Linezolid oral / injection

Follow all directions on your prescription label. Do not use this medicine in larger or smaller amounts or for longer than recommended.

Injectable linezolid is injected into a vein through an IV. You may be shown how to use an IV at home. Do not self-inject this medicine if you do not understand how to give the injection and properly dispose of used needles, IV tubing, and other items used to inject the medicine.

Before taking the oral suspension (liquid), gently mix it by turning the bottle upside down 3 to 5 times. Do not shake. Measure the liquid with a special dose-measuring spoon or medicine cup. If you do not have a dose-measuring device, ask your pharmacist for one.

You may take linezolid with or without food.

While using linezolid, you may need frequent blood tests. Your vision and blood pressure may also need to be checked often.

Use this medication for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Linezolid will not treat a viral infection such as the common cold or flu.

Store all forms of linezolid at room temperature away from moisture, heat, and light. Do not freeze. Throw away any unused oral liquid that is more than 21 days old.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

600 mg IV or orally every 12 hours

Duration of therapy:
-Pneumonia: 10 to 14 consecutive days
-Vancomycin-resistant Enterococcus faecium infections: 14 to 28 consecutive days

Uses: For the treatment of community-acquired pneumonia due to Streptococcus pneumoniae (including cases with concurrent bacteremia) or Staphylococcus aureus (methicillin-susceptible isolates only); for the treatment of nosocomial pneumonia due to S aureus (methicillin-susceptible and -resistant isolates) or S pneumoniae; for the treatment of vancomycin-resistant E faecium infections (including cases with concurrent bacteremia)

600 mg IV or orally every 12 hours

Duration of therapy:
-Pneumonia: 10 to 14 consecutive days
-Vancomycin-resistant Enterococcus faecium infections: 14 to 28 consecutive days

Uses: For the treatment of community-acquired pneumonia due to Streptococcus pneumoniae (including cases with concurrent bacteremia) or Staphylococcus aureus (methicillin-susceptible isolates only); for the treatment of nosocomial pneumonia due to S aureus (methicillin-susceptible and -resistant isolates) or S pneumoniae; for the treatment of vancomycin-resistant E faecium infections (including cases with concurrent bacteremia)

Complicated infections: 600 mg IV or orally every 12 hours
Uncomplicated infections: 400 mg orally every 12 hours

Duration of therapy: 10 to 14 consecutive days

Uses: For the treatment of complicated skin and skin structure infections (including diabetic foot infections, without concomitant osteomyelitis) due to S aureus (methicillin-susceptible and -resistant isolates), S pyogenes, or S agalactiae; for the treatment of uncomplicated skin and skin structure infections due to S aureus (methicillin-susceptible isolates only) or S pyogenes

Less than 7 days, gestational age less than 34 weeks: 10 mg/kg IV or orally every 12 hours
Less than 7 days, gestational age at least 34 weeks: 10 mg/kg IV or orally every 8 hours
7 days through 11 years: 10 mg/kg IV or orally every 8 hours
12 years or older: 600 mg IV or orally every 12 hours

Duration of therapy:
-Pneumonia: 10 to 14 consecutive days
-Vancomycin-resistant E faecium infections: 14 to 28 consecutive days

Comments:
-In preterm neonates younger than 7 days (gestational age less than 34 weeks) with suboptimal clinical response, may consider using 10 mg/kg every 8 hours

Uses: For the treatment of community-acquired pneumonia due to S pneumoniae (including cases with concurrent bacteremia) or S aureus (methicillin-susceptible isolates only); for the treatment of nosocomial pneumonia due to S aureus (methicillin-susceptible and -resistant isolates) or S pneumoniae; for the treatment of vancomycin-resistant E faecium infections (including cases with concurrent bacteremia)

Hemodialysis: Dose should be administered after dialysis.
Peritoneal dialysis: Data not available

Comments:
-About 30% of dose removed in 3-hour hemodialysis session beginning 3 hours after dose administered.

Summary of Use during Lactation

Linezolid is excreted into breastmilk in concentration likely to be effective against staphylococcal strains found in mastitis.[1][2] Limited data indicate that the maximum dose an infant would receive through breastmilk would be much less than the standard infant dose.

If linezolid is required by the mother, it is not a reason to discontinue breastfeeding. Monitor the infant for possible effects on the gastrointestinal tract, such as diarrhea, vomiting, and candidiasis (e.g., thrush, diaper rash). However, because there is no published experience with linezolid during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.

Drug Levels

Maternal Levels. A 32-year-old lactating woman was given a single dose of 600 mg of linezolid orally. Milk samples were taken at 10 time points over the next 24 hours. The peak concentration of linezolid in breastmilk occurred 2 hours after the dose with a value of 12.4 mg/L. Milk concentrations fell with a half-life of 6.5 hours and were detectable up to 24 hours after the dose.[2] Using the peak milk level data from this patient, an exclusively breastfed infant would receive an estimated maximum of about 2 mg/kg daily with the maximum recommended maternal dosage. The established maximum dosage of linezolid for infants is 30 mg/kg daily.

A woman was given oral linezolid 600 mg every 12 hours for methicillin-resistant Staph. aureus mastitis. She pumped milk from both breasts 8 times daily on days 1 and 14 of therapy. Peak breastmilk linezolid levels were 9.75 mg/L on day 1 and 18.73 mg/L on day 14. The authors calculated that a fully breastfed infant would receive 7.85% of the weight-adjusted maternal dosage on day 1 and 15.61% on day 14. Using the average milk level on day 14, a fully breastfed infant would receive a dosage of 1.84 mg/kg daily, which is less than the maximum dosage of linezolid for infants of 30 mg/kg daily.[3]

Infant Levels. Relevant published information was not found as of the revision date.

Effects in Breastfed Infants

Relevant published information was not found as of the revision date.

Effects on Lactation and Breastmilk

Relevant published information was not found as of the revision date.

Alternate Drugs to Consider

(Methicillin-resistant Staph. aureus) Doxycycline, Minocycline, Trimethoprim-Sulfamethoxazole, Vancomycin

References

1. Delgado S, Arroyo R, Jimenez E et al. Staphylococcus epidermidis strains isolated from breast milk of women suffering infectious mastitis: potential virulence traits and resistance to antibiotics. BMC Microbiol. 2009;9:82. PMID: 19422689

2. Sagirli O, Onal A, Toker S, Oztunc A. Determination of linezolid in human breast milk by high-performance liquid chromatography with ultraviolet detection. J AOAC Int. 2009;92:1658-62. PMID: 20166583

3. Rowe HE, Felkins K, Cooper SD, Hale TW. Transfer of linezolid into breast milk. J Hum Lact. 2014;30:410-2. PMID: 25098610

Substance Name

Linezolid

CAS Registry Number

165800-03-3

Drug Class

Anti-Infective Agents

Anti-Bacterial Agents