Lefamulin

Lefamulin is a prescription medication indicated for the treatment of community-acquired bacterial pneumonia (CABP) in adults caused by susceptible microorganisms.

• Lefamulin is available under the following different brand names: Xenleta

Common side effects of Lefamulin include:

• injection site reactions
• elevated liver enzymes
• nausea
• low blood potassium
• insomnia
• headache
• diarrhea
• vomiting

Serious side effects of Lefamulin include

• allergic reactions
• urinary retention
• atrial fibrillation
• palpitations
• oropharyngeal candidiasis
• vulvovaginal candidiasis
• QT prolongation

Rare side effects of Lefamulin include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms such as fast, irregular, or pounding heartbeats; fluttering in your chest; shortness of breath; and sudden dizziness, lightheadedness, or passing out;
• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to the FDA at 1-800-FDA-1088.

Adult dosage

Tablet

• 600 mg

Intravenous solution

• 150 mg/15 mL 0.9% NaCl (further dilution required)

Community-Acquired Bacterial Pneumonia

Adult dosage

• 150 mg IV every 12 hours x 5-7 days or
• 600 mg orally every 12 hours x 5 days

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, 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, healthcare provider, or pharmacist first.

• Lefamulin has no noted severe interactions with any other drugs
• Lefamulin has no noted serious interactions with any other drugs
• Lefamulin has no noted moderate interactions with any other drugs
• Lefamulin has no noted minor interactions with any other drugs

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about 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 healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• Hypersensitivity
• Coadministration with sensitive CYP3A4 substrates that prolong QT interval

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Lefamulin?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Lefamulin?”

Cautions

• Prescribing antibiotics in the absence of proven or strongly suspected bacterial infection increases the risk of drug-resistant bacteria developing
• C difficile-associated diarrhea (CDAD) has been reported with the use of nearly all antibacterial agents, including lefamulin; if suspected or confirmed, ongoing antibacterial drug use not directed against C difficile may need to be discontinued and treatment modalities specific for C difficile initiated; evaluate patients who develop diarrhea
• Based on animal studies, it may cause fetal harm
• QT prolongation
  • Potential to prolong QT interval
  • Avoid in patients with known QT prolongation, ventricular arrhythmias including torsades de pointes, or receiving other drugs known to prolong QT interval (eg, Class IA or Class III antiarrhythmics, antipsychotics, erythromycin, pimozide, moxifloxacin, TCAs)
  • In patients with hepatic impairment or renal failure who require dialysis, metabolic disturbances associated with renal failure may lead to QT prolongation
  • If unable to avoid use in specific populations predisposed to QT prolongation or those receiving another drug that prolongs the QT interval, ECG monitoring is recommended during treatment
  • The magnitude of QT prolongation may increase with increasing lefamulin concentrations or increasing IV infusion rate; do not exceed the recommended dose or infusion rate
• Drug interactions overview
• Lefamulin is a CYP3A4 and P-gp substrate; it is also a moderate CYP3A4 inhibitor
  • Strong or moderate CYP3A or P-gp inducers: Avoid coadministration
  • Strong CYP3A or P-gp inhibitors: Avoid coadministration
  • Moderate CYP3A or P-gp inhibitors: Monitor for lefamulin adverse effects
  • Sensitive CYP3A4 substrates that prolong QT interval: Contraindicated
  • Other sensitive CYP3A4 substrates: Monitor for adverse effects of sensitive CYP3A4 substrates if coadministered with lefamulin tablets (injection does not affect exposure of CYP3A4 substrates
• Other drugs that prolong QT interval: If unable to avoid, ECG monitoring is recommended during treatment

Pregnancy and Lactation

• Based on animal studies, it may cause fetal harm
• Verify pregnancy status in women of reproductive potential before starting treatment
• Contraception
  • Advise females of reproductive potential to use contraception during treatment and for 2 days after the final dose
• Lactation
  • No data are available on the presence of lefamulin in human milk, the effects on the breastfed infant, or the effects on milk production
  • Available data in animals have shown lefamulin excreted in milk
  • If a drug is present in animal milk, it is likely the drug will be present in human milk
  • Owing to the potential for serious adverse effects, instruct lactating women to pump and discard milk for the duration of treatment and for 2 days after the final dose