Drug intelligence / Profile preview

azithromycin microspheres

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Oral, Intravenous, Ophthalmic
01

Overview

Azithromycin microspheres are a novel, single-dose, extended-release oral formulation of the macrolide antibiotic azithromycin. Developed to improve tolerability and patient compliance, this formulation incorporates azithromycin into sustained-release polymeric microspheres (mean diameter 100–300 μm), which release the drug slowly via diffusion through pores formed in situ. Alkalinizing agents delay initial drug release in the stomach; most of the drug is released over two hours in the small intestine. This design reduces gastrointestinal side effects and allows for higher single-dose administration compared to immediate-release forms[1][6][8]. The mechanism of action is inhibition of bacterial protein synthesis by binding to the 50S ribosomal subunit, making it effective against a broad range of respiratory pathogens[1]. Azithromycin microsphere formulations are FDA-approved (as Zmax) for mild-to-moderate community-acquired pneumonia and acute bacterial sinusitis in adults and children over six months old[6][9].

Brand names
Zmax
Other names
azithromycin extended-releaseazithromycin ER microspheresazithromycin controlled-release microspheres
02

Targets

Bacterial 50S ribosomal subunit

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