MACROLIDES, AMINOGLYCOSIDES, POLYENE & POLYPEPTIDE ANTIBIOTICS

Macrolides, aminoglycosides, polyene, and polypeptide antibiotics are important classes of antibiotics used in the treatment of bacterial and fungal infections. Each class of antibiotics has its own unique mechanisms of action, spectrum of activity, and considerations for use. In this article, we will explore the pharmacology of these antibiotics, including their mechanisms of action, common uses, and potential adverse effects.

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Macrolides

Macrolides are a group of antibiotics that inhibit bacterial protein synthesis. They achieve this by binding to the bacterial ribosomes, specifically to the 50S subunit, thereby preventing the translocation of the growing peptide chain. As a result, protein synthesis is inhibited, leading to bacterial cell death.

Macrolides have a broad spectrum of activity against Gram-positive bacteria, including Streptococcus pneumoniae and Staphylococcus aureus. They are also effective against certain atypical pathogens, such as Mycoplasma pneumoniae and Legionella pneumophila. Macrolides are commonly used in the treatment of respiratory tract infections, skin and soft tissue infections, and sexually transmitted infections.

Common examples of macrolides include erythromycin, clarithromycin, and azithromycin. These antibiotics are generally well-tolerated, but they can cause gastrointestinal disturbances, such as nausea and diarrhea, in some individuals. Macrolides may also interact with other medications, so it is important to consult with a healthcare professional before starting treatment.

Aminoglycosides

Aminoglycosides are a group of antibiotics that inhibit bacterial protein synthesis by binding to the bacterial ribosomes, specifically to the 30S subunit. This binding interferes with the decoding process, leading to the production of faulty proteins and ultimately bacterial cell death.

Aminoglycosides have a narrow spectrum of activity and are primarily used against Gram-negative bacteria, including Escherichia coli, Pseudomonas aeruginosa, and Klebsiella pneumoniae. They are often reserved for the treatment of serious infections, such as bloodstream infections and certain types of pneumonia.

Common examples of aminoglycosides include gentamicin, amikacin, and tobramycin. These antibiotics are usually administered intravenously or intramuscularly due to their poor oral absorption. Aminoglycosides can cause serious side effects, including kidney damage and hearing loss, so close monitoring of renal function and hearing is necessary during treatment.

Polyene Antibiotics

Polyene antibiotics are antifungal agents that work by binding to ergosterol, an essential component of fungal cell membranes. This binding disrupts the integrity of the cell membrane, leading to leakage of cellular contents and fungal cell death.

One of the most well-known polyene antibiotics is amphotericin B, which is used in the treatment of serious systemic fungal infections, such as invasive candidiasis and cryptococcal meningitis. Amphotericin B is usually administered intravenously and requires careful monitoring due to its potential for nephrotoxicity and other adverse effects.

Polypeptide Antibiotics

Polypeptide antibiotics, also known as cyclic lipopeptides, are a class of antibiotics that have a unique mechanism of action. They disrupt bacterial cell membranes, causing membrane depolarization and leakage of cellular contents. This ultimately leads to bacterial cell death.

Daptomycin is an example of a polypeptide antibiotic used in the treatment of skin and soft tissue infections caused by Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). It is administered intravenously and may cause muscle toxicity and an increase in creatine phosphokinase (CPK) levels.

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