Generic
Lefamulin
7 brands available in the market
At a glance
Lefamulin is an antibiotic used for the treatment of community-acquired bacterial pneumonia (CABP). It is a first-in-class semi-synthetic pleuromutilin antibiotic that works by inhibiting bacterial protein synthesis.
Description
Lefamulin is a systemic pleuromutilin antibacterial that inhibits bacterial protein synthesis through interactions with the A- and P-sites of the peptidyl transferase center in domain V of the 23S rRNA of the 50S subunit. It is effective against resistant bacteria that cause pneumonia.
Indications
- Community-acquired bacterial pneumonia (CABP) - caused by susceptible microorganisms: Streptococcus pneumoniae, Staphylococcus aureus (methicillin-susceptible), Haemophilus influenzae, Legionella pneumophila, Mycoplasma pneumoniae, Chlamydophila pneumoniae
Therapeutic class
Other Antibacterial Preparations
Pharmacological class
Pleuromutilin Antibiotic
Pharmacology
Lefamulin inhibits bacterial protein synthesis by binding to the peptidyl transferase center of the 50S ribosomal subunit. It works through a novel mechanism that is effective against resistant bacteria that cause pneumonia.
Mechanism of action
Selectively inhibits bacterial translation by binding to the peptidyl transferase component of the ribosome 50S subunit.
Dosage
Adult Dose:
- Injection (IV): 150 mg every 12 hours, 60-minute IV infusion, 5-7 days
- Tablet (PO): 600 mg every 12 hours, 5 days
- Dose adjustment required for severe hepatic impairment (IV: 150 mg every 24 hours; Tablets: not recommended)
Administration
- Tablets: Take at least 1 hour before or 2 hours after a meal; do not crush or divide
- Injection: Dilute in 250 mL citrate buffered 0.9% sodium chloride solution and administer as a 60-minute IV infusion
Missed dose
If a dose is missed, take it as soon as possible and anytime up to 8 hours prior to the next scheduled dose. If less than 8 hours remain, skip the missed dose and resume at the next scheduled dose.
Side effects
Common Side Effects:
- Diarrhea
- Nausea
- Injection site reactions
- Elevated liver enzymes
- Vomiting
- Potential for QT interval prolongation
Precautions & warnings
- Potential for QT interval prolongation - avoid in patients with prolonged QT, ventricular arrhythmias, or taking QT-prolonging drugs
- Clostridioides difficile-associated diarrhea (CDAD) - reported with nearly all systemic antibacterial agents
- Dose adjustment needed for severe hepatic impairment
Contraindications
- Hypersensitivity to Lefamulin, pleuromutilin class drugs, or any components of the product
- Use with CYP3A4 substrates that prolong the QT interval
Drug interactions
- Strong CYP3A4 inducers or P-glycoprotein inducers: Reduced efficacy - avoid use
- Grapefruit products: May increase serum concentration by inhibiting CYP3A - caution
Food interactions
Caution with grapefruit products; may increase serum concentration of Lefamulin by inhibiting CYP3A.
Use in pregnancy
Use in Pregnancy: Animal studies have shown fetal harm; pregnant women should be advised of potential risks. Women who could become pregnant should use effective contraception during treatment and for 2 days after the final dose.
Use in lactation
Use in Lactation: No data on presence in human milk; concentrated in milk of lactating rats. Pump and discard breast milk during treatment and for 2 days after the final dose.
Pediatric use
Safety and efficacy not established in pediatric patients (below 18 years).
Geriatric use
No special studies in elderly; use with caution.
Renal / hepatic impairment
Hepatic Impairment: Mild: no dose adjustment; Moderate-severe: Tablets not recommended; Injection: severe cases 150 mg every 24 hours.
Overdose effects
Overdose treatment: observation and general supportive measures; empty stomach; maintain hydration and monitor electrolytes; ECG monitoring recommended; hemodialysis is not effective.
Storage conditions
Injection: Store refrigerated (2-8°C); do not freeze; protect from light. Tablets: Do not store above 30°C; do not refrigerate or freeze; store in a dry place.
Chemical structure
Lefamulin