Names and pronunciation
(le-FAMue-lin) Xenleta
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Drug reference
(le-FAMue-lin) Xenleta
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Func. class.: Antiifective
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Chem. class.: Pleuromutilin antibiotics
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ACTION: May be bacteriostatic or bactericidal depending on the organism; inhibits bacterial protein synthesis through interactions (hydrogen bonds, hydrophobic interactions, and Van der Waals forces) in rRNA of the 50S subunit
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USES: Treatment of community acquired bacterial pneumonia caused by Chlamydophila pneumoniae, Haemophi- lus influenzae (β-lactamase negative), Haemophilus influenzae (β-lactamase positive), Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Mycoplasma pneumoniae, Staphylococcus aureus (MRSA), Staphy- lococcus aureus (MSSA), Streptococcus agalactiae (group B streptococci), Strep- tococcus anginosus, Streptococcus mitis, Streptococcus pneumoniae, Strep- tococcus pyogenes (group A β-hemolytic streptococci), Streptococcus salivarius
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CONTRAINDICATIONS Hypersensitivity to this product or pleuromu- tilin antibiotics; use with CYP3A4 substrates Precautions: Alcoholism, bradycardia, breastfeeding, car- diac disease, contraception requirements, CAD, diabetes mellitus, dialysis, diarrhea, geriatrics, hepatic disease, hypertension, hy- pocalcemia, hypokalemia, hypomagnese- mia, long QT syndrome, renal failure, repro- ductive risk, thyroid disease, torsades de pointes, ventricular dysrhythmias
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SIDE EFFECTS GI: Nausea, diarrhea, CDAD, vomiting CNS: Insomnia, headache META: Hypokalemia
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INTERACTIONS Decreased: Lefamulin effect—strong or moderate CYP3A inducers or P-gp induc- ers; avoid using together; if used, moni- tor for reduced effect Increased: lefamulin effect—strong CYP3A inhibitors or P-gp inhibitors; avoid using together; if used together, monitor for adverse reactions Increased: QT interval—CYP3A sub- strates; do not use together
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DOSAGE AND ROUTES • Adults: PO 600 mg q12hr × 5 days; IV 150 mg q12hr × 5-7 days Hepatic dose • Adults: IV Give over 60 min q24hr (Child-Pugh Class C); PO not recommended for patients with moderate (Child-Pugh Class B) or severe (Child-Pugh Class C)
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Available forms: Tablet 600 mg; solution for injection 150 mg/15 mL (10 mg/mL)
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Administer: PO route • If a dose is missed, give the dose as soon as possible and anytime up to 8 hr before the next scheduled dose; if less than 8 hr remain before the next scheduled dose, do not give the missed dose, and resume dos- ing at the next scheduled dose • Administer at least 1 hour before a meal or 2 hr after a meal • Swallow tablet whole with 6 to 8 ounces of water; do not crush or divide tablets • Intermittent IV route Visually inspect for particulate matter and discoloration prior to use, do not use if present Dilution: Dilute the entire 15-mL vial into the supplied diluent bag; mix thoroughly; do not use the diluent bag in series con- nections, do not admix Storage: Store up to 24 hr at room tem- perature and up to 48 hr when refriger- ated at 2°C to 8°C (36°F to 46°F) • Infuse over 60 min
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Assess: • Pneumonia: Assess for signs of pneumonia • QT prolongation: Assess for QT prolon gation
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Evaluate: Therapeutic response: decreasing symp- toms of pneumonia, culture negative
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • Advise patients to take at least 1 hr before a meal or 2 hr after a meal and should be swallowed whole with water (6-8 ounces); do not crush or divide • That nausea/vomiting is common • That serious allergic reactions may occur and require immediate attention • To take exactly as directed, not to skip doses or not complete the full course of therapy • CDAD, diarrhea: Assess for diarrhea that is watery or has mucous, with or without fever, stomach cramps that may occur up to 2 months after final dose • Pregnancy/breastfeeding: Identify if pregnancy is planned or suspect, or if breastfeeding, pregnancy testing will be needed before use; use adequate contra ception during use and for 2 days after final dose; not to be used in pregnancy; if used inadvertently during pregnancy or if a pa tient becomes pregnant while receiving product, report exposure by calling 1-855-5NABRIVA to enroll; if breastfeeding, pump and discard milk for the duration of treatment and for 2 days after the final dose
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PHARMACOKINETICS Protein binding 94.8% to 97.1%, metabo- lized by CYP3A4; excreted urine 15.5% (9.6%-14.1% unchanged) after IV, 5.3% (unchanged after PO, excreted feces 77.3% (4.2%-9.1% unchanged) after IV and 88.5% (7.8%-24.8% unchanged) after PO; half-life is 3-20 hr; is a CYP3A4 and P-glycoprotein (P-gp) substrate; inhibits CYP2C8, breast cancer resistance protein (BCRP), and MATE1; PO peak 0.88-2 hr
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• Adults: PO 600 mg q12hr × 5 days; IV 150 mg q12hr × 5-7 days Hepatic dose
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• Adults: IV Give over 60 min q24hr (Child-Pugh Class C); PO not recommended for patients with moderate (Child-Pugh Class B) or severe (Child-Pugh Class C)
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