Tuberculosis ofloxacin

Most of the fluoroquinolones antibiotics (see Chapter 44) have activity against M. tuberculosis and M. avium-intracellulare. Ciprofloxacin, ofloxacin, and levofloxacin inhibit 90% of the strains of susceptible tubercula bacilli at concentrations of less than 2 xg/mL. Levofloxacin is preferred because it is the active L-optical isomer of ofloxacin and is approved for once-daily use. The... 

Quinolones are important recent additions to the therapeutic agents used against M. tuberculosis, especially in MDR strains. Clinical trials of ofloxacin in combination with isoniazid and rifampin have indicated activity comparable to that of ethambutol. In addition, quinolones, particularly ciprofloxacin, are used as part of a combined regimen in HIV-infected patients. 

Ciprofloxacin and ofloxacin are effective for gonococcal infection, including disseminated disease, and ofloxacin is effective for chlamydial urethritis or cervicitis. Ciprofloxacin is a second-line agent for legionellosis. Ciprofloxacin or levofloxacin is occasionally used for treatment of tuberculosis and atypical mycobacterial infections. They may be suitable for eradication of meningococci from carriers or for prophylaxis of infection in neutropenic patients. 

Moxifloxacin s MIC90 value of 1 mg L"1 means that it has the same in vitro activity against M. tuberculosis as levofloxacin, and is more effective than ofloxacin (MIC90 = 2 mg L"1) and ciprofloxacin (MIC90 = 4 mg IT1) [192-194]. A combination of moxifloxacin and isoniazid proved to be more effective in vivo than the individual compounds [195,196], whereas a combination with ethambutol was less effective [196]. Based on the mutant prevention concentration (MPC), which is a parameter for the selection of resistant pathogens during antibiotic treatment, moxifloxacin was found to be the most effective fluoroquinolone against M. tuberculosis [197]. 

Saigal S, Agarwal SR, Nandeesh HP, Sarin SK. Safety of an ofloxacin-based antitubercular regimen for the treatment of tuberculosis in patients with underlying chronic liver disease a preliminary report. J Gastroenterol Hepatol 2001 16(9) 1028-32. 

Aminoglycosides such as capreomycin, viomycin, kana-mycin and amikacin and the newer quinolones (e.g. pefloxacin, ofloxacin and ciprofloxacin) were only used in drug resistance situations. Tuberculosis in particular experienced a resurgence. In the mid-1980s, the worldwide decline in tuberculosis cases levelled off and then began to rise. 

Ciprofloxacin and ofloxacin are often active against strains of M tuberculosis resistant to first-line agents. The fluoroquinolones should always be used in combination regimens with two or more other active agents. 

The second-line drugs for tuberculosis are found to be more toxic but may be required with certain resistance problems. These drugs essentially include fluroquinolones (e.g., ofloxacin, ciprofloxacin), cycloserine, ethionosamide, aminosalicylic acid, aminoglycosides (viz., amikacin, kanamycin), clofazimine, and capreomycin. 

The MICs of ofloxacin and ciprofloxacin for the organism Mycobacterium tuberculosis invariably vaiy between 0.12-2.0 mcg.mL Importantly, both these drygs are bacterial in nature, and the ensuing MBC-MIC ratio being from 2 to 4. 

Isonlazld and ethambutol do not normally interact with ciclosporin. However, there is one case report describing a patient who had a gradual rise in serum ciclosporin levels when isoniazid and ethambutol were stopped, and another which attributed a marked rise in ciclosporin levels to the use of isoniazid." There have been several other case reports of successful treatment of tuberculosis in heart and kidney transplant patients using isoniazid, ethambutoi, pyrazinamide with ofloxacin, or streptomycin.Consider also pyrazinamide , (p.l044), and quinolones , (p.1018). 

Multidrug-resistant tuberculosis (MDR-TB) no longer can be cured by the leading TB antibiotics isoniazid (2) and rifampicin (3). Extensively drug-resistant TB (XDR-TB) is a form of TB caused by organisms that are resistant to isoniazid (2) and rifampicin (3), as well as fluoroquinolones such as ciprofloxacin (7), and ofloxacin (8) and any of the second-line anti-TB injectable drugs such as amikacin, kanamycin, or capreomycin. 

Ofloxacin and its analogs are promising drugs for tuberculosis treatment. Ofloxacin (daily dose 3(X)-800 mg) and levofloxacin (250-500 mg a day) in... 

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