Linezolid

Dosage Forms & Strengths

injectable solution

• 2mg/mL (100mL, 300mL infusion bags)

oral suspension

• 100mg/5mL

tablet

• 600mg

Vancomycin-Resistant Enterococcal Infections

600 mg PO/IV q12hr for 14-28 days

Complicated Skin & Skin Structure Infections

600 mg PO/IV q12hr for 10-14 days

Uncomplicated Skin & Skin Structure Infections

400-600 mg PO q12hr for 10-14 days

Community-Acquired Pneumonia (Including Concurrent Bacteremia)

600 mg PO/IV q12hr for 10-14 days

Nosocomial Pneumonia

600 mg PO/IV q12hr for 10-14 days

Methicillin-Resistant Staphylococcal Infections

600 mg PO/IV q12hr

Methicillin-Susceptible Staphylococcus Aureus

600 mg PO/IV q12hr for 10-14 days

Dosing Considerations

Monitor: CBC count qWeek

Dosage Forms & Strengths

injectable solution

• 2mg/mL (100mL, 300mL infusion bags)

oral suspension

• 100mg/5mL

tablet

• 600mg

Complicated Skin & Skin Structure Infections

<12 years: 10 mg/kg PO/IV q8hr for 10-14 days 

≥12 years: 600 mg PO/IV q12hr for 10-14 days

Uncomplicated Skin & Skin Structure Infections

<5 years: 10 mg/kg PO q8hr for 10-14 days 

5-12 years: 10 mg/kg PO q12hr for 10-14 days

>12 years: 600 mg PO q12hr for 10-14 days

Pneumonia

<12 years: 10 mg/kg PO/IV q8hr for 10-14 days 

≥12 years: 600 mg PO/IV q12hr for 10-14 days

Vancomycin-Resistant Enterococcal Infections

<12 years: 10 mg/kg PO/IV q8hr for 14-28 days 

≥12 years: 600 mg PO/IV q12hr for 14-28 days

Dosing Considerations

Monitor: CBC count qWeek

>10%

Pediatrics

• Diarrhea (7.8-10.8%)

1-10%

Headache (5.7-8.8%)

Diarrhea (8.2-8.3%)

Nausea (5.1-6.6%)

Vomiting (2-4.3%)

Dizziness (1.8-2.6%)

Rash (1.1-2.3%)

Vaginal moniliasis (1.1-1.8%)

Taste alteration (1-1.8%)

Oral moniliasis (0.5-1.7%)

Abnormal LFTs (0.4-1.6%)

Fungal infection (0.3-1.5%)

Localized abdominal pain (1.2-1.3%)

Tongue discoloration (0.3-1.3%)

Generalized abdominal pain (0.9-1.2%)

Pediatrics

• Vomiting (2.9-9.4%)
• Headache (0.9-6.5%)
• Anemia (5.6%)
• Thrombocytopenia (4.7%)
• Nausea (1.9-3.7%)
• Generalized abdominal pain (0.9-2.4%)
• Localized abdominal pain (0.5-2.4%)
• Loose stools (1.6-2.3%)
• Eosinophilia (0.4-1.9%)
• Pruritus, other than application site (0.8-1.4%)
• Vertigo (1.2%)

<1%

Lactic acidosis

Myelosuppression

Peripheral neuropathy

Disorder of optic nerve

Serotonin syndrome

Postmarketing Reports

Superficial tooth discoloration

Superficial tongue discoloration

Avoid eating or drinking large amounts of foods and beverages containing tyraminewhile taking linezolid. Foods and beverages that have been pickled, smoked, or fermented usually contain tyramine. These foods and beverages include alcoholic beverages, especially beer, Chianti, and other red wines; alcohol-free beer; cheeses (especially strong, aged, or processed varieties); sauerkraut; yogurt; raisins; bananas; sour cream; pickled herring; liver (especially chicken liver); dried meats and sausage (including hard salami and pepperoni); canned figs; avocados; soy sauce; turkey; yeast extracts; papaya products (including certain meat tenderizers); fava beans; and broad bean pods.

Serious side effects have been reported with linezolid. See the “Drug Precautions” section.

Common side effects of linezolid include the following:

• diarrhea
• headache
• nausea
• vomiting
• stomach pain
• difficulty falling asleep or staying asleep
• dizziness
• white patches in the mouth
• change in color of the tongue

• an allergic reaction with the following signs and symptoms:
  • hives
  • rash
  • itching
  • difficulty breathing or swallowing
  • swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
• hoarseness
• blisters or peeling skin
• fever
• loss of coordination
• overactive reflexes
• confusion, forgetfulness, or difficulty thinking
• severe diarrhea (watery or bloody stools) that may occur with or without fever and stomach cramps (may occur months or more after your treatment)
• unusual bleeding or bruising
• cough, chills, sore throat, and other signs of infection
• changes in color vision, blurred vision, or other changes in vision
• seizures

This is not a complete list of linezolid side effects. Ask your doctor or pharmacist for more information.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Linezolid comes as a capsule, an oral liquid, and in an IV injection form. The capsules and oral liquid can be taken with or without food. It is usually taken twice daily (every 12 hours) for 10 to 28 days. Children 11 years of age and younger usually take linezolid two to three times a day (every 8 to 12 hours) for 10 to 28 days. The length of treatment depends on the type and severity of your infection.

Linezolid oral liquid

• Gently mix the oral liquid by turning the bottle over three to five times. Do not shake linezolid liquid.
• For accuracy, measure the oral liquid with an oral syringe or a measuring spoon or medicine cup. Do not use a regular household spoon to measure.
• Throw away any unused oral liquid after 21 days.

Take linezolid exactly as prescribed. Do not skip linezolid doses. If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and resume your regular dosing.

Do not stop taking linezolid before your doctor recommends, even if you are feeling better.

Linezolid injection

For adults, linezolid injection is infused into a vein twice daily for 10 to 28 days. The infusion usually lasts between 30 minutes and 2 hours. Children 11 years of age and younger usually receive Linezolid injections 2 to 3 times daily, for 10 to 28 days.

Injections are usually given by a healthcare professional in a medical facility, however, your doctor may decide that you can be taught to give yourself your injections.

The dose your doctor recommends will depend on your age, weight, and the type and severity of your infection.

• Adults - The usual recommended dose of linezolid in adults is 600 mg every 12 hours. For some infections, including certain skin or soft tissue infections, the recommended dose in adults is 400 mg every 12 hours.
• Children (11 years of age and younger) - The usual dose of linezolid in children is based on weight.
• Children (12 years of age and older) - The usual recommended dose is 600 mg every 12 hours.

• MRSA
• Staph Infection (Staphylococcus Aureus)

• Advise patients that antibacterials (including linezolid) should only be used to treat bacterial infections and not used to treat viral infections (e.g., the common cold).1

• Importance of completing full course of therapy, even if feeling better after a few days.1

• Advise patients that skipping doses or not completing the full course of therapy may decrease effectiveness and increase the likelihood that bacteria will develop resistance and will not be treatable with linezolid or other antibacterials in the future.1

• Advise patients that linezolid may be taken orally without regard to meals.1

• If using the oral suspension, importance of not shaking the bottle vigorously and gently inverting the bottle 3–5 times to resuspend the drug prior to administration of each dose.1

• Advise patients of the potential risk of serotonin syndrome, particularly if linezolid is used concomitantly with MAO inhibitors, SSRIs, SNRIs, tricyclic antidepressants, or other serotonergic drugs.28 Importance of immediately contacting clinician if signs and symptoms of serotonin syndrome develop (e.g., confusion, hyperactivity, memory problems, muscle twitching, excessive sweating, shivering, shaking, diarrhea, loss of coordination, fever).28 Importance of not discontinuing serotonergic drugs without first consulting clinician.28

• Advise patients, particularly those with diabetes mellitus, that hypoglycemic reactions (diaphoresis and tremulousness) and low blood glucose concentrations may occur during linezolid treatment.1 Importance of contacting a clinician to obtain proper treatment if such reactions occur.1

• Importance of avoiding large quantities of foods or beverages with high tyramine content during linezolid treatment;1 this includes foods or beverages that have been aged, fermented, pickled, or smoked to improve flavor (e.g., aged cheeses, fermented or air-dried meats, sauerkraut, soy sauce, tap beer, red wine).1 Consider that tyramine content of any protein-rich food may be increased if stored for long periods or improperly refrigerated.1

• Advise individuals with phenylketonuria that the oral suspension contains aspartame, which is metabolized in the GI tract to provide 20 mg of phenylalanine per 5 mL of suspension.1

• Importance of notifying clinician of any history of hypertension or seizures.1

• Importance of notifying clinician if any change in vision occurs.1

• Advise patients that diarrhea is a common problem caused by anti-infectives and usually ends when the drug is discontinued.1 Importance of contacting a clinician if watery and bloody stools (with or without stomach cramps and fever) occur during or as late as 2 months or longer after the last dose.1

• Importance of informing clinicians of existing or contemplated concomitant therapy including prescription drugs (e.g., antidepressants) and OTC drugs (e.g., pseudoephedrine), as well as any concomitant illnesses.1

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

• Importance of advising patients of other important precautionary information.1 (See Cautions.)

• Antibiotic, Oxazolidinone

Enterococcal infections (vancomycin-resistant): Treatment of vancomycin-resistant (VRE) Enterococcus faecium infections, including cases with concurrent bacteremia. Note: Not a preferred agent in resistant E. faecalis infections which are usually susceptible to beta-lactams (O’Driscoll 2015).

Pneumonia:

Community-acquired: Treatment of community-acquired pneumonia (CAP) caused by Streptococcus pneumoniae, including cases with concurrent bacteremia, or Staphylococcus aureus (methicillin-susceptible isolates only). Note: Not a preferred agent for CAP; may be used as an alternate choice in multi-drug resistant S. pneumoniae and MRSA pneumonia. For methicillin-susceptible S. aureus, the use of beta-lactams is preferred (IDSA/ATS [Mandell 2007]).

Hospital-acquired or healthcare-associated: Treatment of hospital-acquired or healthcare-associated pneumonia caused by S. aureus (methicillin-susceptible and -resistant isolates), or S. pneumoniae. Note: For methicillin-susceptible S. aureus, the use of beta-lactams is preferred (IDSA/ATS [Kalil 2016]).

Skin and skin structure infections:

Complicated: Treatment of complicated skin and skin structure infections, including diabetic foot infections, without concomitant osteomyelitis, caused by S. aureus (methicillin-susceptible and -resistant isolates), Streptococcus pyogenes, or Streptococcus agalactiae.

Uncomplicated: Treatment of uncomplicated skin and skin structure infections caused by S. aureus (methicillin-susceptible isolates) or S. pyogenes.

Note: Generally reserved as alternate for skin and skin structure infections due to MRSA (IDSA [Liu 2011]; IDSA [Stevens 2014]).

Limitations of use: Linezolid has not been studied in the treatment of decubitus ulcers. Linezolid is not indicated for treatment of gram-negative infections; if a concomitant gram-negative pathogen is documented or suspected, initiate specific therapy immediately.

Adverse effects were observed in some animal reproduction studies at doses that were also maternally toxic. Information related to linezolid use during pregnancy is limited.