Comparison of azithromycin leukocyte disposition in healthy volunteers andvolunteers with AIDS

Azithromycin, has been proved to be effective in the treatment and prophyla xis of a wide variety of infections. While the penetration of azithromycin into a number of types of mammalian cells has been well characterized, the influence of HIV infection on the intracellular disposition of this agent h as not been studied. We therefore studied the disposition of azithromycin i n polymorphonuclear (PMN) and mononuclear (MONO) leukocytes from six health y volunteers and six volunteers with AIDS. After oral administration of a s ingle 1200-mg dose of azithromycin (two 600-mg tablets), blood samples were collected over 6 days and intracellular azithromycin concentrations in MON Os and PMNs were measured. Analysis of the intracellular pharmacokinetics r evealed an apparent difference in the MONO and PMN profile; this profile wa s similar for both groups. Intracellular concentrations of azithromycin rem ained high throughout the study period. Furthermore, no statistically signi ficant differences in the intracellular area under the curve (11 309 +/- 25 43 vs. 16 650 +/- 6254 for PMN; 14 180 +/- 3802 vs. 21 211 +/- 10 001 for M ONO) were observed between the healthy and AIDS populations, respectively. Our data confirm the extensive uptake of azithromycin by white blood cells both in healthy volunteers and in AIDS patients. (C) 2000 Elsevier Science B.V. and International Society of Chemotherapy. All rights reserved.