Linezolid is an antibiotic primarily used for treating infections resulting due to gram-positive bacteria resistant to other antibiotics. It is quite effective against most of the gram-positive bacteria that result in a disease such as Staphylococcus aureus. It is beneficial for treating infections of pneumonia and skin. However, it can also be used for treating other infections including drug-resistant tuberculosis. It is taken either by mouth or given by injection into a vein.
Linezolid is quite safe when given for a short duration. It can be given to people of all ages including those with poor kidney function and liver disease. The common side effects noted are nausea, rash, diarrhea, and headache.
Linezolid works by suppressing bacterial protein production as a protein synthesis inhibitor. This either results in the death of the bacteria or inhibits the growth entirely. Although most of the antibiotics work this way, the exact mechanism of this drug is unique. It cuts down protein production entirely. This drug belongs to the oxazolidinone class of medications.
Linezolid was approved for medical use in 2000. The wholesale cost of this drug in the developing world is around £2.31 per day. However, the wholesale cost elsewhere is around £11. It is a much cost-effective option in comparison to vancomycin.
Medical uses of Linezolid
The main use of this drug is in the treatment of severe infections resulting due to gram-positive bacteria that have developed resistance against other antibiotics. It cannot be used against bacteria that are sensitive to drugs having a narrow spectrum of activity such as cephalosporins and penicillins.
This drug is called a reserve antibiotic as it can remain effective if it is used sparingly. It should be used as the last drug of resort against intractable infections. The manufacturers in the UK mention cSSSIs and pneumonia as the only indications during product labeling. The best thing about this drug is that it is safe and effective for use in newborns and children.
Synthesis of Linezolid
Linezolid manufacturers derive this drug from a synthetic process. It is not available in nature. Many approaches have been studied for the synthesis of this drug. The original method is lengthy and requires the use of expensive chemicals despite the good yield. The high cost of this drug is because of the expensive procedure involved in its synthesis. A cost-effective and concise mechanism was developed in 1998 by Upjohn. Later, an Indian pharmaceutical company called Dr. Reddy’s developed an atom-economical method in 1999.
History of Linezolid
The oxazolidinones have been known since the 1950s. Researchers discovered their antimicrobial properties in the 1970s. A series of derivatives of this chemical was patented by DuPont in 1978. The scientists at DuPont gave a detailed description of a new class of antibiotics called oxazolidinones. Several research programs were carried out by other laboratories in the 1990s.
Linezolid was quite an expensive drug in 2009. A treatment course cost £1590 alone. This is not inclusive of hospital stay charges. The price decreased drastically when the medication became generic.
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