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Levofloxacin (Levaquin) versus ...

According to the studies, the rank order of phototoxic potential of fluoroquinolones is as follows: enoxacin> ciprofloxacin > norfloxacin = ofloxacin = levofloxacin = gatifloxacin = moxifloxacin 1, 2.

Based on published literature, the approximate order of fluoroquinolones in which they significantly interact with theophylline is as follows: enoxacin > ciprofloxacin > norfloxacin > ofloxacin, levofloxacin, trovafloxacin, gatifloxacin, moxifloxacin.

The side-effect profile of levofloxacin was compared with that of other fluoroquinolones based on European and international data from approximately 130 million prescriptions 12. Levofloxacin was found to be very safe with a low rate of hepatic abnormalities (1/650,000). The main CNS problems associated with fluoroquinolones include dizziness, convulsions, psychosis, and insomnia. Levofloxacin, ofloxacin, and moxifloxacin reportedly have the lowest potential of inducing central nervous system (CNS) adverse events among the fluoroquinolones currently available. Cardiovascular problems were seen in 1/15 million levofloxacin prescriptions compared to 1-3% of sparfloxacin patients having QTc prolongation of greater than 500 msec. Moxifloxacin was also associated with QTc prolongation when compared to non-fluoroquinolone comparators. Nausea, vomiting, and diarrhoea remain the main adverse drug reactions associated with levofloxacin. However, the ADR rate for levofloxacin is still one of the lowest of any fluoroquinolone at 2% (compared to 2-10% for other fluoroquinolones). The tolerance profile of levofloxacin can be considered to be very good, and better than most, if not all of the fluoroquinolones available.

Levofloxacin vs. Lomefloxacin (Maxaquin)

Urinary Tract Infections

Once-daily levofloxacin is as effective as and has a superior tolerability profile than lomefloxacin in the treatment of complicated UTIs 11.

Results of controlled trial of levofloxacin and lomefloxacin in the treatment of complicated urinary tract infection 11.
Levofloxacin
Lomefloxacin
Regimen 250 mg once daily for 7 to 10 days 400 mg once daily for 14 days
The overall microbiologic eradication rate
95.5%
(168 patients of 176)
91.7%
(154 patients of 168)
Eradication rates with respect to patients
95.3%
(163 patients of 171)
92.1%
(152 patients of 165)
Complete resolution of symptoms at the 5 to 9-day post-therapy
84.8%
82.4%
Decreased symptoms
8.2%
6.1%
Clinical success rate
93%
88.5%
Adverse events
10 patients (2.6%)
18 patients (5.2%)
Photosensitivity reactions
0
3 patients (1.3%)
Dizziness
0
2 patients (0.9%)
Nausea
3 patients (1.3%)
1 patients (0.4%)
Gastrointestinal
6 patients (1.7%)
6 patients (1.7%)
Rash
1 patient (0.4%) 4 patients (0.4%)
Discontinuation because of adverse events observed in 8 (3.4%) levofloxacin- and 14 (6.1%) lomefloxacin-treated patients.
8 patients (3.4%)
14 patients (6.1%)

Acute Pyelonephritis

Levofloxacin is more effective than lomefloxacin in the treatment of acute pyelonephritis9

Results of trial comparing levofloxacin with lomefloxacin for acute pyelonephritis 9
Levofloxacin
Lomefloxacin
Regimen 250 mg once daily 400 mg once daily
Eradication of uropathogens rate at 5 to 9 days after the end of treatment (predominant pathogen E. coli)
95%
95%
Clinical cure rate
92%
80%
Adverse events
2%
5%


Levofloxacin vs. Clarithromycin (Biaxin)

Bacterial exacerbation of chronic obstructive pulmonary disease (COPD)

Levofloxacin and clarithromycin provide similar COPD exacerbation-free periods. Levofloxacin treatment results in significantly higher bacteriological eradication rate 4.

Results of study comparing levofloxacin versus clarithromycin in COPD exacerbation4.
Levofloxacin
Clarithromycin
Regimen 7 days course 10 days course
Exacerbation-free interval
300 days
350 days
Exacerbation-free interval for patients with a new documented exacerbation during follow-up
100.5 days
95 days
Clinical success rates
Similar
Bacteriological success rate significantly higher  


Community-acquired pneumonia

Clarithromycin ER has equivalent efficacy and tolerability to the levofloxacin in the treatment of community-acquired pneumonia 7.

Results of study comparing clarithromycin ER and levofloxacin for community-acquired pneumonia7.
Levofloxacin
Clarithromycin
Regimen 500 mg once daily for 7 days 1000 mg once daily for 7 days
Clinical cure rates
86%
(107 patients of 124)
88%
(113 patients of 128)
Radiographic success rates
88%
(104 patients of 118)
95%
(117 patients of 123)
Bacteriologic cure rates
88%
(85 patients of 97)
86%
(80 patients of 93)


Acute sinusitis

Daily levofloxacin therapy is as effective as twice-daily clarithromycin therapy with more complete clearing of symptoms and better tolerability 8.

Results of study comparing levofloxacin with clarithromycin in the treatment of acute sinusitis in adults 8.
Levofloxacin
Clarithromycin
Regimen 500 mg once daily for 10-14 days 500 mg twice daily for 10-14 days
Clinical response rates (cured plus improved)
93.9%
(98 patients of 119)
93.5%
(93 patients of 117)
Proportion of cured patients
40.8%
29.0%
Resolution of individual symptoms
higher rates
Adverse events
22.5%
39.3%


Levofloxacin vs. Azithromycin (Zithromax)

Acute bacterial exacerbations of chronic bronchitis

Standard 5-day course of azithromycin was clinically and bacteriologically equivalent to a 7-day course of oral levofloxacin in the treatment of ABECB 6.

Results of trial of azithromycin vs levofloxacin in the outpatient treatment of acute bacterial exacerbations of chronic bronchitis6.
Levofloxacin
Azithromycin
Regimen 500 mg daily for 7 days 500 mg on day 1; 250 mg daily for days 2 to 5
Favorable clinical results by day 4 of therapy
92%
89%
Favorable clinical results by day 24 of therapy
86%
82%
Bacterial eradication rates of respiratory pathogens
85%
96%

 

Community-acquired pneumonia

A single 2 g dose of azithromycin microspheres is at least as effective as a 7-day course of levofloxacin in the treatment of mild to moderate community-acquired pneumonia 16.
The cure rates were 89.7% for azithromycin microspheres and 93.7% for levofloxacin. Bacteriologic success at test of cure in the "bacteriologic per protocol" population was 90.7% for azithromycin microspheres and 92.3% for levofloxacin. Both medications were well tolerated. The incidence of side effects was 19.9% for azithromycin and 12.3% for levofloxacin.

Results noninferiority study of microsphere formulation of azithromycin versus levofloxacin for mild to moderate community-acquired Pneumonia in adults.16.
Levofloxacin
Azithromycin microspheres
Regimen 500 mg daily for 10 days single 2.0 g dose
Clinical cure rate
93.7%
89.7%
Bacteriologic success
92.3%
(120 patients of 130)
90.7%
(97 patients of 107)
Adverse events
12.3%
19.9%


Sinusitis

Azithromycin microspheres (as a single 2 g dose) has efficacy comparable to 10 days of levofloxacin in the treatment of acute bacterial sinusitis 10.
Clinical success rates were 94.5% with azithromycin-microspheres and 92.8% with levofloxacin. In patients with Streptococcus pneumoniae, Haemophilus influenzae, or Moraxella catarrhalis, clinical cure rates were 97.3%, 96.3%, and 100%, respectively, for the azithromycin and 92.3%, 100%), and 90.9%, respectively, for the levofloxacin.

Results of international trial comparing azithromycin microsphere formulation versus levofloxacin for acute bacterial sinusitis in adults 10.
Levofloxacin
Azithromycin
Regimen 500 mg daily for 7 days single 2.0 g dose
Clinical success rates
92.8%
94.5%
Clinical success rates in patients with documented:
Streptococcus pneumoniae
92.3% (36/39)
97.3% (36/37)
Haemophilus influenzae
100% (30/30)
96.3% (26/27)
Moraxella catarrhalis
90.9% (10/11)
100% (8/8)


Levofloxacin vs. Cefuroxime axetil (Ceftin)

Acute bacterial exacerbations of chronic bronchitis (ABECB)

Both levofloxacin and cefuroxime axetil provide high rate of clinical efficacy and are equally well tolerated.

The clinical response was rated a success, with the patient cured or improved in 94.6% of those receiving levofloxacin and 92.6% of the cefuroxime axetil group. All of the symptoms of bronchitis were resolved in more than 86% of the patients, with the exception of shortness of breath, which resolved in 69.7% of levofloxacin-treated and 72.4% of cefuroxime axetil-treated patients. Resolution or improvement of abnormalities on thoracic auscultation were noted in 85% or more of patients, with the exception of diminished breath sounds, which were resolved or improved in 62.5% of levofloxacin-treated and 55.2% of cefuroxime axetil-treated patients 3.

Results of study comparing the efficacy of antimicrobial therapies in AECOB 3.
Levofloxacin
Cefuroxime axetil
Regimen 500 mg daily for 10 days 250 mg twice daily for 10 days
Clinical cure rate
94.6%
93.8%
The probability that 25% of patients would relapse during follow-up was reached within
93 days
81 days
Safety
comparable
Adverse events
5.0%
2.9%

 

Community-acquired pneumonia

Levofloxacin is superior to ceftriaxone and/or cefuroxime axetil in the treatment of community-acquired pneumonia 14.
Clinical success was higher with levofloxacin treatment (96%) compared with the ceftriaxone and/or cefuroxime axetil (90%). In patients with typical respiratory pathogens the bacteriologic eradication rates were higher with levofloxacin (98%) compared with the ceftriaxone and/or cefuroxime axetil (85%). Levofloxacin eradicated 100% of the most frequently reported respiratory pathogens (i.e., H. influenzae and S. pneumoniae) and provided a >98% clinical success rate in patients with atypical pathogens. Side effects were reported in 5.8% of patients receiving levofloxacin and in 8.5% of patients receiving ceftriaxone and/or cefuroxime axetil. Gastrointestinal and central and peripheral nervous system adverse events were the most common events reported with each treatment.

Sinusitis

Levofloxacin is more effective than cefuroxime for the treatment of sinusitis 15.

Results of comparison of the effectiveness of levofloxacin and cefuroxime for sinusitis 15.
Levofloxacin
Cefuroxime axetil
Regimen 200 mg once daily, 200/100 mg twice daily for 10 to 14 days 250 mg twice daily for 10 to 14 days
Success rate
97.4%
92.8%
Resolution of bacteria rates
91.6%
80.0%

Levofloxacin vs. Cefdinir (Omnicef)

Rhinosinusitis

Cefdinir is as effective as levofloxacin in the treatment of acute rhinosinusitis 17.

Results of study comparing cefdinir and levofloxacin in acute rhinosinusitis 17.
Levofloxacin
Cefdinir
Regimen 500 mg daily for 10 days 600 mg daily for 10 days
Clinical cure rates at the test-of-cure visit
86%
(101 patients of 118)
83%
(102 patients of 123)
Efficacy in the treatment of moderate to severe infections
comparable
Incidence of side effects
comparable
Incidence of:    
vaginal moniliasis in women (candidiasis)
0%
11%
diarrhea
1%
8%
insomnia
4%
0%

Further reading

References
  • 1. Hooper DC. Pharmacology of the fluroquinolones. Up to Date. March 2, 2000.
  • 2. Lipsky BA, Baker CA. Fluroquinolone toxicity profiles: a review focusing on newer agents. Clin Infect Dis 1999;28:352-364.
  • 3. Petitpretz P, Chone' C, Tre'molie`res F; Investigator Study Group. Levofloxacin 500 mg once daily versus cefuroxime 250 mg twice daily in patients with acute exacerbations of chronic obstructive bronchitis: clinical efficacy and exacerbation-free interval. Int J Antimicrob Agents. 2007 Jul;30(1):52-9. Epub 2007 May 18. PubMed
  • 4. Lode H, Eller J, Linnhoff A, Ioanas M; Evaluation of Therapy-Free Interval in COPD Patients Study Group. Levofloxacin versus clarithromycin in COPD exacerbation: focus on exacerbation-free interval. Eur Respir J. 2004 Dec;24(6):947-53. PubMed
  • 6. Amsden GW, Baird IM, Simon S, Treadway G. Efficacy and safety of azithromycin vs levofloxacin in the outpatient treatment of acute bacterial exacerbations of chronic bronchitis. Chest. 2003 Mar;123(3):772-7. PubMed
  • 7. Gotfried MH, Dattani D, Riffer E, Devcich KJ, Busman TA, Notario GF, Palmer RN. A controlled, double-blind, multicenter study comparing clarithromycin extended-release and levofloxacin in the treatment of community-acquired pneumonia. Clin Ther. 2002 May;24(5):736-51. PubMed
  • 8. Lasko B, Lau CY, Saint-Pierre C, Reddington JL, Martel A, Anstey RJ. Efficacy and safety of oral levofloxacin compared with clarithromycin in the treatment of acute sinusitis in adults: a multicentre, double-blind, randomized study. The Canadian Sinusitis Study Group. J Int Med Res. 1998 Dec;26(6):281-91. PubMed
  • 9. Richard GA, Klimberg IN, Fowler CL, Callery-D'Amico S, Kim SS. Levofloxacin versus lomefloxacin in acute pyelonephritis. Urology. 1998 Jul;52(1):51-5. PubMed
  • 10. Murray JJ, Emparanza P, Lesinskas E, Tawadrous M, Breen JD. Efficacy and safety of a novel, single-dose azithromycin microsphere formulation versus 10 days of levofloxacin for the treatment of acute bacterial sinusitis in adults. Otolaryngol Head Neck Surg. 2005 Aug;133(2):194-200. PubMed
  • 11. Klimberg IW, Cox CE 2nd, Fowler CL, King W, Kim SS, Callery-D'Amico S.A controlled trial of levofloxacin and lomefloxacin in the treatment of complicated urinary tract infection. Urology. 1998 Apr;51(4):610-5. PubMed
  • 12. Carbon C. Comparison of side effects of levofloxacin versus other fluoroquinolones. Chemotherapy. 2001;47 Suppl 3:9-14; discussion 44-8. PubMed
  • 14. File TM Jr, Segreti J, Dunbar L, Player R, Kohler R, Williams RR, Kojak C, Rubin A. 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 Sep;41(9):1965-72. PubMed
  • 15. Li XP, Qin ZM, Zheng RH, Tan QL, Zhou YY, Zhu L, Yin AF. Comparison of the effectiveness of levofloxacin and cefuroxime for the treatment of sinusitis. 2000 Dec;14(12):573-5. PubMed
  • 16. D'Ignazio J, Camere MA, Lewis DE, Jorgensen D, Breen JD. Novel microsphere formulation of azithromycin versus 7-day levofloxacin therapy for treatment of mild to moderate community-acquired Pneumonia in adults. Antimicrob Agents Chemother. 2005 Oct;49(10):4035-41. PubMed
  • 17. Henry DC, Kapral D, Busman TA, Paris MM. Cefdinir versus levofloxacin in patients with acute rhinosinusitis of presumed bacterial etiology: a multicenter, randomized, double-blind study. Clin Ther. 2004 Dec;26(12):2026-33. PubMed

Published: March 31, 2008
Last updated: July 20, 2014

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