The disposition and metabolic fate of<sup>14</sup>C-meropenem in man

Harrison, M.; Haworth, Stephen J.; Moss, S. R.; Wilkinson, Diane; Featherstone, A.

doi:10.3109/00498259309059441

Cited by 35 publications

(20 citation statements)

References 11 publications

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“…These carbapenems share generally dose-proportional pharmacokinetics over marketed dose ranges and a short elimination half-life of approximately 1 h. Ertapenem differs, with a high level of protein binding and consequently a nonlinear pharmacokinetic profile and a longer half-life than that of doripenem (Ivanz [ertapenem for injection] U.S. prescribing information; Merck & Co. Inc., February 2008). The disposition of doripenem, reported in this study, is comparable to that of other carbapenems, including imipenem/ cilastatin, meropenem, and ertapenem (4,8,16,18; U.S. prescribing information for Ivanz). The total radioactivity of doripenem in plasma paralleled the plasma carbapenem concentration shortly after infusion of a 14 C-labeled carbapenem.…”

Section: Discussionmentioning

confidence: 48%

Disposition, Metabolism, and Excretion of [ ¹⁴ C]Doripenem after a Single 500-Milligram Intravenous Infusion in Healthy Men

Cirillo

Mannens

Janssen

et al. 2008

Antimicrob Agents Chemother

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In this open-label, single-center study, eight healthy men each received a single 500-mg dose of Doripenem is a new parenteral carbapenem antibiotic with broad-spectrum activity against gram-negative and gram-positive pathogens, including strains resistant to multiple antibiotic classes (1, 6, 7). It is indicated for adults in the treatment of complicated intra-abdominal infections and complicated urinary tract infections, including pyelonephritis. Doripenem exhibits in vitro activity against contemporary strains of gram-negative bacteria that are often responsible for serious, hospital-acquired infections, including Pseudomonas aeruginosa and extended-spectrum betalactamase-and AmpC beta-lactamase-producing Enterobacteriaceae (10-12, 15, 19). In addition, doripenem is less likely than meropenem or imipenem to select for carbapenem-resistant strains of Pseudomonas aeruginosa (17). Because carbapenems produce time-dependent bactericidal activity, the ability to deliver doripenem via prolonged infusion increases the time that drug concentrations are likely to remain above the MIC for the infecting pathogen (2, 5). This may be of critical importance for difficult-to-treat pathogens that are not susceptible to other carbapenems or for which the MICs are near the susceptibility limits of the drug.The present study was designed to characterize the disposition, metabolism, and excretion of doripenem in healthy men following a single 500-mg dose administered as a 1-h intravenous infusion, which is the standard doripenem dose indicated for treatment of subjects with serious bacterial infections. On the basis of clinical-trial data, the proposed dose of doripenem for treatment of moderate to severe infections is 500 mg administered by a 1-h or 4-h infusion (C. Lucasti, A. Jasovich, O. Umeh, J. Jiang, and K. Kaniga, presented at the 17th European Congress of Clinical Microbiology and Infectious Diseases, 2007; O. Malafaia, O. Umeh, and J. Jang, presented at the 46th Interscience Conference on Antimicrobial Agents and Chemotherapy, 2006; K. Naber, R. Redman, P. Kotey, L. Lorens, and K. Kaniga, presented at the 17th European Congress of Clinical Microbiology and Infectious Diseases, 2007). MATERIALS AND METHODSThe study protocol was reviewed and approved by an independent ethics committee. The study was conducted in accordance with the ethical principles of the Declaration of Helsinki and in compliance with good clinical practices and all applicable regulatory requirements. All subjects participating in the study provided written informed consent.Subjects. Eight healthy men characterized by a screening physical examination, medical history, vital signs, 12-lead electrocardiogram, laboratory testing, and normal renal function were enrolled. The study cohort had a median age of 20.5 years (range, 18 to 45 years), a median weight of 87.5 kg (range, 55 to 93 kg), and a median body mass index of 22.9 kg/m 2 (range, 19 to 28 kg/m 2 ); all were Caucasian. Eligible patients had not smoked for at least 6 months and agreed to refrain ...

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Section: Discussionmentioning

confidence: 48%

Disposition, Metabolism, and Excretion of [ ¹⁴ C]Doripenem after a Single 500-Milligram Intravenous Infusion in Healthy Men

Cirillo

Mannens

Janssen

et al. 2008

Antimicrob Agents Chemother

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“…[13] Most of the antibiotics used for treatment in this study are mainly eliminated via the urinary tract, and the amount of antibiotics found in faeces is often low (approximately 1-5%) [14][15][16][17][18][19]. An exception to this in our study is ertapenem where about 10% of the dose is found in the faeces [20].…”

Section: Discussioncontrasting

confidence: 46%

Changes in the aerobic faecal flora of patients treated with antibiotics for acute intra-abdominal infection

Samuelsson

Isaksson

Chabok

et al. 2012

Scandinavian Journal of Infectious Diseases

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Background: An open observational study was performed to investigate changes in the rectal flora and antibiotic susceptibility among faecal bacteria in patients treated with antibiotics for acute intra-abdominal infection. Methods: One hundred and forty patients with acute intra-abdominal infection requiring antibiotic treatment and hospitalization were included. Eight surgical units from the southern part of Sweden participated, between January 2006 and November 2007. Antibiotic treatments were according to local guidelines. Rectal swabs were obtained on admission (sample 1) and 2-14 days after the end of antibiotic treatment (sample 2). Aerobic bacteria and yeasts were analysed. The material was divided into 2 groups: 1 group with Enterobacteriaceae and 1 group with non-fermentative Gram-negative bacteria. The susceptibility to antibiotics in each group was compared between samples 1 and 2. Results: The main finding of this study on patients with severe intra-abdominal infections was a shift in the aerobic faecal flora following antibiotic treatment, from Escherichia coli to other more resistant Enterobacteriaceae, Enterococcus faecium, and yeasts. The susceptibility to cephalosporins and piperacillin-tazobactam decreased in Enterobacteriaceae. Conclusions: Following antibiotic treatment, a shift in the aerobic rectal flora to species with intrinsic antibiotic resistance was observed. This indicates that the emergence of resistance is not due to new mutations, but rather to selection of more resistant species. This should be taken into account when designing treatments for secondary intra-abdominal infections

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“…Further increasing the pH of the buffer solution caused the reduction peak current to decrease. Furthermore, within the pH range of 2.0 to 6.0, the reduction peak potential increased gradually, whereas from 6.0 to 8.0 it decreased gradually, indicating a low electron transfer rate [22].…”

Section: Effect Of Phmentioning

confidence: 99%

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Harrison et al [22] studied the metabolism of meropenem and *Corresponding author: Sreedhar NY, Electroanalytical Lab, Department of Chemistry, Sri Venkateswara University, Tirupati-517502, Andhra Pradesh, India, Tel: +91-9440087124; E-mail: sreedharny.chem@gmail.com

AbstractThe theme of this study was the preparation, characterization, and application of a polyaniline (PAN) and graphene composite modified glassy carbon electrode (PAN/Gr/GCE) for the voltammetric determination of doripenem (DPM) and meropenem metabolites (MPM) in human urine and serum samples. The morphological study of the PAN/ Gr/GCE composite was examined by scanning electron microscopy (SEM) and cyclic voltammetry (CV).

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confidence: 99%

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Graphene and Polyaniline Composite Modified Glassy Carbon Electrode for Electrochemical Determination of Doripenem and Meropenem Metabolites

Sivaprasad¹

2014

J Anal Bioanal Tech

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Harrison et al. [22] studied the metabolism of meropenem and *Corresponding author: Sreedhar NY, Electroanalytical Lab, Department of Chemistry, Sri Venkateswara University, Tirupati-517502, Andhra Pradesh, India, Tel: +91-9440087124; E-mail: sreedharny.chem@gmail.com AbstractThe theme of this study was the preparation, characterization, and application of a polyaniline (PAN) and graphene composite modified glassy carbon electrode (PAN/Gr/GCE) for the voltammetric determination of doripenem (DPM) and meropenem metabolites (MPM) in human urine and serum samples. The morphological study of the PAN/ Gr/GCE composite was examined by scanning electron microscopy (SEM) and cyclic voltammetry (CV). The electrochemical behaviour of DPM and MPM at the PAN/Gr/GCE were investigated using cyclic voltammetry in Ag/ AgCl/KCl supporting electrolyte at pH 2.0-10.0 in phosphate buffer solution. The linear dependence of current versus concentration was reached in a wide concentration range from 2.5×10 -7 M to 3.5×10 -4 M using cyclic voltammetry and differential pulse voltammetric methods. In acidic media a non-reversible diffusion controlled reduction involving two protons and two electrons occurs at carbon and nitrogen double bond (C=N) in the metabolites. The best electroanalytical performances of this composite electrode were achieved with the detection limits 3.6×10 -9 M and 1.75×10 -9 M for DPM and MPM respectively. The simplicity of preparation, high sensitivity and stability of this composite electrode should open novel avenues and applications for fabricating robust sensors for detection of DPM and MPM in human urine and serum samples.

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The disposition and metabolic fate of¹⁴C-meropenem in man

Cited by 35 publications

References 11 publications

Disposition, Metabolism, and Excretion of [ ¹⁴ C]Doripenem after a Single 500-Milligram Intravenous Infusion in Healthy Men

Disposition, Metabolism, and Excretion of [ ¹⁴ C]Doripenem after a Single 500-Milligram Intravenous Infusion in Healthy Men

Changes in the aerobic faecal flora of patients treated with antibiotics for acute intra-abdominal infection

Graphene and Polyaniline Composite Modified Glassy Carbon Electrode for Electrochemical Determination of Doripenem and Meropenem Metabolites

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The disposition and metabolic fate of14C-meropenem in man

Cited by 35 publications

References 11 publications

Disposition, Metabolism, and Excretion of [ 14 C]Doripenem after a Single 500-Milligram Intravenous Infusion in Healthy Men

Disposition, Metabolism, and Excretion of [ 14 C]Doripenem after a Single 500-Milligram Intravenous Infusion in Healthy Men

Changes in the aerobic faecal flora of patients treated with antibiotics for acute intra-abdominal infection

Graphene and Polyaniline Composite Modified Glassy Carbon Electrode for Electrochemical Determination of Doripenem and Meropenem Metabolites

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Product

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The disposition and metabolic fate of¹⁴C-meropenem in man

Disposition, Metabolism, and Excretion of [ ¹⁴ C]Doripenem after a Single 500-Milligram Intravenous Infusion in Healthy Men

Disposition, Metabolism, and Excretion of [ ¹⁴ C]Doripenem after a Single 500-Milligram Intravenous Infusion in Healthy Men