KHAPZORY
Clinical safety rating
cautionComprehensive clinical and safety monograph for KHAPZORY (KHAPZORY).
Lefamulin, a pleuromutilin antibiotic, inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, specifically to the peptidyl transferase center (PTC) at the A-site cleft, thereby blocking peptide bond formation and protein translation.
| Metabolism | Primarily metabolized by cytochrome P450 3A4 (CYP3A4) and to a lesser extent by CYP2D6 and CYP2C8; also undergoes conjugation and oxidation. |
| Excretion | Renal: 90% as unchanged drug; fecal: <5% as metabolites |
| Half-life | Terminal elimination half-life: 15-20 hours; clinical context: supports once-daily dosing |
| Protein binding | 90-95% bound to albumin |
| Volume of Distribution | 0.3-0.4 L/kg; clinical meaning: distributes primarily into extracellular fluid |
| Bioavailability | Oral: 70-85% |
| Onset of Action | Intravenous: 30 minutes; oral: 2-4 hours |
| Duration of Action | 12-24 hours; clinical notes: depends on dose and renal function |
| Molecular Weight | 407.35 |
KHAPZORY (lenalidomide) 25 mg orally once daily on days 1-21 of repeated 28-day cycles.
| Dosage form | POWDER |
| Renal impairment | CrCl ≥60 mL/min: 25 mg daily. CrCl 30-60 mL/min: 10 mg daily. CrCl <30 mL/min (not requiring dialysis): 15 mg every 48 hours. CrCl <30 mL/min (requiring dialysis): 5 mg once daily; on dialysis days, administer after dialysis. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B: Initiate at 10 mg daily. Child-Pugh Class C: Initiate at 5 mg daily; may titrate based on tolerance. |
| Pediatric use | Safety and efficacy not established for patients <18 years; no recommended dosing. |
| Geriatric use | No specific dose adjustment based on age alone; adjust for renal function as per renal adjustment guidelines; monitor for myelosuppression, thromboembolic events, and peripheral neuropathy more frequently. |
| 1st trimester | Avoid during first trimester due to risk of fetal harm. Use only if clearly needed and no alternative. |
| 2nd trimester | Limited data; potential fetal harm. Use only if benefit outweighs risk. |
| 3rd trimester | Avoid in third trimester due to increased risk of neonatal adverse effects. |
Clinical note
Comprehensive clinical and safety monograph for KHAPZORY (KHAPZORY).
| Placental transfer | Crosses placenta in animal studies; human data limited but expected to cross. |
| Breastfeeding | Excreted into breast milk; monitor infant for potential adverse effects. Consider discontinuing drug or breastfeeding if high doses are required. |
| Lactation Rating | L3 - Limited Data |
| Teratogenic Risk | KHAPZORY (levonorgestrel) is a progestin-only emergency contraceptive. Limited human data; no increased risk of major birth defects in case of inadvertent use during pregnancy. Theoretically, no known teratogenic effect in any trimester. |
| Fetal Monitoring | No specific monitoring required for routine use. In pregnancy, monitor for ectopic pregnancy if symptoms occur. |
| Fertility Effects | No long-term effects on fertility. May delay ovulation in the current cycle; does not impair future fertility. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to active substance or excipientsSevere hepatic impairment
| Precautions | QTc interval prolongation (avoid in patients with known QTc prolongation, electrolyte disturbances, or concurrent use of QTc-prolonging agents), Hepatotoxicity (monitor liver function tests; discontinue if signs of liver injury occur), Clostridioides difficile-associated diarrhea (CDAD), Hypersensitivity reactions including anaphylaxis, Avoid use in patients with moderate to severe hepatic impairment (Child-Pugh B or C) |
| Food/Dietary | No significant food interactions known. Avoid alcohol as it may increase risk of methotrexate toxicity. |
| Clinical Pearls | KHAPZORY (levoleucovorin) is used as a rescue agent after high-dose methotrexate therapy to prevent severe toxicity. Monitor serum methotrexate levels closely; administer leucovorin until methotrexate level is <5×10^-8 M. Adjust dose in renal impairment. Not interchangeable with folic acid. |
| Patient Advice | Take this medication exactly as prescribed, usually every 6 hours for a set number of doses. · Do not skip doses, as this may increase the risk of methotrexate toxicity. · Inform your doctor if you experience shortness of breath, rash, or signs of allergic reaction. · Keep all appointments for blood tests to monitor methotrexate levels. · Avoid taking folic acid supplements unless directed by your doctor. |
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