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Macrolide antibiotics are considered the drug of choice for many clinically significant infections in children, including mycoplasma pneumonia, chlamydial infections, pertussis, and campylobacter enteritis. In addition, they are frequently the first alternative in patients allergic to penicillin. Therefore, they are medications with which pediatric nurses should be familiar. Although effective antibiotics, some of the macrolide antibiotics have an extensive drug interaction profile. It is imperative that pediatric nurses be familiar with these drug interactions to safely treat their patients.
Macrolide antibiotics have proven to be valuable alternatives to pencillins and cephalosporins for the treatment of a number of infections. For many pediatric infections they are the drug of choice for treatment. Currently there are a number of macrolides available. When choosing a particular macrolide, the type of organisms causing the infection, the tolerability of the drug, convenience of dosing, and possible drug interactions must all be taken into account. This article will review all of these factors.
Erythromycin, a macrolide antibiotic produced by Streptomyces erythaeus, was first isolated by McGuire and associates in 1952 (McGuire et al., 1952). The term macrolide is from the chemical structure of the compound. The structure of erythromycin includes a macrocyclic lactone ring with ketone side chains; thus the term macrolide antibiotic. The active form of the drug is erythromycin base. It is a bitter crystalline compound readily inactivated in an acidic medium such as that found in the human stomach.
Erythromycin stearate, ethylsuccinate, and estolate have been developed to overcome the bitter taste of erythromycin base. In addition, many commercially available tablets are film-coated to mask the taste or enteric-coated to protect the drugs from inactivation by gastric acidity.
This review will focus on the differences between azithromycin, clarithromycin, and erythromycin. Azithromycin and clarithromycin are semi-synthetic macrolide antibiotics that differ structurally from erythromycin. These structural modifications result in improved resistance to acid degradation and enhanced tissue penetration compared with erythromycin.
Other macrolide antibiotics include dirithromycin and troleandomycin, which are not used extensively in children, and tacrolimus, which is used in solid organ transplantation as an immunosuppressant.
Pharmacology/Mechanism of Action
Macrolide antibiotics reversibly bind to the P site of the 50S ribosomal subunit of susceptible organisms and inhibit RNA-dependent protein synthesis by stimulating the dissociation of peptidyl-t-RNA from ribosomes...