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. Author manuscript; available in PMC: 2017 Aug 3.
Published in final edited form as: Br J Ophthalmol. 2015 Dec 23;100(4):446–452. doi: 10.1136/bjophthalmol-2015-307722

Table 4.

Treatment options for infections caused by reduced vancomycin susceptibility—listed by generic (and commercial) names

Linezolid (Zyvox)5054 Quinupristine/dalfopristine (Synercid)5557 Daptomycin (Cubicin)5862 Tigecycline (Tygacil)6368
Class Oxazolidinone (fermentation byproduct of Streptomyces roseosporus) Streptogramin (isolated from Streptomyces pristinaespiralis) Cyclic lipopeptide Glycylcycline (a derivative of minocycline)
Mechanism of action Inhibits initiation of protein synthesis by binding 23S rRNA of the 50S subunit of bacterial ribosome Inhibits bacterial protein synthesis by interfering with function of 23S RNA (quinidine: dalfopristine=3:7) Terminates bacterial DNA, RNA and protein synthesis and cell death by forming transmembrane channels in cell membrane and depolarisation of membrane potential Inhibits bacterial protein synthesis by irreversibly binding to 30 S ribosomal unit
Route and dose Oral—600 mg twice daily
Intravenous—600 mg twice daily
Intravitreal—300 mg/0.1 mL (rabbits)
Topical—2 mg/mL (rabbits)
Intravenous—7.5 mg/kg 8 hourly
Intravitreal—0.4 mg/0.1 mL
In vitro—MIC90 0.5–2 mg/L
Intravenous—4–6 mg/kg per day
Intravitreal—200 mg/0.05 mL (rabbits)
Topical—1% (rabbits)
Intravenous—100 mg/100 ml over 30–60 min followed by 50 mg twice daily
Intravitreal—0.5–1 mg/0.1 mL (rabbits)
Topical—10–50 mg/mL (rabbits)
Side effects with systemic dose Reversible myelosuppression, irreversible peripheral neuropathy, optic neuropathy (when used for >14 days) Arthralgia, myalgia, pain and Periphlebitis at injection site Not significant
Minor gastrointestinal disturbances
Hypersensitivity-like reaction
Spectrum of activity GPO, MRSA, VRSA, VISA, VRE, CNS, GNO, mycobacteria MRSA, VISA, VRSA, Streptococcus species, CNS VRSA, VRE, Staphylococcus, Streptococcus, Enterococcus species MSSA, MRSA, VISA, VRE, Escherichia coli and Klebsiella pneumonia
Others First pharmacologically active oxazolidinone (fermentation byproduct of Streptomyces roseosporus).
Good intraocular availability after intravenous and oral administration
First intravitreal (0.4 mg/0.1 mL) use of quinupristin/dalfopristin acute postoperative endophthalmitis in 2011 Pharmacokinetics are linear at dose of 4–12 mg/kg/day.
Available only in intravenous formulation
Minimum inhibitory concentration 90 (MIC90) of MDR bacteria range from 0.12–4 μg/mL

CNS, coagulase-negative staphylococci; FDA, US Food and Drug Administration; GNO, Gram-negative organism; GPO, Gram-positive organisms; MDR, multidrug resistant bacteria; MRSA, methicillin-resistant Staphylococcus aureus; VISA, vancomycin intermediate sensitive Staphylococcus aureus; VRE, vancomycin resistant Enterococcus; VRSA, vancomycin-resistant Staphylococcus aureus.