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Table of Contents
Vol. 47, Suppl. 3, 2001
Issue release date: September 2001
Chemotherapy 2001;47(suppl 3):3–8
(DOI:10.1159/000057838)

History of Quinolones and Their Side Effects

Rubinstein E.
Department of Internal Medicine and Unit of Infectious Diseases, Tel Aviv University School of Medicine, Tel Aviv, Israel

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Abstract

Fluoroquinolone development from 1985 to the present was reviewed. Severe drug adverse events were noted for enoxacin, pefloxacin and fleroxacin, which were phototoxic. Temafloxacin was associated with severe hemolytic–uremic syndrome, lomefloxacin caused phototoxicity and central nervous system (CNS) effects, and sparfloxacin was associated with phototoxicity and QTc prolongation. Tosufloxacin caused severe thrombocytopenia and nephritis, and hepatotoxicity was reported for trovafloxacin. Grepafloxacin was withdrawn due to cardiovascular effects, and clinafloxacin was associated with phototoxicity and hypoglycaemia. The structure of the quinolones directly relates to both their activity and side-effect profiles. The relationship among specific substituents attached to the quinolone nucleus are clarified. The incidence of specific adverse events associated with individual fluoroquinolones was reviewed in a five-year post-marketing surveillance (PMS) study in Japan, in which a total adverse drug reaction (ADR) rate of 1.3% was found for levofloxacin, compared to total ADR rates of 3.3% for pazufloxacin, 3.6% for tosufloxacin, 4.5% for gatifloxacin and 5.4% for balofloxacin. Gastrointestinal effects were the most common adverse events for all fluoroquinolones. Levofloxacin had the lowest rate of CNS effects and skin adverse events among the agents listed.



Copyright / Drug Dosage

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Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in goverment regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.
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References

  1. Langtry HD, Lamb HM: Levofloxacin. Its use in infections of the respiratory tract, skin, soft tissues and urinary tract. Drugs 1998;56:487–515.
  2. Lipskey BA, Baker CA: Fluoroquinolone toxicity profiles: A review focusing on newer agents. Clin Infect Dis 1999;28:352–364.
  3. Ball P, Mandell L, Niki Y, Tillotson G: Comparative tolerability of newer fluoroquinolone antibacterials. Drug Saf 1999;21:407–-421.
  4. Bowie WR, Willetts V, Jewesson PJ: Adverse reactions in a dose-ranging study with a new long-acting fluoroquinolone, fleroxacin. Antimicrob Agents Chemother 1989;33:1778–1782.

    External Resources

  5. Blum MD, Graham DJ, McCloskey CA: Temafloxacin syndrome: review of 95 cases. Clin Infect Dis 1994;18:946–950.

    External Resources

  6. Domagala JM: Structure–activity and structure–side-effect relationships for the quinolone antibacterials. J Antimicrob Chemother 1994;33:685–706.


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