Erythromycin

Erythromycin is a macrolide antibiotic that inhibits bacterial protein synthesis by targeting the 50S ribosomal subunit, blocking the progression of nascent polypeptide chains.¹ It is active against a host of bacterial genera, including Streptococcus, Staphylococcus, and Haemophilus (MIC₉₀s = 0.015-2.0 mg/l).² Erythromycin (10-40 mg/kg) dose-dependently inhibits the growth of S. aureus in a mouse model of thigh infection.³ It also inhibits the cytochrome P450 (CYP450) isoform CYP3A4 in vitro with IC₅₀ values of 33 and 27.3 µM for α-hydroxytriazolam and 4-hydroxytriazolam formation, respectively, following administration of triazolam, which is known to be metabolized primarily by CYP3A4.^4,5 Formulations containing erythromycin have been used in the treatment of bacterial respiratory and skin infections, pertussis, and a variety of other bacterial infections.

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1. Wilson, D.N. The A-Z of bacterial translation inhibitors. Crit. Rev. Biochem. Mol. Biol. 44(6), 393-433 (2009).

2. Kanatani, M.S., and Guglielmo, B.J. The new macrolides. Azithromycin and clarithromycin. Western J. Med. 160(1), 31-37 (1994).

3. Hoogeterp, J.J., Mattie, H., and van Furth, R. Activity of erythromycin and clindamycin in an experimental Staphylococcus aureus infection in normal and granulocytopenic mice. A comparative in vivo and in vitro study. Scand. J. Infect. Dis. 25(1), 123-132 (1993).

4. Westphal, J.F. Macrolide - induced clinically relevant drug interactions with cytochrome P-450A (CYP) 3A4: An update focused on clarithromycin, azithromycin and dirithromycin. Br. J. Clin. Pharmacol. 50(4), 285-295 (2000).

5. Greenblatt, D.J., von Moltke, L.L., Harmatz, J.S., et al. Inhibition of triazolam clearance by macrolide antimicrobial agents: In vitro correlates and dynamic consequences. Clin. Pharmacol. Ther. 64(3), 278-285 (1998).