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What is the mechanism of action (MOA) of linezolid?
What is the mechanism of action (MOA) of linezolid?
What percentage of linezolid is excreted unchanged in urine?
What percentage of linezolid is excreted unchanged in urine?
30%
Which of the following organisms are treated by linezolid? (Select all that apply)
Which of the following organisms are treated by linezolid? (Select all that apply)
One major setback of linezolid is ___.
One major setback of linezolid is ___.
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Linezolid is associated with thrombocytopenia.
Linezolid is associated with thrombocytopenia.
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What is the recommended dosage of linezolid for treating an infection?
What is the recommended dosage of linezolid for treating an infection?
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Match the following side effects with linezolid:
Match the following side effects with linezolid:
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Study Notes
Mechanism of Action (MOA)
- Linezolid is an oxazolidinone antibiotic.
- It inhibits bacterial protein synthesis by binding to the 23S ribosomal RNA of the 50S subunit.
- This binding prevents the formation of the 70S initiation complex, differentiating its MOA from other antibiotics.
Elimination
- Non-renal clearance accounts for approximately 65% of linezolid elimination.
- 30% of the drug is excreted unchanged in urine.
- 40% is eliminated as metabolite B, and 10% as metabolite A.
- Low renal clearance suggests net tubular reabsorption of the drug.
Spectrum of Activity
- Effective against Enterococcus faecium, including vancomycin-resistant strains (VRE).
- Active against Staphylococcus aureus, including MRSA.
- Also targets Enterococcus faecalis, coagulase-negative staphylococci, and various Streptococcus species.
Adverse Effects (AE)
- Thrombocytopenia is a significant side effect.
- Monoamine oxidase inhibition can lead to serotonin syndrome, presenting as hypertension, fever, confusion, and can be fatal.
- Other adverse effects include diarrhea, headache, and nausea.
Dosage
- Standard dosage is 600 mg administered every 12 hours, either intravenously (IV) or orally (PO).
- For uncomplicated skin infections, a reduced dosage of 400 mg every 12 hours is recommended.
Treatment Indications
- Linezolid treats skin infections, MRSA pneumonia, and VRE-related urinary tract infections (UTIs) and bacteremia.
Cost Implications
- A major disadvantage of linezolid is its high cost, which can limit access and utilization in clinical settings.
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Description
Test your knowledge of linezolid with these informative flashcards. This quiz covers key concepts such as its mechanism of action and elimination pathways. Perfect for students in pharmacology or medicine.