.jpeg)
{{ variable.name }}
Linezolid (Linezolid) Instructions
Common name: Linezolid
Trade name: Zyvox
All names: Linezolid, Zyvox, Linezolid, Zyvox, Linospan
Vancomycin-resistant Enterococcus faecium infection, including associated bacteremia.
Complicated skin and skin and soft tissue infections, community-acquired pneumonia and associated bacteremia, nosocomial pneumonia:
Adults and adolescents (12 years and older): 600 mg intravenously or orally every 12 hours.
Pediatric patients (from birth to 11 years old): 10 mg/kg intravenously or orally every 8 hours.
Recommended treatment course: continuous treatment for 10-14 days.
Vancomycin-resistant Enterococcus faecium infection and associated bacteremia:
Adults and adolescents (12 years and older) 600 mg intravenously or orally every 12 hours.
Pediatric patients (from birth to 11 years old): 10 mg/kg intravenously or orally every 8 hours.
Recommended treatment course: continuous treatment for 14-28 days.
Simple skin and skin and soft tissue infections:
Adults: 400 mg orally every 12 hours.
Adolescents (over 12 years old): 600 mg orally every 12 hours.
Children 5-11 years old: 10 mg/kg orally every 12 hours.
Neonates <7 days old: Most patients born prematurely (<34 weeks of gestation) within 7 days of birth have a lower systemic clearance rate of Sivo and a larger AUC value than full-term infants and other infants. The initial dose for these neonates should be 10 mg/kg every 12 hours. When clinical response is insufficient, a dose of 10 mg/kg every 8 hours should be considered. All newborns over 7 days old should be dosed at 10 mg/kg every 8 hours.
Adult patients with MRSA (methicillin-resistant Staphylococcus aureus) infection are treated with Sivo 600 mg every 12 hours.
No dosage adjustment is required when switching from intravenous to oral administration. For patients who are initially treated with linezolid injection, doctors can continue treatment with linezolid tablets or oral suspension based on clinical conditions.
Adverse reactions:
>10%:
Gastrointestinal tract: diarrhea (8%-11%)
Hematology and tumors: leukopenia (neonates, infants, and children: 12%; children, adolescents, and adults : ≤2%), thrombocytopenia (adults: ≤10%)
1%-10%:
Central nervous system: headache (children, adolescents, and adults: 6%-9%; neonates, infants, and children: <1%), dizziness (adults: 2% to 3%), Dizziness (children and adolescents: 1%)
Skin: rash (adults: 1%-2%), pruritus (neonates, infants, children and adolescents: ≤1%; not applicable sites)
Endocrine metabolism: increased amylase (≤2%), increased lactate dehydrogenase ( Adults: ≤2%)
Gastrointestinal tract: vomiting (3%-9%), nausea (2%-7%), elevated serum lipase (adults: 3%-4%; children and adolescents: <1%), loose stools (neonates, infants, children and adolescents: 2%), abdominal pain (≤ 2%), oral candidiasis (adults: ≤2%), halitosis (adults: 1% to 2%), tongue coating discoloration (≤1%)
Genitourinary system: vulvovaginal candidiasis (adults: 1%-2%)
Hematology and oncology: anemia (neonates, Infants and children: 6%; adults ≤2%), neutropenia (neonates, infants, and children: 6%; children, adolescents, and adults: ≤1%), thrombocytopenia (neonates, infants, and children: 5%), eosinophilia (neonates, infants, children: and adolescents: ≤2%)
Liver: elevated serum ALT (2%-10%), elevated serum bilirubin (neonates, infants, and children: 6%, adults: <1%), elevated serum AST (aspartate aminotransferase) (adults: 2%-5%), serum alkalinity Elevated sex phosphatase (adults: ≤4%), abnormal liver function (adults: ≤2%)
Infection: fungal infection (adults: ≤2%)
Kidney: elevated blood urea nitrogen (adults: ≤2%), elevated serum creatinine (≤2%)
<1%
Postmarketing or case reports: Anaphylaxis, angioedema, blurred vision, myelosuppression, bullous dermatoses, Clostridium difficile-associated diarrhea, tooth discoloration, hypoglycemia, lactic acidosis, optic neuropathy, pancytopenia, peripheral neuropathy, seizures, serotonin syndrome (concomitant use of other serotonergic agents ), severe skin disease, sideroblastic anemia, Stevens-Johnson syndrome, toxic epidermal necrolysis, vision loss
Contraindications:
Hypersensitivity to linezolid or any of its components; concurrent use or within 2 weeks of use of MAO inhibitors.
Precautions:
Lactic acidosis: Use has been reported. Patients who develop recurrent nausea and vomiting, unexplained acidosis, or low bicarbonate levels require immediate evaluation.
Myelosuppression: Has been reported and may depend on the duration of therapy (usually >2 weeks of therapy); use with caution in patients with pre-existing myelosuppression and in patients receiving other drugs that may cause myelosuppression or in chronic infections (previous or concomitant antibiotic therapy). Weekly CBC monitoring is recommended; consider discontinuing treatment in patients who develop myelosuppression (or whose myelosuppression worsens during treatment). Thrombocytopenia is the most common blood disorder.
Peripheral nerve and optic neuropathy (with vision loss): has been reported in adults and children and may occur primarily with treatment courses longer than 28 days; any symptoms of vision change or impairment require immediate ophthalmological evaluation and possible discontinuation of treatment.
Serotonin Syndrome: Symptoms associated with anxiety, restlessness, hallucinations, agitation, myoclonus, tremor, and tachycardia may occur concurrently with gonadotropin drugs, drugs that reduce the metabolism of linezolid, or in patients with carcinoid syndrome. Avoid use in such patients unless clinically appropriate and closely monitor for symptoms of serotonin syndrome or neuroleptic malignant syndrome.
Superinfections: Long-term use may result in fungal or bacterial superinfections, including Clostridium difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD is observed more than 2 months after antibiotic treatment.
Carcinoid Syndrome: Use with caution and closely monitor patients with carcinoid syndrome for serotonin syndrome; linezolid agents have not been studied in such patients. Do not use without close supervision.
Diabetes: Hypoglycemic events have been reported; use with caution and monitor blood glucose closely in patients with diabetes. A dose reduction or discontinuation of concurrent antidiabetic agents or discontinuation of linezolid may be necessary.
Hypertension: Use with caution and close monitoring of blood pressure in patients with uncontrolled hypertension; linezolid has not been studied in this setting. Do not use without close supervision.
Hyperthyroidism: Use caution and close blood pressure monitoring in patients with untreated hyperthyroidism; linezolid drugs have not been studied in patients with this condition. Do not use without close supervision.
Pheochromocytoma: Use with caution and closely monitor blood pressure in patients with pheochromocytoma; linezolid drugs have not been studied in patients with pheochromocytoma. Do not use without close supervision.
Seizure Disorders: Seizures have been reported; use with caution in patients with a history of epilepsy.
Drug-Drug Interactions: Significant interactions may exist that may require dose or frequency adjustment, additional monitoring, or the selection of alternative therapies.
Pediatrics: The manufacturer does not recommend the use of linezolid for the empiric treatment of central nervous system infections in children because therapeutic concentrations of linezolid are not consistent in the cerebrospinal fluid of patients with ventriculo-peritoneal shunts. However, limited data available in the form of case reports in pediatric and adult patients suggest that linezolid may be useful in the treatment of Gram-positive CNS infections that are unresponsive to other treatment regimens described in the literature that are successful in treating VRE and S. aureus CNS and shunt infections.
Benzyl alcohol and its derivatives: Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid is a metabolite of benzyl alcohol, and large amounts of benzyl alcohol (99 mg/kg/day) have been associated with potentially fatal toxicity in neonates (wheezing syndrome); wheezing syndrome includes metabolic acidosis, respiratory distress, wheezing, and central nervous system dysfunction ( including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse. Some data suggest that benzoates displace bilirubin from protein binding sites. Avoid or use with caution in neonatal dosage forms containing benzyl alcohol derivatives.
Phenylalanine: Some products may contain phenylalanine.
Appropriate use: Unnecessary use may result in adverse effects on linezolid. Amine resistance develops; consider alternatives before initiating outpatient treatment.
Catheter-related bloodstream infection (CRBSI): Linezolid should not be used for empiric treatment of CRBSI but may be appropriate for targeted therapy.
Pregnancy: Limited information is available regarding the use of linezolid drugs during pregnancy. Some pharmacokinetic properties of linezolid drugs may be altered due to physiological changes caused by pregnancy.
Storage:
Infusion: Store at 25°C (77°F). Protect from light and freezing. Keep the infusion bag in its outer packaging until ready for use.
Oral suspension: 25°C ( 77°F); store at room temperature after reconstitution and use suspension within 21 days. Avoid light.
Tablets: Store at 25°C (77°F). Protect from light and moisture.
Mechanism of action:
Linezolid is a bacterial protein synthesis inhibitor that binds to the 23s site of ribosomal RNA on the bacterial 50s subunit, thereby preventing the formation of the 70s initiator complex. The former is a very important component in the bacterial translation process. Since linezolid does not affect the activity of peptidyl transferase, it only acts on the initial stage of the translation system, inhibiting the connection between mRNA and ribosomes, thereby inhibiting bacterial protein synthesis. < /p>