Vancomycin-resistant Enterococcus faecium infection; nosocomial pneumonia or community-acquired pneumonia caused by Staphylococcus aureus, or Streptococcus pneumonia; complicated SSTI (skin, soft tissue infection).
藥理
Antibiotic, Oxazolidinone
Linezolid is a synthetic oxazolidinone antimicrobial agent. Inhibits bacterial protein synthesis by binding to bacterial 23S ribosomal RNA of the 50S subunit. This prevents the formation of a functional 70S initiation complex, which is essential for the bacterial translation process.
藥動學
Distribution:
1. Vd: (Infants <3 months) 0.79 L/kg; (Infants ≥3 months and Children ≤11 years of age) 0.69 L/kg; (Children ≥12 years and Adolescents) 0.61 L/kg; (Adults) 0.65 L/kg
2. Bone (cancellous): 40%; CSF: ~60% to 70%; Lung penetration: ≥100%; Tissue: ~49%
3. Protein binding: 31% Metabolism:
Hepatic via oxidation of the morpholine ring, resulting in two inactive metabolites (aminoethoxyacetic acid, hydroxyethyl glycine); minimally metabolized, may be mediated by cytochrome P450. Half-life elimination:
(Infants <3 months) 1.8 hours; (Infants ≥3 months and Children ≤11 years of age) 2.9 hours; (Children ≥12 years and Adolescents) 4.1 hours; (Adults) 4.9 hours Excretion:
Urine (~30% of total dose as parent drug, ~50% of total dose as metabolites); two metabolites of linezolid may accumulate in patients with severe renal impairment; feces (~9% of total dose as metabolites)
禁忌症
Hypersensitivity to linezolid or any of the other product components
懷孕分類
C
哺乳分類
Excretion in breast milk unknown
副作用
Common
Diarrhea, headache, nausea, decreased white blood cell count Significant
1. Clostridioides difficile infection: including diarrhea and colitis; may start on the first day or up to 3 months post-antibiotic
2. Lactic acidosis: nausea and vomiting, unexplained acidosis, or low bicarbonate levels have been reported
3. Myelosuppression: thrombocytopenia and anemia have been reported
4. Peripheral neuropathy and optic neuropathy: symptoms include pain, numbness, paresthesia, and weakness
5. Serotonin syndrome: Concurrent use with serotonergic agents (SSRI, TCA, 5-HT1 receptor agonist, Bupropion, Buspirone, or opioids<20220322>) is not recommended
劑量和給藥方法
Adult and child ≥12 years: IV 600 mg Q12H
Dose adjustments are unnecessary when converting from IV to oral administration.
小兒調整劑量
Neonates <7 days of age: 10 mg/kg Q12H Neonates >7 days of age: 10 mg/kg Q8H
腎功能調整劑量
No dosage adjustment is recommended for renal impairment patient.
肝功能調整劑量
No dosage adjustment is recommended for hepatic impairment patient.