Summary
Synopsis
Ofloxacin1 is one of a new generation of fluorinated quinolones structurally related to nalidixic acid. It is an orally administered broad spectrum antibacterial drug active against most Gram-negative bacteria, many Gram-positive bacteria and some anaerobes. Ciprofloxacin is the only other quinolone with superior in vitro antibacterial activity. However, the pharmacokinetic profile of ofloxacin is superior to that of ciprofloxacin, with more rapid absorption and a peak serum concentration several times higher. Moreover, ofloxacin achieves high concentrations in most tissues and body fluids.
The results of clinical trials with ofloxacin have confirmed the potential for use in a wide range of infections, which was indicated by its in vitro antibacterial and pharmacokinetic profiles. It has proven effective against a high percentage of infections caused by Gram-negative organisms, slightly less effective against Gram-positive infections, and effective against some anaerobic infections. Clinical efficacy has also been confirmed in a variety of systemic infections as well as in acute and chronic urinary tract infections, and ofloxacin has generally appeared to be at least as effective as alternative orally administered antibacterial drugs. Ofloxacin is well tolerated and, although experience with the drug in clinical practice to date is limited, bacterial resistance does not appear to develop readily. Thus, ofloxacin is an orally active drug which offers a valuable alternative to other broad spectrum antibacterial drugs.
Antibacterial Activity
Ofloxacin is a fluorinated quinolone. In vitro it has been shown to be active against most Gram-negative bacteria, including Citrobacter, Enterobacter, Klebsiella, Proteus, Salmonella and Shigella species, Yersinia enterocolitica, Escherichia coli, Neisseriaceae and Haemophilus influenzae, with MIC90 values of ⩽ 1 mg/L. Against such organisms ofloxacin was as active as other quinolones, except ciprofloxacin. Compared with non-quinolone antibacterial drugs it was a more potent inhibitor than gentamicin of Enterobacteriaceae, and equivalent in potency to aztreonam or cefotaxime against Enterobacteriaceae and H. influenzae. Among 38 antibacterial drugs only cefotaxime was more potent than ofloxacin against penicillinase-producing Neisseria gonorrhoea.
Ofloxacin was slightly less potent an inhibitor of Providencia, Serratia and Pseudomonas species, although against Pseudomonas aeruginosa it had similar activity to enoxacin or norfloxacin, was at least as potent as gentamicin and was several times more potent than aztreonam or cefotaxime. Other Gram-negative organisms which were highly susceptible to ofloxacin included Aeromonas hydrophila, Plesiomonas shigelloides and Vibrio cholerae. It had an MIC90 of 0.0625 mg/L against Legionella pneumophila, and had equivalent activity to ciprofloxacin against Campylobacter jejuni (MIC range 0.03 to 2 mg/L). Gardnerella vaginalis was moderately susceptible to ofloxacin (MIC range 1 to 2 mg/L).
Among Gram-positive bacteria, ofloxacin was the most potent quinolone (among the 6 reviewed) against staphylococci (including S. aureus; MIC90 0.2 to 1 mg/L), and only ciprofloxacin had equivalent activity against streptococci (including S. pneumoniae and S. faecalis; MIC90 1 to 4 mg/L). Against S. aureus it was considerably more potent than cefotaxime, gentamicin or co-trimoxazole, while against streptococci it was more potent than latamoxef (moxalactam) but less so than cefotaxime, ceftriaxone or ceftazidime. Ofloxacin was active against Listeria monocytogenes, with an MIC90 value of 2 mg/L. Some anaerobic organisms, including Bacteroides melaninogenicus, Bacteroides fragilis and Clostridium welchii were moderately susceptible to ofloxacin (MIC90 1 to 8 mg/L). Ofloxacin was active against Chlamydia trachomatis and Mycoplasma pneumoniae with MIC90 values of 4 and 1.56 mg/L, respectively; and the limited data available with Mycobacterium tuberculosis indicate an MIC90 of ⩽ 1.5 mg/L.
Growth medium, inoculum size and serum had little influence on the activity of ofloxacin, but reduction of pH or the presence of urine markedly reduced it. Bacterial resistance to non-quinolone antibacterial drugs did not influence the activity of ofloxacin, but some reduction in activity has been reported against nalidixic acid-resistant strains. The antibacterial activity of the quinolones has been attributed to inhibition of the A subunits of the enzyme DNA gyrase, a type II topoisomerase, which controls supercoiling of DNA in bacteria; ofloxacin may have an additional mechanism of action possibly involving inhibition of the B subunits of this enzyme. Inhibition of eukaryotic topoisomerases could confer mutagenic properties on the quinolones. However, studies in vitro and in vivo have shown ofloxacin to have no mutagenic potential, except at very high concentrations, and to have less influence than ciprofloxacin or norfloxacin on eukaryotic topoisomerases.
Pharmacokinetic Properties
After oral administration of a single 300mg dose of ofloxacin a peak serum concentration of about 3 mg/L is reached within 2 hours. Multiple dose administration for up to 14 days in healthy subjects did not produce accumulation at a dosage of 300mg twice daily, with peak concentrations ranging from 3 to 6 mg/L on the final day. Food had no significant effect on the pharmacokinetics of ofloxacin except to delay absorption, but concurrent antacid consumption may markedly reduce absorption. In comparison with norfloxacin and ciprofloxacin, at the same dose, ofloxacin was more rapidly absorbed, and produced a higher serum concentration and area under the plasma concentration-time curve (AUC; 4 times that of norfloxacin or ciprofloxacin).
The volume of distribution of ofloxacin has been calculated to be > 1 L/kg. The tissue concentrations achieved were at least as high as the serum concentration for most tissues. In pregnant women, umbilical cord serum concentrations have been recorded at up to 90% of maternal serum concentrations, with drug detected in amniotic fluid in over 50% of cases.
After single doses of 100 to 600mg in healthy subjects 70% to 98% of the drug was excreted unchanged in the urine within 48 hours, and the urinary concentration remained well above the MIC90 for most bacterial species at 48 hours after administration. Small amounts of desmethyl ofloxacin and ofloxacin N-oxide have been detected in the urine in some subjects. The elimination half-life of ofloxacin after doses of ⩾ 200mg has generally been reported at about 6 hours or greater (up to 7.5 hours). The pharmacokinetics of ofloxacin are altered in patients with renal impairment: after single doses peak serum concentrations are delayed, and the elimination half-life and AUC are substantially increased depending on the degree of renal impairment. Thus, dosage adjustments may be required in such subjects.
Therapeutic Trials
With its broad spectrum of antibacterial activity and widespread distribution to most tissues and body fluids at relatively high concentrations, ofloxacin could be of potential therapeutic application in many types of infection. In controlled and uncontrolled clinical trials ofloxacin (at dosages of 300 to 800mg daily for 5 to 14 days in most cases) was usually clinically effective in a high percentage of patients (about 70 to 98%) with respiratory tract infections (including bronchitis, pneumonia and otorhinolaryngological infections), upper or lower urinary tract infections, gonococcal or non-gonococcal urethritis, skin and soft tissue infections, obstetric and gynaecological infections and biliary tract infections. Bacteriological response rates were equally good, although in biliary tract infections there was some discrepancy between clinical and bacteriological response. Few patients with non-gonococcal urethritis have been treated with ofloxacin, but available results are encouraging. In patients with urinary or lower respiratory tract infections there tended to be a higher response rate among patients with acute than chronic infections, as might be expected. Moreover, ofloxacin proved effective in many patients previously resistant to other antibacterial drugs. Preliminary studies have shown some encouraging results with ofloxacin in patients with cystic fibrosis and pulmonary tuberculosis.
In bronchitis the efficacy of ofloxacin was significantly greater than that of cefaclor and similar to that of co-trimoxazole, while in pneumonia it was similar to that of cotrimoxazole and doxycycline. The efficacy of ofloxacin in urinary tract infections was significantly greater than that of pipemidic acid, and at least as good as that of nalidixic acid, amoxycillin plus clavulanic acid, nitrofurantoin and co-trimoxazole. Other comparative studies showed ofloxacin to be at least as effective as amoxycillin and doxycycline in obstetric and gynaecological infections, pipemidic acid in otitis media, cefaclor, co-trimoxazole and doxycycline in skin and soft tissue infections, and amoxycillin in tonsillitis.
The response rate to ofloxacin in patients with otitis media was lower than for other types of infection (50 to 70% cure clinically and/or bacteriologically). Patients with tonsillitis showed an excellent bacteriological response rate (98%) but a lower clinical response (71%), and a similar relationship was seen in patients with enteritis (82% vs 45% response rates). Bacteriological results from clinical trials have confirmed the findings of in vitro studies, with ofloxacin eradicating 75 to 95% of Gram-negative aerobic bacteria, except Pseudomonas aeruginosa which was slightly less sensitive (60% of strains eradicated), and also being active against a high percentage of Gram-positive aerobic bacteria and some anaerobic bacteria. Superinfections were reported following ofloxacin therapy in 2 to 17% of trial populations, although the terminology was not defined in most studies; the rate tended to be lower than with most comparative treatments.
Side Effects
Ofloxacin has been administered to nearly 16,000 patients in clinical trials, and side effects have been reported in 3.3% of this population. The incidence of drug-related adverse clinical reactions in individual studies has ranged from 2.5 to 8.5%. Gastrointestinal symptoms, mainly nausea/vomiting, pain/discomfort, diarrhoea and anorexia, were reported most frequently, followed by central nervous system events and dermatological or hypersensitivity reactions. The incidence of side effects did not appear to be dose related, and serious reactions were rare. Minor changes in mean laboratory values were not considered clinically significant and were usually attributable to the disease process, but some cases of eosinophilia were considered possibly drug related. About 1.5 million patients have been treated with ofloxacin subsequent to its first launch, and post-marketing surveillance in this time has revealed 806 spontaneously reported adverse reactions in 338 patients. A number of previously unidentified reactions were reported, including some cases of hallucinations and psychotic reactions, but most symptoms were mild and reversible.
Dosage and Administration
The recommended oral dosage of ofloxacin in respiratory tract infections is 400 to 600mg daily, and in urinary tract infections it is 200 to 600mg daily, in divided doses (usually twice daily) for 3 to 10 days. Higher dosages (up to 800mg daily) may be required in patients with severe or complicated infections. A dosage of 400mg daily has been used most frequently in patients with skin and soft-tissue infections, obstetric and gynaecological infections and biliary tract infections, while 600mg daily has been used most frequently in patients with otitis media or enteritis. Single-dose therapy has been used successfully for the treatment of uncomplicated gonococcal urethritis. Treatment has been continued for up to 3 months in some studies in patients with chronic infections, but too few patients have been included to date in such studies to fully establish the long term tolerability of ofloxacin. In a preliminary study of pulmonary tuberculosis a dosage of 300mg once daily was administered for 8 months.
Despite reports of a pharmacokinetic interaction between enoxacin and theophylline, this does not seem to occur with ofloxacin and dosage adjustments for either theophylline or ofloxacin are probably not necessary. Patients receiving antacids may respond poorly to ofloxacin because of reduced absorption. It is important that the dosage of ofloxacin be adjusted in patients with renal insufficiency.
Ofloxacin is contraindicated in children or adolescents during the growth phase, and the drug should not be administered during pregnancy or in breast-feeding mothers.
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Various sections of the manuscript reviewed by: W. Cullmann, Ruhr-Universität Bochum, Medizinische Fakultät, Universitätsstrasse 150, Bochum 1, West Germany; B.I. Davies, Streeklaboratorium voor de Volksgeszondheid, de Wever-Ziekenhius, Heerlen, The Netherlands; A. Digrams, Department of Microbiology and Immunology, The Grade Institute, Haukeland Hospital, Bergen, Norway; D. Felmingham, Department of Clinical Microbiology, Grafton Way, London, England; G.G. Grossi, Università di Pa via, Facolta di Medicina e Chirurgia, Cattedra di Chemioterapia, Pavia, Italy; R. Janknegt, Medisch Centrum Alkmaar, Klinische Farmacie, Alkmaar, The Netherlands; S. Kawamura, Department of Oto-rhino-laryngology, Juntendo University School of Medicine, Tokyo, Japan; H.C. Neu, Department of Medicine, College of Physicians and Surgeons of Columbia University, New York, New York, USA; Y. Sekine, Department of Microbiology, School of Medicine, Gunma University, Showa Machi, Maebashi, Japan; J.T. Smith, Department of Pharmaceutics, School of Pharmacy, University of London, London, England; H. Tanimura, Second Department of Surgery, Kyoto University School of Medicine, Kyoto, Japan; R. Wise, Department of Medical Microbiology, Dudley Road Hospital, Birmingham, England; J.S. Wolfson, Harvard Medical School, Massachusetts General Hospital, Boston, Massachusetts, USA; H.W. Van Landuyt, A.Z. St-Jan, Ruddershove 10, Brugge, Belgium
Tradenames: ‘Flobacin’, ‘Oflozet’, ‘Tabrin’, ‘Tarivid’, ‘Viseren’
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Monk, J.P., Campoli-Richards, D.M. Ofloxacin. Drugs 33, 346–391 (1987). https://doi.org/10.2165/00003495-198733040-00003
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DOI: https://doi.org/10.2165/00003495-198733040-00003