Population pharmacokinetics of azithromycin in whole blood, peripheral blood mononuclear cells, and polymorphonuclear cells in healthy adults

CPT: Pharmacometrics and Systems Pharmacology

Volumn 3, Issue 3, 2014, Pages

  Sampson, M R ^a   Dumitrescu, T P ^a,b   Brouwer, K L R ^a   Schmith, V D ^b  

^a UNIVERSITY OF NORTH CAROLINA   (United States)

^b GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AZITHROMYCIN;

ADULT; ARTICLE; BODY MASS; BODY WEIGHT; BOOTSTRAPPING; CLINICAL ARTICLE; CONTROLLED STUDY; CYSTIC FIBROSIS; DENSITY GRADIENT CENTRIFUGATION; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; FEMALE; HUMAN; IN VITRO STUDY; MALE; PERIPHERAL BLOOD MONONUCLEAR CELL; POLYMORPHONUCLEAR CELL; PRIORITY JOURNAL; PROSPECTIVE STUDY; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION; TREATMENT DURATION;

EID: 84901036665     PISSN: None     EISSN: 21638306     Source Type: Journal    
DOI: 10.1038/psp.2013.80     Document Type: Article

References (38)

1. United States Food and Drug Administration. Azithromycin label; 2011.
2. Shinkai, M., Henke, M.O. & Rubin, B.K. Macrolide antibiotics as immunomodulatory medications: proposed mechanisms of action. Pharmacol. Ther. 117, 393-405 (2008).
3. Piacentini, G.L. et al. Azithromycin reduces bronchial hyperresponsiveness and neutrophilic airway inflammation in asthmatic children: a preliminary report. Allergy Asthma Proc. 28, 194-198 (2007).
4. Vos, R. et al. A randomised controlled trial of azithromycin to prevent chronic rejection after lung transplantation. Eur. Respir. J. 37, 164-172 (2011).
5. Culic, O., Erakovic, V. & Parnham, M.J. Anti-inflammatory effects of macrolide antibiotics. Eur. J. Pharmacol. 429, 209-229 (2001). (Pubitemid 33043997)
6. Labro, M.T. Intracellular bioactivity of macrolides. Clin. Microbiol. Infect. 1(suppl. 1), S24-S30 (1996). (Pubitemid 126682670)
7. Murphy, B.S., Sundareshan, V., Cory, T.J., Hayes, D. Jr, Anstead, M.I. & Feola, D.J. Azithromycin alters macrophage phenotype. J. Antimicrob. Chemother. 61, 554-560 (2008).
8. Gotfried, M.H. Macrolides for the treatment of chronic sinusitis, asthma, and COPD. Chest 125, 52S-60S; quiz 60S (2004).
9. Guchelaar, H.J., Schultz, M.J., van der Poll, T. & Koopmans, R.P. Pharmacokineticpharmacodynamic modeling of the inhibitory effect of erythromycin on tumour necrosis factor-alpha and interleukin-6 production. Fundam. Clin. Pharmacol. 15, 419-424 (2001). (Pubitemid 34227109)
10. Serisier, D.J. et al. Effect of long-term, low-dose erythromycin on pulmonary exacerbations among patients with non-cystic fibrosis bronchiectasis: the BLESS randomized controlled trial. JAMA 309, 1260-1267 (2013).
11. Albert, R.K. et al.; COPD Clinical Research Network. Azithromycin for prevention of exacerbations of COPD. N. Engl. J. Med. 365, 689-698 (2011).
12. Verleden, G.M., Vanaudenaerde, B.M., Dupont, L.J. & Van Raemdonck, D.E. Azithromycin reduces airway neutrophilia and interleukin-8 in patients with bronchiolitis obliterans syndrome. Am. J. Respir. Crit. Care Med. 174, 566-570 (2006). (Pubitemid 44330550)
13. Yates, B. et al. Azithromycin reverses airflow obstruction in established bronchiolitis obliterans syndrome. Am. J. Respir. Crit. Care Med. 172, 772-775 (2005). (Pubitemid 41324235)
14. Ekici, A., Ekici, M. & Erdemoglu, A.K. Effect of azithromycin on the severity of bronchial hyperresponsiveness in patients with mild asthma. J. Asthma 39, 181-185 (2002).
15. Hahn, D.L., Grasmick, M., Hetzel, S. & Yale, S.; AZMATICS (AZithroMycin-Asthma Trial In Community Settings) Study Group. Azithromycin for bronchial asthma in adults: an effectiveness trial. J. Am. Board Fam. Med. 25, 442-459 (2012).
16. Beringer, P. et al. Absolute bioavailability and intracellular pharmacokinetics of azithromycin in patients with cystic fibrosis. Antimicrob. Agents Chemother. 49, 5013-5017 (2005). (Pubitemid 41778914)
17. Wildfeuer, A., Laufen, H. & Zimmermann, T. Uptake of azithromycin by various cells and its intracellular activity under in vivo conditions. Antimicrob. Agents Chemother. 40, 75-79 (1996). (Pubitemid 26019681)
18. Gladue, R.P., Bright, G.M., Isaacson, R.E. & Newborg, M.F. In vitro and in vivo uptake of azithromycin (CP-62,993) by phagocytic cells: possible mechanism of delivery and release at sites of infection. Antimicrob. Agents Chemother. 33, 277-282 (1989). (Pubitemid 19071957)
19. Carbon, C. Clinical relevance of intracellular and extracellular concentrations of macrolides. Infection 23(suppl. 1), S10-S14 (1995).
20. 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. 51, 103-109 (2007). (Pubitemid 46047694)
21. McDonald, P.J. & Pruul, H. Phagocyte uptake and transport of azithromycin. Eur. J. Clin. Microbiol. Infect. Dis. 10, 828-833 (1991).
22. Amsden, G.W., Nafziger, A.N. & Foulds, G. Pharmacokinetics in serum and leukocyte exposures of oral azithromycin, 1,500 milligrams, given over a 3- or 5-day period in healthy subjects. Antimicrob. Agents Chemother. 43, 163-165 (1999). (Pubitemid 29069218)
23. Ballow, C.H., Amsden, G.W., Highet, V.S. & Forrest, A. Pharmacokinetics of Oral Azithromycin in Serum, Urine, Polymorphonuclear Leucocytes and Inflammatory vs Non-Inflammatory Skin Blisters in Healthy Volunteers. Clin. Drug Investig. 15, 159-167 (1998). (Pubitemid 28101496)
24. Wilms, E.B., Touw, D.J. & Heijerman, H.G. Pharmacokinetics of azithromycin in plasma, blood, polymorphonuclear neutrophils and sputum during long-term therapy in patients with cystic fibrosis. Ther. Drug Monit. 28, 219-225 (2006). (Pubitemid 44314952)
25. Wilms, E.B., Touw, D.J. & Heijerman, H.G. Pharmacokinetics and sputum penetration of azithromycin during once weekly dosing in cystic fibrosis patients. J. Cyst. Fibros. 7, 79-84 (2008).
26. McNabb, J., Owens, R.C., Xuan, D., Quintiliani, R., Nightingale, C.H. & Nicolau, D.P. Comparison of azithromycin leukocyte disposition in healthy volunteers and volunteers with AIDS. Int. J. Antimicrob. Agents 16, 37-43 (2000). (Pubitemid 30665423)
27. Le T. First Aid for the USMLE Step 1 2008. (McGraw-Hill Medical: New York, 2008).
28. Wajima, T., Yano, Y. & Oguma, T. A pharmacokinetic model for analysis of drug disposition profiles undergoing enterohepatic circulation. J. Pharm. Pharmacol. 54, 929-934 (2002).
29. Gladue, R.P. & Snider, M.E. Intracellular accumulation of azithromycin by cultured human fibroblasts. Antimicrob. Agents Chemother. 34, 1056-1060 (1990). (Pubitemid 20177355)
30. Pillay, J. et al. In vivo labeling with 2H2O reveals a human neutrophil lifespan of 5.4 days. Blood 116, 625-627 (2010).
31. Pene Dumitrescu, T. et al. Development of a population pharmacokinetic model to describe azithromycin whole-blood and plasma concentrations over time in healthy subjects. Antimicrob. Agents Chemother. 57, 3194-3201 (2013).
32. Foulds, G., Shepard, R.M. & Johnson, R.B. The pharmacokinetics of azithromycin in human serum and tissues. J. Antimicrob. Chemother. 25(suppl. A), 73-82 (1990).
33. Equi, A., Balfour-Lynn, I.M., Bush, A. & Rosenthal, M. Long term azithromycin in children with cystic fibrosis: a randomised, placebo-controlled crossover trial. Lancet 360, 978-984 (2002). (Pubitemid 35284109)
34. Wolter, J., Seeney, S., Bell, S., Bowler, S., Masel, P. & McCormack, J. Effect of long term treatment with azithromycin on disease parameters in cystic fibrosis: a randomised trial. Thorax 57, 212-216 (2002). (Pubitemid 34214405)
35. Saiman, L. et al.; Macrolide Study Group. Azithromycin in patients with cystic fibrosis chronically infected with Pseudomonas aeruginosa: a randomized controlled trial. JAMA 290, 1749-1756 (2003).
36. Wildfeuer, A., Laufen, H. & Zimmermann, T. Distribution of orally administered azithromycin in various blood compartments. Int. J. Clin. Pharmacol. Ther. 32, 356-360 (1994). (Pubitemid 24212081)
37. Nibbering, P.H., Zomerdijk, T.P., Corsel-Van Tilburg, A.J. & Van Furth, R. Mean cell volume of human blood leucocytes and resident and activated murine macrophages J. Immunol. Methods. 129(1), 143-145 (1990).
38. Comets, E., Brendel, K. & Mentré, F. Computing normalised prediction distribution errors to evaluate nonlinear mixed-effect models: the npde add-on package for R. Comput. Methods Programs Biomed. 90, 154-166 (2008).