II. Indications
- Vancomycin Resistant Enterococcus
- Nosocomial Pneumonia
- Complicated Skin Infections
-
Community Acquired Pneumonia (Not first line agent)
- Does not cover Haemophilus Influenzae
- Methicillin Sensitive Staphylococcus Aureus
- Penicillin Sensitive Streptococcus Pneumoniae
III. Mechanism
- Linezolid is a prototype for new Oxazolidinone Class
- Inhibits Protein synthesis at unique site
- Spectrum
- Minimal activity against Gram Negative Bacteria
- Bacteriostatic activity
- Bactericidal activity
IV. Medications
- Tablets 600 mg
- Suspension 100 mg/5 ml
- Gently turn bottle 5 times to mix (do not shake)
- May store at room Temperature
V. Dosing
- Adult (or child age >12 years)
- Take 600 mg orally or IV infused over 30 to 120 min every 12 hours
- Child (age <12 years)
- Take 10 mg/kg (up to 600 mg) orally or IV infused over 30 to 120 min every 8 hours
VI. Adverse Effects
- Rash
- Headache
- Diarrhea
- Nausea or Vomiting
- Insomnia
- Constipation
- Fever
- Lactic Acidosis
- Myelosuppression (requires discontinuation)
- Thrombocytopenia (2.4%)
-
Neuropathy (with use >1 month)
- Optic Neuropathy (dilated Eye Exam if symptoms occur)
- Peripheral Neuropathy
VII. Safety
- Pregnancy category C
- Unknown safety in Lactation
VIII. Pharmacokinetics
- Half Life: 5 hours
- Near 100% Bioavailability after oral intake
IX. Drug Interactions
- No Cytochrome P450 activity or related Drug Interaction
- Reversible MAO Inhibitor (Hypertensive response)
- Limit Tyramine Containing Foods (<100 mg/meal)
- Avoid with adrenergic drugs
- Avoid concurrent Pseudoephedrine use
- Use caution with concurrent Dopamine or Epinephrine (decrease initial dosing)
-
Serotonin Syndrome (theoretical, rare)
- Not observed in Clinical Trials
- Use caution with SSRI and SNRI Antidepressants
-
Rifampin
- May decrease Linezolid levels and effect
- Hypoglycemic agents or Insulin
- Increased Hypoglycemia risk
X. Monitoring
- See Tedizolid (Sivextro) which does not require cbc monitoring
- Linezolid (Zyvox)
- Weekly Complete Blood Count Indications
- Linezolid use longer than 2 weeks
- Preexisting Myelosuppression or risk factors
- Chronic infection on concurrent other Antibiotics
- Weekly Complete Blood Count Indications
XI. Resources
Images: Related links to external sites (from Bing)
Related Studies
| linezolid (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| LINEZOLID 600 MG TABLET | Generic | $1.66 each |
Ontology: linezolid (C0663241)
| Definition (NCI) | A synthetic oxazolidinone derivative, Linezolid selectively inhibits an early step in bacterial protein synthesis and affects blood pressure through monoamine oxidase inhibition. It is effective against Gram-positive organisms, including methicillin-resistant Staphylococcus aureus strains, coagulase-negative Staphylococci, vancomycin-resistant Enterococci, and penicillin-resistant Streptococcus pneumoniae strains. (NCI04) |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C098010 |
| SnomedCT | 125695009, 387056004 |
| LNC | LP21256-0, MTHU013614 |
| English | N-((3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazolidinyl)methyl)acetamide, linezolid (medication), linezolid, linezolid [Chemical/Ingredient], LINEZOLID, linezolide, Linezolid (product), Linezolid (substance), Linezolid |
| Spanish | linezolid, linezolid (producto), linezolida (producto), linezolid (sustancia), linezolida, linezolida (sustancia) |
Ontology: Zyvox (C0876226)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C098010 |
| English | Zyvox, zyvox |
Ontology: Oxazolidinones (C0887953)
| Definition (MSH) | Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents. |
| Concepts | Organic Chemical (T109) , Antibiotic (T195) |
| MSH | D023303 |
| SnomedCT | 125686001, 372649007 |
| Swedish | Oxazolidinoner |
| Czech | oxazolidinony |
| Finnish | Oksatsolidinonit |
| Russian | OKSAZOLIDINONY, 1,3-OKSAZOLIDIN-2-ON, OKSAZOLIDIN-2-ON, ОКСАЗОЛИДИН-2-ОН, ОКСАЗОЛИДИНОНЫ, 1,3-ОКСАЗОЛИДИН-2-ОН |
| Japanese | オクサゾリジン-2-オン, 1,3-オキサゾリジン-2-オン, オキサゾリジノン |
| Croatian | Not Translated[Oxazolidinones] |
| English | Oxazolidinones [Chemical/Ingredient], oxazolidinone, oxazolidinones, Oxazolidinones, Oxazolidinone -class of antibiotic- (product), Oxazolidinone -class of antibiotic- (substance), Oxazolidinone -class of antibiotic-, Oxazolidinone Antibacterials |
| Polish | Oksazolidynony |
| Spanish | oxazolidinona (clase de antibiótico) (producto), oxazolidinona (clase de antibiótico) (sustancia), oxazolidinona (clase de antibiótico), oxazolidinona - clase de antibiótico (sustancia), oxazolidinona - clase de antibiótico, Oxazolidinonas |
| French | 1,3-oxazolidine-2-one, Oxazolidine-2-one, Oxazolidinones |
| German | Oxazolidinone |
| Italian | Oxazolidinoni |
| Portuguese | Oxazolidinonas |
