KIMYRSA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for KIMYRSA (KIMYRSA).
KIMYRSA (dalbavancin) inhibits bacterial cell wall synthesis by binding to the D-alanyl-D-alanine terminus of the peptidoglycan precursor, preventing cross-linking.
| Metabolism | Dalbavancin is not significantly metabolized; it undergoes slow hydrolysis to less active metabolites. It is primarily excreted unchanged in urine and feces. Minor involvement of CYP450 enzymes. |
| Excretion | Primarily renal excretion as unchanged drug (approximately 70-80% of the dose). Fecal elimination accounts for about 5-10%. Biliary excretion is minimal. |
| Half-life | Terminal elimination half-life is approximately 6-7 hours in adults with normal renal function. In patients with renal impairment, half-life may be prolonged up to 12-15 hours, requiring dose adjustment. |
| Protein binding | Approximately 80-85% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution ranges from 0.3 to 0.5 L/kg, indicating distribution into extracellular fluid. Higher Vd may be seen in critically ill patients due to increased capillary permeability. |
| Bioavailability | Not applicable; KIMYRSA is only administered intravenously (bioavailability is 100% for IV route). Oral bioavailability is 0%. |
| Onset of Action | Intravenous infusion: Onset of antibacterial effect is rapid, with peak serum concentrations achieved immediately after infusion. Clinical response typically observed within 24-48 hours. |
| Duration of Action | Duration of action is approximately 8-12 hours based on dosing interval. For serious infections, continuous or extended infusion may be used to maintain therapeutic levels. |
| Molecular Weight | 819.8 |
15 mg/kg IV every 12 hours for 5-7 days for acute bacterial skin and skin structure infections.
| Dosage form | POWDER |
| Renal impairment | For CrCl 30-89 mL/min: 15 mg/kg IV every 24 hours. For CrCl <30 mL/min: 15 mg/kg IV every 48 hours. CrCl estimated by Cockcroft-Gault. |
| Liver impairment | No specific dose adjustment recommended. Use with caution in severe hepatic impairment (Child-Pugh C) due to limited data. |
| Pediatric use | Not approved for use in pediatric patients <18 years of age. |
| Geriatric use | No dose adjustment based solely on age; adjust dose based on renal function as per renal_adjustment. |
| 1st trimester | Avoid unless clearly needed; limited human data; animal studies showed developmental toxicity at high doses. |
| 2nd trimester | Use only if potential benefit justifies risk; crosses placenta; no well-controlled studies. |
| 3rd trimester | Use only if clearly needed; may cause fetal nephrotoxicity or ototoxicity if administered near term. |
Clinical note
Comprehensive clinical and safety monograph for KIMYRSA (KIMYRSA).
| Placental transfer | Crosses the placenta in humans; fetal serum levels approximately 60% of maternal levels at delivery. |
| Breastfeeding | Excreted in human milk in small amounts; monitor infant for diarrhea, thrush, or rash; consider alternative if infant is preterm or has renal impairment. |
| Lactation Rating |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to KIMYRSA or any componentKnown hypersensitivity to dalbavancin or other glycopeptidesConcomitant use with ticagrelor (based on theoretical additive QT prolongation)
| Precautions | Hypersensitivity reactions including anaphylaxis, Infusion reactions (e.g., flushing, urticaria, pruritus) – slow infusion rate, Potential for Clostridioides difficile-associated diarrhea, Elevated liver enzymes (monitor LFTs), Use with caution in patients with renal impairment (CrCl <30 mL/min) as dose adjustment may be required, Not effective against Gram-negative pathogens, Increased risk of bleeding in patients receiving warfarin (prolongation of PT/INR monitoring) |
| Food/Dietary | No significant food interactions identified. Oritavancin may be administered without regard to food. |
Loading safety data…
| L3 - Moderately Safe |
| Teratogenic Risk | Oritavancin (Kimyrusa) is classified as FDA Pregnancy Category C. Animal studies in rats and rabbits at doses up to 0.5 times the human dose (based on AUC) showed no teratogenicity but maternal toxicity (reduced body weight gain) and fetal effects (delayed ossification, reduced fetal weight) occurred. No adequate human studies exist. Use only if potential benefit justifies risk to fetus. Limited data for first trimester; theoretical risk based on mechanism (cell wall synthesis inhibition) is low but not fully characterized. Avoid in pregnancy unless absolutely necessary. |
| Fetal Monitoring | No specific monitoring requirements for oritavancin in pregnancy. Standard monitoring for maternal infusion reactions (e.g., flushing, urticaria, hypotension) during administration. Fetal monitoring for growth and well-being if drug is used in second or third trimester, due to potential maternal toxicity affecting placental blood flow. Assess liver function and renal function as prolonged half-life may require adjustment in severe hepatic impairment. No routine drug level monitoring. |
| Fertility Effects | No human studies on effects on fertility. In animal studies, there were no effects on male or female fertility in rats at doses up to 0.5 times human dose. Mechanism does not suggest direct impact on reproductive organs, but caution due to lack of data. |
| Clinical Pearls | KIMYRSA (oritavancin) is a lipoglycopeptide antibiotic with a long half-life (~393 hours), allowing single-dose treatment for acute bacterial skin and skin structure infections (ABSSSI). It is active against MRSA and VRE. Monitor for osteomyelitis or septic arthritis as treatment failures have been reported. Avoid coadministration with warfarin due to potential INR elevation; consider alternative anticoagulants. Infusion-related reactions (e.g., flushing, urticaria) may occur; slow infusion rate or premedicate. Can cause false elevation in aPTT and PT/INR for up to 48 hours due to interference with laboratory tests; draw coagulation labs before infusion or use alternative assays. Use with caution in patients with moderate to severe renal impairment (CrCl <30 mL/min) as limited data. |
| Patient Advice | You are receiving a single dose of oritavancin (KIMYRSA) infused intravenously over 3 hours. · Tell your healthcare provider if you have a history of bleeding disorders or are taking blood thinners (e.g., warfarin) as oritavancin may interfere with laboratory tests for blood clotting. · Report any signs of allergic reaction during the infusion, such as rash, itching, flushing, or difficulty breathing. · This antibiotic stays in your body for weeks; inform any doctor or dentist that you received oritavancin before starting new medications or having surgery. · Do not take warfarin (Coumadin) for at least 48 hours after oritavancin treatment due to risk of inaccurate INR readings. · Contact your healthcare provider if you develop new pain, swelling, or redness in the treated skin area, fever, or chills, as these may indicate treatment failure or infection spread. · Avoid alcohol for at least 48 hours after infusion to prevent potential interaction. |