Erythromycin-13C-d3

Erythromycin-¹³C-d₃ is intended for use as an internal standard for the quantification of erythromycin by GC- or LC-MS. 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.

1.Wilson, D.N.The A-Z of bacterial translation inhibitorsCrit. Rev. Biochem. Mol. Biol.44(6)393-433(2009) 2.Kanatani, M.S., and Guglielmo, B.J.The new macrolides. Azithromycin and clarithromycinWestern 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 studyScand. 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 dirithromycinBr. 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 consequencesClin. Pharmacol. Ther.64(3)278-285(1998)