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瑞普明——一种具有广谱抗菌及免疫调节特性的抗生素。

Reprimun--an antibiotic with large spectrum and immunomodulatory properties.

作者信息

Păunescu E

机构信息

Marius Nasta Institute of Pneumophthisiology, Bucharest.

出版信息

Pneumoftiziologia. 1994 Jul-Dec;43(3-4):189-95.

PMID:7767104
Abstract

Reprimun contains an oxyminomethyl rifamycin-SV derivative as the active substance and has a large spectrum antibiotic activity, on Mycobacterium tuberculosis too. Reprimun also shows an inhibitory activity on viral and human lymphocyte reverse transcriptases, an antiproliferative effect on retrovirus, as well as a selective immunomodulator action at the level of TCD4+ lymphocyte. In animal, the toxicity tests demonstrated a good tolerance. In human subject, the drug is quite well tolerated: no severe adverse reactions were noted during and after its administration for 10-12 months. In man, Reprimun administration demonstrated a therapeutical effect in bacterial infections (tuberculosis included), sarcoidosis, immune thrombocytopenia, as well as in Kaposi's sarcoma. The drug is only for oral administration. It is well absorbed at the level of duodenum, achieving a repeated entero-hepatic circuit that provides a prolonged efficient concentration of Reprimun in blood serum. Like many other ansamycin derivatives, Reprimun can be given intermittently (e.g. twice or three times weekly). In case of antisarcoidosis therapy, Reprimun was applied with good results in 112 supervised cases, including 37 failures of a prior cortisone treatment its administration could be of a high benefit in HIV serum positive persons in which it can prevent both tuberculosis and HIV infection developments.

摘要

利福平含有一种氧代甲基利福霉素 - SV 衍生物作为活性物质,具有广谱抗菌活性,对结核分枝杆菌也有效。利福平还对病毒和人类淋巴细胞逆转录酶显示出抑制活性,对逆转录病毒具有抗增殖作用,以及在 TCD4 + 淋巴细胞水平上具有选择性免疫调节作用。在动物身上,毒性试验表明耐受性良好。在人体试验中,该药物耐受性也相当好:在给药 10 - 12 个月期间及之后未观察到严重不良反应。在人类中,利福平给药在细菌感染(包括结核病)、结节病、免疫性血小板减少症以及卡波西肉瘤中显示出治疗效果。该药物仅用于口服。它在十二指肠水平吸收良好,实现了重复的肠肝循环,从而在血清中提供利福平的长效有效浓度。与许多其他安莎霉素衍生物一样,利福平可以间歇给药(例如每周两次或三次)。在抗结节病治疗中,利福平在 112 例受监督的病例中应用效果良好,其中包括 37 例先前皮质类固醇治疗失败的病例;在 HIV 血清阳性人群中使用它可能非常有益,因为它可以预防结核病和 HIV 感染的发展。

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