Ofloxacin: Its Pharmacology, Pharmacokinetics, and Potential for Clinical Application

Ofloxacin is a 4‐quinolone antibiotic with rapid bactericidal activity against a wide variety of organisms. Its proposed mechanism of activity is interference with DNA gyrase, an enzyme essential for the replication of bacterial DNA. In vitro activity of ofloxacin includes a variety of aerobic and anaerobic bacteria. Enteric gram‐negative bacilli and cocci are generally sensitive to ofloxacin; nonaeruginosa strains of Pseudomonas are less so. Numerous bacterial pathogens of the gastrointestinal tract are also sensitive to the drug. Although its MIC values for gram‐positive aerobic organisms are generally higher, ofloxacin's bactericidal activity against these organisms is considered by some to be adequate, and superior to that of most other fluoroquinolones. Ofloxacin is well absorbed after oral administration. Wide tissue and body fluid distribution is demonstrated. Urinary excretion is thought to be the primary route of elimination, with 80% of the dose recovered in the urine within 24 hours. The serum half‐life ranges between 2.9 and 9 hours in a dose‐dependent manner. Only modest accumulation is reported after multiple‐dose administration. Clinical trials using daily dosages of 100–800 mg/day in single or divided doses have been reported in the treatment of a variety of conditions such as skin and soft tissue infections, tonsillitis, sexually transmitted disease, respiratory tract infections, cystitis, and complicated and uncomplicated urinary tract infections. English reports of these trials, however, are generally limited to abstract form, making evaluation of trial design difficult. Side effects most frequently encountered include gastrointestinal and central nervous system reactions.

[1]  J. Monk,et al.  A Review of its Antibacterial Activity, Pharmacokinetic Properties and Therapeutic Use , 2012 .

[2]  D. Hooper,et al.  Mechanisms of action of and resistance to ciprofloxacin. , 1987, The American journal of medicine.

[3]  S. Pattyn.  Activity of ofloxacin and pefloxacin against Mycobacterium leprae in mice , 1987, Antimicrobial Agents and Chemotherapy.

[4]  Jerome J. Schentag,et al.  Inhibition of theophylline clearance by coadministered ofloxacin without alteration of theophylline effects , 1987, Antimicrobial Agents and Chemotherapy.

[5]  J. Fillastre,et al.  Ofloxacin pharmacokinetics in renal failure , 1987, Antimicrobial Agents and Chemotherapy.

[6]  A. Andremont,et al.  Effect of oral ofloxacin on fecal bacteria in human volunteers , 1987, Antimicrobial Agents and Chemotherapy.

[7]  H. Neu,et al.  Factors influencing the in vitro activity of two new aryl-fluoroquinolone antimicrobial agents, difloxacin (A-56619) and A-56620 , 1986, Antimicrobial Agents and Chemotherapy.

[8]  T. Bergan,et al.  Ofloxacin: serum and skin blister fluid pharmacokinetics in the fasting and non-fasting state. , 1986, The Journal of antimicrobial chemotherapy.

[9]  R. Smith,et al.  Comparative antimicrobial activity of enoxacin, ciprofloxacin, amifloxacin, norfloxacin and ofloxacin against 177 bacterial isolates. , 1986, The Journal of antimicrobial chemotherapy.

[10]  H. Neu,et al.  In vitro activity of CI-934, a new quinolone, compared with that of other quinolones and other antimicrobial agents , 1986, Antimicrobial Agents and Chemotherapy.

[11]  H. Neu,et al.  In vitro activity of Ro 23-6240, a new fluorinated 4-quinolone , 1986, Antimicrobial Agents and Chemotherapy.

[12]  M. Cynamon,et al.  Comparative in vitro activities of ciprofloxacin and other 4-quinolones against Mycobacterium tuberculosis and Mycobacterium intracellulare , 1986, Antimicrobial Agents and Chemotherapy.

[13]  S. Smith.  In vitro comparison of A-56619, A-56620, amifloxacin, ciprofloxacin, enoxacin, norfloxacin, and ofloxacin against methicillin-resistant Staphylococcus aureus , 1986, Antimicrobial Agents and Chemotherapy.

[14]  M. Delmée,et al.  Comparative in vitro activity of seven quinolones against 100 clinical isolates of Clostridium difficile , 1986, Antimicrobial Agents and Chemotherapy.

[15]  A L Barry,et al.  In vitro evaluation of A-56619 and A-56620, two new quinolones , 1986, Antimicrobial Agents and Chemotherapy.

[16]  I. Hayakawa,et al.  Synthesis and antibacterial activities of optically active ofloxacin , 1986, Antimicrobial Agents and Chemotherapy.

[17]  D. Wittmann,et al.  Further methodological improvement in antibiotic bone concentration measurements: penetration of ofloxacin into bone and cartilage. , 1986, Infection.

[18]  Ofloxacin II. , 1986, Infection.

[19]  J. Carlet,et al.  The new quinolones and their combinations with other agents for therapy of severe infections. , 1986, The Journal of antimicrobial chemotherapy.

[20]  S. Baba.  Clinical efficacy of ofloxacin in the treatment of otorhinolaryngological infections , 1986, Infection.

[21]  H. Neu,et al.  In-vitro activity of ofloxacin, a quinolone carboxylic acid compared to other quinolones and other antimicrobial agents. , 1985, The Journal of antimicrobial chemotherapy.

[22]  D. Hooper,et al.  The fluoroquinolones: pharmacology, clinical uses, and toxicities in humans , 1985, Antimicrobial Agents and Chemotherapy.

[23]  D. Hooper,et al.  The fluoroquinolones: structures, mechanisms of action and resistance, and spectra of activity in vitro , 1985, Antimicrobial Agents and Chemotherapy.

[24]  K. Yamaguchi,et al.  Susceptibility of Legionella pneumophila to ofloxacin in vitro and in experimental Legionella pneumonia in guinea pigs , 1985, Antimicrobial Agents and Chemotherapy.

[25]  I. Phillips,et al.  The in-vitro activities of enoxacin and ofloxacin compared with that of ciprofloxacin. , 1985, The Journal of antimicrobial chemotherapy.

[26]  H. Goossens,et al.  Comparative in vitro activities of aztreonam, ciprofloxacin, norfloxacin, ofloxacin, HR 810 (a new cephalosporin), RU28965 (a new macrolide), and other agents against enteropathogens , 1985, Antimicrobial Agents and Chemotherapy.

[27]  P. Valero-Guillén,et al.  In-vitro activity of some quinoline derivatives against Mycobacterium fortuitum. , 1985, Journal of Antimicrobial Chemotherapy.

[28]  E. Perea,et al.  Activities of new quinoline derivatives against genital pathogens , 1985, Antimicrobial Agents and Chemotherapy.

[29]  M. Stieglitz,et al.  Comparative evaluation of recently developed quinolone compounds--with a note on the frequency of resistant mutants. , 1985, Chemotherapy.

[30]  A. Pernet,et al.  Mechanism of inhibition of DNA gyrase by analogues of nalidixic acid: the target of the drugs is DNA. , 1985, Proceedings of the National Academy of Sciences of the United States of America.

[31]  R. Goering,et al.  Selection of multiple antibiotic resistance by quinolones, beta-lactams, and aminoglycosides with special reference to cross-resistance between unrelated drug classes , 1984, Antimicrobial Agents and Chemotherapy.

[32]  P. Piot,et al.  In vitro activities of the spectinomycin analog U-63366 and four quinolone derivatives against Neisseria gonorrhoeae , 1984, Antimicrobial Agents and Chemotherapy.

[33]  S. Richmond,et al.  Comparison of the in vitro activities of ofloxacin and tetracycline against Chlamydia trachomatis as assessed by indirect immunofluorescence , 1984, Antimicrobial Agents and Chemotherapy.

[34]  S. Pattyn,et al.  In vitro activity of ciprofloxacin compared with those of other new fluorinated piperazinyl-substituted quinoline derivatives , 1984, Antimicrobial Agents and Chemotherapy.

[35]  R. Wise,et al.  In-vitro activity of enoxacin (CL-919), a new quinoline derivative, compared with that of other antimicrobial agents. , 1984, The Journal of antimicrobial chemotherapy.

[36]  H. Tanimura.  CHEMOTHERAPY OF BILIARY TRACT INFECTION (XXI):EXCRETION INTO BILE, TISSUE LEVEL OF GALLBLADDER AND CLINICAL EFFECTS OF DL-8280 FOR BILIARY TRACT INFECTIONS , 1984 .

[37]  M. Kenwright,et al.  Investigations into the mechanism of action of the antibacterial agent norfloxacin. , 1984, The Journal of antimicrobial chemotherapy.

[38]  R. Wise,et al.  The pharmacokinetics and tissue penetration of ofloxacin. , 1984, The Journal of antimicrobial chemotherapy.

[39]  M. Tsukamura.  In Vitro Antimycobacterial Activity of a New Antibacterial Substance DL‐8280—Differentiation between Some Species of Mycobacteria and Related Organisms by the DL‐8280 Susceptibility Test , 1983, Microbiology and immunology.

[40]  Y. Osada,et al.  Antimycoplasmal activity of ofloxacin (DL-8280) , 1983, Antimicrobial Agents and Chemotherapy.

[41]  S. Mitsuhashi,et al.  In vitro and in vivo activity of DL-8280, a new oxazine derivative , 1982, Antimicrobial Agents and Chemotherapy.

[42]  J. Smith,et al.  Nalidixic Acid: an Antibacterial Paradox , 1975, Antimicrobial Agents and Chemotherapy.

[43]  C. Thornsberry,et al.  Broth-Dilution Method for Determining the Antibiotic Susceptibility of Anaerobic Bacteria , 1975, Antimicrobial Agents and Chemotherapy.