Pharmacokinetics of ertapenem in colorectal tissue.

Abstract:

BACKGROUND:There are only limited data on tissue kinetics of ertapenem in colorectal tissue more than 3 h after administration of the drug. The purpose of this study was to assess the pharmacokinetics (PK) of ertapenem in colorectal tissue via population PK modeling. PATIENTS AND METHODS:Patients ≥18 years requiring surgical intervention at the colon and/or rectum were eligible (ClinicalTrials.gov identifier: NCT 00535652). Tissue and blood samples were taken during surgery after a single dose of 1 g ertapenem. Ertapenem concentration was determined by high-performance liquid chromatography/mass spectrometry. Population PK modeling was performed in S-ADAPT. RESULTS:Twenty-three patients were enrolled. The highest tissue concentration was 6.4 ± 2.3 mg/kg, the highest total plasma concentration 51.34 ± 9.4 mg/l, the highest unbound plasma concentration 7.05 ± 1.1 mg/l, and the unbound fraction in plasma was 14-15% for total ertapenem concentrations below approximately 22 mg/l, 19% at 100 mg/l, and 25% at 250 mg/l. The estimated geometric mean terminal half-life was 2.5 h for plasma and tissue. In the Monte Carlo simulation, a single dose of 1,000 mg ertapenem achieved robust (≥90%) probabilities of target attainment up to a minimum inhibitory concentration (MIC) of approximately 2 mg/l for the bacteriostasis target (free time above MIC, fT(>)(MIC) = 20%) and up to 0.25-0.5 mg/l for the near-maximal killing target (40% fT(>)(MIC)). CONCLUSION:Our data indicate an adequate penetration of ertapenem into uninfected colorectal tissue up to 8.5 h (35% of the dosing interval) after administration of 1 g intravenously.

journal_name

Chemotherapy

journal_title

Chemotherapy

authors

Wittau M,Scheele J,Bulitta JB,Mayer B,Kaever V,Burhenne H,Henne-Bruns D,Isenmann R,Brockschmidt C

doi

10.1159/000333377

subject

Has Abstract

pub_date

2011-01-01 00:00:00

pages

437-48

issue

5

eissn

0009-3157

issn

1421-9794

pii

000333377

journal_volume

57

pub_type

杂志文章
  • Penetration of latamoxef, cefoperazone and piperacillin into the sputum of patients with cystic fibrosis.

    abstract::Concentrations of latamoxef, cefoperazone and piperacillin, administered intravenously, were measured in serum and sputum of cystic fibrosis patients with recurrent pulmonary infections, chronically colonized with Pseudomonas aeruginosa. Serum pharmacokinetic data were consistent with prior reports. Peak sputum to pea...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000238344

    authors: Laferriere C,Stutman HR,Marks MI,Kramer J,Flux M

    更新日期:1985-01-01 00:00:00

  • Analytical studies on beta-lactam antibiotics. II. Displacement effect of beta-lactam antibiotics on bilirubin bound to human serum albumin.

    abstract::We established a method for determining the KD value as a measure of the bilirubin-displacing effect for drugs by using bilirubin oxidase, which is produced by Myrothecium verrucaria MT-1. This method makes it possible to conduct measurements of many beta-lactam antibiotics, including those which could not be determin...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000238590

    authors: Matsuura A,Nagayama T,Kitagawa T

    更新日期:1988-01-01 00:00:00

  • Sensitivity of clinical isolates from German hospitals to amoxicillin/clavulanic acid (Augmentin) compared with other antibiotics.

    abstract::17,244 pathogens isolated from clinical specimens of 24 hospitals in the Moers area (North-Rhine Westphalia, FRG) were tested in regard to their susceptibility to Augmentin (amoxicillin and clavulanic acid). For this purpose, minimal inhibitory concentrations were determined by use of microbroth dilution technique. 80...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000238588

    authors: Focht J,Klietmann W,Nösner K,Rolinson GN,Johnsen J

    更新日期:1988-01-01 00:00:00

  • Antibacterial effects of niridazole. I. Effect on infection of mice with Salmonella typhimurium.

    abstract::Niridazole was shown to be an effective chemotherapeutic agent for mice infected intravenously with a niridazole-sensitive strain of Salmonella typhimurium. Death rates as well as bacterial counts per spleen were reduced, even in compromised animals. Histologic examination of spleens proved the reduction of inflammato...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000238069

    authors: Hof H,Müller KM,Heine WD

    更新日期:1982-01-01 00:00:00

  • In vitro activity of A-56619 and A-56620 against multi-resistant and routine clinical isolates.

    abstract::A-56619 and A-56620 are two new quinolone compounds that are currently being studied. They were found to be active against multi-resistant and routine isolates of Staphylococcus aureus, enterobacteria, aminoglycoside-sensitive and resistant strains of Pseudomonas aeruginosa. Most of the enterobacteria were inhibited b...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000238573

    authors: Fernandes CJ,Wilson RD,Ackerman VP

    更新日期:1988-01-01 00:00:00

  • A Difference in the Incidences of Hypersensitivity Reactions to Original and Generic Taxanes.

    abstract:PURPOSE:To compare incidences of hypersensitivity reaction (HSR) between original and generic taxanes including paclitaxel and docetaxel. METHODS:We conducted a prospective study enrolling all patients receiving taxanes at King Chulalongkorn Memorial Hospital. Taxanes were infused accordingly to the step-wise rate esc...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000450748

    authors: Ratanajarusiri T,Sriuranpong V,Sitthideatphaiboon P,Poovoravan N,Vinayanuwat C,Parinyanitikul N,Angspatt P,Thawinwisan W,Tanasanvimon S

    更新日期:2017-01-01 00:00:00

  • Efficacy of S-1 for patients with peritoneal metastasis of gastric cancer.

    abstract:BACKGROUND:This study was designed to examine the efficacy and compliance of S-1 for the patients with peritoneal metastasis of gastric cancer. METHODS:Sixteen consecutive patients with peritoneal metastasis of gastric cancer were treated with S-1. Their survival was compared with that of the historical control group ...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000096002

    authors: Ishizone S,Maruta F,Saito H,Koide N,Sugiyama A,Nakayama J,Miyagawa S

    更新日期:2006-01-01 00:00:00

  • Correlation between growth curves and killing curves of Escherichia coli in the presence of fleroxacin and ampicillin.

    abstract::Fleroxacin, a new long-acting quinolone, induces rapid killing and bacterial filamentation as do other quinolones. Ten strains of Escherichia coli were exposed comparatively to fleroxacin and ampicillin in order to determine the effect of sub- and supra-inhibitory concentrations of each of these two compounds on turbi...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000238706

    authors: Yourassowsky E,Van der Linden MP,Crokaert F

    更新日期:1989-01-01 00:00:00

  • Effect of probenecid on the pharmacokinetics of DQ-2556, a new 3-quaternary ammonium cephalosporin antibiotic, in humans.

    abstract::A total of 5 healthy volunteers were enrolled in a crossover study on the dose dependency and the effect of probenecid on pharmacokinetics of DQ-2556. They were administered intravenously 0.5 and 1.0 g of DQ-2556, and 1.0 g of DQ-2556 with oral administration of probenecid. The linearity in pharmacokinetics of DQ-2556...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000239029

    authors: Shiba K,Yoshida M,Shimada J,Saito A,Matsubayashi K,Hashimoto S,Yoshida K,Osada Y,Sakai O

    更新日期:1992-01-01 00:00:00

  • Fosfomycin trometamol versus norfloxacin in the treatment of uncomplicated lower urinary tract infections of the elderly.

    abstract::Ten years of controlled clinical trials supported single-dose therapy efficacy and safety in uncomplicated lower urinary tract infections (UTI). Both local and systematic factors contribute to the high UTI prevalence seen in elderly people. A controlled open randomized study was undertaken to evaluate the clinical eff...

    journal_title:Chemotherapy

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1159/000238817

    authors: Ferraro G,Ambrosi G,Bucci L,Palmieri R,Palmieri G

    更新日期:1990-01-01 00:00:00

  • Micro test for assaying sensitivity of Plasmodium vivax in vitro.

    abstract::A modified Rieckmann test was developed for assessing chloroquine sensitivity of Plasmodium vivax strains. This test envisages the evaluation of parasite growth with different concentrations of the drug and its comparison with controls, at the end of a 48-hour experimental period. Using this test, 16 strains were asse...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000238664

    authors: Renapurkar DM,Pradhan VR,Sutar NK,Deshmukh RA,Pandit CH,Marathe SN

    更新日期:1989-01-01 00:00:00

  • In vitro activity of BMY-28142, a new cephalosporin.

    abstract::BMY-28142 was compared in vitro with ceftazidime, cefotaxime and cefoperazone and was found to be more active against Pseudomonas aeruginosa and Staphylococcus aureus. Essentially no effect of increasing inoculum size 100-fold was seen-on MICs with BMY-28142 or ceftazidime; some effect was noted with cefotaxime and ce...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000238470

    authors: Norden CW,Neiderriter K

    更新日期:1987-01-01 00:00:00

  • Mutant prevention concentration of isoniazid, rifampicin and rifabutin against Mycobacterium tuberculosis.

    abstract:BACKGROUND:Mutant prevention concentration (MPC) is a new parameter that may be of aid in determining the risk of resistant mutants being selected. METHODS:The MPCs of 224 Mycobacterium tuberculosis clinical isolates were estimated by plating more than 10(10) cells on drug-containing agar and determining the concentra...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000085613

    authors: Rodríguez JC,Cebrián L,Ruiz M,López M,Royo G

    更新日期:2005-05-01 00:00:00

  • Thyroid tuberculosis: diagnosis and treatment.

    abstract:OBJECTIVE:It was the aim of this study to report clinical characteristics and treatment of thyroid tuberculosis (TT). METHODS:During 16 years, 2,426 patients have been operated on the thyroid in the surgical department 'A' in Ibn Sina Hospital, Rabat, Morocco. Anatomopathological results of the removed thyroid were an...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000090244

    authors: El Malki HO,Mohsine R,Benkhraba K,Amahzoune M,Benkabbou A,El Absi M,Ifrine L,Belkouchi A,Balafrej S

    更新日期:2006-01-01 00:00:00

  • Visualization of doxycycline in lung tissue and sinus secretions by fluorescent techniques.

    abstract::The two studies which are reviewed in this paper demonstrate the value of fluorescent microscopic observations in the studying of the distribution of antibiotics in lung tissue and in sinus secretions. In the lung tissue study, the standard microbiologic assay data on doxycycline concentrations in respiratory tissue t...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000221889

    authors: Liss RH,Norman JC

    更新日期:1975-01-01 00:00:00

  • Acute infantile pneumonopathies treated with fosfomycin.

    abstract::Reference is made to the results obtained in 24 children, from 11 months to 12 years, affected with acute pneumopathies and treated with fosfomycin with a dosage of 200 mg/kg/day. In all cases a clinical, radiological, biological and bacteriological study was carried out. At the same time, levels of fosfomycin in plas...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000222069

    authors: Llorens J,Ley G,Forés A,Olay T

    更新日期:1977-01-01 00:00:00

  • No Therapeutic Effect of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor Retreatment Despite T790M Disappearance: Case Report of 3 Cases.

    abstract:BACKGROUND:T790M is a major cause of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) resistance, but the clinical significance of T790M disappearance is unknown. CASE REPORT:We report 3 cases of pulmonary adenocarcinoma which did not respond to EGFR-TKI retreatment even with T790M disappearance...

    journal_title:Chemotherapy

    pub_type:

    doi:10.1159/000491937

    authors: Kodama T,Watanabe K,Shinkai M,Kaneko T

    更新日期:2018-01-01 00:00:00

  • Cost-effectiveness of ceftriaxone and amikacin as single daily dose for the empirical management of febrile granulocytopenic children with cancer.

    abstract::In children undergoing anticancer chemotherapy, a granulocytopenic febrile episode is a life-threatening condition. Prompt initiation of empirical broad-spectrum antibiotics is essential to limit morbidity and mortality. To evaluate the cost-effectiveness of combination antibiotics consisting of a third generation cep...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000239590

    authors: Pession A,Prete A,Paolucci G

    更新日期:1997-09-01 00:00:00

  • Biochemical and pharmacological effects of mitoxantrone and acetyl-L-carnitine in mice with a solid form of Ehrlich tumour.

    abstract:BACKGROUND:Dysfunction of the carnitine system in non-tumour tissue following anticancer therapy has been reported. In this setting, supplementation with carnitine derivatives might increase the general metabolic activity of normal cells so that they might better withstand the adverse effects of chemotherapy aimed at t...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000321296

    authors: Niang M,Soukup T,Zivný P,Tomšík P,Bukač J,Rezáčová M,Stoklasová A,Cerman J,Sišpera L

    更新日期:2011-01-01 00:00:00

  • Tapering and discontinuation of glucocorticoid prophylaxis during prolonged weekly to biweekly paclitaxel administration.

    abstract:BACKGROUND:Taxanes cause hypersensitivity reactions, averted by premedication with H1 blockers and high glucocorticoid (GC) doses. Prolonged weekly taxane administration may lead to GC toxicity. PURPOSE:To determine whether patients not hypersensitive to initial paclitaxel (PTX) infusion after high-dose GC premedicati...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000085618

    authors: Braverman AS,Rao S,Salvatti ME,Adamson B,McManus M,Pierre S

    更新日期:2005-05-01 00:00:00

  • Changes in serum erythropoietin levels during chemotherapy for lung cancer.

    abstract::Serial serum erythropoietin (EPO) levels were measured in 12 adult lung cancer patients during cancer chemotherapy. In major cases, EPO levels increased significantly after chemotherapy while the hemoglobin (Hb) remained at initial levels. EPO fell gradually or rapidly to initial levels after a peak, although the pati...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000239014

    authors: Saijo Y,Nakai Y,Saito J,Sugawara S,Suzuki S,Numata Y,Motomiya M

    更新日期:1992-01-01 00:00:00

  • Association between antibiotic resistance and the expression of Dr adhesin among uropathogenic Escherichia coli.

    abstract:BACKGROUND:Urinary tract infections (UTIs) are a significant health problem and Escherichia coli has been exported to be the primary pathogen in approximately 80% of cases. E. coli express structures called adhesins, fimbriae or pili that help them bind to specific tissue receptors. One such adhesin is Dr, which binds ...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000048507

    authors: Kachroo BB

    更新日期:2001-03-01 00:00:00

  • Mammary tumor and melanoma cell transport of PTT.119, a bis-(2-chloroethyl)amino-L-phenylalanine derivative with carrier amino acids.

    abstract::Uptake of the bifunctional alkylating agent, PTT.119, p-F-Phe-m-bis-(2-chloroethyl)amino-L-Phe-Met-ethoxy-HCl, by the MJY-alpha mammary tumor and B16 melanoma cell lines occurred via two natural pathways for amino acid transport. The primary route of PTT.119 entry was the classical L System, whereas, the ASC System ca...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000238549

    authors: Yagi MJ,Scanlon KJ,Chin SE,Bekesi JG

    更新日期:1988-01-01 00:00:00

  • Phase II trial of XELOX as first-line treatment for patients with advanced gastric cancer.

    abstract:BACKGROUND:The prognosis of patients with advanced gastric cancer (AGC) remains poor, and no single chemotherapy regimen is recognized as a global standard. A phase II trial was conducted to determine the efficacy and tolerability of capecitabine and oxaliplatin (XELOX) given every 3 weeks in combination in patients wi...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000305256

    authors: Luo HY,Xu RH,Wang F,Qiu MZ,Li YH,Li FH,Zhou ZW,Chen XQ

    更新日期:2010-01-01 00:00:00

  • Comparative antibacterial activity of the penem ALP 201.

    abstract::The minimum inhibitory concentration (MIC) of the new penem ALP 201 was tested against 243 recent clinical isolates of which 95 were from the family Enterobacteriaceae, 50 were from the genus Streptococcus, 50 were Staphylococcus aureus and 48 were Staphylococcus epidermidis. An agar dilution technique was used to det...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000238888

    authors: Bergan T,da Fonseca J

    更新日期:1991-01-01 00:00:00

  • Population pharmacokinetics of a novel histone deacetylase inhibitor, cyclo{(2S)-2-amino-8-[(aminocarbonyl)hydrazono] decanoyl-1-L-tryptophyl-L-isoleucyl-(2R)-2-piperidinecarbonyl} (SD-2007), and its metabolic conversion to apicidin after intravenous inje

    abstract:BACKGROUND:This study assessed the population pharmacokinetics and metabolic conversion of a novel histone deacetylase (HDAC) inhibitor, SD-2007, into its active metabolite, apicidin, in rats. METHODS:SD-2007 was given to rats by intravenous injection (4 mg/kg) and oral administration (40 mg/kg). Serum concentrations ...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000328027

    authors: Shin BS,Bulitta JB,Hong DK,Kim HY,Kim MK,Choi Y,Lee JB,Hwang SW,Lee MH,Yoo SD

    更新日期:2011-01-01 00:00:00

  • Combined effects of S-1, a new form of oral tegafur, plus modulators on ovarian cancer in nude rats.

    abstract::We evaluated the efficacy of S-1 as a new oral antitumor agent in ovarian cancer-bearing nude rats. This drug consists of tegafur, 5-chloro-2,4-dihydroxypyridine, and oxonic acid in a molar ratio of 1:0.4:1.S-1 was given alone or in combination with cisplatin. When administered alone at a daily dose of 20 mg/ kg, S-1 ...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000239479

    authors: Suzuki M,Sekiguchi I,Sato I,Shirasaka T

    更新日期:1996-11-01 00:00:00

  • Effects of isoniazid on viability, cell morphologies and acid fastness properties of Mycobacterium avium NCTC 8559 during the growth cycle.

    abstract::Our previous study demonstrated that the effects of isoniazid (INH) on Mycobacterium tuberculosis at the cellular level varied according to the growth phases. In this study, the variations in the INH action on M. avium strain NCTC 8559 are reported. M. avium cells grown on Middlebrook 7H10 agar were harvested at diffe...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000104470

    authors: Mohamad S,Ibrahim P,Wahab HA

    更新日期:2007-01-01 00:00:00

  • Studies with cefuroxime: a new beta-lactamase resistant cephalosporin.

    abstract::28 patients suffering from a variety of bacterial infections have been treated with cefuroxime. 18 were cured and 6 improved during treatment. Side effects were minimal and intramuscular injection was well tolerated. Serum and urine levels well in excess of the MICs of sensitive organisms were obtained using dosages o...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000237842

    authors: Ball AP,Brookes GR,Farrell ID,Geddes AM,Gould I

    更新日期:1979-01-01 00:00:00

  • Broad spectrum antiviral fractions from the lichen Ramalina farinacea (L.) Ach.

    abstract:BACKGROUND:An ethylacetate-soluble fraction (ET4) from the lichen Ramalina farinacea has previously been shown to inhibit the infectivity of lentiviral and adenoviral vectors, as well as wild-type HIV-1. We now determined the antiviral activity of ET4 against other wild-type viruses, including the herpes simplex virus ...

    journal_title:Chemotherapy

    pub_type: 杂志文章

    doi:10.1159/000194974

    authors: Esimone CO,Grunwald T,Nworu CS,Kuate S,Proksch P,Uberla K

    更新日期:2009-01-01 00:00:00