1、,Anti-amebiasis and anti-trichomoniasis drugs (抗阿米巴病和抗滴虫病药) & Anthelmintic drugs (抗肠蠕虫药),A. Anti-amebiasis and anti-trichomoniasis drugs,(抗阿米巴病和抗滴虫病药),Amebiasis is infection with Entamoeba histolytica(溶组织内阿米巴), A tiny, one-celled organism.,A1. Anti-amebiasis drugs (amebicides),Life cycle of amebic p
2、arasite,Multiplication and life cycle of E histolytica,A1. Anti-amebiasis drugs (amebicides),Classification of amebiasis:Luminal amebiasis(肠内阿米巴):Amebic dysentery(阿米巴痢疾), Asyptomatic carrier(无症状带虫者)Systemic amebiasis(肠外阿米巴)Amebic hepatitis(阿米巴肝炎),hepatic abscess(阿米巴肝脓肿) Mixed amebiasis.,Anti-amebias
3、is drugs,Intestinal Amebiasis,Extraintestinal Amebiasis,Features of Amebiasis,A1. Anti-amebiasis drugs (amebicides),(肠内阿米巴),(肠外阿米巴),非痢疾性肠胃炎,The drugs used in amebiasis:Metronidazole(甲硝唑), Tinidazole(替硝唑);Emetine(依米丁), Dehydroemetine;Halogenate quinolines(卤化喹啉类):Chiniofon(喹碘仿), Clioquinol(氯碘羟喹), Diio
4、dohydroxyquinoline(双碘喹啉); Diloxannide(二氯尼特); Paromomycin(巴龙霉素); Chlorpromaquin(氯喹), etc.,Anti-amebiasis drugs,Metronidazole(甲硝唑, 灭滴灵),(1)Pharmacological effects & clinical uses:Anti-amebiasis effects:It has potent amebicidal activity to large trophozoite(大滋养体) grown, but no affect to small trophozoi
5、te(小滋养体).Effective to acute amebic dysentery and all systemic amebiasis, but ineffec-tive to asyptomatic passers. Therefore, it need be used comban-tion of purely intestinal amebicides, such as diloxanide to radically treatment.,Anti-amebiasis drugs,Metronidazole,Anti-trichomoniasis effects:Metronid
6、azole can kill Trichomonas vaginalis(阴道毛滴虫) directly. After oral administration, it is absorbed fast, distribute to the whole body, and secreted into vaginal secretion(in female), sperm(in male) and urine. Therefore, it is effective toTrichomonas infection of male and female.Its curative rate(治愈率) r
7、each 90%.,Anti-amebiasis drugs,Metronidazole,Anti-anaerobic bacteria infection:The sensitive anaerobic bacteria to metronidazole including:All anaerobic cocci(所有的厌氧球菌); G- anaerobic bacillus(G-厌氧杆菌) and G+ spore anaerobic bacillus(G+芽孢厌氧杆菌);Therefore, this drug is used to treat:1)vary anaerobic bact
8、eria infection of pelvic cavity and abnormal cavity; 2)peridentitis(牙周炎);3)infection of helicobacter pylori (HP) also, HP is the main cause of gastric and duodenal ulcer.,Anti-amebiasis drugs,Metronidazole,Anti-giardiasis:Giardiasis(贾第鞭毛虫病) caused by Giardia lamblia(蓝氏贾第鞭毛虫), which is a intestinal p
9、rotozoiasis(肠道原虫病), and there are process of cyst and trophozoite also, Giardia lamblia is mainly parasitic lived in duodenum and biliary tract(胆道).Metronidazole is the most effective drug to treat Giardiasis, Its curative rate reach 90%. (2)Adverse reaction:GI and CNS reaction, there is WBC reducti
10、on in some patients.,Anti-amebiasis drugs,Metronidazole,Tinidazole (替硝唑),(1)The t(1224h) is longer than metronidazole(t 8h), (2) After once oral adminis-tration, its effective blood concentration keep 72h, (3) its toxicity is less than metronidazole.,Anti-amebiasis drugs,Emetine(依米丁, 吐根碱) & Dehydroe
11、metine(去氢依米丁),They can kill amebic trophozoite (阿米巴滋养体)in tissue directly. Their adverse reaction are more and severe, their irritative action is strong, can cause vomiting(emesis) by oral administration, therefore, they are only injected by deep muscle.And they may cause heart toxicity, so that the
12、y are only used in severe amebic infection and when metronidazole is no effect.,Anti-amebiasis drugs,Diloxanide(二氯尼特),It can kill amebic cyst(阿米巴囊肿). The parts of unabsorption can kill amebic cyst and small trophozoite in intestinal cavity, effective to asymptomatic passers and the patients of evacu
13、ating amebic cyst. The therapeutic effect is not so good to acute amebic dysentery(急性阿米巴性痢疾), after controlling symptoms by metronidazole, treat it with diloxanide to kill the small trophozoite in intestinal tract, can radically cure amebic infection. Diloxanide is ineffective to systematic amebiasi
14、s.,Anti-amebiasis drugs,Paromomycin(巴龙霉素),After oral administration it cannot be absorbed.Direct action: It can kill the amebic trophozoite in intestinal tract. Indirect action:It can inhibit the symbiotic bacteria (共生细菌)of amebic protozoan(阿米巴原虫), then inhibit survivor and proliferation of ameba.It
15、 is used to treat acute amebiasis.,Anti-amebiasis drugs,Chloroquine(氯喹),It can kill amebic trophozoite also.Owing to absorption fast by p.o. and the concentration in intestinal cavity low, it is ineffective to intestinal amebiasis, but the concentration of chloroquine is very high in liver (the Conc
16、entration in liver is 700 times higher than the Cp). Clinical use: exo-intestinal amebic infection(e.g. amebic hepatitis & hepatic abscess). Its toxicity larger than metronidazole, only used in the patients ineffective or un-tolerant to metronidazole.,Anti-amebiasis drugs,抗阿米巴病药物治疗,Anti-amebiasis dr
17、ugs,A2. Anti-trichomoniasis drugs (Trichomonacides),Trichomoniasis(滴虫病, 滴虫性阴道炎) caused byTrichomonas vaginalis(阴道毛滴虫) infection.Male and female all can be infected, male is not onset, but can become the source of infection. Therefore, only should husband and wife be treated at the same time that tho
18、rough cure.,Metronidazole(甲硝唑),It is the most effective drug to infection of Trichomonas vaginalis. It is effective to patients, regardless of male and female patient. 0.2g, tid, po.7 days. Its curative rate(治愈率) reach 90%, or once large dose(2 g) po. 0.5g suppository(栓剂) of metronida-zole, local ap
19、plication.,Anti-trichomoniasis drugs,Acetarsol(乙酰胂胺),Acetarsol is a preparation of five-valence arsine. In clinic, devegan(滴维净) the complex preparation of acetarsol, one tablet of devegan contains acetarsol 0.25g, and boric acid 0.03g, local appli-cation, can kill Trichomonas vaginalis directly, use
20、d to the patients of metronidazole resistance.,Anti-trichomoniasis drugs,B. Anthelmintic drugs (抗肠蠕虫药),hookworm (钩虫),Pinworm(蛲虫),Whipworm(鞭虫),Fasciolopsis (姜片虫),ascaris(蛔虫),Tapeworm(绦虫),Intestinal helminth(肠蠕虫) including eelworm(线虫): ascaris(蛔虫), hookworm (钩虫), pinworm(蛲虫), whipworm(鞭虫), fasciolopsi
21、s(姜片虫) and tapeworm(绦虫), et al. In the past, the kinds of anthelmintic drugs are very more, and the sensitivity to intestinal helminth is different also. Now, the main anthelmintic drugs are broad spectrum and high potency, therefore, to treat helminthiasis become very easy in clinic. At the same ti
22、me, the drugs that we learn are very less.,Mebendazole(甲苯达唑),(1)Anthelmintic action:It is a broad spectrum and high potency anthelmintic drug, it can kill many kinds of nematoindea(线虫), e.g. ascaris(蛔虫), hookworm(钩虫), pinworm(蛲虫), whipworm(鞭虫), and tapeworm(绦虫), including imago, larva and ovum. The
23、effective rate is over 90%, it is suit-ed to mixed infection of helminth especially.It can kill ovum of helminth, and control the transmission of helminth too. (2)Adverse reaction: less, GI reaction; anaphylaxis; terato-genesis and embryotoxicity.,Anthelmintic drugs,Albendazole(阿苯达唑, “肠虫清”),It is a
24、broad spectrum Tapeworm(绦虫): pork tapemorm(猪肉绦虫), beef tapemorm(牛肉绦虫). The therapeutic effects are the same as mebendazole.,Anthelmintic drugs,Albendazole,Exo-intestinal parasitosis:It is a very efficacious drug for exo-intestinal parasitic disease, such as hyda-tidosis(包虫病), cysticercosis(囊虫病), tri
25、-chinosis(旋毛虫病), clonorchiasis(华支睾吸虫), paragonimiasis(肺吸虫病).Mebendazole is ineffective to those diseases, because albendazole is absorbed fast, its blood concentration is 100 times higher than that of mebendazole, the concentration in liver and lung is relatively high, therefore, albendazole can ent
26、er hydatidocystis(棘球幼囊).,Anthelmintic drugs,Albendazole,(2)Clinical Uses:,Intestinal nematodiasis(肠线虫病):including Ancylostomiasis(钩虫病), Ascariasis(蛔虫病), Trichuriasis(鞭虫病), once draft: 400mg;Intestinal taeniasis(肠绦虫病):effective to infection of pork t. and beef t., 800mg/day, 3 days;Cysticercosis(囊虫病)
27、:common patients(皮下-肌肉型): 200 300mg, tid, 10 days course, 23 courses.cerebral patients(脑型病例): hospita-lization.,Anthelmintic drugs,Albendazole,Hydatidosis(包虫病, 细粒棘球蚴病):a course: 30 days, the second course after 2 weeks.Clonorchiasis(华支睾吸虫病):a course: 7 days.Trichinosis(旋毛虫病):a course: 5 days, 1 or 2
28、 courses.Paragonimiasis(肺吸虫病).,Anthelmintic drugs,Albendazole,(3)Adverse reaction:,To treat intestinal parasitosis: the ADRs are less. To treat exo-intestinal parasitosis:e.g. cysticercosis(囊虫病) and hydatidosis (包虫病): The ADRs are more, because the therapeutic dose is larger and the course of treatm
29、ent is longer. The toxicity of albendazole is less. after getting therapeutic effect, cysticerci(囊尾蚴) died and disintegrated, releasing allo-protein to cause anaphylaxis, such as skin rash, headache, fever, and muscular aching pain(肌肉酸痛), etc.,Anthelmintic drugs,Albendazole,Piperazine 哌嗪 Levamisole
30、左旋咪唑 Pyrantel 噻嘧啶 Niclosamide 氯硝柳胺 Praziquantel 吡喹酮,Other Anthelmintic Drugs,Anthelmintic drugs,Piperazine(哌嗪, 驱蛔灵)Effective to ascaris(蛔虫) & pinworm (蛲虫), but the curative effect is less than albendazole, the merit of albendazole is side action less.Pyrantel(噻嘧啶, 驱虫灵)Broad spectrum antiematodiasis
31、drug (抗线虫病药), effective to ascaris(蛔虫), hookworm(钩虫), pinworm(蛲虫) and trichostrongylus(毛圆线虫) infection, but ineffective to whipworm (鞭虫).,Anthelmintic drugs,Pyrvinum ambonate (恩波吡维胺, 扑蛲灵)It is a cyanine dyes(花青类染料), the therapeutic effect to pinworm(蛲虫) is high, and its toxicity is less. 5 mg/kg/day
32、, total dose0.25 g, an interval of 23 week treated again, 23 times.,Anthelmintic drugs,Niclosamide(氯硝柳胺),It was formerly an molluscacide(灭螺剂) to be sprinkled in paddy field and riverside to kill oncomelania(钉螺), which is intermediate host(中间宿主) of schistosoma(血吸虫). It can also kill cercaria(尾蚴) and
33、miracidium(毛蚴) of schistosoma also. Later found it effective to varied taenia (绦虫) infection, especially effective to beef taenia infection. Application:draft 1 g, and draft 1 g again 1 h later, after 1 2 hr then orally take MgSO4 to purgation(导泻).,Anthelmintic drugs,Praziquantel(吡喹酮),It is a broad
34、spectrum anti-parasitic drug too. It can be used to treat schistosomiasis, and used to treat certain intestinal parasitosis also.It is ineffective to nematodiasis(线虫病) and amebiasis. It can be used to treat Taeniasis(绦虫病): Including varied imago(成虫) and larva (幼虫) infective disease, such as cysticer
35、cisis(囊虫病) and hydatidosis(包虫病).,Anthelmintic drugs,Praziquantel,(1)intestinal taenia infection(肠绦虫感染):10 or 25mg/kg, 一次顿服.(2)cysticercosis(囊虫症):common patients(皮下-肌肉型): 4 days course;cerebral patients(脑型病例):9 days course, after 34 months to 2nd course.(3)hydatidosis(包虫病):the drug can kill protoscol
36、ex(原头蚴), have its infective ability , but cant get cure, the effect is less than albendazole.,Anthelmintic drugs,Praziquantel,病 种 Therapiutic drugs蛔虫感染: Mebendazole, Albendazole,Pyrantel, Piperazine蛲虫感染: Mebendazole, Albendazole, Pyrantel, Pyrvinum ambonates钩虫感染: Mebendazole, Albendazole, Pyrantel鞭虫感染: Mebendazole绦虫感染: Praziquantel, Niclosamide, 囊虫病: Praziquantel, Albendazole 包虫病: Albendazole, Praziquantel, Mebendazole,Anthelmintic drugs,Anthelmintic drugs,The class is over !,
