Table 4.
Linezolid (Zyvox)50–54 | Quinupristine/dalfopristine (Synercid)55–57 | Daptomycin (Cubicin)58–62 | Tigecycline (Tygacil)63–68 | |
---|---|---|---|---|
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.