Linezolid
ZYVOX
What it isOxazolidinone inhibiting the bacterial 50S subunit; MRSA and vancomycin-resistant Enterococcus infections.
Why this oneComplete oral absorption lets tablets replace IV therapy without loss of exposure, and lung penetration is strong.
What limits it⚑ It reversibly inhibits MAO, creating serotonin-syndrome risk with serotonergic drugs. Myelosuppression and optic or peripheral neuropathy emerge with prolonged use.
FDA-approved for
- resistant gram-positive infections (2000)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Nosocomial/community-acquired pneumonia, complicated SSSI, VRE infections | Adults & adolescents >=12 yr | 600 mg PO q12h | 600 mg q12h | 600 mg q12h |
| Uncomplicated SSSI | Adults | 400 mg PO q12h | 400 mg q12h | 400 mg q12h |
| Uncomplicated SSSI | Adolescents >=12 yr | 600 mg PO q12h | 600 mg q12h | 600 mg q12h |
| Pneumonia, complicated SSSI, VRE infections | Pediatric birth–11 yr | 10 mg/kg PO q8h | 10 mg/kg q8h | |
| Uncomplicated SSSI | Pediatric <5 yr / 5–11 yr | <5 yr: 10 mg/kg q8h; 5–11 yr: 10 mg/kg q12h |
Renal Undefined
Hepatic Undefined
Preterm neonates <7 days old: start 10 mg/kg q12h, increase to q8h by day 7 of life.
Instructions
- No dose adjustment when switching from IV to oral.
- Duration by indication: pneumonia/complicated & uncomplicated SSSI 10–14 days; VRE infections 14–28 days.
- Monitor complete blood counts weekly, especially with therapy >2 weeks.
- Observe MAOI/serotonergic/sympathomimetic and tyramine-food precautions (reversible nonselective MAO inhibitor).
Contraindications
- Concurrent use with, or within 2 weeks of, any MAO inhibitor (e.g., phenelzine, isocarboxazid)
Cautions
- Myelosuppression (anemia, leukopenia, thrombocytopenia, pancytopenia) — worse in severe renal or moderate-severe hepatic impairment
- Peripheral and optic neuropathy, primarily with therapy >28 days
- Serotonin syndrome with concomitant serotonergic agents
- Lactic acidosis; convulsions
- Hypoglycemia in diabetics on insulin/oral agents
- Hyponatremia and/or SIADH
- Blood-pressure elevation with sympathomimetics, tyramine-rich foods, uncontrolled hypertension, pheochromocytoma, thyrotoxicosis
- C. difficile-associated diarrhea; mortality imbalance in catheter-related bloodstream infections (not an approved use)
Adverse reactions
- Diarrhea
- Nausea, vomiting
- Headache
- Anemia, thrombocytopenia
- Taste alteration
Pregnancy Available data have not identified a drug-associated risk of major birth defects or miscarriage; animal embryo-fetal toxicity/lethality at maternally toxic doses.
Lactation Present in breast milk (~6–9% of the infant therapeutic dose); monitor breastfed infant for diarrhea and vomiting.
NO BOXED WARNINGS
Principal riskA reversible MAOI: serotonin syndrome with SSRIs
Cost, est. cash$10–$500/month
Generic entryBy 2023
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityAllergy, gastrointestinal effects and agent-specific renal, hepatic, hematologic or interaction risks.
Mechanism of action: Linezolid ballicule
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