A systemic antibacterial drug with a novel mechanism of action to combat community acquired bacterial pneumonia.
Marketed as Xenleta, administered both orally and intravenously.
A semi synthetic pleiromutilin that inhibits prokaryotic ribosomal proteins synthesis that reduces its likelihood of developing resistance to bacteria or cross resistance with the beta-lactam, fluoroquinolone, glycopeptide, macrolide, and tetracycline antibiotic classes.
It binds to the peptidyl transfer center of the 50S subunit of the bacterial ribosome, inhibiting bacterial protein synthesis.
The probability of cross resistance to beta-lactams, macrolides, fluoroquinolones, tetracyclines, or glycopeptides appears to be low.
It’s spectrum of activity is similar to fluoroquinolones.
A semi synthetic pleuromutilin antibiotic approved for IV and oral treatment of community acquired bacterial pneumonia in adults.
An antibiotic used it to treat adults with community-acquired bacterial pneumonia.
It is active against the most common community acquired bacterial pneumonia pathogens, including some strains resistant to others antimicrobial classes.
Has in vitro activity against Streptococcus viridans, Moraxella catarrhalis, Enterococcus faecium, methicillin-resistant Staphylococcus aureus (MRSA), among other bacteria.
Relatively common side effects include diarrhea, nausea, pain at the site of injection, and liver inflammation.
It can prolong the QT interval.
Patients with liver or renal disease or are at increased risk for prolongation of the QT interval.
It is also being investigated for treatment of acute bacterial skin and skin-structure infections.
A five day trial of oral lefamulin was found to be non-inferior to seven day oral moxifloxacin in the management of community acquired bacterial pneumonia.
Use can be associated with C. difficile associated diarrhea.
Metabolized primarily by CYP3A4.
Dosage-600 mg orally every 12 hours for five days or 150 mg infused IV over 60 minutes every 12 hours for 5-7 days.
Tablets should be swallowed whole.
Dose should be reduced significantly with IV treatment for patients with severe hepatic impairment.
Oral drug is not recommended for use in patients with moderate or severe liver involvement.
No adjustment is needed for renal impairment.