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1.
Jpn J Antibiot ; 45(5): 557-68, 1992 May.
Article in Japanese | MEDLINE | ID: mdl-1512942

ABSTRACT

Evaluations were made on biliary excretion and penetration into the gallbladder tissue of levofloxacin (LVFX, DR-3355), a new quinolone antibacterial agent, and its clinical efficacy in biliary tract infections. 1. Gallbladder tissue concentrations and biliary concentrations of LVFX at 2-6 hours at oral administration of 100 mg were 0.58-1.99 micrograms/g and 0.49-5.63 micrograms/ml, respectively. These tissue and biliary levels are almost equal or somewhat higher than the serum levels (0.55-1.63 micrograms/ml) of the compound. 2. The concentrations of LVFX and optical isomer DR-3354 in the serum, gallbladder tissue, and bile were determined after a single or a concomitant administration of LVFX 100 mg and/or ofloxacin (OFLX) 100 to 200 mg. The concentration ratio of LVFX to DR-3354 paralleled with the ratio of the 2 compounds administrated. 3. At a dose of 100 mg, the glucuronide of LVFX in the common duct bile was detected at proportions between 0.9 and 36.0%. 4. A total of 11 patients with biliary tract infections, including 6 cholecystitis 3 cholangitis, and 1 each of cholecystocholangitis and liver abscess was treated with LVFX at 100-200 mg t.i.d. for 3-14 days. Clinical results were excellent or good in 8 cases and fair in 3 cases, resulting in an efficacy rate of 72.7%. 5. A side effect and an abnormal change in laboratory findings were observed in both 1 case each and they were both mild. It was concluded that LVFX showed good penetration to the biliary tract as does OFLX, and that it would be a useful oral agent for the treatment of biliary tract infections.


Subject(s)
Bile/metabolism , Cholangitis/drug therapy , Cholecystitis/drug therapy , Gallbladder/metabolism , Levofloxacin , Ofloxacin/pharmacokinetics , Adult , Aged , Cholangitis/metabolism , Cholecystitis/metabolism , Drug Evaluation , Female , Humans , Male , Middle Aged , Ofloxacin/administration & dosage , Ofloxacin/therapeutic use
2.
Gan To Kagaku Ryoho ; 16(2): 225-34, 1989 Feb.
Article in Japanese | MEDLINE | ID: mdl-2493222

ABSTRACT

The usefulness of UFTMO therapy (combined chemotherapy with UFT, MMC and OK-432) performed in 40 cases of recurring or advanced cancer of the digestive organs was investigated. According the response criteria by Koyama et al., of 40 eligible cases, the treatment was judged effective in 13, 2 CR and 11 PR cases with a response rate of 32.5%, while of the 35 complete cases, 2 CR and 9 PR cases made for 11 effective cases and a response rate of 31.4%. Side effects were observed in 58.3% of the 36 evaluated cases; of the subjective and objective side effects, however, none were serious enough to require cessation of administration, while stopping administration in the cases of abnormal laboratory findings resulted in rapid recovery. UFTMO therapy, therefore, is considered to be one of the beneficial treatments for recurring or advanced cancer of the digestive organs.


Subject(s)
Antineoplastic Combined Chemotherapy Protocols/therapeutic use , Digestive System Neoplasms/drug therapy , Neoplasm Recurrence, Local/drug therapy , Adult , Aged , Aged, 80 and over , Antineoplastic Combined Chemotherapy Protocols/adverse effects , Digestive System Neoplasms/pathology , Drug Evaluation , Female , Humans , Male , Middle Aged , Mitomycin , Mitomycins/administration & dosage , Multicenter Studies as Topic , Neoplasm Metastasis , Neoplasm Recurrence, Local/pathology , Picibanil/administration & dosage , Remission Induction , Tegafur/administration & dosage , Uracil/administration & dosage
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