CLINICAL PHARMACOLOGY OF FLOROCHINOLONS: A FOCUS ON SAFETY. Review

Abstract

Fluoroquinolones are effective in the treatment of infections of almost any localization (upper and lower respiratory tract, urinary system, skin and soft tissues, bones and joints, liver and bile ducts, gastrointestinal tract, female genital tract, central nervous system, intra-abdominal), sexually transmitted infections. Resistance is slowly formed to fluoroquinolones. Among the benefits of certain fluoroquinolones are that they can be administered either orally or intravenously. Fluoroquinolones can also be combined with antibacterial agents of other groups. Levofloxacin (the left-turning isomer of ofloxacin) has now become one of the most commonly used antibiotics. This is because the drug exhibits high tissue penetration, creating in the alveolar macrophages, the mucous membranes of the bronchi and fluid lining the respiratory epithelium, a concentration that is significantly higher than the MIC to respiratory pathogens. The literature review presents current insights on the pharmacokinetics, pharmacodynamics, and adverse effects of fluoroquinolones. The risks of tendinitis, tendon ruptures, aortic aneurysm / dissection, QT prolongation, recurrence of C.difficile antibiotic-associated diarrhea, hypo- and hyperglycemic conditions are emphasized. The clinical role of fluoroquinolones inhibitory effect on cytochrome P450 isoenzymes CYP1A2 and CYP2C9 activities, which metabolize many drugs with low therapeutic index (derivatives of sulfonylureas, warfarin, phenytoin, and theophylline etc). Therefore, when deciding on the prescription of fluoroquinolones, especially for elderly patients, the doctor should collect a detailed anamnesis, in particular regarding the administration of drugs with a small therapeutic index, and conduct therapeutic drug monitoring, including monitoring blood glucose levels.