Aziro-500 Mechanism of Action

Pharmacology: Azithromycin dihydrate, a macrolide of the azalide subclass, exerts its antibacterial action by binding to the 50s ribosomal subunit of susceptible bacteria and suppressing protein synthesis.
Pharmacokinetics: Azithromycin given orally is rapidly absorbed and about 40% bioavailable. Absorption from capsules, but not tablets or suspension, is reduced by food. Peak plasma concentrations occur 2 to 3 hours after an oral dose. However, Azithromycin is extensively distributed into the tissues, and tissue concentrations subsequently remain much higher than those in the blood; in contrast to most other antibacterials, plasma concentrations are therefore of little value as a guide to efficacy.
High concentrations are taken up into white blood cells. There is little diffusion into the CSF when the meninges are not inflamed. Data from animal studies indicate that azithromycin crosses the placenta. Small amounts of azithromycin are demethylated in the liver, and it is excreted in bile as unchanged drug and a number of inactive metabolites have also been detected. About 6% of an oral dose (representing about 20% of the amount in the systemic circulation) is excreted in the urine. The terminal elimination half-life is about 68 hours.
Microbiology: Antimicrobial activity: Azithromycin is less than erythromycin against streptococci and staphylococci, but has greater activity than erythromycin in vitro against some Gram-negative organisms such as Haemophilus influenzae and Moraxella catarrhalis (Branhamella catarrhalis), as well as having activity against some of the Enterobacteriaceae such as Escherichia coli and Salmonella and Shigella spp. Azithromycin is also more active than erythromycin against Chlamydia trachomatis and Ureaplasma urealyticum, and some opportunistic mycobacteria, including Mycobacterium avium complex. It has activity against the protozoa Taxoplasma gondii and Plasmodium falciparum.