Linezolid

Linezolid is a prescription drug used as an antibiotic to treat certain serious bacterial infections. It works by stopping the growth of bacteria.

Linezolid treats only bacterial infections. It will not work for viral infections (such as common cold, flu). Using any antibiotic when it is not needed can cause it to not work for future infections.

Linezolid also belongs to a class of drugs known as monoamine oxidase (MAO) inhibitors. It can increase the levels of certain natural substances in the body (such as dopamine, norepinephrine, and, serotonin) which can increase the chance of certain side effects and food and drug interactions.

Linezolid is available under the following different brand names: Zyvox.

Dosage of Linezolid:

Adult and Pediatric Dosages:

Injectable solution

• 2 mg/ml (100 ml, 300 ml infusion bags)

Oral suspension

• 100 mg/ml

Tablet

• 600 mg

Dosing Considerations – Should be Given as Follows:

Vancomycin-Resistant Enterococcal Infections

Adults:

• 600 mg orally/intravenously every 12 hours for 14-28 days

Pediatric:

• Children under 12 years old: 10 mg/kg orally/intravenously every 8 hours for 14-28 days
• Children 12 years and older: 600 mg orally/intravenously every 12 hours for 14-28 days

Complicated Skin and Skin Structure Infections

Adults:

• 600 mg orally/intravenously every 12 hours for 10-14 days

Pediatric:

• Children under 12 years old: 10 mg/kg orally/intravenously every 8 hours for 10-14 days
• Children 12 years and older: 600 mg orally/intravenously every 12 hours for 10-14 days

Uncomplicated Skin and Skin Structure Infections

Adults:

• 400-600 mg orally every 12 hours for 10-14 days

Pediatric:

• Children under 5 years old: 10 mg/kg orally every 8 hours for 10-14 days
• Children 5-12 years old: 10 mg/kg orally every 12 hours for 10-14 days
• Children 12 years and older: 600 mg orally every 12 hours for 10-14 days

Community-Acquired Pneumonia (Including Concurrent Bacteremia)

Adults:

• 600 mg orally/intravenously every 12 hours for 10-14 days

Pneumonia

Pediatric:

• Children under 12 years old: 10 mg/kg orally/intravenously every 8 hours for 10-14 days
• Children 12 years and older: 600 mg orally/intravenously every 12 hours for 10-14 days

Nosocomial Pneumonia

• 600 mg orally/intravenously every 12 hours for 10-14 days

Methicillin-Resistant Staphylococcal Infections

• 600 mg orally/intravenously every 12 hours

Methicillin-Susceptible Staphylococcus aureus

• 600 mg orally/intravenously every 12 hours for 10-14 days

Dosing Considerations

• Monitor, CBC count each week

Side effects of linezolid include:

Pediatric:

• diarrhea
• vomiting
• headache
• red blood cell deficiency
• low blood platelet count
• nausea
• abdominal pain
• loose stools
• increased white blood cells
• itching, other than application site
• spinning sensation

Adult:

• headache
• diarrhea
• nausea
• vomiting
• dizziness
• rash
• vaginal yeast infection
• taste alteration
• oral thrush
• abnormal liver function tests
• abnormal blood tests
• fungal infection
• abdominal pain
• tongue discoloration

Postmarketing side effects of linezolid reported include:

• superficial tooth discoloration
• superficial tongue discoloration
• low blood platelet count
• low white blood cell count
• reduced white, red, and platelet blood cell count
• platelet deficiency in the blood
• numbness and tingling in arms and legs
• damage to the nerve of the eye
• lactate buildup (lactic acidosis)
• serotonin syndrome (high body temperature, agitation, increased reflexes, shakiness, sweating, dilated pupils, and diarrhea)
• convulsions (seizures)
• severe allergic reaction (anaphylaxis)
• rapid swelling
• bullous skin disorders (Stevens-Johnson Syndrome)
• low blood glucose

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Linezolid has severe interactions with at least 48 different drugs.
• Linezolid has serious interactions with at least 112 different drugs.
• Linezolid has moderate interactions with at least 43 different drugs.
• Linezolid has mild interactions with at least 23 different drugs.

This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns, or for more information about this medicine.

Warnings

This medication contains a linezolid. Do not take Zyvox if you are allergic to linezolid or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately

Contraindications

• Hypersensitivity
• Within 14 days of taking MAO inhibitor

Effects of Drug Abuse

• No information available

Short-Term Effects

• See "What Are Side Effects Associated with Using Linezolid?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Linezolid?"

Cautions

• Use caution in patients with pheochromocytoma, concurrent apraclonidine, brimonidine, uncontrolled hypertension, thyrotoxicosis, carcinoid syndrome, diabetes mellitus, or seizure disorders
• Use oral suspension with caution in phenylketonuria (contains phenylalanine)
• Not approved for gram-negative bacteria or for catheter-related infections; the clinical study showed a higher mortality rate with linezolid than with other antibiotics for these conditions
• Monitor for myelosuppression, consider discontinuation in patients who develop or have worsening myelosuppression
• Evaluate for Clostridium difficile if diarrhea occurs
• Peripheral and optic neuropathy were reported, especially in patients given extended courses of therapy exceeding 28 days
• May cause low blood sugar (hypoglycemia); monitor blood glucose levels
• Lactic acidosis reported with use; immediately evaluate patients who develop recurrent unexplained acidosis with nausea and vomiting
• Superinfection may develop
  • Serotonin syndrome
• Avoid coadministration with serotonergic psychiatric drugs (SSRIs, SNRIs, TCAs, and MAOIs) unless indicated for life-threatening or urgent infections (vancomycin-resistant enterococcal infections, nosocomial pneumonia, complicated skin and skin structure infections such as methicillin-resistant S aureus), due to increased risk of serotonin syndrome
• Linezolid may increase serotonin central nervous system levels by MAO-A inhibition
• If linezolid must be administered to a patient currently taking a serotonergic drug, stop the serotonergic drug immediately and monitor for central nervous system toxicity; serotonergic therapy may be resumed 24 hours after the last linezolid dose or after 2 weeks of monitoring (5 weeks if fluoxetine was taken), whichever comes first
• Serotonergic psychiatric medications should be stopped at least 2 weeks in advance of linezolid therapy; fluoxetine should be stopped at least 5 weeks in advance due to longer half-life

Pregnancy and Lactation

• Use linezolid during pregnancy with caution if benefits outweigh risks
• Animal studies show risk and human studies are not available, or neither animal nor human studies were done
• Safety of linezolid when breastfeeding is unknown; consult your physician