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Investigation of the Correlation Between Plasma Concentration of Linezolid Antibiotic and Treatment Response and Adverse Reactions

Conditions
Peripheral Neuropathy
Myelosuppression
Lactic Acidosis
Registration Number
NCT03126890
Lead Sponsor
National Taiwan University Hospital
Brief Summary

Linezolid is the second line agent in the treatment of MRSA and PRSP infections, and it is also the drug of choice for VRE infections. It can be an alternative option against multidrug resistant tuberculosis and non-tuberculosis mycobacterium. However, Patients who receive more than 2 weeks of treatment duration and who have renal dysfunction or severe cirrhosis may prone to experience anemia, thrombocytopenia, and leukopenia. Long-term use may also result in lactic acidosis, peripheral neuropathy and optic neuropathy due to mitochondrial toxicity. Thus, this study will analysis the medical charts in National Taiwan University Hospital (NTUH) from 2011 to 2016 to get the population demographics who use linezolid and analysis the occurrence rate of myelosuppression, neuropathy and lactic acidosis. Simultaneously, the investigators also use therapeutic drug monitoring (TDM) to prospectively evaluate the association of linezolid blood concentration and clinical efficacy and safety. The result of this study will provide physicians more information to prevent concentration-dependent adverse effects.

Detailed Description

The increasing resistance of methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci (VRE), and penicillin-resistant Streptococcus pneumoniae (PRSP) has caused significant medical issue. With limited antimicrobial agents available, it has been an increasing challenge in infection control and disease treatment. Linezolid is the second line antibiotics in the treatment of MRSA and PRSP infections, and it is also the drug of choice for VRE infections. It can be an alternative against multidrug resistant tuberculosis and non-tuberculosis mycobacterium. Linezolid has almost 100% of bioavailability. It has excellent tissue penetration. It metabolized via non-enzymatic oxidation. Two major metabolites, aminoethoxyacetic acid (chemical name) and hydroxyethyl glycine (chemical name), are final forms before excreted through kidneys. Even though the manufacturer does not recommend dosing adjustment for patients with renal or hepatic dysfunction, recent studies demonstrated accumulation of linezolid and 2 metabolites in the body. Patients who receive more than 2 weeks of treatment duration and who have renal dysfunction or severe cirrhosis may present higher plasma linezolid concentration. Patients may experience anemia, thrombocytopenia, and leukopenia under long-term use of linezolid. However, there is lack of study on lactic acidosis, peripheral neuropathy, and optic neuropathy due to mitochondrial toxicity.

This study has two parts. This study will analysis the medical charts in NTUH from 2011 to 2016 to get the population demographics who use linezolid and the occurrence rate of myelosuppression, neuropathy and lactic acidosis. Then, followed by a prospective study which aim is to monitor the plasma peak and trough concentration of linezolid (total and free drug) and 2 metabolites by different sample collecting method (plasma, dry blood spot; DBS). If clinical necessity, the investigators may also monitor tissue fluid concentration. Clinical response and toxicity were monitored by liquid chromatography (LC) analysis. The investigators plan to evaluate the association between plasma concentration and toxicity including bone marrow suppression, peripheral neuropathy, and lactic acidosis. It is important to determine if dose adjustment in patients with renal and/or hepatic dysfunction is required. Simultaneously, the investigators want to develop DBS method which can ease patients' uncomfortable sense and simplify the drug monitor process. The result of this study will provide physicians more information to prevent concentration-dependent adverse effects.

Recruitment & Eligibility

Status
UNKNOWN
Sex
All
Target Recruitment
1000
Inclusion Criteria

Not provided

Exclusion Criteria

Retrospective study 1. Patients without baseline complete blood count (CBC) data (RBC or Hb, WBC, platelet) before linezolid treatment. Prospective study

  1. Patients with severe disease status (assess by clinicians) might die within 2 days or treatment duration less than 2 days

Study & Design

Study Type
OBSERVATIONAL
Study Design
Not specified
Primary Outcome Measures
NameTimeMethod
Safety - lactic acidosisObservation periods: entire linezolid treatment course until resolution of side effect, loss of follow up, death or December 2020 (up to 4 years).

Definition of lactic acidosis:

1. Definite lactic acidosis: lactic acid \> 4 mmol/L and blood potential of hydrogen (pH) value \< 7.35

2. Probable lactic acidosis: lactic acid \> 4 mmol/L without or not achieved pH value data

Clinical efficacyObservation periods: entire linezolid treatment course until 30 days after the completion of treatment, loss of follow up, death or December 2020 (up to 4 years).

Clinical efficacy definition:

Cure: biological eradication or clinical improvement. (Biological eradication: Eradication of bacterial culture prior to study drug) (Clinical improvement: White blood cell (WBC), C reactive protein (CRP) back to normal range (WBC: 3500 - 9000/mm3; CRP: \< 1 mg/dL) or without sepsis symptom (body temperature, pulse, heart rate returned to normal))

Intermittent cure: same bacteria culture positive (with same minimum inhibitory concentration (MIC) data) within 2 weeks after linezolid treatment ends.

Failure: persistent bacteria culture after linezolid treatment or unresolved clinical sign and symptoms.

Indeterminate outcome: loss of follow up or discontinue linezolid due to adverse drug reaction

Safety - thrombocytopeniaObservation periods: entire linezolid treatment course until resolution of side effect, loss of follow up, death or December 2020 (up to 4 years).

Definition of thrombocytopenia: platelet count \< 100,000/mm3 and platelet count of \< 75% of the baseline counts.

Safety - anemiaObservation periods: entire linezolid treatment course until resolution of side effect, loss of follow up, death or December 2020 (up to 4 years).

Definition of anemia: Hemoglobin (Hb) \< 10 g/dL and Hb level of \< 75% of the baseline level.

Safety - leukopeniaObservation periods: entire linezolid treatment course until resolution of side effect, loss of follow up, death or December 2020 (up to 4 years).

Definition of leukopenia: WBC count \< 3000/mm3 and WBC count of \< 50% of baseline count.

Safety - peripheral neuropathyObservation periods: entire linezolid treatment course until resolution of side effect, loss of follow up, death or December 2020 (up to 4 years).

Definition of peripheral neuropathy (PN):

1. Definite PN: with nerve conduction velocity test (+)

2. Probable PN: patient reported symptoms

Secondary Outcome Measures
NameTimeMethod

Trial Locations

Locations (1)

National Taiwan University Hospital

🇨🇳

Taipei, Test2, Taiwan

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