Azithromycin Dihydrate

Reference

• 1) Antimicrobial Sub-MIC induces Staphylococcus aureus biofilm formation without affecting the bacterial count
  • R. Elawady, A.G. Aboulela, A. Gaballah, A.A. Ghazal, A.N. Amer, BMC Infect. Dis. 2024, 24, 1065.


应用
Azithromycin: A More Acid-Stable Semi-Synthetic Macrolide Antibiotic
Macrolide antibiotics are classified by the size of the macrocyclic lactone ring of aglycone as 14-, 15- or 16-membered ring macrolides. Macrolides are characterized by similar chemical structures, mechanisms of action and resistance, but vary in the different pharmacokinetic parameters, and spectrum of activity. Azithromycin (abbrev: AZM), the first azalide macrolide, is chemically synthesized from erythromycin [E0751], with a methyl-substituted nitrogen atom incorporated into the acid-stable lactone ring, thus making the 15-membered lactone ring. AZM is marginally less active than erythromycin in vitro against Gram-positive organisms, but is more active than erythromycin and clarithromycin [C2220] against many Gram-negative pathogens including Haemophilus influenzae and Neisseria gonorrhoeae, and Mycoplasma pneumoniae. However, erythromycin-resistant organisms are also resistant to AZM. AZM is subsequently slowly released, reflecting its long terminal phase elimination half-life relative to that of erythromycin. AZM inhibits protein synthesis in susceptible organisms by binding to specific nucleotides in 23S rRNA within the 50S subunit of the bacterial ribosome.

References

• Azithromycin: a review of its antimicrobial activity, pharmacokinetic properties and clinical efficacy
  • D. H. Peters, H. A. Friedel, D. McTavish, Drugs 1992, 44, 750.
• The macrolides: erythromycin, clarithromycin, and azithromycin (a review)
  • S. Alvarez-Elcoro, M. J. Enzler, Mayo Clin. Proc. 1999, 74, 613.
• Macrolide-induced clinically relevant drug interactions with cytochrome P-450A (CYP) 3A4: an update focused on clarithromycin, azithromycin and dirithromycin (a review)
  • J. F. Westphal, Br. J. Clin. Pharmacol. 2000, 50, 285.
• Analysis of macrolide antibiotics (a review)
  • I. Kanfer, M. F. Skinner, R. B. Walker, J. Chromatogr. A 1998, 812, 255.
• Development, characterization and solubility study of solid dispersions of azithromycin dihydrate by solvent evaporation method
  • S. C. Arora, P. K. Sharma, R. Irchhaiya, A. Khatkar, N. Singh, J. Gagoria, J. Adv. Pharm. Technol. Res. 2010, 1, 221.


PubMed Literature