Pharmacokinetic and clinical studies of gatifloxacin on otorhinolaryngological infections

Abstract

Pharmacokinetic and clinical studies were carried out with gatifloxacin (GFLX) in otorhinolaryngological infections. The results were as follows:
1. In the middle ear mucosa, the concentration of GFLX ranged from undetectable levels (ND) to 0.66/μg at 120 to 165 minutes after oral administration of 100 mg, and from ND to 1.11 μg/g at 140 to 510 minutes after oral administration of 200 mg, and the penetration ratio (tissue/serum) ranged from 0.23 to 6.00. In the paranasal sinus mucosa, the concentration of GFLX ranged from 1.06 to 1.91 μg/g at 120 to 170 minutes after oral administration of 100 mg, and from 1.79 to 4.29 μg at 110 to 160 minutes after oral administration of 200 mg, and the penetaration ratio ranged from 1.41 to 2.20. In the paroid gland, the concentraion of GFLX ranged from 0.34 to 2.52 μg at 150 to 350 minutes after oral administration of 100mg, and the penetration ratio ranged from 1.82 to 7.20.
2. The clinical efficacy rate was 75.7%(28/37) for otitis media, 88.2%(15/17) for paranasal sinusitis, 85.2%(23/27) for tonsillitis, 81.8%(9/11) for pharyngolaryngitis, 86.7%(13/15) for otitis externa, and 4/4 for suppurative sialadenitis. The overall clinical efficacy was excellent in 39, good in 53, fair in 14, and poor in 5, with the efficacy rate of 82.9%(92/111).
3. The elimination rate was 87.0%(67/77) for gram-positive aerobes, 90.9%(30/33) for gram-negative aerobes, and 100%(8/8) for anaerobes, and resulted in the overall rate of 89.0%(105/108).
4. Although adverse reactions were observed in 5 of 115 cases (4.3%) and abnormal laboratory test findings were recorded in 4 of 92 cases (4.3%), none were serious.
These results indicate that GFLX is a very useful drug for the treatment of otorhinolaryngological infections.