode of action of morganocin 174.

    abstract::Morganocin 174-induced lethality was characterized by one-hit kinetics. Although it induced simultaneous inhibition of deoxyribonucleic acid, ribonucleic acid, and protein syntheses, the most striking effect of morganocin was a rapid reduction of intracellular adenosine 5'-triphosphate to less than 10% of the initial ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.12.3.395

    authors: Williams JA,Krizsanovich-Williams K

    更新日期:1977-09-01 00:00:00

  • Antimicrobial and antileishmanial activities of hypocrellins A and B.

    abstract::Hypocrellins A and B were evaluated for in vitro antimicrobial and antileishmanial activities. Hypocrellin A exhibited promising activity against Candida albicans and moderate activity against Staphylococcus aureus, methicillin-resistant S. aureus, Pseudomonas aeruginosa, and Mycobacterium intracellulare. Hypocrellin ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.48.11.4450-4452.2004

    authors: Ma G,Khan SI,Jacob MR,Tekwani BL,Li Z,Pasco DS,Walker LA,Khan IA

    更新日期:2004-11-01 00:00:00

  • In vitro susceptibilities of isolates of Haemophilus ducreyi from Thailand and the United States to currently recommended and newer agents for treatment of chancroid.

    abstract::We determined the in vitro susceptibilities of 54 isolates of Haemophilus ducreyi from Thailand (29 isolates) and San Francisco (25 isolates) to penicillin G, tetracycline, amoxicillin-clavulanic acid, ceftriaxone, cefixime, erythromycin, azithromycin, ciprofloxacin, ofloxacin, and trimethoprim-sulfamethoxazole. Isola...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.37.7.1552

    authors: Knapp JS,Back AF,Babst AF,Taylor D,Rice RJ

    更新日期:1993-07-01 00:00:00

  • Piperacillin plus vancomycin in the therapy of febrile episodes in cancer patients.

    abstract::Piperacillin and vancomycin were used as initial empirical therapy for 211 febrile episodes in cancer patients. The response rate in 95 episodes of documented infection was 72%. The response of bacteremias, soft tissue infections, and pneumonias was 78, 71, and 38%, respectively. The response in infections caused by g...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.26.3.295

    authors: Jadeja L,Bolivar R,Fainstein V,Keating M,McCredie K,Hay M,Bodey GP

    更新日期:1984-09-01 00:00:00

  • Characterization of a novel AmpC β-lactamase produced by a carbapenem-resistant Cedecea davisae clinical isolate.

    abstract::A Cedecea davisae isolate, which was intermediate or resistant to third-generation cephalosporins and carbapenems, was recovered from a urine sample. Susceptibility testing, isoelectric focusing, and analysis of outer membrane proteins showed that AmpC β-lactamase expression combined with porin deficiency accounted fo...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.03237-14

    authors: Ammenouche N,Dupont H,Mammeri H

    更新日期:2014-11-01 00:00:00

  • In Vitro Activity of Retapamulin and Antimicrobial Susceptibility Patterns in a Longitudinal Collection of Methicillin-Resistant Staphylococcus aureus Isolates from a Veterans Affairs Medical Center.

    abstract::Mupirocin is a topical antimicrobial used to decolonize patients who carry methicillin-resistant Staphylococcus aureus (MRSA), and the topical agent retapamulin may be a potential alternative therapy. The goal of this study was to determine the in vitro activity of retapamulin as well as a panel of 15 antimicrobial ag...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01568-15

    authors: Harrington AT,Black JA,Clarridge JE 3rd

    更新日期:2015-12-14 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

  • Serum bactericidal activity of rifampin in combination with other antimicrobial agents against Staphylococcus aureus.

    abstract::Because rifampin-resistant strains of Staphylococcus aureus emerge during monotherapy with this drug, a search was made for potentially useful companion drugs. Bactericidal titers of spiked serum were determined, and time kill studies were performed for 10 strains of methicillin-susceptible S. aureus. We tested rifamp...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.29.4.611

    authors: Hackbarth CJ,Chambers HF,Sande MA

    更新日期:1986-04-01 00:00:00

  • Novel mutations in reverse transcriptase of human immunodeficiency virus type 1 reduce susceptibility to foscarnet in laboratory and clinical isolates.

    abstract::Foscarnet (phosphonoformic acid) is a pyrophosphate analog that inhibits the replication of human immunodeficiency virus type 1 (HIV-1) in vitro and in patients with AIDS. HIV-1 resistance to foscarnet has not been reported despite long-term foscarnet therapy of AIDS patients with cytomegalovirus disease. We therefore...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.39.5.1087

    authors: Mellors JW,Bazmi HZ,Schinazi RF,Roy BM,Hsiou Y,Arnold E,Weir J,Mayers DL

    更新日期:1995-05-01 00:00:00

  • Novel strategy for biofilm inhibition by using small molecules targeting molecular chaperone DnaK.

    abstract::Biofilms are complex communities of microorganisms that attach to surfaces and are embedded in a self-produced extracellular matrix. Since these cells acquire increased tolerance against antimicrobial agents and host immune systems, biofilm-associated infectious diseases tend to become chronic. We show here that the m...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.04465-14

    authors: Arita-Morioka K,Yamanaka K,Mizunoe Y,Ogura T,Sugimoto S

    更新日期:2015-01-01 00:00:00

  • Olorofim Susceptibility Testing of 1,423 Danish Mold Isolates Obtained in 2018-2019 Confirms Uniform and Broad-Spectrum Activity.

    abstract::Olorofim is a novel antifungal drug in phase 2 trials. It has shown promising in vitro activity against various molds, except for Mucorales. Initially, we observed a broad range of EUCAST MICs for Aspergillus fumigatus Here, we explored the MIC variability in more detail and prospectively investigated the susceptibili...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01527-20

    authors: Astvad KMT,Jørgensen KM,Hare RK,Datcu R,Arendrup MC

    更新日期:2020-12-16 00:00:00

  • Antimicrobial-related severe adverse events during treatment of bone and joint infection due to methicillin-susceptible Staphylococcus aureus.

    abstract::Prolonged antimicrobial therapy is recommended for methicillin-susceptible Staphylococcus aureus (MSSA) bone and joint infections (BJI), but its safety profile and risk factors for severe adverse events (SAE) in clinical practice are unknown. We addressed these issues in a retrospective cohort study (2001 to 2011) ana...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02032-13

    authors: Valour F,Karsenty J,Bouaziz A,Ader F,Tod M,Lustig S,Laurent F,Ecochard R,Chidiac C,Ferry T,Lyon BJI Study Group.

    更新日期:2014-01-01 00:00:00

  • Development and Characterization of Monoolein-Based Liposomes of Carvacrol, Cinnamaldehyde, Citral or Thymol with anti-Candida Activities.

    abstract::There is an increasing need for novel drugs and new strategies for the therapy of invasive candidiasis. This study aimed to develop and characterize liposome-based nanoparticles of carvacrol, cinnamaldehyde, citral or thymol with anti-Candida activities. Dioctadecyldimethylammonium bromide- and monoolein-based liposom...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01628-20

    authors: Miranda-Cadena K,Dias M,Costa-Barbosa A,Collins T,Marcos-Arias C,Eraso E,Pais C,Quindós G,Sampaio P

    更新日期:2021-01-19 00:00:00

  • CTX-M-2 and a new CTX-M-39 enzyme are the major extended-spectrum beta-lactamases in multiple Escherichia coli clones isolated in Tel Aviv, Israel.

    abstract::The rate of occurrence of the extended-spectrum beta-lactamase (ESBL)-producing phenotype among Escherichia coli isolates in Tel Aviv is 12% (22). The aim of this study was to understand the molecular epidemiology of E. coli ESBL producers and to identify the ESBL genes carried by them. We studied 20 single-patient ES...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.49.11.4745-4750.2005

    authors: Chmelnitsky I,Carmeli Y,Leavitt A,Schwaber MJ,Navon-Venezia S

    更新日期:2005-11-01 00:00:00

  • Characterization of bactericidal activity of clindamycin against Bacteroides fragilis via kill curve methods.

    abstract::Kill curves were determined for five isolates of Bacteroides fragilis with clindamycin at concentrations equal to the MIC or to 4, 16, and 64 times the MIC. Examination of plots of log CFU per milliliter versus time revealed no association between the clindamycin concentration and the rate and extent of the bactericid...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.40.8.1941

    authors: Klepser ME,Banevicius MA,Quintiliani R,Nightingale CH

    更新日期:1996-08-01 00:00:00

  • In vitro susceptibility of Clostridium difficile isolates from patients with antibiotic-associated diarrhea or colitis.

    abstract::In vitro susceptibility tests were performed on 84 strains of Clostridium difficile to 11 antimicrobial agents. All isolates were from the stools of patients with antibiotic-associated diarrhea or colitis in which there was a cytopathic toxin that was neutralized by Clostridium sordellii antitoxin. Over 95% of the str...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.17.4.695

    authors: Dzink J,Bartlett JG

    更新日期:1980-04-01 00:00:00

  • Characterization of an integron carrying blaIMP-1 and a new aminoglycoside resistance gene, aac(6')-31, and its dissemination among genetically unrelated clinical isolates in a Brazilian hospital.

    abstract::Seven bla(IMP-1)-harboring Acinetobacter sp. isolates and one Pseudomonas putida clinical isolate were recovered from hospitalized patients. All isolates possessed a class 1 integron, named In86, carrying the same cassette array [bla(IMP1), aac(6')-31, and aadA1], which was plasmid located in five of the isolates. Thi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00838-06

    authors: Mendes RE,Castanheira M,Toleman MA,Sader HS,Jones RN,Walsh TR

    更新日期:2007-07-01 00:00:00

  • Toxicological profile and pharmacokinetics of a unilamellar liposomal vesicle formulation of amphotericin B in rats.

    abstract::AmBisome (ABLP) is a unilamellar liposomal preparation of amphotericin B that has demonstrated an improved safety profile compared to conventional amphotericin B. Single- and multiple-dose pharmacokinetics were determined by using noncompartmental methods for rats administered ABLP at 1, 3, 9, and 20 mg/kg/day. The to...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:

    authors: Boswell GW,Bekersky I,Buell D,Hiles R,Walsh TJ

    更新日期:1998-02-01 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

  • Propagation of TEM- and PSE-type beta-lactamases among amoxicillin-resistant Salmonella spp. isolated in France.

    abstract::A survey conducted between 1987 and 1994 at the University Hospital of Besançon, France, demonstrated a dramatic increase (from 0 to 42. 5%) in the prevalence of amoxicillin resistance among Salmonella spp. Of the 96 resistant isolates collected during this period (including 77 Typhimurium), 54 were found to produce T...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.43.10.2430

    authors: Llanes C,Kirchgesner V,Plesiat P

    更新日期:1999-10-01 00:00:00