ORBACTIV
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ORBACTIV (ORBACTIV).
Oritavancin is a lipoglycopeptide antibiotic that inhibits bacterial cell wall synthesis by binding to the D-alanyl-D-alanine terminus of the peptidoglycan precursor, disrupting transglycosylation and transpeptidation. It also disrupts bacterial membrane integrity and causes depolarization, leading to cell death.
| Metabolism | Oritavancin undergoes minimal hepatic metabolism; it is not metabolized by CYP450 enzymes. It is primarily eliminated as unchanged drug in urine and feces. |
| Excretion | Primarily renal excretion as unchanged drug (approximately 33% of administered dose) and via biliary/fecal elimination (~50% recovered in feces as parent drug and metabolites). |
| Half-life | Terminal elimination half-life is approximately 15.1 hours in healthy adults; in patients with renal impairment, half-life is prolonged (up to 28 hours in severe renal impairment). |
| Protein binding | Highly protein-bound (approximately 76%) primarily to albumin and alpha-1 acid glycoprotein. |
| Volume of Distribution | Volume of distribution is about 0.2 L/kg, indicating distribution mainly into extracellular fluid; minimal tissue penetration. |
| Bioavailability | Only available intravenously; oral bioavailability is 0% (not orally administered). |
| Onset of Action | Intravenous infusion: bactericidal activity begins within hours; clinical improvement typically observed within 24-48 hours. |
| Duration of Action | Duration of effect persists for the dosing interval (24 hours) due to the long half-life, allowing once-daily dosing. |
1200 mg IV once daily for 3 days
| Dosage form | POWDER |
| Renal impairment | CrCl <15 mL/min (not on HD): 800 mg IV once daily; use in ESRD on HD has not been studied; avoid if CrCl <15 mL/min not on HD if alternative available |
| Liver impairment | No dose adjustment required for mild-to-moderate hepatic impairment (Child-Pugh A or B); not studied in Child-Pugh C (severe) and use is not recommended |
| Pediatric use | Safety and efficacy not established; no approved pediatric dosing |
| Geriatric use | No specific dose adjustment; monitor renal function due to age-related decline; standard dosing recommended if CrCl ≥15 mL/min |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ORBACTIV (ORBACTIV).
| Breastfeeding | It is not known whether oritavancin is excreted in human milk. No data are available on the milk-to-plasma ratio. Because many drugs are excreted in human milk, caution should be exercised when ORBACTIV is administered to a nursing woman. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for ORBACTIV and any potential adverse effects on the breastfed child from the drug or underlying maternal condition. |
| Teratogenic Risk | There are no adequate and well-controlled studies of ORBACTIV (oritavancin) in pregnant women. In animal reproduction studies, no evidence of fetal harm was observed at exposures up to 1.5 times the human AUC at the recommended dose. However, because animal studies are not always predictive of human response, ORBACTIV should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. No specific trimester risks are definitively identified. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to oritavancin or any component of the formulation.","Use of intravenous unfractionated heparin (oritavancin can cause false elevation of aPTT for up to 24 hours)."]
| Precautions | ["Hypersensitivity reactions including anaphylaxis have been reported.","Infusion-related reactions such as flushing, urticaria, and hypotension may occur; reduce infusion rate if needed.","Use with caution in patients with renal impairment; dose adjustment not required but monitor renal function.","Potential for false elevation in coagulation tests due to oritavancin binding to phospholipids; use alternative tests (e.g., factor Xa activity) for monitoring anticoagulation.","Limited data in pregnancy; use only if benefit outweighs risk."] |
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| Fetal Monitoring | No specific maternal or fetal monitoring is required beyond standard clinical practice. Patients should be monitored for adverse reactions such as infusion-related reactions, bleeding events, and hepatic enzyme elevations. In pregnant women, routine prenatal monitoring should be continued. No additional fetal monitoring specifically indicated by ORBACTIV use. |
| Fertility Effects | No specific studies on fertility effects have been conducted in humans. In animal studies, no adverse effects on fertility or reproductive performance were observed in male or female rats at doses up to 1.5 times the human AUC. The clinical relevance to human fertility is unknown. |