Lefamulin
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Omid Afkhami-Ardakani
Disclaimer
WikiDoc MAKES NO GUARANTEE OF VALIDITY. WikiDoc is not a professional health care provider, nor is it a suitable replacement for a licensed healthcare provider. WikiDoc is intended to be an educational tool, not a tool for any form of healthcare delivery. The educational content on WikiDoc drug pages is based upon the FDA package insert, National Library of Medicine content and practice guidelines / consensus statements. WikiDoc does not promote the administration of any medication or device that is not consistent with its labeling. Please read our full disclaimer here.
Overview
Lefamulin is a Pleuromutilin Antibiotic that is FDA approved for the treatment of adults with community-acquired bacterial pneumonia (CABP) caused by susceptible microorganisms.. Common adverse reactions include injection: administration site reactions, hepatic enzyme elevation, nausea, hypokalemia, insomnia, headache.
Oral: diarrhea, nausea, vomiting, hepatic enzyme elevation..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
There is limited information regarding Lefamulin FDA-Labeled Indications and Dosage (Adult) in the drug label.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Lefamulin in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Lefamulin in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
There is limited information regarding Lefamulin FDA-Labeled Indications and Dosage (Pediatric) in the drug label.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Lefamulin in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Lefamulin in pediatric patients.
Contraindications
There is limited information regarding Lefamulin Contraindications in the drug label.
Warnings
QT Prolongation: Lefamulin may cause QT interval prolongation, which can lead to an increased risk of ventricular arrhythmias, including torsades de pointes. Avoid use in patients with known QT prolongation, ventricular arrhythmias, and patients receiving drugs that prolong the QT interval.
Embryo-Fetal Toxicity: Lefamulin may cause fetal harm. Advise females of reproductive potential to use effective contraception during treatment and for two days after the final dose.
Clostridium difficile-associated Diarrhea (CDAD): Evaluate patients who develop diarrhea for CDAD, as it has been reported with nearly all systemic antibacterial agents.
Adverse Reactions
Clinical Trials Experience
njection: administration site reactions, hepatic enzyme elevation, nausea, hypokalemia, insomnia, headache.
Oral: diarrhea, nausea, vomiting, hepatic enzyme elevation.
Postmarketing Experience
There is limited information regarding Lefamulin Postmarketing Experience in the drug label.
Drug Interactions
CYP3A4 Substrates That Prolong the QT Interval: Concomitant use of Lefamulin tablets with CYP3A substrates that prolong the QT interval is contraindicated.
Strong or Moderate CYP3A Inducers or P-gp Inducers: Avoid Lefamulin unless the benefit outweighs the risk. Monitor for reduced efficacy.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
May cause fetal harm. Advise females of reproductive potential to use effective contraception during treatment and for two days after the final dose.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Lefamulin in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Lefamulin during labor and delivery.
Nursing Mothers
A lactating woman should pump and discard human milk for the duration of treatment with Lefamulin and for two days after the final dose.
Pediatric Use
There is no FDA guidance on the use of Lefamulin in pediatric settings.
Geriatic Use
There is no FDA guidance on the use of Lefamulin in geriatric settings.
Gender
There is no FDA guidance on the use of Lefamulin with respect to specific gender populations.
Race
There is no FDA guidance on the use of Lefamulin with respect to specific racial populations.
Renal Impairment
No dosage adjustment is necessary in patients with renal impairment, including those on hemodialysis.
Hepatic Impairment
Reduce the dosage of Lefamulin Injection to 150 mg infused over 60 minutes every 24 hours in patients with severe hepatic impairment (Child-Pugh Class C). Lefamulin Tablets have not been studied in and are not recommended for patients with moderate (Child-Pugh Class B) or severe hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Lefamulin in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Lefamulin in patients who are immunocompromised.
Administration and Monitoring
Administration
Injection: Administer by intravenous infusion over 60 minutes. Must dilute in a 250 mL solution of 10 mM citrate buffered 0.9% sodium chloride for injection before use.
Tablets: Take at least 1 hour before a meal or 2 hours after a meal. Swallow tablets whole with water (6 to 8 ounces).
Monitoring
QT Interval: Monitor ECG in patients with known risk factors for QT prolongation. Liver Function Tests: Monitor hepatic enzymes during treatment.
IV Compatibility
Dilution: Dilute the entire 15 mL vial of Lefamulin Injection into the diluent bag supplied that contains 250 mL of 10 mM citrate buffered 0.9% sodium chloride.
Overdosage
There is limited information regarding Lefamulin overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.
Pharmacology
There is limited information regarding Lefamulin Pharmacology in the drug label.
Mechanism of Action
Lefamulin is a pleuromutilin antibiotic that inhibits bacterial protein synthesis by binding to the peptidyl transferase center of the 50S ribosomal subunit. This unique mechanism interferes with the positioning of transfer RNA, thereby preventing peptide bond formation and inhibiting bacterial growth.
Structure
There is limited information regarding Lefamulin Structure in the drug label.
Pharmacodynamics
Lefamulin exhibits bactericidal activity against certain pathogens, including Streptococcus pneumoniae, Haemophilus influenzae, and Mycoplasma pneumoniae, and bacteriostatic activity against Staphylococcus aureus and Streptococcus pyogenes.
Pharmacokinetics
Absorption: After oral administration, lefamulin reaches peak plasma concentrations within approximately 1 hour. Distribution: Lefamulin is extensively distributed throughout the body, with a volume of distribution of about 100 L. Metabolism: It is metabolized primarily by the liver, involving cytochrome P450 enzymes, particularly CYP3A4. Elimination: The elimination half-life is approximately 8 hours. Excretion occurs via feces (approximately 77%) and urine (approximately 16%).
Nonclinical Toxicology
There is limited information regarding Lefamulin Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Lefamulin Clinical Studies in the drug label.
How Supplied
Tablets: 600 mg, oval, white to off-white, debossed with "LEF" on one side. Injection: 150 mg/15 mL solution in a single-dose vial.
Storage
Tablets: Store at room temperature, 20°C to 25°C (68°F to 77°F), with permissible excursions between 15°C and 30°C (59°F to 86°F).
Injection: Store refrigerated at 2°C to 8°C (36°F to 46°F). Do not freeze.
Images
Drug Images
{{#ask: Page Name::Lefamulin |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}
Package and Label Display Panel
{{#ask: Label Page::Lefamulin |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}
Patient Counseling Information
QT Prolongation: Advise patients of the potential risk of QT interval prolongation and to inform their healthcare provider of any history of cardiac conditions or use of medications that may prolong the QT interval. Diarrhea: Inform patients that diarrhea is a common side effect. Instruct them to contact their healthcare provider if they experience severe or persistent diarrhea, as this may indicate Clostridium difficile-associated diarrhea (CDAD). Pregnancy and Lactation: Advise females of reproductive potential to inform their healthcare provider if they are pregnant or plan to become pregnant. Discuss the potential risks to the fetus and the need for effective contraception during treatment and for two days after the final dose. Drug Interactions: Counsel patients to inform their healthcare provider of all medications they are taking, including over-the-counter drugs and herbal supplements, due to potential interactions.
Precautions with Alcohol
There are no specific contraindications regarding alcohol consumption with lefamulin. However, patients should consult their healthcare provider regarding alcohol use during treatment, especially if they have liver disease or are taking other medications that may interact with alcohol.
Brand Names
Lefamulin is marketed under the brand name XENLETA.
Look-Alike Drug Names
There is limited information regarding Lefamulin Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.