Azithromycin Clinical Pharmacokinetics

Nestor J. Lalak, David L. Morris

Azalide antibiotics, of which azithromycin is the first demonstrated, have different pharmacokinetics from other antibiotics currently used. The bioavailability of the drug is approximately 37%. Extensive and rapid distribution from serum into the intracellular compartments is followed by rapid distribution to the tissues. Tissue concentrations exceed serum concentrations by up to 100-fold following a single azithromycin 500mg dose. Concentration of the drug within phagocytes aids in its ability to combat infections. High concentrations of azithromycin are found in the tonsil, lung, prostate, lymph nodes and liver, with only small concentrations found in fat and muscle. A 500mg dose on day 1, followed by 250mg daily on days 2 to 5, has been demonstrated to maintain azithromycin concentrations at sites of infection and continues to be effective for several days after administration has ceased. The pharmacokinetics of azithromycin make it a drug with diverse therapeutic applications.