Telithromycin

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An article about the antibiotic Telithromycin


Telithromycin
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Telithromycin is a ketolide antibiotic used to treat certain types of bacterial infections. It is derived from the macrolide antibiotic erythromycin and is specifically designed to overcome resistance mechanisms that affect macrolides.

Mechanism of Action

Telithromycin works by inhibiting bacterial protein synthesis. It binds to the 50S subunit of the bacterial ribosome, thereby blocking the translocation of peptides. This action is similar to that of macrolides, but telithromycin has a higher affinity for the ribosomal subunit, which makes it effective against certain macrolide-resistant strains.

Clinical Uses

Telithromycin is primarily used to treat community-acquired pneumonia, acute bacterial sinusitis, and acute exacerbations of chronic bronchitis. It is effective against a range of Gram-positive bacteria, including Streptococcus pneumoniae and Staphylococcus aureus.

Side Effects

Common side effects of telithromycin include nausea, vomiting, diarrhea, and dizziness. Serious side effects can include hepatotoxicity, visual disturbances, and loss of consciousness. Due to these potential risks, its use is often limited to cases where other antibiotics are not suitable.

Resistance

Resistance to telithromycin can occur through various mechanisms, including mutations in the ribosomal RNA and efflux pump activation. However, its design allows it to evade some of the common resistance mechanisms that affect other macrolides.

Regulatory Status

Telithromycin was approved by the Food and Drug Administration (FDA) in 2004. However, due to concerns about its safety profile, its use has been restricted in some countries.

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Contributors: Prab R. Tumpati, MD