Summary
Quinolones are a class of antibiotics structurally related to nalidixic acid. They exhibit bactericidal activity primarily by inhibiting bacterial DNA gyrase. The early quinolones had a limited spectrum of activity, low potency, high frequency of spontaneous bacterial resistance, low serum drug concentrations and short half-lives, which virtually restricted their use to urinary tract infection.
The new fluorinated quinolones differ from their predecessors in their broad antibacterial spectrum, including both Gram-negative and Gram-positive aerobic, and facultative anaerobic bacteria as well as many Mycobacterium spp., Chlamydia spp., Legionella spp. and Mycoplasma spp., in addition to many strains of bacteria that are multiresistant to β-lactam antibiotics and aminoglycosides. They also exhibit high potency, a low incidence of resistance, high oral bioavailability, extensive tissue penetration, low protein binding and long elimination half-lives. They are generally well tolerated apart from some gastrointestinal disturbance and rashes, including photosensitive eruptions and a propensity to cause central nervous system excitation. Clinically important interactions include those with antacids, theophylline, fenbufen and warfarin. Potential toxic effects include cartilage damage, ocular toxicity, teratogenicity and impairment of spermatogenesis. The role of fluoroquinolones continues to widen, encompassing infections of the urinary tract, respiratory tract, skin and soft tissues, bone and joints, infections in immunocompromised patients, sexually transmitted diseases, infectious diarrhoea, gynaecological infections and surgical prophylaxis. The convenience of oral therapy is an added advantage of the new fluoroquinolones.
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References
Acar JF, Franconal S. The clinical problems of bacterial resistance to the new quinolones. Antimicrobial Chemotherapy 26(Suppl. B): 207–212, 1990
Allegra L, Hosie J, Konietzko M, et al. Acute exacerbations of chronic obstructive pulmonary diseases. 33rd Annual Conference on Antimicrobial Agents and Chemotherapy, New Orleans, October, 1993
Andriole VT. Use of quinolones in treatment of prostatitis and lower urinary tract infections. European Journal of Clinical Microbiology and Infectious Diseases 10 4: 342–350, 1991
Ash SA. Bacterial skin and soft tissue infections. In Lambert & O’Grady (Eds) Antibiotic and Chemotherapy, pp. 396–406, Churchill Livingstone, New York, 1992
Aubier M, Verster R, Regamey C. Treatment of suspected pneumococcal community-acquired pneumonia. 33rd Annual Conference on antimicrobial Agents and Chemotherapy, New Orleans, October 1993
Aujard Y. Quinolones in neonates. Fortschritte der Antimikrobiellen Antineoplastischen Chemotherapie 11–12: 233–237, 1992
Bailey RR. Quinolones in the treatment of uncomplicated urinary tract infections. International Journal of Antimicrobial Agents 2 1: 19–28, 1992
Barry AL. In Siporin et al. (Eds). In vitro activity of quinolones and related compounds: the new generation of quinolones, pp. 79–105, Marcel Dekker, New York, 1990
Bauernfeind A. In vitro activity of Sparfloxacin in comparison with ciprofloxacin. 3rd International Symposium on New Quinolones, Vancouver, Canada, July 1980
Burckhardt JE, Hill MA, Carlton WW. Morphologic and biochemical changes in articular cartilage of immature Beagle dogs with difloxacin. Toxicologic Pathology 20: 246–252, 1992
Carbon C. Quinolones in the treatment of lower respiratory tract infections in adult patients. Drugs (Suppl. 3): 91-97, 1993
Carsenti-Etesse H, Bernard E, Bensoussan F, et al. Induction of resistance in vitro of Streptococcus pneumoniae to pefloxacin, ofloxacin, ciprofloxacin, Sparfloxacin, temafloxacin. 33rd Annual Conference on Antimicrobial Agents and Chemotherapy, New Orleans, October 1993
Cantón E, Ramon MA, Jiminez MT, et al. Killing kinetics of four quinolones against gram-positive cocci. Chemotherapy 39: 394–399, 1993
Chartrand SA. Quinolones in animal models of infection. In Siporin et al. (Eds) The new generation of quinolones, pp. 123–143, Marcel Dekker, New York, 1990
Cheesbrough JS, Ilunga Mwema F, Green SE, et al. Quinolones in children with invasive salmonellosis. Lancet 338: 127, 1991
Childs SJ. Quinolones for the urinary tract. In Siporin et al. (Eds) The new generation of quinolones, pp. 223–242, Marcel Dekker, New York, 1990
Chodosh S. Quinolones in acute bacterial exacerbations of chronic bronchitis. In Siporin et al. (Eds) The new generation of quinolones, pp. 249–276, Marcel Dekker, New York 1990
Christ W, Lenert T. Toxicity of the quinolones. In Siporin et al. (Eds) The new generation of quinolones, pp. 165–187, Marcel Dekker, New York, 1990
Chysky V, Hullmann R. How safe is ciprofloxacin in pediatrics: worldwide clinical experience based on compassionate use. Fortschritte der Antimikrobiellen Antineoplastischen Chemotherapie 11–12: 277–287, 1992
Cohen J. Antimicrobial therapy in the immunocompromised host. In Lambert & O’Grady (Eds) Antibiotic and Chemotherapy, pp. 321–335, Churchill Livingstone, New York 1992
Corrado MI. The clinical experience of ofloxacin in the treatment of sexually transmitted diseases. American Journal of Obstetrics and Gynecology 164: 1396–1399, 1991
Corret G, Flandrois JP, Lobry JR. Biphasic kinetics of bacterial killing by quinolones. Journal of Antimicrobial Chemotherapy 27 3: 319–327, 1991
Dab I, Desmyttere S, Malfoot A. Repeated use of ciprofloxacin in pediatric cystic fibrosis population. Fortschritte der Antimikrobiellen Antineoplastischen Chemotherapie 11–12: 143–146, 1992
Dabernat H, Delmas C, Seguy M, et al. Comparative in vitro activity of Sparfloxacin against Haemophilus influenzae and Branhamella catarrhalis. 3rd International Symposium on New quinolones, Vancouver, Canada, July, 1990
De Mouy D. Fluoroquinolone resistance in the hospital versus outpatient setting. International Journal of Antimicrobial Agents 2(1): 15–18, 1992
Drlica K, Coughlin S, Gennaro ML. Mode of action of quinolones: biochemical aspects. In Siporin et al. (Eds) The new generation of quinolones, pp. 45–62, Marcel Dekker, New York, 1990
Fliegelman RM, Maltingly PM, Dempsey CL, et al. Economic impact of oral ciprofloxacin following standard intravenous therapy. Diagnostic Microbiology and Infectious Diseases 13: 187–189, 1990
Fuchs P, Barry AL, Pfaller MA, et al. Multicenter evaluation of the in vitro activities of three new quinolones, Sparfloxacin, (CJ-960) and PD 131,628, compared with the activity of ciprofloxacin against 5,252 clinical bacterial isolates. Antimicrobial Agents and Chemotherapy 35 4: 764–766, 1991
Garan J, Grassi C, Hosie J, et al. Treatment of community-acquired pneumonia; a comparison of Sparfloxacin, amoxicillin clavulanic acid and erythromycin. 33rd Annual Interscience Conference on Antimicrobial Agents and Chemotherapy, New Orleans, October, 1993
Gehanno P, Berche P. Treatment of acute purulent sinusitis in adults: a comparison of two Sparfloxacin regimens and cefuroxime axetil. 33rd Annual Interscience Conference on Antimicrobial Agents and Chemotherapy, New Orleans, October 1993
Gentry LO. Therapy with newer oral β-lactam and quinolone agents for infections of the skin and skin structures: a review. Clinical Infectious Diseases 14 1: 285–297, 1992
Gentry LO, Rodriguez-Gomez G. Ofloxacin versus parenteral therapy for chronic osteomyelitis. Antimicrobial Agents and Chemotherapy 35: 538–541, 1991
Grenier B. Use of fluoroquinolones in children: an overview. Fortschritte der Antimikrobiellen Antineoplastischen Chemotherapie 11–2: 135–140, 1992
Hamilton BA, O’Bryan-Fear CG, Markenday S. Lomefloxacin vs amoxicillin in patients with acute exacerbations of chronic bronchitis: a UK multicentre study. Drugs 45(Suppl. 3): 9–10, 1993
Hammerschlag MR, Hyman CL, Roblin PM. In vitro activities of five quinolones against Chlamydia pneumoniae. Antimicrobial Agents and Chemotherapy 36 3: 682–683, 1992
Hara K, Yamaguchi K, Kohno S, et al. In vitro activity of Sparfloxacin against major pathogens related to respiratory tract infections. 3rd International Symposium on New Quinolones, Vancouver, Canada, July 1990
Heisig P, Wiedemann B. Genetische Grundlagen und Verbreitung von Fluorochinolonresistenz. Fortschritte der Antimikrobiellen Antineoplastischen Chemotherapie 10–13: 233–251, 1991
Hohl P, Felber AMR. Effect of method, medium, pH and inoculum on the in-vitro antibacterial activities of fleroxacin and norfloxacin. Journal of antimicrobial Chemotherapy 22(Suppl. D): 71–80, 1988
Hooper DC, Wolfson JS. Fluoroquinolone antimicrobial agents. New England Journal of Medicine 324 6: 384–394, 1991
Hooper DC, Wolfson JS, Eva Y, et al. Mechanisms of action of and resistance to ciprofloxacin. American Journal of Medicine 82(Suppl. 4A): 12–20, 1987
Human CL, Roblin PM, Hammershlag MR. In vitro activity of Sparfloxacin, a novel quinolone, ofloxacin and fleroxacin against Chlamydia pneumonia. 3rd International Symposium on New Quinolones, Vancouver, Canada, July 1990
Jauregui L, Mclnnes S. Therapy of gastrointestinal, central nervous system, and bone infections with new quinolones. In Siporin et al. (Eds) The new generation of quinolones, pp. 289–316, Marcel Dekker, New York, 1990
Just PM. Overview of the fluoroquinolone antibiotics. Pharmacotherapy 13(Suppl. 2): S5–S17, 1993
Kojima T, Inoue M, Mitsuhashi S. In vitro activity of AT-4140 against clinical bacterial isolates. Antimicrobial Agents and Chemotherapy 33(11): 1980–1988, 1989
Kuhn RJ, Palmejar A, Kanga JF. Tolerability of ciprofloxacin in pediatric patients with cystic fibrosis. Fortschritte der Anti-mikrobiellen Antineoplastischen Chemotherapie 11–12: 269–271, 1992
Lamaire N, Rosenkranz B, Malerczyk V, et al. Ofloxacin pharmacokinetics in chronic renal failure and dialysis. Clinical Pharmacokinetics 21 5: 357–371, 1991
Lambert HP, O’Grady FW. Quinolones, infective endocarditis, septicaemia, infections of the respiratory tract; meningitis; infections of the alimentary tract. In Lambert & O’Grady (Eds) Antibiotic and Chemotherapy, pp. 245–262, 336-386, Churchill Livingstone, New York, 1992
LeBel M. Fluoroquinolones in the treatment of cystic fibrosis: a critical appraisal. European Journal of Clinical Microbiology and Infectious Diseases 10: 316–324, 1991
Levin S, Trenholme GM. Comparison of intravenous followed by oral ciprofloxacin and intravenous ceftazidime in the treatment of lower respiratory infections. In Lode (Ed) Ciprofloxacin in clinical practise: new light on established and emerging uses, Congress, May, 1990, Berlin, pp. 177–182, Schwer, Stuttgart, 1990
Leysen DC, Haemers A, Pattyn SR. Mycobacteria and the new quinolones. Antimicrobial Agents and Chemotherapy 33: 1–5, 1989
Lightfoot MF, Ahmed F, Cowden J. Management of institutional outbreaks of salmonella gastroenteritis. Journal of Antimicrobial Chemotherapy 26(Suppl. F): 37–46, 1990
Loza E, Cantón R, Martinez-Beltrán J, et al. Activity of Sparfloxacin against Gram-positive bacteria: effect on organisms with PBP-me-diated beta-lactam resistance. 3rd International Symposium on New Quinolones, Vancouver, Canada, 1990
Maesen FPV, Davies BJ, Teengs JP. Pefloxacin in acute exacerbations of chronic bronchitis. Journal of Antimicrobial Chemotherapy 16: 379–388, 1985
Maiche AG. Use of quinolones in the immunocompromised host. European Journal of Clinical Microbiology and Infectious Diseases 10 4: 361–367, 1991
Malik IA, Abbas Z, Zarim M. Randomised comparison of oral ofloxacin alone and with combination of parenteral antibiotics in neutropenic febrile patients. Lancet 330: 1092–1096, 1992
Mandell LA. Role of quinolones in surgical prophylaxis. European Journal of Clinical Microbiology and Infectious Diseases 10 4: 368–377, 1991
Masecar BL, Celesk RA, Robillard HJ. Analysis of acquired ciprofloxacin resistance in a clinical strain of Pseudomonas aeruginosa. Antimicrobial Agents and Chemotherapy 34: 281–286, 1990
McDonald PJ, Pruul H. Quinolones and the immune system. In Siporin et al. (Eds) The new generation of quinolones, pp. 107–122, Marcel Dekker, New York, 1990
Meyer RD. Role of the quinolones in the treatment of legionellosis. Journal of Antimicrobial Chemotherapy 28: 623–625, 1991
Miller ARO. Sexually transmitted diseases. In Lambert & O’Grady (Eds). Antibiotic and Chemotherapy, pp. 428–438, Churchill Livingstone, New York, 1992
Montay G, Giallot J. Pharmacokinetics of fluoroquinolones in hepatic failure. Journal of Antimicrobial Chemotherapy 26(Suppl. 3): 61–67, 1990
Norrby SR, Pernet AG. Assessment of adverse events during drug development: experience with temafloxacin. Journal of Antimicrobial Chemotherapy 28(Suppl. C): 111–120, 1991
Naber KG. Lomefloxacin versus norfloxacin versus ciprofloxacin in the treatment of complicated urinary tract infections. International Journal of Antimicrobial Agents 2 1: 33–38, 1992
National Committee for Clinical Laboratory Standards (NCCLS). Performance standards for antimicrobial susceptibility testing. Second International Supplement, table II, M100-W27, 1988
Neu HC. Synergy and antagonism of combinations with quinolones. European Journal of Clinical Microbiology and Infectious Diseases 10 4: 255–261, 1991
Neu HC (Ed.) Ciprofloxacin monograph. Leverkusen, Bayer AG, Germany, 1992
Oguri T, Hayashi Y In vitro activity of Sparfloxacin against clinical isolates. 3rd International Symposium on New Quinolones, Vancouver, Canada, July 1990
Parish LC, Witkowski JA. Quinolones and cutaneous disease. In Siporin et al. (Eds) The new generation of quinolones, pp. 243–248, Marcel Dekker, New York, 1990
Perez-Tallero E, Garcia-Arenzana JM, Jiminez JA, et al. Therapeutic failure and selection of resistance in a case of pneumococcal pneumonia treated with ciprofloxacin. European Journal of Clinical Microbiology and Infectious Diseases 9 12: 905–906, 1990
Petrikkos G, Giamarellou H, Kolokythas E, et al. Passage of three newer quinolones in the human breast milk and the amniotic fluid. Fortschritte der Antimikrobiellen Antineoplastischen Chemotherapie 11–12: 241–247, 1992
Pithie AD, Wood MJ. Treatment of typhoid fever and infectious diarrhoea with ciprofloxacin. Journal of Antimicrobial Chemotherapy 26(Suppl. F): 47–53, 1990
Radandt JM, Marchbanks CR, Dudley MN. Interactions, of fluoroquinolones: mechanisms, variability, clinical significance, and management. Clinical Infectious Diseases 14 1: 272–284, 1992
Rajagopalan-Levasseur P, Dameron G, Bauchet J, et al. Inhibitory postantibacterial effect of Sparfloxacin on virulent Legionella pneumophila. 3rd International symposium on New Quinolones, Vancouver, Canada, July 1990
Reinhardt SP, Trotter JP. An economic assessment of ofloxacin. Drugs 45: 88–89, 1993
Rizk E. A worldwide clinical overview of lomefloxacin, a once-daily fluoroquinolone. International Journal of Antimicrobial Agents 2 1: 67–78, 1992
Robson RA. Quinolone pharmacokinetics. International Journal of Antimicrobial Agents 2 1: 3–10, 1992
Rohatgi K, Courtright JB. Major change in the structure and morphology of the bacterial nucleotide after treatment of cells with quinolones. In Siporin et al. (Eds) The new generation of quinolones, pp. 317–326, Marcel Dekker, New York, 1990
Ronald AR, Peeling RW. Chlamydial infections and the quinolones. European Journal of Clinical Microbiology and Infectious Diseases 1: 351–354, 1991
Rubio TT. Clinical and laboratory experience with ciprofloxacin in children two to sixteen years of age. Fortschritte der Antimikrobiellen Antineoplastischen Chemotherapie 11–2: 151–154, 1991
Saavedra S, Rivera-Vazquez CR, Ramirez-Ronda CH. Quinolones and sexually transmitted diseases. In Siporin et al. (Eds) The new generation of quinolones, pp. 277–287, Marcel Dekker, New York, 1990
Savitskaya KJ, Trapeznikova MF, Nasonov VN, et al. Lomefloxacin versus ciprofloxacin in the treatment of complicated or recurrent UTI. Drugs 45(Suppl. 3): 341–342, 1993
Schaad UB. Toxicity of quinolones in pediatric patients. Fortschritte der Antimikrobiellen Antineoplastischen Chemotherapie 11–12: 259–265, 1992
Schentag JJ, Nix DE, Wise R. Pharmacokinetics and tissue penetration of quinolones. In Siporin et al. (Eds) The new generation of quinolones, pp. 189–222, Marcel Dekker, New York, 1990
Schmidt M, Hoffmann K. The use of quinolones in children — toxi-cological aspects. Fortschritte der Antimikrobiellen Antineoplastischen Chemotherapie 11–2: 252–255, 1992
Scully BE, Clynes N, Neu HC. Oral ofloxacin therapy of infections due to multiply-resistant bacteria. Diagnostic Microbiology and Infectious Diseases 14 5: 435–441, 1991
Seto W-H, Lau FL, Gotuzzo EH, et al. Lomefloxacin versus trimethoprim/sulfamethoxazole in the treatment of adults with acute bacterial diarrhea. International Journal of Antimicrobial Agents 2 1: 67–78, 1992
Shimada J, Mogita T, Ishibashi Y. Clinical pharmacokinetics of Sparfloxacin. Clinical Pharmacokinetics 25 5: 358–368, 1993
Slack RCB. Urinary tract infections. In Lambert & O’Grady (Eds) Antibiotic and Chemotherapy, pp. 407–415, Churchill Livingstone, New York, 1992
Sonstein SA. Mode of action of quinolones: antibacterial aspects. In Siporin et al. (Eds) The new generation of quinolones, pp. 63–78, Marcel Dekker, New York, 1990
Stahlmann R, Förster C, van Sickle D. Quinolones in children. Are concerns over arthropathy justified? Drug Safety 9 6: 397–403, 1993
Stuck AE, Donbosco KK, Frey FJ. Fleroxacin clinical pharmacokinetics. Clinical Pharmacokinetics 22 2: 116–131, 1992
Takagi K, Yamaki K, Madai M, et al. Effect of a new quinolone, sparfloxcin, on the pharmacokinetics of theophylline in asthmatic patients. Antimicrobial Agents and Chemotherapy 35 6: 1137–1141, 1991
Todd PA, Faulds D. Ofloxacin: a reappraisal of its antimicrobial activity, pharmacology and therapeutic use. Drugs 42 5: 825–876, 1991
Traub WH, Spohr M, Bauer D. Pseudomonas aeruginosa: in vitro susceptibility to antimicrobial drugs, single and combined, with and without defibrinated human blood. Chemotherapy 34: 284–297, 1988
Unertl KE, Lenhart FP, Forst H, et al. Response of legionellosis infection to ciprofloxacin in critically ill patients. In Lode (Ed) Ciprofloxacin in clinical practice: new light on established and emerging uses, Congress, May 1990, Berlin, pp. 161–168, Schwer, Stuttgart, 1990
Van der Auwera P. Synergistic, additive, and antagonistic activity of antimicrobial agents: how to measure? What are the clinical consequences? Applications to the new fluoroquinolones. Infectious Diseases Newsletter 11 7: 49–56, 1992
Van Wijk JAE, de Jong TPVM, Van Gool JD, et al. Using quinolones in urinary tract infections in children. Fortschritte der Antimikrobiellen Antineoplastischen Chemotherapie 11–2: 157–161, 1992
Verbist L, Verhaegen J. In vitro activity of ciprofloxacin: an overview. In Lode (Ed) Ciprofloxacin in clinical practice: new light on established and emerging uses, Congress, May 1990, Berlin, pp. 5–12, Schwer, Stuttgart, 1990
Wadworth AN, Goa KL. Lomefloxacin: a review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs 42 6: 1018–1060, 1991
Walker RC, Wright AJ. The fluoroquinolones. Mayo Clinic Proceedings 66: 1249–1259, 1991
Weisser J, Wiedemann B. Brief report. Effects of ciprofloxacin on plasmids. American Journal of Medicine 82(Suppl. 4A): 21–22, 1987
Wentland MP. Structure-activity relationships of fluoroquinolones. In Siporin et al. (Eds) The new generation of quinolones, pp. 1–43, Marcel Dekker, New York, 1990
Wise R, Andrews JM, Ashby JP, et al. The in vitro activity of Sparfloxacin (AT4140) in comparison with other quinolones and β-lactams. 3rd International Symposium on New quinolones, Vancouver, Canada, July 1990
Wolfson JS, Hooper DC. Overview of fluoroquinolone safety. American Journal of Medicine 91(Suppl. 6A): S153–S161, 1991
Wolfson JS, Hooper DC. Pharmacokinetics of quinolones: newer aspects. European Journal of Clinical Microbiology and Infectious Diseases 10 4: 274–276, 1991
Yernault J-C, Russell D. Lomefloxacin versus amoxicillin in the treatment of acute exacerbations of chronic bronchitis: results of multinational studies. International Journal of Antimicrobial Agents 2 1: 39–48, 1992
Yuen GJ, Dusano GL, Brooks J, et al. Use of nonlinear mixed-effects modeling for population analysis of ofloxacin effects of age on oral drug pharmacokinetics. Pharmacotherapy 12 2: 88–92, 1992
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An erratum to this article is available at http://dx.doi.org/10.1007/BF03260131.
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von Rosenstiel, N., Adam, D. Quinolone Antibacterials. Drugs 47, 872–901 (1994). https://doi.org/10.2165/00003495-199447060-00003
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DOI: https://doi.org/10.2165/00003495-199447060-00003