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PubMed · 11051638

Warning for oral solution.

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2000. Warning for oral solution.. https://pubmed.ncbi.nlm.nih.gov/11051638/

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An open label, multicenter, non-comparative study of the efficacy and safety of oral gatifloxacin in the treatment of community-acquired pneumonia: a Brazilian study in five centers.

We made an open label, multicenter, non-comparative study to assess the efficacy and safety of oral gatifloxacin, 400 mg PO given once-daily during 7 to 14 days for the treatment of adult outpatients with community-acquired pneumonia at five Brazilian medical facilities. Among the 86 subjects available for clinical evaluation, 84 (98%) were cured. The bacteriological eradication and presumed eradication rate was 98% (52/53) among the 44 (51%) patients who were bacteriologically evaluated. Drug-related adverse events were reported by 27% of the patients, diarrhea being the most frequent, occurring in 12% of patients. Adverse events were considered mild (89%) or moderate (11%). We conclude that a 7-14 day course of gatifloxacin, 400 mg PO given once daily is safe and effective for the treatment of community-acquired pneumonia. The drug had a favorable safety profile and a good clinical and bacteriological efficacy.

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Effects of oral UFT combined with or without zoledronic acid on bone metastasis in the 4T1/luc mouse breast cancer.

Bone metastasis is one of the major causes of increased morbidity and eventual mortality in breast cancer patients. Therefore, intervention of bone metastases is one of the important targets in the management of breast cancer. In the present study, we examined the effects of the orally administrable chemotherapeutic agent UFT (a combination of tegafur and uracil at a molar ratio of 1:4) on bone metastases using an animal model of the 4T1/luc mouse breast cancer. The 4T1/luc cells developed spontaneous metastases to bone following orthotopic cell inoculation. Oral daily administration of UFT (20 mg/kg/day) significantly reduced the orthotopic tumor burden; however, the lower dose (15 mg/kg/day) did not. In contrast, histologic examination showed that both doses of UFT significantly suppressed bone metastases in a dose-dependent manner. Since clinical studies have demonstrated that bisphosphonates (BPs), specific inhibitors of osteoclastic bone resorption, are beneficial for breast cancer patients with bone metastases, we next examined the effects of UFT combined with the BP zoledronic acid (ZOL) on established bone metastases. The combination of UFT (20 mg/kg/day) with ZOL (250 microg/kg) caused an enhanced reduction of bone metastases compared with UFT alone. In vitro studies showed that 5-fluorouracil (5-FU), an active metabolite of UFT, and ZOL increased apoptosis in 4T1/luc cells and inhibited osteoclast-like cell formation in an additive fashion. Our results suggest that oral UFT is an effective chemotherapeutic agent for advanced breast cancer accompanying bone metastases and that the combination with BP increases its benefits for bone metastases.

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The effects of certain H(1)-antagonists on visual evoked potential in rats.

The present study was undertaken to clarify the effects of certain H(1)-antagonists on visual evoked potential (VEP) in rats. Pyrilamine (5 and 10 mg/kg), diphenhydramine (5 and 10 mg/kg) and chlorpheniramine (10 and 20 mg/kg) caused a significant reduction in the amplitude of late VEP components (P(3)-N(3), N(3)-P(4)), although these drugs showed no significant changes in early VEP components (P(1)-N(1), N(1)-P(2)). Cyproheptadine caused a slight enhancement of late components of VEP at a dose of 20 mg/kg. On the other hand, epinastine caused no significant effect on late VEP components even at a dose of 20 mg/kg. The reduction in the late VEP components induced by pyrilamine and diphenhydramine was significantly antagonised by pre-treatment of histidine (200 and 500 mg/kg), but not by physostigmine even at a dose of 0.01 mg/kg. The effect induced by cyproheptadine was significantly potentiated by histidine (500 mg/kg), and significantly reduced by DOI (2 mg/kg). These results indicate that an inhibition of the late VEP components induced by H(1)-antagonist pyrilamine, diphenhydramine and chlorpheniramine may be due to an inhibition of specific sensory system relating the histaminergic mechanisms. In addition, slight enhancement of these components induced by cyproheptadine may be attributable to its anti-serotonergic effects.

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