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History Of Quinolone Antibiotics
By Generic Medications. Online Pharmacy
The fluoroquinolone family is a relatively new group of antibiotics. They were first introduced in 1986, but they are really modified quinolones. The parent of the group is nalidixic acid. The majority of quinolones belong to a subgroup called fluoroquinolones, which have a fluoro group attached the central ring system. Both terms are used to describe antibiotics in this class. The fluoroquinolones have become an increasingly popular class of antibiotics for use in a variety of infections. These drugs are the only class of antimicrobial agents in clinical use that are direct inhibitors of bacterial DNA synthesis. Fluoroquinolones inhibit two bacterial enzymes, DNA gyrase and topoisomerase IV, which have essential and distinct roles in DNA replication. The fluoroquinolones are classified into generations based on their antibacterial spectrum, with earlier generation quinolones more effective against Gram-negative bacteria and the spectrum of activity expanding to include more Gram-positive bacteria with the later generations. The first-generation agents ("quinolones") had poor distribution into the body tissues and limited activity. They were used mainly for treatment of urinary tract infections. The early quinolones include: cinoxacin, nalidixic acid and oxolinic acid. Second-generation fluoroquinolones have significantly increased antibacterial activity. These antibacterial agents have increased gram-negative activity, as well as some gram-positive and atypical pathogen activity. Compared with earlier quinolones, these drugs have broader clinical use in the treatment of complicated urinary tract infections and pyelonephritis, sexually transmitted diseases, pneumonias
and skin infections. Ciprofloxacin and ofloxacin are the most widely used second-generation fluoroquinolones because of their availability in oral and intravenous formulations and their broad set of FDA-approved indications. The third-generation fluoroquinolones (levofloxacin, gatifloxacin, moxifloxacin, sparfloxacin, trovafloxacin) have expanded activity against gram-positive bacteria and atypical pathogens, such as Mycoplasma pneumoniae and Chlamydia pneumoniae. Third-generation antibiotics are widely used in the treatment of community-acquired pneumonia, acute sinusitis and acute exacerbations of chronic bronchitis. The fourth-generation fluoroquinolones (e.g. garenoxacin, gemifloxacin, trovafloxacin) add significant antimicrobial activity against anaerobes while maintaining the gram-positive and gram-negative activity of the third-generation antibiotics. The quinolones have evolved from drugs used solely for the treatment of urinary tract infections to molecules with potent activity against a wide spectrum of bacterial pathogens and clinical utility in many indications throughout body tissues and fluids. Progressive modifications in molecular configuration have resulted in improved breadth and potency of activity and pharmacokinetics, which have identified those agents fit to survive in today's therapeutic environment. Yury Bayarski is the contributing author of HealthyStock.net. More information about fluoroquinolone antibiotics such as Cipro and Levaquin is available on author's website.
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