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Chapter: Clinical Pharmacology: Anti-infective drugs


Fluoroquinolones are structurally similar synthetic antibiotics.



Fluoroquinolones are structurally similar synthetic antibiotics.They are primarily administered to treat UTIs, upper respiratory tract infections, pneumonia, and gonorrhea and include:

·                 ciprofloxacin


·                 levofloxacin


·                 moxifloxacin


·                 norfloxacin


·                 ofloxacin.



After oral administration, fluoroquinolones are absorbed well.

Metabolism and excretion


Fluoroquinolones aren’t highly protein-bound, are minimally me-tabolized in the liver, and are excreted primarily in urine.



Fluoroquinolones interrupt deoxyribonucleic acid (DNA) synthe-sis during bacterial replication by inhibiting DNA gyrase, an essen-tial enzyme of replicating DNA. As a result, the bacteria can’t re-produce.


Fluoroquinolones can be used to treat many UTIs. Each drug in this class also has specific indications.

§    Ciprofloxacin is used to treat lower respiratory tract infections, infectious diarrhea, and skin, bone, and joint infections.


§    Levofloxacin is indicated for the treatment of lower respiratory tract infections, skin infections, and UTIs.


§    Moxifloxacin is used to treat acute bacterial sinusitis and mild to moderate community-acquired pneumonia.


§    Norfloxacin is used to treat UTIs and prostatitis.


§    Ofloxacin is used to treat selected sexually transmitted dis-eases, lower respiratory tract infections, skin and skin-structure infections, and prostatitis (inflammation of the prostate gland).


Drug interactions

Several drug interactions may occur with the fluoroquinolones.


§    Administration with antacids that contain magnesium or alu-minum hydroxide results in decreased absorption of the fluoro-quinolone.


§    Some fluoroquinolones, such as ciprofloxacin, norfloxacin, and ofloxacin, interact with xanthine derivatives, such as amino-phylline and theophylline, increasing the plasma theophylline lev-el and the risk of theophylline toxicity.


§    Giving ciprofloxacin or norfloxacin with probenecid results in decreased kidney elimination of these fluoroquinolones, increas-ing their serum levels and half-life.


§    Drugs that prolong the QT interval, such as antiarrhythmics, should be used cautiously during moxifloxacin therapy. (See Ad-verse reactions to fluoroquinolones.)


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