74．利福平
出处：按学科分类—医药、卫生 军事医学科学出版社《临床常用进口药物手册》第417页（9132字）
【中文释文】：
利福平是一种新的半合成抗生素，口服给药有效，具有杀菌性，为里派得(Lepetit)研究所发现。它的化学结构式为3，4-(甲基-哌嗪基-亚氨甲基)利福霉素SV。
本品的体外抗菌活性表明：当浓度为1μg／ml以下时对革兰阳性菌及包括结核杆菌在内的细菌有效：浓度为数μg／ml时对大多数革兰阴性菌有效。
本品同其他抗生素(利福霉素除外)不产生交叉耐药性，因此，它对那些对抗生素有耐药性的细菌也具有抗菌活性。另一方面，必须看到在治疗期间(有时甚至是在开始用本品治疗后不久)依据微生物种属的不同可能出现利福平的耐药菌株。
利福平对不同感染的药效，在实验中得到充分验证，它的药效超过所有已被研究过的其他抗生素的药效，特别是对葡萄球菌感染药效；现已证明它对不同病因引起的几种感染的疗效特别显着，并且是介于抗结核病的异烟肼与链霉素之间。
分别口服本品150mg、300mg剂量之后，在近第1小时末记录到最大血药浓度；在8h甚至12h后其残留浓度仍可测得，它在机体组织和体液的扩散极为良好。本品以很高的浓度由胆汁和尿中排出。
大量的临床研究证明，本品对由革兰阳性细菌引起的疾病，由革兰阴性菌丛引起的感染和结核病均有效。一般来说，利福平耐受良好。有时它可确诊胃部疾患。极少病例出现过敏现象(包括血小板减少性紫癜)。使用本品治疗的某些病人曾出现白细胞减少，同使用其他抗生素的情况一样，不可能确定与使用利福平有什么因果关系。现已观察到某些病例出现黄疸和(或)血清转氨酶升高的病例，在绝大多数病例中，这种问题来源于病人，关于此问题可能是利福平与其他药物，特别是结核菌抑制药有关。
〔适应证〕
敏感细菌引起的感染。呼吸器官感染：支气管炎、肺炎、支气管肺炎、支气管扩张、肺脓肿、脓胸、胸膜炎。
皮肤和软组织感染：疖、脓肿、黄癣、蜂窝织炎、瘭疽、感染性创伤。
胆道感染：胆囊炎
淋病
外科感染：耳炎等
肺和泌尿生殖系结核病。
为了慎重使用抗生素，有必要通过抗生素图谱来确定病原菌的敏感性(可能是原发性的或后天性的耐药性)。同样做法也适用于利福平(可通过平盘或微生物片测定抗生素谱)。如果在相当的时间内对疾病未产生有效作用，治疗应考虑改变；老病复发，在没有前述的微生物学检验的情况下，应禁止给病人服用利福平。
在因甲型和乙型溶血性链球菌引起疾病的感染(咽炎、扁桃体炎)的情况下，有必要在治疗结束时证明引起疾病的病原菌消失。在这种情况下，不适合作用利福平来预防远期并发症的出现。甚至有临床已经愈合之后，某些链球菌由于出现继发的耐药性而有可能持续存在。
〔剂量学和给药方法〕
利福平的包装为150mg胶囊和300mg胶囊。
1．非特异性感染
(1)成人：建议剂量为600mg／d；严重病例可增加到900～1200mg／d。
尿路感染情况下，建议剂量为900～1200mg／d。
淋病情况下建议剂量900mg／d；本剂量应1次服下(上述给定剂量服用2次)。
(2)儿童：推荐剂量：以1次或2次服下，最高20mg／(kg·d)体重。淋病除外，对所列其他感染要求在疾病的临床改善之后应继续治疗数日。
2．结核病
剂量一般应为600mg／d，一次服下。
本品通常与其他结核菌抑制药合用。
若考虑达到更迅速，更完全的吸收，建议空腹服用本品，距开饭时间间隔较远为宜。
〔包装〕
100粒胶囊装，每粒胶囊含150mg本品。
〔注意事项〕
在有黄疸或对本品过敏情况下禁用，妊娠头3个月内也禁用。在妊娠后6个月中，以及正在哺乳的婴儿，本品仅在紧急需要时，并且只能在医师直接监护下才能使用。
对肝病病人(特别是患有慢性酒精中毒，肝硬变病人)，也仅在绝对需要而且是在医师直接监护下才能使用。在这种情况下本品和其他有关药物(特别是对肝脏毒性强的药物)都应减少剂量，并对肝功能要加以监测。
如本品和口服抗凝剂同时服用，需要记住利福平会削弱抗凝剂的作用，因而有时需要增加后者的剂量。
附注：服用本品之后，尿、眼泪和唾液出现不同程度的玫瑰色。
〔生产厂家〕
罗马尼亚布加勒斯特U．M．B药厂
(附本品别名：甲哌力复霉素，Rimactane，Benemicin，Rifampin，Rifadin，Rifaldin，Rifaldazine，Riforal，RFP)
【外文释文】：
Rifampicin is a new semisynthetic antibiotic product efficient when administered by oral way，endowed with bactericide properties，discovered in the Research Laboratories of Lepetit．Its chemical structure is that of a 3-4(methyl-piperazinil iminomethyl)rifamycin SV(Rifampicin)．
The antimicrobial activity“in vitro”is manifested in concentrations less than Imcg／ml against the gram-positive germs and against the microbacteria including Mycobacterium tuberculosis，and in concentrations of a few mcg／ml against the majority of the gram-negative germs．
Rifampicin gives no cross-resistance with other antibiotics(excepting the rifamycins)；consequently，it is active also against the germs resistant to antibiotics．On the other hand，it is compulsory to observe that during treatment，(sometimes even very soon after its beginning)，Rifampicin-resistant strains may appear with a variable incidence depending on the microbial species．
The efficiency of Rifampicin in different infections was fully verified in experiments；it overtakes that of all other antibiotics already studied，especially in staphylococcic infections；it proved especially remarkable in several infections of a different etiology and is placed between isoniazid and streptomycin in tuberculosis．
After“per os”administration of a 150mg dose，respectively 300mg，maximum sanguine concentrations shall be recorded towards the first hour’s end；the sanguine remanence is appreciable after 8 or even 12 hours．Its diffusion in tissues and humours is excellent．Rifampicin is eliminated predominantly by bile and by urine where it reaches very high concentrations．
Numerous clinical studies certify the therapeutic efficiency of Rifampicin in diseases determined by gram-positive germs，in numerous infections caused by gram-negative microbial flora and in tuberculosis．
Rifampicin is generally well tolerated．Sometimes it can determine gastric troubles．In very few cases hypersensibility phenomena were signalled(including thrombopenic purple)．At some patients treated with rifampicin，leucopenia appeared，like in the cases of using other antibiotics，without being possible to establish any causal relation with the drug(Rifampicin)administration．Some cases of icterus and／or serum transaminases increase were observed in the majority of cases．The question being of patients to which Rifampicin was associated with other drugs，especially tuberculostatics．
Indication
Infections provoked by sensible germs．
Breathing apparatus infections：brochitis，pneumoniae，bronchopneumoniae，bronchiectasies，pulmonary abscesses，empiemae，pleuresies．Skin and soft tissues infections：furuncules，abscesses，favus，flegmona，whitlows，infected wounds．
Biliary ways infections：cystitis．
Gonorrhoea
Surgical infections：otitis etc．
Pulmonary and uro-genital tuberculosis．
For a judicious use of the antibiotics，it is necessary to determine the pathogenous agents sensibility(respectively their possible resistance primary or acquired)，by means of the antibiogram．
The same procedure is required in the case of Rifampicin(the antibiograms)．If the disease is not favourably influenced in a convenient period of time，the treatment shall be modified；if a recidivation occurs，it is contraindicated to administer rifamycins without previous microbiological tests．
In cases of infections with alpha and beta-haemolytic streptococcus(pharingitis，amygdalitis)it is necessary to prove，by the end of the treatment，the disappearance of the causal agent of the disease．In such cases，Rifampicin is not indicated for far complications prevention，as even after clinical healing，some streptococci could persist because of a secondary resistance development．
Posology and Administration Mode
Rifampicin is presented as capsule of 150mg and 300mg．
1．Nonspecific infections
(1)Adults：
The recommended daily dose is of 600 mg；in grave cases it can be increased up to900-1 200mg．
In urinary infections a daily dose of 900-1 200mg is recommended．
In gonorrhoea，a 900mg dose is recommended；it should be taken in a single dose(the doses indicated above should be taken in two doses)．
(2)Children：
The daily recommended posology：up to 20mg／kg of body weight in one or two doses．Except gonorrhoea，the other enumerated infections require a treatment continued for some days after the amelioration of the clinical symptoms of the disease．
2．Tuberculosis
The daily dose is 600mg，to be administered，in general，in a single dose．
As a rule，Rifampicin should be administered with other tuberculostatics．
In view of a more rapid and complete resorption，it is recommended to take Rifampicin tablets on an empty stomach and at great intervals from meal-times．
Presentation
100 capsules of 150mg．
Cautions
It is contraindicated to administer Rifampicin in the presence of an icterus or of a Rifampicin hypersensibility，also during the first trimester of pregnancy．During the other two trimesters of gestation，as well as to the suckling babies，this drug should be administered only in cases of urgent necessity and only under direct medical supervision．
In the case of hepatic patients(especially with chronic alcoholism and cirrhosis)，Rifampicin should be administered also only if it is absolutely necessary and under medical supervision．In such cases，the Rifampicin dose should be reduced，as well as the doses of other associated drugs(especially if they are potentially hepatotoxic)，and the liver function should be supervised．
If Rifampicin is administered with oral anticoagulants，it is necessary to keep in mind that it can diminish their activity，sometimes being necessary to increase their posology．
Remarks：after Rifampicin administration，urine，tears and saliva get a rosy colour of variable intensity．
Manufacturer
U．M．B-Drug Factory Bucharest