Teicoplanin

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Teicoplanin core and major components

Teicoplanin core components

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Teicoplanin P450 Oxidations

Teicoplanin is a glycopeptide antibiotic used primarily in the treatment of serious Gram-positive bacterial infections. It is often utilized for patients who cannot tolerate the more commonly used glycopeptide antibiotic, vancomycin, or for infections resistant to vancomycin. Teicoplanin works by inhibiting the synthesis of the bacterial cell wall, leading to cell death. It is effective against a range of Gram-positive bacteria including Staphylococcus aureus, Streptococcus spp., and Enterococcus spp.

Mechanism of Action

Teicoplanin acts by binding to the D-alanyl-D-alanine terminus of cell wall precursors, preventing the cross-linking of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This action is similar to that of vancomycin. However, teicoplanin is lipid-soluble, which allows it to penetrate tissues well and provides a longer half-life than vancomycin, enabling less frequent dosing.

Pharmacokinetics

The pharmacokinetics of teicoplanin are characterized by its long half-life, which allows for once-daily dosing in many cases. After intravenous administration, teicoplanin distributes widely into body tissues and fluids. It is metabolized minimally and is primarily excreted unchanged in the urine. The drug's pharmacokinetic profile makes it suitable for the treatment of deep-seated infections.

Clinical Uses

Teicoplanin is indicated for the treatment of serious infections caused by Gram-positive bacteria, including:

• Methicillin-resistant Staphylococcus aureus (MRSA) infections
• Endocarditis
• Bone and joint infections
• Bacteremia
• Skin and soft tissue infections

It is also used as a prophylactic agent in surgical procedures where there is a high risk of infection by Gram-positive organisms.

Adverse Effects

The most common adverse effects of teicoplanin include local reactions at the injection site, such as pain and inflammation, as well as systemic reactions like rash, fever, and gastrointestinal disturbances. Ototoxicity and nephrotoxicity are less common but can occur, particularly with high doses or in patients with pre-existing renal impairment.

Resistance

Resistance to teicoplanin can develop through various mechanisms, including modifications to the target site of the antibiotic, changes in cell wall permeability, and active efflux of the drug. Resistance is generally less common than with vancomycin but can occur, especially in enterococci.

Comparison with Vancomycin

While both teicoplanin and vancomycin are glycopeptide antibiotics used to treat similar infections, there are key differences. Teicoplanin has a longer half-life, allowing for less frequent dosing, and may have a lower risk of nephrotoxicity. However, vancomycin has a broader availability and may be preferred in certain clinical situations.