Lefabac

Lefamulin Acetate is indicated for the treatment of adults with community-acquired bacterial pneumonia (CABP) caused by the following susceptible microorganisms: Streptococcus pneumoniae, Staphylococcus aureus (methicillin susceptible isolates), Haemophilus influenzae, Legionella pneumophila, Mycoplasma pneumoniae, and Chlamydophila pneumoniae.

Lefamulin Acetate is a semi-synthetic antibacterial agent for oral and intravenous administration. Lefamulin features a novel mechanism of action that shows benefits against resistant bacteria that cause pneumonia. Lefamulin is a systemic pleuromutilin antibacterial. It inhibits bacterial protein synthesis through interactions (hydrogen bonds, hydrophobic interactions, and Van der Waals forces) with the A-and P-sites of the peptidyl transferase center (PTC) in domain V of the 23s rRNA of the 50S subunit.

With Medicine: Concomitant use of oral or intravenous Lefamulin IV with strong CYP3A4 inducers or P-glycoprotein inducers decreases Lefamulin AUC and C which may reduce the efficacy of Lefamulin IV. Avoid concomitant use of Lefamulin IV Injection with strong and moderate CYP3A4 inducers or P-glycoprotein inducers unless the benefit outweighs the risks.

With Food and Others: Exercise caution with grapefruit products. Grapefruit inhibits CYP3A, which may increase the serum concentration of Lefamulin.

Lefamulin Acetate has the potential to prolong the QT interval. Avoid Lefamulin in patients with known QT prolongation, ventricular arrhythmias, and patients receiving drugs that may prolong the QT interval. Clostridioides difficile-associated diarrhea (CDAD) has been reported with nearly all systemic antibacterial agents, including Lefamulin, with severity ranging from mild diarrhea to fatal colitis.

Pregnancy: No clinical studies have been performed in pregnant women Animal studies indicate that administration of Lefamulin Acetate resulted in an increased incidence of stillbirth Malformations were also observed in rats at systemic exposures lower than the systemic exposure in CAP patients Lefamulin IV should be used during pregnancy only if the potential benefit justifies the potential risk to the mother and fetus

Lactation: There are no data on the presence of Lefamulin Acetate in human milk, its effects on the breastfed infant or its effects on milk production. Animal studies indicate that Lefamulin was concentrated in the milk of lactating rats. Because of the potential for senous adverse reactions, including QT interval prolongation, a woman should pump and discard human milk for the duration of treatment with Lefamulin IV and for 2 days after the final dose.

Clostridium Difficile-Associated Disease (CDAD) has been reported with the use of many antibacterial agents, including Lefamulin IV CDAD may range in severity from mild diarrhea to fatal colts. It is important to consider this diagnosis in patients who present with diarrhea or symptoms of colitis, pseudomembranous colitis, toxic megacolon or perforation of the colon subsequent to the administration of any antibacterial agent. Lefamulin IV has the potential to prolong the QT interval of the electrocardiogram (ECG) in some patients. Avoid Lefamulin IV use in the following patients

• Patients with known prolongation of the QT interval
• Patients with ventricular arrhythmias including torsades de pointes
• Patients receiving Class IA (for example, quinidine, procainamide) or Class IIIA (for example, amiodarone, sotalol) antiarrhythmic agents
• Patients receiving other drugs that prolong the QT interval, such as antipsychotics, erythromycin, pimozide, moxifloxacin, and tricyclic anti-depressants

Other antibacterial preparation

Treatment of overdose with Lefamulin IV should consist of observation and general support measures. The stomach should be emptied Adequate hydration should be maintained and electrolytes monitored. Electrocardiogram (ECG) monitoring is recommended. Hemodialysis will not significantly remove Lefamulin IV from systemic circulation

IV Infusion: Store in a refrigerator at 2°C to 8°C. Do not freeze and protect from light. Keep out of the reach of children.
Tablet: Do not store above 30°C. Do not refrigerate or freeze. Keep in a dry place. Protect from light & keep out of the reach of children.