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Details

Linezolid
ID Week 2
7
Pharmacology
Graduate
04/13/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
Is linezolid bacteriostatic or bactericidal?
Definition

Bacteriostatic.

Term
How does linezolid work?
Definition

Blocks formation of the translation initiation complex by binding to the 23S portion of the 50S subunit. 

Term
What are mechanisms of resistance to linezolid?
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.

Term
What are structural features of linezolid?
Definition

Linezolid is entirely synthetic and quite complex

 

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Term
How is linezolid administered, distributed, metabolized, and excreted?
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.

Term
What are some adverse effects of linezolid?
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

Term
What are clinical uses of linezolid?
Definition

Reserved for infections resistant to other drugs.

-- VRE

-- MRSA

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