Population Pharmacokinetics and Pharmacodynamics of Beta-lactams of Interest in Adult Patients From Intensive Care Units

NCT ID: NCT03440216

Last Updated: 2022-05-25

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

UNKNOWN

Clinical Phase

NA

Total Enrollment

20 participants

Study Classification

INTERVENTIONAL

Study Start Date

2018-03-15

Study Completion Date

2022-12-15

Brief Summary

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Antibiotics are still most often administered on an empiric fashion, as defined for the general population with dosages only adapted based on weight and renal and/or hepatic functions. As a result, serum concentrations show important interpatient variations with the risk of being subtherapeutic or toxic. Recent studies with temocillin, ceftriaxone, or meropenem confirm this for patients in intensive care units.

The aim of the study will be to measure the total and free concentrations of temocillin, ceftriaxone, and meropenem in patients hospitalized in Intensive Care Units for pulmonary infections or another infection for which one of the above mentioned antibiotics is indicated. Patients will be stratified according to the level of their renal function. The antibiotics will be assayed in plasma as well as other accessible fluids in order to assess their pharmacokinetic properties.

Detailed Description

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1. Background, Literature Survey and Justification of The Study

1.1. Introduction

β-lactams efficacy depends primarily from the time interval during which the plasma concentration remains above the minimal inhibitory concentration (MIC) of the antibiotic against the target organism(s) (Craig, 1998). It is generally accepted that the free concentration of the antibiotic must remain above the MIC for at least 40 to 70% of the interval between two successive administrations, and should even reach 100% for severe infections in patients hospitalized in Intensive Care Units (MacGowan, 2011). The free concentration must reach a value of 4 x the MIC for 40 to 70% (Mohd Hafiz et al., 2012) or even 100 % (Tam et al., 2005) of the dosing interval in order to prevent the emergence of resistance.

Due to the large inter- and intraindividual variations between patients, it is difficult to reach the desired concentrations if relying only on usual dosage recommendations and/or using standard dosing regimens. Moreover, Intensive Care patients are difficult patients in this context (Roberts et al., 2014) due to gross perturbations related to underlying diseases and abnormalities (arterial hypertension, cardiac rhythm alterations, renal and/or hepatic insufficiency) and the necessary interventions (artificial ventilation, surgery, artificial feeding, and so on…). They also show important variations in the level of plasma proteins and rapid and unpredictable fluctuations of their renal function (Beumier et al., 2015; Goncalves-Pereira and Povoa, 2011; Roberts and Lipman, 2009), all of which are known to modulate the pharmacokinetics of β-lactams (Goncalves-Pereira and Povoa, 2011; Hayashi et al., 2013; Sime et al., 2012; Udy et al., 2012; Wong et al., 2013). The concentration of the free fraction will be especially modified for those β-lactams with large protein binding such as temocillin or ceftriaxone (Schleibinger et al., 2015; Ulldemolins et al., 2011; Van Dalen et al., 1987; Wong et al., 2013), but may also be altered for β-lactams that are mainly excreted via the renal route (temocillin, ceftriaxone, meropenem) (Carlier et al., 2013; Simon et al., 2006; Vandecasteele et al., 2015).

1.2. Clinical Interest of temocillin, ceftriaxone and meropenem and State of the Art Concerning their dosing

Temocillin is a carboxypenicillin with useful activity against Gram-negative bacteria (excluding P. aeruginosa) and with a large stability towards most β-lactamases, including ESBL), AmpC cephalosporinases, and some carbapenemases (Livermore et al., 2006; Zykov et al., 2016). Temocillin may stand as an alternative to carbapenems (Balakrishnan et al., 2011; Livermore and Tulkens, 2009). About 85% of temocillin in plasma is protein-bound and about 80% of the administered dose is eliminated in 24 h under an intact form by glomerular filtration and tubular secretion (Temocillin Summary of Product Characteristics \[SmPC\], 2015)

Ceftriaxone shows a moderately enlarged spectrum of activity and is stable towards certain β-lactamases but not to ESBLs, AmpC cephalosporinases and certain carbapenemases (Suankratay et al., 2008). It is an alternative to carbapenems when dealing with an infection with susceptible organisms (Paradis et al., 1992). Its protein binding is about 95%, and its elimination is mainly via the renal route (50 to 60% under an unchanged form) with the remaining eliminated via the bile to form microbiologically inactive metabolites (Ceftriaxone SmPC, 2015).

Meropenem shows a very large spectrum and is used in empiric therapy when fearing the presence of ESBL-producing organisms to which other antibiotics are resistant (Zykov et al., 2016). Meropenem has an unpredictable pharmacokinetic profile in patients with renal insufficiency or under hemodialysis (Carlier et al., 2013; Goncalves-Pereira et al., 2014). Meropenem is mainly excreted via the renal route (50 - 75 % under an unchanged form; SmPC meropenem, 2014).

Antibiotic are often prescribed empirically with doses based on what has been found appropriate for the general population, with some adaptation for weight and renal and/or hepatic function. As for any drug, however, there is increasing evidence that the concentrations observed after administration of a standard dose are actually highly variable and often different from the expected ones, leading to risks of sub-therapeutic or toxic effects.

Recent studies have shown that an intravenous administration of 6 g of temocillin by continuous infusion (Laterre et al., 2015), of 4 g of ceftriaxone in two administrations at 12 h interval (Roberts et al., 2007; Salvador et al., 1983), or of 6 g of meropenem in 3 administrations by prolonged infusion (3 h) at 8 h interval (Dulhunty et al., 2013; Frippiat et al., 2015; Jamal et al., 2015), allow to reach free plasma concentrations of 4 x the MIC against susceptible organisms during 40-70%, or even 100% of the dosing interval, with, however, large inter-individual variations, especially for molecules with high protein biding (temocillin, ceftriaxone) due to variations in their renal elimination. Very little information is available about their tissue levels but it is suspected that large inter-individual variations are also frequent.
2. Study Objectives

The goal is to measure the total and free concentrations of the antibiotics in plasma, accessible body fluids and, if possible, tissues after intravenous administration of:
* temocillin: 6 g by continuous infusion over 24 h;
* ceftriaxone: bolus administration of 2 g in a 30 min infusion twice daily;
* meropenem: prolonged infusion (3 h) of 2 g three times daily.

These doses will be adjusted in patients based on their renal function.

Primary objective:

To calculate and assess the values of key pharmacokinetic parameters (total clearance, volume of distribution, constants of elimination, plasma and tissue total exposure, and maximal and minimal plasma and body fluid concentrations.

Secondary objectives:
* the correlation between the plasma protein profile and the actual free antibiotic concentrations;
* the impact of the alterations of the renal function on the free and total plasma concentrations of the antibiotics;
* the impact of the level and nature of circulating proteins on the free fraction of the antibiotics;
* the extent of the tissular penetration of the antibiotics (in accessible samples) and of their penetration in pertinent body fluids (bronchoalveolar lavage, drainage and ascites fluids.
* to model the population pharmacokinetics of the antibiotics in the whole set of patients included in the study;
* to investigate and assess the influence of co-variates (using biometric, biochemical and clinical data) on the variability of the individual pharmacokinetic profiles.
3. Outcome measures

• Primary Outcome Measure: Impact of renal function on total plasma concentrations (Measurement of total plasma antibiotic concentrations)

• Secondary Outcome Measures:
* Impact of the plasma protein concentration and of their nature on the free concentration of antibiotics
* Tissular and fluid penetration of antibiotics (lung tissue, bronchoalveolar lavage, drainage fluids)
* Pharmacokinetic modeling
* Co-variates analysis
4. Conduct of the Study

4.1. Eligible patients

Patients hospitalized in Intensive Care Units and treated for pulmonary or abdominal infection, septicemia, or any other infection calling for the prescription of one of the three antibiotics mentioned above.

4.2. Study groups

Patients will be divided in two groups: :
* Group 1: patients with a glomerular filtration rate (GFR) ≥ 30 mL/min
* Group 2: patients with renal insufficiency or under hemodialysis

4.3. Safety considerations

The three β-lactams have each a long record of safe use in patients hospitalized in Intensive Care Units but may cause an alteration of the commensal flora, allergic reactions, neurotoxicity (at high doses). Ceftriaxone may case hemolytic anemia.

4.4. Exclusion criteria
* Patients of \<18 years
* Allergy to β-lactams
* Hypersensitivity to penicillin (IgE-mediated)
* Any biological abnormality considered by the attending physician as susceptible to interfere in a significant manner on the interpretation of the data
* Absence of consensus
* Therapeutic limitation

4.5. Treatment duration: 7 days except for deep, non-controlled foci (extended to 10-14 days).

4.6. Follow up: First visit (visit #1) to determine eligibility criteria. Additional visits: each day during the treatment period.
5. Calculation of the number of patients

As this is a descriptive pharmacokinetic study without formal predefined hypothesis, no calculation of the size of the population has been made. Based on literature data and the experience of the investigators, a total of 20 patients in each arm should be sufficient to draw meaningful conclusions.
6. Sampling and processing of samples

* Sampling of serum and body fluids: typically at equilibrium for all three antibiotics, and at fixed times after administration of the bolus (ceftriaxone) or the prolonged infusion (meropenem), and performed by a research nurse according to a predefined schedule.
* Sampling of tissues: by Medical personnel when justified for diagnostic or treatment reasons.
* All samples will transferred to the laboratory where they will be treated using predefined and validated protocols.

Antibiotic assay: validated liquid chromatography - mass spectrometry methods (protocols and performance of the assay methods available upon request). The free fraction of each antibiotic will be measured after separation of the bound fraction by molecular sieving (Ngougni Pokem et al., 2015).
7. Statistical analysis and data analysis

Pharmacokinetic analyses will be performed using either NONMEM (NONlinear Mixed Effect Modeling) (http://www.iconplc.com/innovation/nonmem/ ) or PMETRICS (http://www.lapk.org/pmetrics.php) software. Mono-, bi-, and tri-compartmental models will be tested using plasma, tissular and body fluids antibiotic free and total antibiotic concentrations. The First-Order Conditional Estimation with Interaction (FOCE-I) method will be used to assess the objective functions (Jaruratanasirikul et al., 2015) in order to select the most appropriate model for the calculation of the pharmacokinetic parameters (Roberts et al. 2009).
8. Confidentiality and Rights of patients.

The identity and the personal data of the patients will remain confidential according to the applicable Belgian Law

Before enrollment, each patient (or his/her guardian) will provide a written informed consent. Each enrolled patients (or his/her guardian) will be allowed to withdraw from the study at any time without impact on his/her treatment.
9. Contacts

All questions concerning the study can be addressed to

* the responsible investigator: Professor Pr Pierre-François Laterre (phone: 00-32-2-764- 2733 (Intensive Care Unit) or 764-2735 (direct) at the Cliniques universitaire St Luc, Brussels, Belgium
* the associated investigators: Professor Françoise Van Bambeke (phone: 00-32-2-764-7378) and Pharm. Perrin Ngougni Pokem (phone 00-32-2-764-7225) at the Université catholique de Louvain (Louvain Drug Research Institute), Brussels, Belgium.

Conditions

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Pharmacokinetics Anti-Bacterial Agents Infection, Bacterial Infections, Respiratory Infection Drug Monitoring

Study Design

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Allocation Method

NON_RANDOMIZED

Intervention Model

PARALLEL

2 groups of patients studied in parallel
Primary Study Purpose

OTHER

Blinding Strategy

NONE

Study Groups

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Sampling if GFR = or > 30 mL/min

Note: GFR = Glomerular Filtration Rate

Patients with a normal of moderately decreased renal function

* Temocillin: 6 g in continuous infusion over 24 h;
* Ceftriaxone: bolus 2 g (in 30 min) every 12h
* Meropenem: prolonged infusion (3 h) of 2 g every 8h

Blood sampling for antibiotic (temocillin, ceftriaxone or meropenem) pharmacokinetic analysis / Tissue sampling (lung) for determination of antibiotic content when possible / Collection of fluid samples (bronchoalveolar lavage, drainage fluid) for determination of antibiotic concentration when possible

Group Type EXPERIMENTAL

blood sampling

Intervention Type DRUG

* temocillin: blood sampling every day for 7 days
* ceftriaxone: blood sampling 12h after administration for 7 days
* meropenem: blood sampling at 1h, 3h, 5h and 8h after initiation of the administration at days 1 and 2; one sampling at 8h on days 3 to 7

Tissue sampling (lung)

Intervention Type DRUG

Sampling of tissue (lung) when possible during treatment for measurement of the content in antibiotic (temocillin, ceftriaxone, or meropenem, depending on the drug received by the patient)

Collection of fluid samples

Intervention Type DRUG

Collection of fluid samples (bronchoalveolar lavage, drainage fluid) for determination of antibiotic ((temocillin, ceftriaxone, or meropenem, depending on the drug received by the patient) concentration when possible during treatment

Sampling if GFR < 30 mL/min

Patients with severe renal insufficiency or hemodialysis:

* Temocillin: 6 g in continuous infusion over 24 h;
* Ceftriaxone: bolus 2 g (in 30 min) every 12h
* Meropenem: prolonged infusion (3 h) of 2 g every 8h

Blood sampling for antibiotic (temocillin, ceftriaxone or meropenem) pharmacokinetic analysis / Tissue sampling (lung) for determination of antibiotic content if possible / Collection of fluid samples (bronchoalveolar lavage, drainage fluid) for determination of antibiotic concentration if possible

Group Type EXPERIMENTAL

blood sampling

Intervention Type DRUG

* temocillin: blood sampling every day for 7 days
* ceftriaxone: blood sampling 12h after administration for 7 days
* meropenem: blood sampling at 1h, 3h, 5h and 8h after initiation of the administration at days 1 and 2; one sampling at 8h on days 3 to 7

Tissue sampling (lung)

Intervention Type DRUG

Sampling of tissue (lung) when possible during treatment for measurement of the content in antibiotic (temocillin, ceftriaxone, or meropenem, depending on the drug received by the patient)

Collection of fluid samples

Intervention Type DRUG

Collection of fluid samples (bronchoalveolar lavage, drainage fluid) for determination of antibiotic ((temocillin, ceftriaxone, or meropenem, depending on the drug received by the patient) concentration when possible during treatment

Interventions

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blood sampling

* temocillin: blood sampling every day for 7 days
* ceftriaxone: blood sampling 12h after administration for 7 days
* meropenem: blood sampling at 1h, 3h, 5h and 8h after initiation of the administration at days 1 and 2; one sampling at 8h on days 3 to 7

Intervention Type DRUG

Tissue sampling (lung)

Sampling of tissue (lung) when possible during treatment for measurement of the content in antibiotic (temocillin, ceftriaxone, or meropenem, depending on the drug received by the patient)

Intervention Type DRUG

Collection of fluid samples

Collection of fluid samples (bronchoalveolar lavage, drainage fluid) for determination of antibiotic ((temocillin, ceftriaxone, or meropenem, depending on the drug received by the patient) concentration when possible during treatment

Intervention Type DRUG

Other Intervention Names

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temocillin, ceftriaxone, meropenem temocillin, ceftriaxone, meropenem temocillin, ceftriaxone, meropenem

Eligibility Criteria

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Inclusion Criteria

* Patients with suspicion or documentation of of an infection requiring intravenous antibiotic therapy (this includes any patient admitted to the Intensive Care Unit for an infection (or developing an infection) that calls for administration of temocillin, ceftriaxone or meropenem).

Exclusion Criteria

* Patients allergic to β-lactams
* IgE-mediated hypersensibility to penicillins
* any biological abnormality that the attending physician considers as susceptible to delay or perturb in a significant manner the interpretation of the trial
* lack of accepted informed consent
* patient with therapeutic limitations
Minimum Eligible Age

18 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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Université Catholique de Louvain

OTHER

Sponsor Role lead

Responsible Party

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Paul M. Tulkens

Professor

Responsibility Role PRINCIPAL_INVESTIGATOR

Principal Investigators

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Pierre-François Laterre, MD

Role: PRINCIPAL_INVESTIGATOR

Université Catholique de Louvain

Locations

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Cliniques universitaires Saint-Luc

Brussels, , Belgium

Site Status RECRUITING

Countries

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Belgium

Central Contacts

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Pierre-François Laterre, MD

Role: CONTACT

+3227642733

Françoise Van Bambeke, PharmD

Role: CONTACT

+3227647378

Facility Contacts

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Pierre F. Laterre, MD

Role: primary

References

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McWhinney BC, Wallis SC, Hillister T, Roberts JA, Lipman J, Ungerer JP. Analysis of 12 beta-lactam antibiotics in human plasma by HPLC with ultraviolet detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Jul 15;878(22):2039-43. doi: 10.1016/j.jchromb.2010.05.027. Epub 2010 May 24.

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Ngougni Pokem P, Miranda Bastos AC, Tulkens PM, Wallemacq P, Van Bambeke F, Capron A. Validation of a HPLC-MS/MS assay for the determination of total and unbound concentration of temocillin in human serum. Clin Biochem. 2015 May;48(7-8):542-5. doi: 10.1016/j.clinbiochem.2015.02.006. Epub 2015 Feb 21.

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Wong G, Briscoe S, Adnan S, McWhinney B, Ungerer J, Lipman J, Roberts JA. Protein binding of beta-lactam antibiotics in critically ill patients: can we successfully predict unbound concentrations? Antimicrob Agents Chemother. 2013 Dec;57(12):6165-70. doi: 10.1128/AAC.00951-13. Epub 2013 Sep 30.

Reference Type RESULT
PMID: 24080664 (View on PubMed)

Zykov IN, Sundsfjord A, Smabrekke L, Samuelsen O. The antimicrobial activity of mecillinam, nitrofurantoin, temocillin and fosfomycin and comparative analysis of resistance patterns in a nationwide collection of ESBL-producing Escherichia coli in Norway 2010-2011. Infect Dis (Lond). 2016 Feb;48(2):99-107. doi: 10.3109/23744235.2015.1087648. Epub 2015 Sep 28.

Reference Type RESULT
PMID: 26414659 (View on PubMed)

Related Links

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http://www.cbip.be

Ceftriaxone. Ceftriaxone Summary of Product Characteristics. Centre Belge d'Information Pharmacothérapeutique (C.B.I.P.asbl). Available from: http://www.cbip.be Last updated: 2015

http://www.cbip.be

Méropénème. Meropenem Summary of Product Characteristics. Centre Belge d'Information Pharmacothérapeutique (C.B.I.P.asbl). Available from: http://www.cbip.be Last updated: 9-1-2014

http://www.cbip.be

Temocilline. Temocillin Summary of Product Characteristics. Centre Belge d'Information Pharmacothérapeutique (C.B.I.P.asbl). Available from: http://cbip.be/ Last updated: 2014

Other Identifiers

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Pop PK/PD betalactams ICU

Identifier Type: -

Identifier Source: org_study_id

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