Drug Interactions of Quinolone ( fluoroquinolones) - Antibiotics and Antibacterials

Theophylline, non-steroidal anti-inflammatory drugs and corticosteroids enhance the toxicity of fluoroquinolones.

Products containing multivalent cations, such as aluminum- or magnesium-containing antacids and products containing calcium, iron, or zinc, invariably result in marked reduction of oral absorption of fluoroquinolones.

Other drugs that interact with fluoroquinolones include Antacids, Sucralfate, Probenecid, Cimetidine, Warfarin, Antiviral agents, Phenytoin, Cyclosporine, Rifampin, Pyrazinamide, and Cycloserine.

Many fluoroquinolones, especially ciprofloxacin, inhibit the cytochrome P450 isoform CYP1A2.This inhibition causes an increased level of, for example, antidepressants such as amitriptyline and imipramine, Clozapine (an atypical antipsychotic), Caffeine, Olanzapine (an atypical antipsychotic), Ropivacaine (a local anaesthetic), Theophylline (a xanthine) and Zolmitriptan (a Serotonin receptor agonist).

Mechanism of action of Quinolone ( fluoroquinolones) - Antibiotics and Antibacterials

Quinolones and fluoroquinolones are chemotherapeutic bactericidal drugs, eradicating bacteria by interfering with DNA replication. The other antibiotics used today, (e.g., tetracyclines, lincomycin, erythromycin, and chloramphenicol) do not interact with components of eukaryotic ribosomal particle and thus have proven not to be toxic to eukaryotes, as opposed to the fluoroquinolone class of drugs. Safer drugs used to treat bacterial infections, such as penicillins and cephalosporins, inhibit cell wall biosynthesis, thereby causing bacterial cell death, as opposed to the interference with DNA replication as seen within the fluoroquinolone class of drugs.

Quinolones are synthetic chemotherapeutic agents which have a broad spectrum of antimicrobial activity as well as a unique mechanism of action resulting in inhibition of bacterial DNA gyrase and topoisomerase IV. Quinolones inhibit the bacterial DNA gyrase or the topoisomerase IV enzyme, thereby inhibiting DNA replication and transcription. Quinolones can enter cells easily via porins and therefore are often used to treat intracellular pathogens such as Legionella pneumophila and Mycoplasma pneumoniae. For many gram-negative bacteria DNA gyrase is the target, whereas topoisomerase IV is the target for many gram-positive bacteria. It is believed that eukaryotic cells do not contain DNA gyrase or topoisomerase IV.

However, there is debate concerning whether the quinolones still have such an adverse effect on the DNA of healthy cells, in the manner described above, hence contributing to their adverse safety profile. This class has been shown to damage mitochondrial DNA.