Oritavancin

Summary

Oritavancin is a semisynthetic lipoglycopeptide antibiotic approved for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible gram-positive organisms including MRSA. Its long half-life (~245 hours) allows for single-dose intravenous administration, distinguishing it from other glycopeptides.

Mechanism of Action

Inhibits bacterial cell wall synthesis by binding to peptidoglycan precursors (D-Ala-D-Ala and D-Ala-D-Lac termini), disrupts cell membrane integrity via lipophilic side chain insertion, and inhibits transglycosylation and transpeptidation steps; also disrupts membrane potential in gram-positive bacteria.

Routes of Administration

Goals & Uses

• Single-dose outpatient antibiotic therapyHealthcare UtilizationHigh
• Treatment of MRSA infectionsAntimicrobialHigh
• Treatment of VRE infectionsAntibacterial TherapyLow
• Treatment of ABSSSI due to gram-positive pathogensAntibacterial TherapyHigh

Contraindications

• Unfractionated heparin sodium use within 120 hoursDrug InteractionHigh
• Known hypersensitivity to oritavancin or glycopeptidesAllergyHigh

Adverse Effects

• HepatotoxicityHepaticUncommonLiver injury or dysfunction
• OsteomyelitisMusculoskeletalUncommon
• Infusion-related reactions (flushing, pruritus, urticaria)Infusion ReactionCommon
• HeadacheNeurologicCommonPain in the head or upper neck
• Clostridium difficile-associated diarrheaGastrointestinalRare
• NauseaGastrointestinalCommonFeeling of sickness or urge to vomit

Drug Interactions

• CYP2C9/CYP2C19 substrates (e.g., phenytoin, warfarin)Low
• WarfarinModerate
• Unfractionated HeparinHigh

Population Constraints

• PregnancyReproductive SafetyRelative
• Hepatic impairment (severe)HepaticRelative
• Renal impairmentOrgan ImpairmentRelative
• Pediatric patients (<18 years)AgeRelative

Regulatory Status

• European UnionApprovedApproved: Acute bacterial skin and skin structure infections (ABSSSI) in adultsEMA approved under brand name Orbactiv; indicated for adults when other alternatives not suitable.
• United StatesApprovedApproved: Acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible gram-positive bacteriaFDA approved August 2014 (Orbactiv); second brand Kimyrsa approved 2021 as ready-to-use formulation.
• United KingdomApprovedApproved: Acute bacterial skin and skin structure infections (ABSSSI) in adultsApproved by MHRA; indications consistent with EU approval.

Approved by the FDA in August 2014 under the brand name Orbactiv. Also approved in the EU. Single 1200 mg IV dose regimen approved for ABSSSI.

Evidence & Sources

No sources recorded yet.