Linezolid: The First Oxazolidinone Antimicrobial

  1. Robert C. Moellering, Jr., MD
  1. From Beth Israel Deaconess Medical Center, Boston, Massachusetts.

    Abstract

    Linezolid is the first of a new class of antimicrobial agents, the oxazolidinones, to be approved for clinical use in the United States and elsewhere. The drug is a totally synthetic compound, which lessens the likelihood of naturally occurring resistance mechanisms. It has excellent activity against virtually all important gram-positive pathogens, including methicillin-resistant staphylococci, penicillin-resistant pneumococci, macrolide-resistant streptococci, and vancomycin-resistant enterococci. Development of resistance to the compound has been infrequent thus far. Linezolid is 100% bioavailable, so it can be given in equal doses orally or parenterally. Its elimination half-life allows dosing twice per day, and alteration of drug dosage is not required in patients with impaired renal or hepatic function. Linezolid has approved indications for skin and soft tissue infections; lower respiratory tract infections; and vancomycin-resistant Enterococcus faecium infections, including cases with concurrent bacteremia. The drug has an acceptable profile of adverse events, but reversible myelosuppression has occurred in patients receiving high doses for more than 2 weeks.

    Article and Author Information

    • Potential Financial Conflicts of Interest: Dr. Moellering has served as a consultant to the anti-infective therapy groups at DuPont Pharmaceuticals (formerly DuPont Merck Pharmaceuticals, a division of E.I. DuPont de Nemours, Wilmington, Delaware), Pharmacia (formerly Upjohn Laboratories, Kalamazoo, Michigan), and Aventis Pharmaceuticals (formerly Rhône-Poulenc Rorer Pharmaceuticals, Inc., Collegeville, Maryland). In addition, he has received funding for basic laboratory research (not clinical research) from DuPont Merck Pharmaceuticals, Upjohn Laboratories, and Rhône-Poulenc Rorer Pharmaceuticals, Inc.

    • Requests for Single Reprints: Robert C. Moellering Jr., MD, Department of Medicine, Beth Israel Deaconess Medical Center, 110 Francis Street, Suite 6A, Boston, MA 02215.

    Summary for Patients

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    This Article

    1. Ann Intern Med January 21, 2003 vol. 138 no. 2 135-142
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