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Linezolid: The First Oxazolidinone Antimicrobial

Robert C. Moellering Jr., MD
[+] Article and Author Information

From Beth Israel Deaconess Medical Center, Boston, Massachusetts.


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.


Ann Intern Med. 2003;138(2):135-142. doi:10.7326/0003-4819-138-2-200301210-00015
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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.

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Summary for Patients

Linezolid

The summary below is from the full report titled “Linezolid: The First Oxazolidinone Antimicrobial.” It is in the 21 January 2003 issue of Annals of Internal Medicine (volume 138, pages 135-142). The author is RC Moellering Jr.

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