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Published on: February 23, 2021
Sinus tissue concentration of moxifloxacin after a single oral dose
Paulo Borges Dinis1, Maria Conceição Monteiro, Maria Luz Martins
1Department of Otorhinolaryngology, Hospital de Pulido Valente, Lisbon, Portugal.
Abstract:
Moxifloxacin is a new fluoroquinolone antimicrobial approved for the treatment of acute bacterial rhinosinusitis. In order to assess its distribution pattern into the paranasal sinuses, and specifically to evaluate how the histopathologic changes associated with chronic inflammation affect its tissue penetration, we conducted the present investigation, a randomized, open-label, single dose, sinus-tissue pharmacokinetic study with oral moxifloxacin. Twenty adult subjects, selected for surgery because of recalcitrant chronic rhinosinusitis, were preoperatively randomly allocated to receive a tablet of 400 mg moxifloxacin 3 or 4 hours before the procedure. During the operation, tissue samples were collected at specific sinonasal sites, and the concentration levels of the antimicrobial in the different parts of the paranasal sinuses were assayed. Simultaneously, the degree of inflammation at each site was evaluated. We found that moxifloxacin was distributed extensively throughout the sinuses, in both inflamed and noninflamed mucosae, but tended to be concentrated in maxillary sinus cysts. The tissue-to-blood ratios exceeded 4:1 at most sites, with mucosal concentration levels well above the MIC90 values of the drug against a wide range of microorganisms. We concluded that the oral moxifloxacin tissue kinetics provides an extremely potent antimicrobial activity in all parts of the sinuses, regardless of the inflammatory status of the mucosa.
Insights
Moxifloxacin effectively penetrates sinonasal tissues, offering potent antimicrobial activity throughout the sinuses. This fluoroquinolone demonstrates excellent distribution, even in inflamed mucosa, supporting its use for chronic rhinosinusitis.
Area of Science:
- Pharmacology
- Otolaryngology
- Infectious Diseases
Background:
- Moxifloxacin, a fluoroquinolone antibiotic, is approved for acute bacterial rhinosinusitis.
- Understanding drug distribution in sinonasal tissues is crucial for effective treatment, especially in chronic inflammation.
Purpose of the Study:
- To assess moxifloxacin distribution in paranasal sinus tissues.
- To evaluate the impact of chronic inflammation on moxifloxacin tissue penetration.
Main Methods:
- A randomized, open-label, single-dose pharmacokinetic study.
- Oral administration of 400 mg moxifloxacin to 20 adult subjects undergoing surgery for chronic rhinosinusitis.
- Collection of sinonasal tissue samples at specific sites for drug concentration assay and inflammation evaluation.
Main Results:
- Moxifloxacin distributed widely across inflamed and non-inflamed sinonasal mucosa.
- Higher concentrations were observed in maxillary sinus cysts.
- Tissue-to-blood ratios exceeded 4:1, with levels above MIC90 for many pathogens.
Conclusions:
- Oral moxifloxacin exhibits potent antimicrobial activity in all sinus regions, irrespective of mucosal inflammation.
- The drug's pharmacokinetic profile supports its efficacy in treating sinonasal infections, including those with chronic inflammation.
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