Clarithromycin: Pharmacokinetic and pharmacodynamic interrelationships and dosage regimen

Journal of Chemotherapy

Volumn 11, Issue 1, 1999, Pages 11-27

  Periti, Piero ^a,b   Mazzei, T ^a  

^a UNIVERSITY OF FLORENCE   (Italy)

^b NONE   (Italy)

Author keywords

Clarithromycin; Macrolides; Pharmacodynamics; Pharmacokinetics

Indexed keywords

14 HYDROXYCLARITHROMYCIN; AMINOGLYCOSIDE ANTIBIOTIC AGENT; ANTIBIOTIC AGENT; AZITHROMYCIN; BETA LACTAM ANTIBIOTIC; CARBAPENEM DERIVATIVE; CEPHEM DERIVATIVE; CLARITHROMYCIN; DIRITHROMYCIN; ERYTHROMYCIN; GLYCOPEPTIDE; LINCOSAMIDE DERIVATIVE; MACROLIDE; MONOBACTAM DERIVATIVE; NITROIMIDAZOLE DERIVATIVE; PENAM DERIVATIVE; PENICILLIN G; QUINOLINE DERIVED ANTIINFECTIVE AGENT; TUBERCULOSTATIC AGENT;

ANTIBIOTIC RESISTANCE; ANTIBIOTIC THERAPY; AREA UNDER THE CURVE; BACTERICIDAL ACTIVITY; DOSE TIME EFFECT RELATION; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG EXCRETION; DRUG HALF LIFE; DRUG INDICATION; DRUG MECHANISM; DRUG PENETRATION; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG STRUCTURE; DRUG TISSUE LEVEL; HUMAN; MINIMUM INHIBITORY CONCENTRATION; REVIEW;

EID: 0033008152     PISSN: 1120009X     EISSN: None     Source Type: Journal    
DOI: 10.1179/joc.1999.11.1.11     Document Type: Review

References (84)

1. 1 Benet LZ. General Principles - Introduction - Section I. In: Goodman & Gilman's The Pharmacological Basis of Therapeutics (Hardman JG, Goodman Gilman A, Limbird LE, Molinoff PB, Ruddon RW, Eds) 9th Ed. The McGraw-Hill Companies, Inc, New York 1996a: 1-2.
2. 2 Cars O. Pharmacokinetics of antibiotics in tissue and tissue fluids: a review. Scand J Infect Dis 1991; Suppl 74: 23-33.
3. 3 Ross EM. Pharmacodynamics - Mechanisms of drug action and the relationship between drug concentration and effect. In: Goodman & Gilman's The Pharmacological Basis of Therapeutics (Hardman JG, Goodman Gilman A, Limbird LE, Molinoff PB, Ruddon RW, Eds) 9th Ed. The McGraw-Hill Companies, Inc, New York 1996: 29-42.
4. 4 Bax RP. Antibiotic resistance: a view from the pharmaceutical industry. Clin Infect Dis 1997; 24 (suppl 1): 151-153.
5. 5 Periti P. Razionalità nella scelta di una betalattamina orale. Farm Ter 1997; XIV (1/2): 1-24.
6. 6 Periti P. Preclinical and clinical evaluation of once-daily aminoglycoside chemotherapy. J Chemother 1995; 7 (4): 311-337.
7. 7 Craig WA. Interrelationship between pharmacokinetics and pharmacodynamics in determining dosage regimens for broad-spectrum cephalosporins. Diagn Microbiol Infect Dis 1995; 22: 89-96.
8. 8 Periti P, Mazzei T, De Gaudio AR, Tonelli F. Attuali orientamenti nella scelta e modalità di somministrazione degli agenti antimicrobici per una razionale chemioterapia della sepsi grave. Farm Ter 1998; XV (1/2), in corso di stampa.
9. 9 Nightingale CH. Pharmacokinetics and pharmacodynamics of newer macrolides. Pediatr Infect Dis J 1997; 16: 438-443.
10. 10 Craig WA. Selecting the antibiotic. Proceedings of a Symposium, Sonoma 26-27/1/1993a, Vol 28 (Suppl 1): 16-20.
11. 11 Eagle H, Fleischman R, Levy M. "Continuous" vs. "discontinuous" therapy with penicillin. The effect of the interval between injections on therapeutic efficacy. N Engl J Med 1953; 248: 481-488.
12. 12 Schentag JJ, Nix DE, Forrest A, Adelman MH. AUIC -the universal parameter within the constraint of a reasonable dosing interval. Ann Pharmacother 1996; 30: 1029-1031.
13. 13 Thomas JK, Forrest A, Bhavnani SM, et al. Pharmacodynamic evaluation of factors associated with the development of bacterial resistance in acutely ill patients during therapy. Antimicrob Agents Chemother 1998; 42: 521-527.
14. 14 Redington J, Ebert S, Craig WA. Role of antimicrobial pharmacokinetics and pharmacodynamics in surgical prophylaxis. Rev Infect Dis 1991; 13: 790-799.
15. 15 Granger HJ. Role of the interstitial matrix and lymphatic pump in regulation of transcapillary fluid balance. Microvasc Res 1979; 18:209-216.
16. 16 Tulkens PM. Intracellular pharmacokinetics and localization of antibiotics as predictors of their efficacy against intraphagocytic infections. Scand J Infect Dis 1991; 23 (suppl 74): 209-217.
17. 17 Merrikin DJ, Briant J, Rolinson GN. Effect of protein binding on antibiotic activity in vivo. J Antimicrob Chemother 1983; 11:233-238.
18. 18 Benet LZ, Kroetz DL, Sheiner LB. Pharmacokinetics - The dynamics of drug absorption, distribution, and elimination. In: "Goodman & Gilman's The Pharmacological Basis of Therapeutics" (Hardman JG, Goodman Gilman A, Limbird LE, Molinoff PB, Ruddon RW, Eds) 9th Ed. The McGraw-Hill Companies, Inc, New York 1996b: 3-28.
19. 19 Periti P, Mazzei T, Mini E, Novelli A, Reali EF. Altualità delle cefalosporine in chemioterapia. Edizioni Riviste Scientifiche, Firenze 1988: 3-207.
20. 20 Den Hollander JG, Mouton JW, Verbrugh HA. Use of pharmacodynamic parameters to predict efficacy of combination therapy by using fractional inhibitory concentration kinetics. Antimicrob Agents Chemother 1998; 42 (4): 744-748.
21. 21 Drusano GL, Goldstein FW. Relevance of the Alexander Project: pharmacodynamic considerations. J Antimicrob Chemother 1996; 38 (Suppl A): 141-154.
22. 22 Morimoto S, Takahashi Y, Watanabe Y, et al. Chemical modification of erythromycins. I. Synthesis and antibacterial activity of 6-O-methylerythromycins A. J Antibiot 1984; 37: 187-189.
23. 23 Fraschini F, Scaglione F, Demartini G. Clarithromycin clinical pharmacokinetics. Clin Pharmacokinet 1993; 25 (3): 189-204.
24. 24 Sturgill MG, Rapp RP. Clarithromycin: review of a new macrolide antibiotic with improved microbiologic spectrum and favorable pharmacokinetic and adverse effect profiles. Ann Pharmacother 1992; 26: 1099.
25. 25 Ishii K, Saito Y, Itai S, Nemoto M, Takayama K, Nagai T. Comparative study of pharmacokinetic parameters between Clarithromycin and erythromycin stearate in relation to their physicochemical properties. Drug Develop Ind Pharm 1998; 24 (2): 129-137.
26. 26 Mazzei T, Mini E, Novelli A, Periti P. Chemistry and mode of action of macrolides. J Antimicrob Chemother 1993; 31 (Suppl C): 1-9.
27. 27 Champney WS, Burdine R. 50S Ribsomal subunit synthesis and translation are equivalent targets for erythromycin inhibition in Staphylococcus aureus. Antimicrob Agents Chemother 1996; 40: 1301-1303.
28. 28 Champney WS, Burdine R. Azithromycin and clarithromycin inhibition of 50S ribosomal subunit formation in Staphylococcus aureus cells. Curr Microbiol 1998; 36: 119-123.
29. 29 Hardy DJ. Extent and spectrum of the antimicrobial activity of Clarithromycin. Pediatr Infect Dis J. 1993; 12 (12): S99-S105.
30. 30 Peters DH, Clissold SP. Clarithromycin. A review of its antimicrobial activity, pharmacokinetic properties and therapeutic potential. Drugs 1992; 44 (1): 117-164.
31. 31 National Committee for Clinical Laboratory Standards. Jorgensen JH et al, eds. Performance standards for antimicrobial susceptibility testing. National Committee for Clinical Laboratory Standards, publication M100-S4 Villanova, Pa. 1992.
32. 32 Barradell LB, Plosker GL, McTavish D. Clarithromycin - A review of its pharmacological properties and therapeutic use in Mycobacterium avium-intracellulare complex infection in patients with acquired immune deficiency syndrome. Drugs 1993; 46 (2): 289-312.
33. 33 Grüneberg RN. The Alexander Project: using in-vitro susceptibility data for choosing empirical therapy in LRTI. J Antimicrob Chemother 1996; 38 (Suppl A): 155-170.
34. 34 Hardy DJ, Seanson RN, Rode RA, et al. Enhancement of the in vitro and in vivo activities of clarithromycin against Haemophilus influenzae by 14-hydroxyclarithromycin, its major metabolite in humans. Antimicrob Agents Chemother 1990; 34: 1407-1413.
35. 35 Zuckerman JM, Kaye KM. The newer macrolides. Azithomycin and clarithromycin. Infect Dis Clin N Am 1995; 9 (3): 731-745.
36. 36 Charles L, Segreti J. Choosing the right macrolide antibiotic. A guide to selection. Drugs 1997; 53 (3): 349-357.
37. 37 Neu HC. Activity of macrolides against common pathogens in vitro. In: "Macrolides: chemistry, pharmacology, and clinical use" (Bryskier J, Butzler JP, Neu HC, Tulkens PM, Eds), Arnette Blackwell, Oxford 1993: 167-182.
38. 38 Fraschini F, Scaglione F. La claritromicina. Masson, 1990:31.
39. 39 Hardy DJ, Guay DRP, Jones RN. Clarithromycin, a unique macrolide: a pharmacokinetic, microbiological, and clinical overview. Diagn Microbiol Infect Dis 1992; 15: 39.
40. 40 Chu S-Y, Sennello LT, Bunnell ST, Varga LL, Wilson DS, Sonders RC. Pharmacokinetics of clarithromycin, a new macrolide, after single ascending oral doses. Antimicrob Agents Chemother 1992; 36 (11): 2447-2453.
41. 41 Wise R. The development of macrolides and related compounds - Leading article. J Antimicrob Chemother 1989; 23: 299-300.
42. 42 Piscitelli SC, Danziger LH, Rodvold KA. Clarithromycin and azithromycin: new macrolide antibiotics. Clin Pharm 1992; 11: 137-152.
43. 43 Kees F, Wellenhofer M, Grobecker H. Serum and cellular pharmacokinetics of clarithromycin 500 mg q.d. and 250 mg b.i.d. in volunteers. Infection 1995; 23 (3): 168-172.
44. 44 Ferrero JL, Bopp BA, Marsh KC et al. Metabolism and disposition of clarithromycin in man. Drug Metab Dispos 1990; 18:441-446.
45. 45 Chu S-Y, Wison DS, Deaton RL, Mackenthun AV, Eason CN, Cavanaugh JH. Single-and multiple-dose pharmacokinetics of clarithromycin, a new macrolide antimicrobial. J Clin Pharmacol 1993; 33: 719-726.
46. 46 Rapp RP, McCraney SA, Goodman NL, Shaddick DJ. New macrolide antibiotics: usefulness in infections caused by mycobacteria other than Mycobacterium tuberculosis. Ann Pharmacother 1994; 28: 1255-1263.
47. 47 Wise R, Andrews JM, Honeybourne D, Kees F. The penetration of azalides and macrolides into the respiratory tract. 2nd Internatl Conf Macrolides, Azalides and Streptogramins, Venice, Jan 19-22 1994: Abstr 193.
48. 48 Drusano GL, Craig WA. Relevance of pharmacokinetics and pharmacodynamics in the selection of antibiotics for respiratory tract infections. J Chemother 1997; 9 (Suppl 3): 38-44.
49. 49 Carbon C. Clinical relevance of intracellular and extracellular concentrations of macrolides. Infection 1995; 23 (suppl 1): 10-14.
50. 50 Hardy DJ, Hensey DM, Beyer JM, et al. Comparative in vitro activities of new 14-, 15-, and 16-membered macrolides. Antimicrob Agents Chemother 1988; 32 (11): 1710-1719.
51. 51 Sedlmayr T, Peters F, Raasch W, Kees F. Clarithromycin, ein neues Makrolid-Antibiotikum. Wirksamkeit bei puerperalen Infektionene und Ubertritt in die Muttermilch. Geburtshilfe und Frauenheilkunde 1993; 53: 489-491.
52. 52 Mazzei T, Periti P. Tissue distribution of antimicrobial drugs. J Chemother 1989; 1 (2): 75-79.
53. 53 Patel KB, Xuan D, Tessier PR, Russomanno JH, Quintiliani R, Nightingale CH. Comparison of bronchopulmonary pharmacokinetics of clarithromycin and azithromycin. Antimicrob Agents Chemother 1996; 40 (10): 2375-2379.
54. 54 Mazzei T. Intracellular levels are more important than interstitial levels of antibiotics. 2nd European Congress of Chemotherapy and 7th Biennial Conference on Antiinfective Agents and Chemotherapy, May 10-13, 1998 Hamburg, Final Programme. Futuramed, Germany 1998: 26.
55. 55 Honeybourne D, Kees F, Andrews JM, Baldwin D, Wise R. The levels of clarithromycin and its 14-hydroxy-metabolite in the lung. Eur Respir J 1994; 7: 1275-1280.
56. 56 Conte JE, Golden JA, Duncan S, McKenna E, Zurlinden E. Intrapulmonary pharmacokinetics of clarithromycin and of erythromycin. Antimicrob Agents Chemother 1995; 39 (2): 334-338.
57. 57 Conte JE, Golden F, Duncan S, McKenna E, Lin E, Zurlinden E. Single-dose intrapulmonary pharmacokinetics of azithromycin clarithromycin, ciprofloxacin, and cefuroxime in volunteer subjects. Antimicrob Agents Chemother 1996; 40 (7): 1617-1622.
58. 58 Rodvold KA, Gotfrierd MH, Danziger LH, Servi RJ. Intrapulmonary steady-state concentrations of clarithromycin and azithromycin in healthy adult volunteers. Antimicrob Agents Chemother 1997; 41 (6): 1399-1402.
59. 59 Fish DN, Gotfried MH, Danziger LH, Rodvold KA. Penetration of clarithromycin into lung tissues from patients undergoing lung resection. Antimicrob Agents Chemother 1994; 38 (4): 876-878.
60. 60 Bauernfeind A, Jungwirth R, Eberlein E. Comparative pharmacodynamics of clarithromycin and azithromycin against respiratory pathogens. Infection 1995; 23: 316-321.
61. 61 Periti P, Mazzei T, Mini E, Novelli A. Clinical pharmacokinetic properties of the macrolide antibiotics - Effects of age and various pathophysiological states (Part II). Clin Pharmacok 1989; 16: 261-282.
62. 62 Wildfeuer A, Resert I, Laufen H. Uptake and subcellular distribution of azithromycin in human phagocytic cells. Arzneim Forsch Drug Res 1993; 43: 484-486.
63. 63 Daikos GK. Continuous versus discontinuous antibiotic therapy: the role of the post-antibiotic effect and other factors. J Antimicrob Chemother 1991; 27 (2): 157-160.
64. 64 Craig WA, Gudmundsson S. Postantibiotic effect. In: Antibiotics in Laboratory Medicine (Lorian V, Ed), Third Ed. Williams & Wilkins, New York 1991: 403-431.
65. 65 Craig WA. Post-antibiotic effect of macrolides. In: Macrolides: Chemistry, Pharmacology and Clinical Uses, (Bryskier AJ, Butzler J-P, Neu HC, Tulkens PM, Eds). Arnette Blackwell, Paris 1993: 205-208.
66. 66 MacKenzie FM, Gould IM. The post-antibiotic effect -Review. J Antimicrob Chemother 1993; 32: 519-537.
67. 67 Periti P. The chemotherapeutic formula revisited. J Chemother 1997; 8 (Suppl 1): 123-133.
68. 68 Shibl AM. Effect of antibiotics on adherence of microorganisms to epithelial cell surfaces. Rev Infect Dis 1985; 7: 51-56.
69. 69 Baddour LM, Christensen GD, Simson WA, Beachey EH. In: Principles and Practice of Infectious Diseases, (Mandel GL, Douglas RG-Jr, Bennett JE, Eds), Third Edition, Churchill Livingstone, New York 1990: 9-25.
70. 70 Drusano GL. Role of pharmacokinetics in the outcome of infections. Antimicrob Agents Chemother 1988; 32: 289-297.
71. 71 Craig WA. Post-antibiotic effects in experimental infection models: relationship to in-vitro phenomena and to treatment of infections in man. J Antimicrob Chemother 1993; 31 (Suppl D): 149-158.
72. 72 Craig WA, Andes D. Pharmacokinetics and pharmacodynamics of antibiotics in otitis media. Pediatr Infect Dis J 1996; 15: 255-259.
73. 73 Zinner SH, Dudley MN, Gilbert D, Bassignani M. Effect of dose and schedule on cefoperazone pharmacodynamics in an in vitro model of infection in a neutropenic host. Am J Med 1988; 85 (Suppl 1A): 56-58.
74. 74 Stahlmann R, Lode H. Concentration-effect relationship of the fluoroquinolones. In: Quinolone Antibacterials (Kuhlman J, Dalhoff A, Zeiler HJ, Eds), Springer-Verlag, Berlin 1998: 407-420.
75. 75 Scaglione F, Dugnani S, Demartini G, Saudelli M, Galmozzi G, Fraschini F. The postantibiotic effect of clarithromycin and its major human metabolite, 14-hydroxy clarithromycin. J Antimicrob Chemother 1993; 32: 507-509.
76. 76 Ellis LC, Benson CA, Koenig GI, Trenholme GM. Postantibiotic effect of clarithromycin alone and combined with ethambutol against Mycobacterium avium complex. Antimicrob Agents Chemother 1995; 39 (12): 2803-2806.
77. 77 Fuursted K. Evaluation of the post-antibiotic effect of six anti-mycobacterial agents against Mycobacterium avium by the BACTEC radiometric method. J Antimicrob Chemother 1997; 40: 33-38.
78. 78 Mülazimoglu L, Periti P. Macrolides. In: Antimicrobial Chemotherapy (Yu V, Merigan T, Barriere S, Eds). Williams & Wilkins, Baltimore 1998, in corso di stampa.
79. 79 Periti P, Mazzei T, Mini E, Novelli A. Recenti progressi nella chemioterapia antimicrobica orale: la claritromicina. Farm Ter 1990; VII (Suppl 1): 5-63.
80. 80 Den Hollander JG, Knudsen JD, Mouton JW, et al. Comparison of pharmacodynamics of azithromycin and erythromycin in vitro and in vivo. Antimicrob Agents Chemother 1998; 42 (2): 377-382.
81. 81 Schentag JJ, Ballow CH. Tissue-directed Pharmacokinetics. Am J Med 1991; 91 (Suppl 3A): 5-10.
82. 82 Dabernat H, Delmas C, Seguy M, et al. The activity of clarithromycin and its 14-hydroxy metabolite against Haemophilus influenzae determined by in vitro and serum batericidal tests. J Antimicrob Chemother 1991; 27 (Suppl A): 19-30.
83. 83 Wallace RJ-Jr, Brown AB, Griffith DE, Girard WM, Murphy DT. Clarithromycin regimens for pulmonary Mycobacterium avium Complex. The first 50 patients. Am J Resp Crit Care Med 1996; 153: 1766-1772.
84. 84 Dautzenberg B, Truffot-Pernot C, Hazebroucq J, et al. A randomized comparison of two clarithromycin doses for treatment of Mycobacterium avium complex infections. Infection 1997; 25 (1): 16-21.