Ofloxacin otic solution in patients with otitis media: an analysis of drug concentrations.

OBJECTIVE: To measure the concentration of ofloxacin in otorrhea, serum, and middle ear mucosa after topical administration of 0.3% ofloxacin otic solution. DESIGN: Study of 0.3% ofloxacin otic solution administered in a single dose of 0.5 mL in adults or 0.25 mL in children with chronic suppurative otitis media and perforated tympanic membrane, with serial sampling of otorrhea and serum up to 8 hours after dosing and middle ear mucosa up to 2 hours after dosing. SETTING: Three hospitals in Kagoshima, Japan. PATIENTS: Thirty-eight patients (age range, 3-81 years) with chronic suppurative otitis media and perforated tympanic membrane; 20 patients had sampling of otorrhea and serum and 18 patients (who required middle ear surgery) had middle ear mucosa and serum sampling. RESULTS: High concentrations of ofloxacin were measured in otorrhea samples taken immediately after dosing, followed by a rapid, nonlogarithmic decline. Elimination of the drug through otorrhea was believed to be related to loss from the application site with ear drainage, rather than to biologic mechanisms. Maximum concentration of ofloxacin in otorrhea was seen at the initial sampling time, 30 minutes after dosing, with concentrations measured up to the last sampling at 8 hours. Very low concentrations of ofloxacin were found in serum after topical administration of the drug. Concentrations were not detected in serum samples of most of the patients. The highest concentration measured was 10 ng/mL. Drug concentrations were detected primarily in samples obtained up to 1 hour after the dose was administered. Mucosal drug concentrations were highly variable, ranging from nondetectable to 602 pg/g. For the 6 bacterial strains isolated from the middle ear, the highest minimum inhibitory concentration of ofloxacin was covered by otorrhea drug concentrations measured at up to 8 hours after dosing in some patients. No adverse events were observed. No clinically significant adverse changes in laboratory test results or audiometric results were observed. CONCLUSIONS: Drug concentrations were high in otorrhea, very low or not detected in serum, and highly variable in middle ear mucosa. Nonbiologic loss of the drug with the ear drainage through the external auditory canal and eustachian tube was probably related to the high concentration in otorrhea samples. Drug concentrations in middle ear mucosa suggest that the drug reaches the infection site.

[A comparative study of UFT enteric-coated granules with UFT capsules on the occurrence of side effects in patients with head and neck cancers--a special attention to the upper gastrointestinal tract disorders].

A comparative study on the occurrence of gastrointestinal side effects between UFT enteric-coated granules (UE) and UFT capsules (UC) was made by crossover method in 50 patients with head and neck cancer who were treated by these drugs as a surgical and/or radiation adjuvant chemotherapy. UE was significantly low in the occurrence of upper gastrointestinal side effects; remarkably low in such side effects as nausea and vomiting, in particular. On the other hand, there was little difference between UE and UC in the occurrence of such side effects as diarrhea, stomatitis, dry mouth and hematotoxic signs. The present result suggests that UE is clinically useful for treating the patients with cancer, with less occurrence of gastrointestinal side effects.

[Clinical evaluation of ototoxicity associated with intravenous drip infusion of amikacin].

On the 53 patients with ENT (ears, nose, and throat) diseases, ototoxicity after intravenous drip infusion of amikacin (Biklin AMK) was studied. Each dose of AMK was 400 mg/day in adults and 4--8 mg/kg/day in children. From audiometric analysis, there were no patients with any hearing disturbances and subjective complaints concerning labyrinth injury. Also abnormal laboratory findings were not found in them. An intravenous drip infusion of AMK in adequate dosage would be beneficial to use against some infectious diseases of otorhinolaryngologic field.