利奈唑胺(Linezolid)的功效与作用及注意事项？

Linezolid is a synthetic antibiotic that belongs to the oxazolone class of antibiotics and has antibacterial effects. It mainly achieves antibacterial purposes by inhibiting the activity of bacterial DNA gyrase and preventing the replication of bacterial DNA.

Linezolid was developed by Pfizer and was first approved for marketing by the U.S. Food and Drug Administration (FDA) on April 18, 2000.

Efficacy and role of linezolid

It is mainly used to treat infectious diseases caused by sensitive bacteria, such as nosocomial pneumonia, community-acquired pneumonia, complicated skin and soft tissue infections, uncomplicated skin and soft tissue infections, complicated intra-abdominal infections, etc.

In addition, linezolid can also treat meningitis, acute bacterial sinusitis, community-acquired pneumonia, complicated skin and skin and soft tissue infections caused by Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Haemophilus influenzae, etc., and can also treat drug-resistant tuberculosis.

Linezolid has a broad antibacterial spectrum and has good antibacterial activity against most Gram-positive bacteria, Gram-negative bacteria and anaerobic bacteria. It is effective against acute bacterial skin and skin structure infections caused by Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, and Streptococcus agalactiae.

Linezolid Medication

1. Myelosuppression: including anemia, leukopenia, pancytopenia and thrombocytopenia. Complete blood cell count should be checked weekly in patients treated with linezolid. For patients who develop myelosuppression or worsening of myelosuppression, discontinuation of linezolid should be considered.

2. Antimicrobial drug-associated diarrhea and colitis: If antimicrobial drug-associated colitis is suspected or confirmed, linezolid may need to be discontinued and appropriate treatment measures should be taken, such as rehydration, maintaining electrolyte balance, and protein supplementation.

3. Hypoglycemia: If hypoglycemia occurs after taking medication, the dose of insulin or oral hypoglycemic drugs should be reduced, or treatment with oral hypoglycemic drugs, insulin or linezolid should be stopped.

4. Lactic acidosis: If repeated nausea, vomiting, abdominal pain, unexplained acidosis, hypocapnia or hyperventilation occur during medication, immediate examination is required.

5. Peripheral neuropathy and optic neuropathy: Eye examinations should be carried out in time.

6. Convulsions: If the patient has a history of epileptic seizures, the doctor should be informed in time before taking medication.

7. Superinfection: Drug-related candidiasis may occur, and appropriate measures should be taken.

8. Dietary attention: Avoid eating a large amount of foods rich in tyramine, such as chocolate, cheese, bacon, luncheon meat, etc.

9. Other precautions: The dosage does not need to be adjusted when changing from intravenous administration to oral administration. Patients with high blood pressure or those taking antidepressants should use their medications with caution to avoid adverse reactions such as dizziness, headache, diarrhea, and nausea.

Usage and dosage

1. Complicated skin and skin and soft tissue infections, community-acquired pneumonia and associated bacteremia, and nosocomial pneumonia:

1. Adults and adolescents (12 years and above): 600 mg every 12 hours, intravenously or orally.

2. Children from birth to 11 years old: 10 mg/kg intravenously or orally every 8 hours.

2. Vancomycin-resistant Enterococcus faecium infection and associated bacteremia:

1. Adults and children 12 years and older: 600 mg every 12 hours, intravenously or orally.

2. From birth to 11 years old: 10 mg/kg intravenously or orally every 8 hours.

3. Simple skin and skin and soft tissue infections:

1. Adults: 400 mg orally every 12 hours.

2. Children over 12 years old: 600mg orally every 12 hours.

3. Children aged 5-11 years: 10 mg/kg every 12 hours.

4. Children <5 years old: 10 mg/kg orally every 8 hours.

Storage conditions

Keep sealed and protected from light, and should be stored in an environment of 10-30°C under normal temperature conditions.

Drug absorption and excretion

1. Absorption: After oral administration, linezolid is absorbed rapidly and completely. Peak plasma concentration is reached about 1-2 hours after administration. The absolute bioavailability is approximately 100%. No dose adjustment is required for linezolid oral or intravenous administration.

2. Excretion: Non-renal clearance accounts for approximately 65% ​​of the total clearance of linezolid.

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