Publication: Linezolid: estudio de utilización, farmacocinética, efectividad y seguridad
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2017-07-18
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Universidad Complutense de Madrid
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Abstract
El linezolid es un antibiótico perteneciente al grupo de las oxazolidinonas cuya comercialización se aprobó en el año 2001. Actúa inhibiendo la síntesis de proteínas bacterianas, presentando un efecto fundamentalmente bacteriostático frente a la gran mayoría de microorganismos sensibles. Su espectro de actividad se dirige hacia bacterias grampositivas, especialmente cocos grampositivos, incluidos los multirresistentes (Staphylococcus aureus, Streptococcus pyogenes, Enterococcus faecium, etc…). Los puntos de corte de la concentración mínima inhibitoria (CMI) establecidos por el Comité Europeo de Evaluación de Sensibilidad Antimicrobiana (EUCAST) para estafilococos y enterococos son: sensibles ≤4 mg/L y resistentes >4 mg/L. Desde un punto de vista farmacocinético se caracteriza por presentar una elevada biodisponibilidad tras su administración oral, de un 100%, con una velocidad de absorción rápida. Se distribuye ampliamente a tejidos, con un volumen de distribución (Vd) medio en adultos sanos de unos 50 L. El metabolismo se realiza en un 60% por vía hepática, mediante oxidación no microsomal, dando lugar a dos metabolitos inactivos que se excretan predominantemente por orina. En torno a un 30% de la dosis se excreta por orina de forma inalterada. Presenta una vida media de eliminación en torno a 5h (3,5h a 6h), por lo que el estado de equilibrio estacionario se alcanza a los dos o tres días de iniciarse la administración o incluso antes. Diversos estudios ponen de manifiesto la presencia de variabilidad farmacocinética de linezolid en distintos grupos de pacientes (pacientes ancianos, pacientes con alteraciones renales o hepática, pacientes críticos, etc…) por lo que la monitorización farmacocinética de linezolid podría ser de utilidad. La pauta posológica habitual, para las distintas indicaciones aprobadas en la ficha técnica de la AEMPS, es de 600 mg/12h. Estas indicaciones son: neumonía nosocomial y neumonía adquirida en la comunidad, cuando se tenga la certeza o sospecha de que están causadas por bacterias gram positivas sensibles a linezolid, e infecciones de piel y partes blandas (IPPB), sólo cuando las pruebas microbiológicas muestren que la infección está originada por bacterias gram positivas sensibles a linezolid...
Linezolid is an oxazolidinone-class antibiotic first approved to market in 2001. It inhibits bacterial protein synthesis, having mainly bacteriostatic effect against the vast majority of susceptible organisms. It is active against gram-positive bacteria, especially gram-positive cocci, including multidrug resistant strains (Staphylococcus aureus, Streptococcus pyogenes, Enterococcus faecium, etc ...). The cutoffs of the minimum inhibitory concentration (MIC) established by the European Committee on Antimicrobial Susceptibility Assessment (EUCAST) for staphylococci and enterococci are: sensitive ≤4 mg / L and resistant >4 mg / L. Pharmacokinetically, it is characterized by a rapid and complete absorption after oral administration. It is widely distributed into tissues with an average volume of distribution (Vd) in healthy adults of about 50 L. Around 60% of the dose is metabolized by a hepatic nonmicrosomal oxidation, giving rise to two inactive metabolites excreted predominantly in urine. Approximately one third of the dose is excreted in urine unchanged. As the elimination half-life averages 5 hours (3.5 hours to 6 hours), the steady state is reached within two or three days after the initial administration, or sooner. Several studies reveal the presence of pharmacokinetic variability of linezolid in different groups of patients (elderly patients, patients with renal or hepatic disorders, critically ill patients, etc ...), which is why monitoring its serum levels may be useful. The usual linezolid dosage regimen is 600 mg every 12 hours, for the indications approved in the product labeling issued by The Spanish Agency of Medicines and Medical Devices (AEMPS). Those indications are: nosocomial pneumonia and community-acquired pneumonia, proven or strongly suspected to be caused by gram-positive bacteria sensitive to linezolid, and infections of skin and soft tissue (SSTIs), when microbiological testing shows that the infection is caused by susceptible bacteria...
Linezolid is an oxazolidinone-class antibiotic first approved to market in 2001. It inhibits bacterial protein synthesis, having mainly bacteriostatic effect against the vast majority of susceptible organisms. It is active against gram-positive bacteria, especially gram-positive cocci, including multidrug resistant strains (Staphylococcus aureus, Streptococcus pyogenes, Enterococcus faecium, etc ...). The cutoffs of the minimum inhibitory concentration (MIC) established by the European Committee on Antimicrobial Susceptibility Assessment (EUCAST) for staphylococci and enterococci are: sensitive ≤4 mg / L and resistant >4 mg / L. Pharmacokinetically, it is characterized by a rapid and complete absorption after oral administration. It is widely distributed into tissues with an average volume of distribution (Vd) in healthy adults of about 50 L. Around 60% of the dose is metabolized by a hepatic nonmicrosomal oxidation, giving rise to two inactive metabolites excreted predominantly in urine. Approximately one third of the dose is excreted in urine unchanged. As the elimination half-life averages 5 hours (3.5 hours to 6 hours), the steady state is reached within two or three days after the initial administration, or sooner. Several studies reveal the presence of pharmacokinetic variability of linezolid in different groups of patients (elderly patients, patients with renal or hepatic disorders, critically ill patients, etc ...), which is why monitoring its serum levels may be useful. The usual linezolid dosage regimen is 600 mg every 12 hours, for the indications approved in the product labeling issued by The Spanish Agency of Medicines and Medical Devices (AEMPS). Those indications are: nosocomial pneumonia and community-acquired pneumonia, proven or strongly suspected to be caused by gram-positive bacteria sensitive to linezolid, and infections of skin and soft tissue (SSTIs), when microbiological testing shows that the infection is caused by susceptible bacteria...
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Tesis inédita de la Universidad Complutense de Madrid, Facultad de Farmacia, Departamento de Farmacología (Farmacognosia y Farmacología Experimental), leída el 05/07/2016