Erythromycin estolate

Erythromycin Estolate is a prodrug form of the macrolide antibiotic erythromycin. It is designed to be less prone to acid degradation in the stomach, thus improving oral absorption and bioavailability.

Pharmacology

Erythromycin estolate is converted in the body to the active drug erythromycin, which inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit. This prevents the translocation of peptide chains, disrupting protein synthesis and ultimately leading to bacterial cell death.

Erythromycin has a broad spectrum of activity, effective against a wide range of Gram-positive bacteria and some Gram-negative bacteria. It is particularly useful in the treatment of respiratory tract infections, skin and soft tissue infections, and certain sexually transmitted infections.

Pharmacokinetics

The estolate form of erythromycin is more lipophilic than the base form, allowing for better absorption in the gastrointestinal tract. It also has a longer half-life, allowing for less frequent dosing.

Side Effects

Common side effects of erythromycin estolate include gastrointestinal disturbances such as nausea, vomiting, and diarrhea. More serious side effects can include hepatotoxicity, which is more common with the estolate form than other forms of erythromycin.

Interactions

Erythromycin estolate can interact with a number of other medications, including certain statins, warfarin, and other antibiotics. It is also known to inhibit the cytochrome P450 enzyme system, which can affect the metabolism of other drugs.

See Also

• Erythromycin
• Macrolide
• Prodrug
• Antibiotic