Term
Is linezolid bacteriostatic or bactericidal? |
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Definition
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Term
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Definition
Blocks formation of the translation initiation complex by binding to the 23S portion of the 50S subunit. |
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Term
What are mechanisms of resistance to linezolid? |
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Definition
In vitro: Mutations in 23S RNA (the portion of the 50S ribosomal subunit to which Linezolid binds) can confer resistance
Note: Resistance is correlated to number of mutated 23S genes
In vivo: Some reports of resistance in patients using linezolid long-term. |
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Term
What are structural features of linezolid? |
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Definition
Linezolid is entirely synthetic and quite complex.
[image]
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Term
How is linezolid administered, distributed, metabolized, and excreted? |
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Definition
Administered orally or parenterally; 100% bioavailability.
Well-distributed to all tissues (including CSF) but bone and fat
Minimal metabolism
80% excreted renally, mostly unchanged. |
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Term
What are some adverse effects of linezolid? |
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Definition
Fairly safe, but some:
-- Hematologic toxcitiy: reduction in platelet count, hematocrit; related to duration of therapy.
-- Serotonin toxicity: linezolid acts as an MAOI; problematic for patients on SSRIs, or any drug that increases serotonin.
-- Peripheral or optic neuropathy with long term use (>28 days).
Note: Optic neuropathy generally reversible. Peripheral neuropathy may not be.
-- Headache |
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Term
What are clinical uses of linezolid? |
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Definition
Reserved for infections resistant to other drugs.
-- VRE
-- MRSA |
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