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甲硝唑的放射增敏作用。通过口服片剂、栓剂和灌肠剂形式的“甲硝唑”后血药浓度曲线进行的药代动力学比较(作者译)

[Radiosensitization with metronidazole. Pharmacocinetical comparison by means of blood level curves after administration of "metronidazol" in the form of tablets, suppositories, and enemas (author's transl)].

作者信息

Kärcher K H, Nitsche V, Kogelnik H D, Szepesi T

出版信息

Strahlentherapie. 1979 Dec;155(12):811-6.

PMID:516104
Abstract

Severe acute gastrointestinal side-effects following high oral doses of metronidazole (6 g/m2) could be avoided by a combined oral and rectal application. With tablets and an enema (1 g metronidazole/2 ml) in a ratio 1:4 and an increased dosage of 10 g/m2, maximal serum concentrations of about 200 micrograms/ml are obtained like after an oral dosage of 6 g/m2. The maximal radiosensitizing effect on hypoxic tumor cells is seen five hours after oral application and seven hours after the combined oro-rectal application. No longterm toxicity was found following six high doses of metronidazole.

摘要

高口服剂量甲硝唑(6 g/m²)后出现的严重急性胃肠道副作用可通过口服与直肠联合用药避免。采用片剂与灌肠剂(1 g甲硝唑/2 ml)按1:4的比例,并将剂量增至10 g/m²,可获得约200微克/毫升的最大血清浓度,这与口服6 g/m²后的情况相同。对缺氧肿瘤细胞的最大放射增敏作用在口服给药后5小时以及口服与直肠联合给药后7小时出现。在六次高剂量甲硝唑给药后未发现长期毒性。

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