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Comparative pharmacokinetics of azithromycin in serum and white blood cells of healthy subjects receiving a single-dose extended-release regimen versus a 3-day immediate-release regimen.
Antimicrob Agents Chemother. 2007 Jan; 51(1):103-9.AA

Abstract

The pharmacokinetic profiles of azithromycin given as a single-dose regimen (2.0-g extended-release microspheres) were characterized in serum and white blood cells (WBC) and compared with those of a 3-day regimen (a 500-mg immediate-release tablet once daily; total dose, 1.5 g) in an open-label, randomized, parallel-group study of 24 healthy adult subjects. Serial blood samples were collected up to 5 days after the start of dosing for both regimens. Safety assessments were conducted throughout the study. A single 2.0-g dose of azithromycin microspheres achieved significantly higher exposures in serum and WBC during the first 24 h after the start of dosing than a 3-day regimen: an approximately threefold higher area under the curve from time zero to 24 h postdose (AUC(0-24)) and an approximately twofold higher mean peak concentration on day 1. The single-dose regimen provided total azithromycin exposures in serum and WBC similar to those of the 3-day regimen, as evidenced by the similar AUC(0-120) and trough azithromycin concentrations in serum and WBC (mononuclear leukocytes [MNL] and polymorphonuclear leukocytes [PMNL]). For both regimens, the average total azithromycin exposures in MNL and PMNL were approximately 300- and 600-fold higher than those in serum. Azithromycin concentrations in MNL and PMNL remained above 10 microg/ml for at least 5 days after the start of dosing for both regimens. This "front-loading" of the dose on day 1 is safely achieved by the extended-release microsphere formulation, which maximizes the drug exposure at the time when the bacterial burden is likely to be highest.

Authors+Show Affiliations

Department of Clinical Pharmacology, Pfizer Global Research and Development, 50 Pequot Ave., New London, CT 06320, USA.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Randomized Controlled Trial

Language

eng

PubMed ID

17060516

Citation

Liu, Ping, et al. "Comparative Pharmacokinetics of Azithromycin in Serum and White Blood Cells of Healthy Subjects Receiving a Single-dose Extended-release Regimen Versus a 3-day Immediate-release Regimen." Antimicrobial Agents and Chemotherapy, vol. 51, no. 1, 2007, pp. 103-9.
Liu P, Allaudeen H, Chandra R, et al. Comparative pharmacokinetics of azithromycin in serum and white blood cells of healthy subjects receiving a single-dose extended-release regimen versus a 3-day immediate-release regimen. Antimicrob Agents Chemother. 2007;51(1):103-9.
Liu, P., Allaudeen, H., Chandra, R., Phillips, K., Jungnik, A., Breen, J. D., & Sharma, A. (2007). Comparative pharmacokinetics of azithromycin in serum and white blood cells of healthy subjects receiving a single-dose extended-release regimen versus a 3-day immediate-release regimen. Antimicrobial Agents and Chemotherapy, 51(1), 103-9.
Liu P, et al. Comparative Pharmacokinetics of Azithromycin in Serum and White Blood Cells of Healthy Subjects Receiving a Single-dose Extended-release Regimen Versus a 3-day Immediate-release Regimen. Antimicrob Agents Chemother. 2007;51(1):103-9. PubMed PMID: 17060516.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Comparative pharmacokinetics of azithromycin in serum and white blood cells of healthy subjects receiving a single-dose extended-release regimen versus a 3-day immediate-release regimen. AU - Liu,Ping, AU - Allaudeen,Hameed, AU - Chandra,Richa, AU - Phillips,Kem, AU - Jungnik,Arvid, AU - Breen,Jeanne D, AU - Sharma,Amarnath, Y1 - 2006/10/23/ PY - 2006/10/25/pubmed PY - 2007/7/3/medline PY - 2006/10/25/entrez SP - 103 EP - 9 JF - Antimicrobial agents and chemotherapy JO - Antimicrob Agents Chemother VL - 51 IS - 1 N2 - The pharmacokinetic profiles of azithromycin given as a single-dose regimen (2.0-g extended-release microspheres) were characterized in serum and white blood cells (WBC) and compared with those of a 3-day regimen (a 500-mg immediate-release tablet once daily; total dose, 1.5 g) in an open-label, randomized, parallel-group study of 24 healthy adult subjects. Serial blood samples were collected up to 5 days after the start of dosing for both regimens. Safety assessments were conducted throughout the study. A single 2.0-g dose of azithromycin microspheres achieved significantly higher exposures in serum and WBC during the first 24 h after the start of dosing than a 3-day regimen: an approximately threefold higher area under the curve from time zero to 24 h postdose (AUC(0-24)) and an approximately twofold higher mean peak concentration on day 1. The single-dose regimen provided total azithromycin exposures in serum and WBC similar to those of the 3-day regimen, as evidenced by the similar AUC(0-120) and trough azithromycin concentrations in serum and WBC (mononuclear leukocytes [MNL] and polymorphonuclear leukocytes [PMNL]). For both regimens, the average total azithromycin exposures in MNL and PMNL were approximately 300- and 600-fold higher than those in serum. Azithromycin concentrations in MNL and PMNL remained above 10 microg/ml for at least 5 days after the start of dosing for both regimens. This "front-loading" of the dose on day 1 is safely achieved by the extended-release microsphere formulation, which maximizes the drug exposure at the time when the bacterial burden is likely to be highest. SN - 0066-4804 UR - https://www.unboundmedicine.com/medline/citation/17060516/Comparative_pharmacokinetics_of_azithromycin_in_serum_and_white_blood_cells_of_healthy_subjects_receiving_a_single_dose_extended_release_regimen_versus_a_3_day_immediate_release_regimen_ L2 - http://aac.asm.org/cgi/pmidlookup?view=long&pmid=17060516 DB - PRIME DP - Unbound Medicine ER -