Abstract
According to international post-marketing trials, levofloxacin now belongs to the antimicrobial agents being in a great demand in clinical practice. One of the main indications for its use is community-acquired pneumonia (CAP). This review article is dedicated to 20-year on-market experience of levofloxacin and provides data on clinical efficacy of levofloxacin in the treatment of CAP, pharmacokinetics, pharmacodynamics, and safety. Despite the 20-year clinical experience, levofloxacin remains one of the most successful antimicrobials for the treatment of CAP, and it is reflected in current international guidelines presented in this review.
-
1.
Andriaenssens N., Coenen S., Versporten A., et al. European Surveillance of Antimicrobial Consumption (ESAC): outpatient quinolone use in Europe (1997- 2009). J Antimicrob Chemother 2011; 66(Suppl.6):47-56.
-
2.
Drlica K. & Zhao X. DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiology and Molecular Biology Reviews 1997; 61:377-92.
-
3.
Hawkey P.M. Mechanisms of quinolone action and microbial response. J Antimicrob Chemother 2003; 51 (Suppl. S1):29-35.
-
4.
Hooper D.C. Mechanisms of fluoroquinolone resistance. Drug Resistance Updates 1999; 2:38-55.
-
5.
Hoshino K., Kitamura A., Morrissey I., Sato K., Kato J. & Ikeda H. Comparison of inhibition of Escherichia coli topoisomerase IV by quinolones with DNA gyrase inhibition. Antimicrob Agents Chemother 1994; 38:2623-7.
-
6.
Huband M.D., Cohen M.A., Zurack M., et al. In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant grampositive and fastidious organism groups. Antimicrob Agents Chemother 2007; 51(4):1191-201.
-
7.
Huband M.D., Brightly K.E., Monohan R., et al. In vitro antibacterial activity of CE-156811, CP-919474, and CP-929898: novel hygromycin A analogs compared to levofloxacin and other antibacterial agents against 1220 recent clinical isolates [abstract no. F1-1963]. 46th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2006 Sep 27-30; San Francisco.
-
8.
Nilius A.M., Shen L.L., Hensey-Rudolf D., et al. In vitro antibacterial potency and spectrum of ABT-492, a new fluoroquinolone. Antimicrob Agents Chemother 2003; 47 (10):3260-9.
-
9.
Fritsche T.R., Sader H.S., Jones R.N. Potency and spectrum of garenofloxacin tested against an international collection of skin and soft tissue infection pathogens: report from SENTRY antimicrobial surveillance program (1999- 2004). Diagn Microbiol Infect Dis 2007; 58(1):19-26.
-
10.
Goff D.A., Dowzicky M.J. Prevalence and regional variation in meticillin-resistant Staphylococcus aureus (MRSA) in the USA and comparative in vitro activity of tigecycline, a glycylcycline antimicrobial. J Med Microbiol 2007; 56(9):1189-95.
-
11.
Hoban D., Waites K., Felmingham D. Antimicrobial susceptibility among community-acqiured respiratory tract pathogens in North America in 1999-2000: findings of the PROTEKT surveillance study. Diagn Microbiol Infect Dis 2003; 45(4):251-9.
-
12.
Gordon K.A., Sader H.S., Jones R.N. Contemporary re-evaluation of the activity and spectrum of grepafloxacin tested against isolates in the United States. Diagn Microbiol Infect Dis 2003; 47(1):377-83.
-
13.
Woodhead M., Blasi F., Ewig S. and the ERS/ESCMID Task Force. Guidelines for the management of adult lower respiratory tract infections. Clin Microbiol Infect 2011; 17 (Suppl. 6):1-59.
-
14.
Козлов Р.С., Сивая О.В., Кречикова О.И. и группа исследователей проекта «ПеГАС». Динамика резистентности Streptococcus pneumoniae к антибиотикам в России за период 1999 -2009 гг. (Результаты многоцентрового проспективного исследования ПеГАС) Клин микробиол антимикроб химиотер 2010; 12(4):29-41.
-
15.
Чучалин А.Г., Синопальников А.И., Козлов Р.С. и др. Внебольничная пневмония у взрослых: практические рекомендации по диагностике, лечению и профилактике. Пособие для врачей. Москва, 2010, 106 с.
-
16.
Bouchillon S., Hackel M., Johnson J., et al. The carbapenem PZ-601 has potent in vitro Gram-positive, Gram-negative and anaerobic bacterial activity (poster F1-343). 47th Interscience Conference on Antimicrobial Agents and Chemotherapy; 2007 Sep 17-20; Chicago.
-
17.
Soriano F., Granizo J.J., Coronel P., et al. Antimicrobial susceptibility of Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis isolated from adult patients with respiratory tract infections in four southern European countries. The ARISE project. Int J Antimicrob Agents 2004; 23(3):296-9.
-
18.
Critchley I., Jones M.E., Heinze P. et al. In vitro activity of levofloxacin against contemporary clinical isolates of Legionella pneumophila, Mycoplasma pneumoniae and Chlamydia pneumoniae from North America and Europe. Clin Microbiol Infect 2002; 8:214-21.
-
19.
Anderson M.I., MacGowan A.P. Development of the quinolones. J Antimicrob Chemother 2003; 51 (Suppl. S1):1-11.
-
20.
Croom K.F., Goa K.L. Levofloxacin: a review of its use in the treatment of bacterial infections in the United States. Drugs 2003; 63(24):2769-802.
-
21.
Spangler S., Bajaksouzian S., Jacobs M.R. et al. Postantibiotic effect of levofloxacin against pneumococci. Drugs 1999; 58 (Suppl.2):378-80.
-
22.
Fish D.N., Chow A.T. The clinical pharmacokinetics of levofloxacin. Clin Pharmacokinet 1997; 32:101-19.
-
23.
Holland M., Chien S., Corrado M. et al. The pharmacokinetic profile of levofloxacin following once- or twicedaily 500 mg administration. Proceedings of Fifth International Symposium on New Quinolones; 1994 Aug 25-27; Singapore.
-
24.
Holland M., Chien S., Corrado M. et al. The pharmacokinetic profile of intravenous levofloxacin following once- or twice-daily administration. Proceedings of Fifth International Symposium on New Quinolones; 1994 Aug 25-27; Singapore.
-
25.
Chow A.T., Fowler C.L., Williams R.R., et al. Safety and pharmacokinetics of multiple 750-milligram doses of intravenous levofloxacin in healthy volunteers. Antimicrob Agents Chemother 2001; 45(7):2122-5.
-
26.
Chien S.C. Wong F.A., Fowler C.L., et al. Double-blind evaluation of the safety and pharmacokinetics of multiple oral once-daily 750-milligram and 1-gram doses of levofloxacin in healthy volunteers. Antimicrob Agents Chemother 1998; 42(4):885-8.
-
27.
LeBel M., Vallee F., Bergeron M. Tissue penetration of ciprofloxacin after single and multiple doses. Antimicrob Agents Chemother 1986; 29:501-5.
-
28.
Gonzalez M., Moranchel A., Duran S. et al. Multipledoses pharmacokinetics of ciprofloxacin administered intravenously to normal volunteers. Antimicrob Agents Chemother 1985; 28:235-9.
-
29.
Stass H., Dalhoff A., Kubitza D. et al. Pharmacokinetics, safety and tolerability of ascending single doses of moxifloxacin, a new 8-methoxy quinolone, administered to healthy subjects. Antimicrob Agents Chemother 1998; 42:2060-5.
-
30.
Stass H., Kubitza D. Basic pharmacokinetics of moxifloxacin. Drugs 1999; 58 (Suppl. 2):225-6.
-
31.
Stass H., Kubitza D. Pharmacokinetics and elimination of moxifloxacin after oral and intravenous administration in man. J Antimicrob Chemother 1999; 43:83-90.
-
32.
Gatifloxacin T. Princeton (NJ): Bristol-Meyers Squibb Co, 2000. (Data on file).
-
33.
Keller I., Lubasch A., Rau M. et al. Comparative pharmacokinetics of ciprofloxacin, gatifloxacin, levofloxacin, moxifloxacin, and trovafloxacin after a single in healthy volunteers [abstract 30]. 39th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1999 Sep 26-29:San Francisco.
-
34.
Drusano G.L., Preston S.L., Gotfried M.H. et al. Levofloxacin penetration into epithelial lining fluid as determined by population pharmacokinetic modeling and Monte Carlo simulation. Antimicrob Agents Chemother 2002; 46:586-9.
-
35.
Guay D.R.P. Implications of quinolones pharmacocinetic drag interactions. Hosp Pharm 1997; 32:677–90.
-
36.
Langtry H.D, Lamb H.M. Levofloxacin: its use in infections of respiratory tract, skin, soft tissues and urinary tract. Drugs 1998 Sep; 56:487-515.
-
37.
Zhanel G.G., Walkty A., Vercaigne L. et al. The new fluoroquinolones: a critical review. Can J Infect Dis 1999; 10(3):207-38.
-
38.
File TM Jr., Segreti J., Dunbar L. et al. A multicenter, randomized study comparing the efficacy and safety of intravenous and/or oral levofloxacin versus ceftriaxone and/or cefuroxime axetil in treatment of adults with community-acquired pneumonia. Antimicrob Agents Chemother 1997; 41(9):1965-72.
-
39.
Kahn J.B., Weisinger B.A., Olson W.H. et al. Treatment of patients with commmunity-acquired pneumonia at high risk of mortality (abstract); American Society of Health-System Pharmacists (ASHP) Midyear Clinical Meeting. New Orleans, 2001.
-
40.
Carbon C., Ariza H., Rabie W.J., et al. Comparative study of levofloxacin and amoxycillin/clavulanic acid in adults with mild-to-moderate community-acquired pneumonia. Clin Microbiol Infect 1999; 5(12):724-32.
-
41.
Gotfried M.H., Dattani D., Riffer E. et al. A controlled, double-blind, multicenter study comparing clarithromycin extended-release tablets with levofloxacin tablets in the treatment of community-acquired pneumonia. Clin Ther 2002; 24:736-51.
-
42.
D′Ignazio J., Camere M.A., Lewis D.E., et al. Novel, single-dose microsphere formulation of azithromycin versus 7-day levofloxacin therapy for threatment of mild to moderate community-acquired pneumonia in adults. Antimicrob Agents Chemother 2005; 49:4035-41.
-
43.
Frank E., Liu J., Kinasewitz G., et al. A multicenter, open-label, randomized comparison of levofloxacin and azithromycin plus ceftriaxone in hospitalized adults with moderate to severe community-acquired pneumonia. Clin Ther 2002; 24:1292-308.
-
44.
Frei C.R., Jaso T.C., Mortensen E.M., et al. Medical resourse utilization among community-acqiured pneumonia patients initially treated with levofloxacin 750 mg daily versus ceftriaxone 1000 mg plus azithromycin 500 mg daily: a US-based study. Curr Med Res Opin 2009; 25:859-68.
-
45.
Ramirez J.A., Cooper A.C., Wiemken T., et al. Switch therapy in hospitalized patients with community-acqiured pneumonia: Tigecycline vs. Levofloxacin. BMC Infectious Disease 2012; 12:159.
-
46.
Menendez R., Torres A., Zalacain R., et al. Risk factors of treatment failure in community-acqiured pneumonia: implications for disease outcome. Thorax 2004; 59:960-65.
-
47.
Olive D., Georges H., Devos D., et al. Severe pneumococcal pneumonia: impact of new quinolones on prognosis. BMC Infectious Diseases 2011; 11:66.
-
48.
Vardakas K.Z., Siempos I.I., Grammatikos A., et al. Respiratory fluoroquinolones for the treatment of community-acquired pneumonia: a meta-analysis of randomized controlled trials. CMAJ 2008; 179(12):1269-77.
-
49.
Yu V.L., Williams R.R., Stout J.E. et al. Levofloxacin is safe and effective in the management of community-acquired pneumonia (CAP) due to Legionella. J Antimicrob Chemother 2001; 47 (Suppl. 1):45.
-
50.
Blazquez-Garrido R.M., Espinosa Parra F.J., Alemany France′s L. et al. Antimicrobial chemotherapy for Legionnaire’s disease: levofloxacin versus macrolides. Clin Infect Dis 2005; 40:800–6.
-
51.
Mykietiuk A., Carratala J., Ferna′ndez-Sabe′ N. et al. Clinical outcomes for hospitalized patients with Legionella pneumonia in the antigenuria era: the influence of levofloxacin therapy. Clin Infect Dis 2005; 40:794-9.
-
52.
Sabria M, Pedro-Botet ML, Go′mez J et al. For the Legionniares’ disease therapy group. Fluoroquinolones versus macrolides in the treatment of Legionnaire’s disease. Chest 2005; 128:1401–5.
-
53.
Anderson V.R., Perry C.M. Levofloxacin. A review of its use a high-dose, short-course treatment for bacterial infection. Drugs 2008; 68(4):535-65.
-
54.
Dunbar L.M., Wunderink R.G., Habib M.P., et al. Highdose, short-course levofloxacin for community-acquired pneumonia: a new treatment paradigm. Clin Infect Dis 2003; 37(6):752-60.
-
55.
Dunbar L.M., Khashab M.M., Kahn J.B., et al. Efficacy of 750-mg, 5-day levofloxacin in the treatment of community-acquired pneumonia caused by atypical pathogens. Curr Med Res Opin 2004; 20(4):555-63.
-
56.
Shorr A.F., Khashab M.M., Xiang J.X., et al. Levofloxacin 750-mg for 5 days for the treatment of hospitalized fine risk class III/IV community-acquired pneumonia patients. Respir Med 2006; 100(12):2129-36.
-
57.
Shorr A.F., Zadeikis N., Xiang J.X., et al. A multicenter, randomized, double-blind, retrospective comparison of 5- and 10-day regimens of levofloxacin in a subgroup of patients aged ≥65 years with community-acquired pneumonia. Clin Ther 2005; 27(8):1251-9.
-
58.
Khashab M.M., Xiang J., Kahn J.B. Comparison of the adverse event profiles of levofloxacin 500 mg and 750 mg in clinical trial for the treatment of respiratory infections. Curr Med Res Opin 2006; 22(10):1997-2006.
-
59.
Owens RC, Ambrose PG. Atnimicrobial safety: focus on fluoroquinolones. Clin Infect Dis 2005; 41 (Suppl. 2):144-57.