抗寄生虫药专题知识课件.ppt

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1、Human parasite,Protozoa （原虫）：孢子虫疟原虫 鞭毛虫阴道毛滴虫 叶足虫阿米巴原虫 纤毛虫结肠小袋纤毛虫 Helminth （蠕虫）：吸虫血吸虫 绦虫链状带绦虫 线虫蛔虫、丝虫Arthropod （节肢动物）：蛛形纲蜱、螨 昆虫纲蚊、蝇、虱,Human parasiteProtozoa （原虫）：孢子,Antimalarial drugs,Antimalarial drug,The malarial parasite, Plasmodium, is a very small, single-cell organism. It lives as a parasite in

2、 other organisms, namely man and mosquito. The parasite is the cause of the tropical or subtropical disease malaria.,Antimalarial drugs -Malarial parasite,The malarial parasite, Plasmod,抗寄生虫药专题知识课件,Four species of plasmodium can produce the disease in its various forms: Plasmodium falciparum （恶性疟原虫）

3、Plasmodium vivax （间日疟原虫）Plasmodium ovale （卵形疟原虫）Plasmodium malaria （三日疟原虫）,Four species of plasmodium can,Antimalarial drugs - Parasite Life Cycle,红细胞外期,红细胞内期,按蚊有性繁殖,人体无性繁殖,Antimalarial drugs - Parasite,No one available agent can reliably effect a radical cure, ie, eliminate both exo-erythrocytic an

4、d erythrocytic stages. Few available agents are causal prophylactic drugs, ie, capable of preventing erythrocytic infection.,Antimalarial drugs,No one available agent can rel,控制复发Primaquine（伯氨喹） 迟发,病因预防Pyrimethamine（乙胺嘧啶）速发,控制症状Chloroquine（氯喹）Quinine（奎宁）Mefloquine（甲氟喹）Artemisinin（青蒿素）,阻止传播Pyrimetham

5、ine（乙胺嘧啶）,阻止传播Primaquine （伯氨喹） Chloroquine （氯喹）Quinine （奎宁）（恶性疟无效）,红细胞外期,红细胞内期,按蚊有性繁殖,控制复发病因预防控制症状阻止传播阻止传播红细胞外期红细胞内期,Antimalarial drugs Chloroquine （氯喹）,Chloroquine is a synthetic 4-aminoquinoline derivate,控制症状Chloroquine 氯喹Quinine 奎宁Mefloquine 甲氟喹Artemisinin 青蒿素,红细胞内期,Antimalarial drugs Chloroqui,P

6、harmacological effects1. Antimalarial effectsRapid schizonticidal activity （裂殖体杀灭剂） against all infections of malaria species . Also gametocytocidal（杀配子体）against P. vivax, P. malariae and P. ovale . It is not active against exo-erythrocytic form, and should therefore be used with primaquine（伯氨喹）to e

7、ffect radical cure of P. vivax.,Antimalarial drugs - Chloroquine,Pharmacological effectsAntimal,Pharmacological effects2. Immune inhibitionTreatment of rheumatoid arthritis, lupus erythematosus 3. Extraintestinal amebiasisAmoeba trophozoite amebic liver abscess,Antimalarial drugs - Chloroquine,Pharm

8、acological effectsAntimal,Mechanism of actionsAccumulation in erythrocytepH malarial pigment synthesis hemeHeme-quinoline compound heme accumulate in plasmodium Insert in the double stranded DNA helix DNA replication and RNA transcription ,Antimalarial drugs - Chloroquine,Mechanism of actionsAntimal

9、ari,Adverse effectsRare at the usual antimalarial dosagesPruritus (瘙痒症) common among dark-skinned people.Transient headaches, nausea, vomiting, gastrointestinal symptoms and “blurred vision”.Others: aplastic blood and neurological disorders, such as polyneuritis (多发性神经炎), seizures and neuromyopathy.

10、,Antimalarial drugs - Chloroquine,Adverse effectsAntimalarial dr,Quinine （奎宁）Mefloquine （甲氟喹）Pyronaridine (咯萘啶)Artemisinin (青蒿素)Artemether and artesunate (蒿甲醚和青蒿琥酯),Other angents kill erythrocytic parasites,Quinine （奎宁）Other angents kill,控制复发Primaquine(伯氨喹) 迟发,阻止传播Primaquine (伯氨喹) Chloroquine (氯喹)Qu

11、inine (奎宁)（恶性疟无效）,红细胞外期,红细胞内期,按蚊有性繁殖,Antimalarial drugs Primaquine （伯氨喹）,控制复发阻止传播红细胞外期红细胞内期按蚊有性繁殖Antim,Pharmacological effectsHighly active against the gametocytes (配子体) of all malaria species dissemination Active against hypnozoites (迟发型子孢子) of the relapsing malarial parasites The only drug current

12、ly used for the treatment of relapsing malaria,Antimalarial drugs Primaquine （伯氨喹）,Pharmacological effectsAntimal,Mechanism of actionsInhibition of coenzyme Q Inhibition of reduction of NADPAdverse effectsTransient dizziness , nausea, vomiting, gastrointestinal symptomsAcute hemolytic anemia, methem

13、oglobinemia (高铁血红蛋白血症),Antimalarial drugs Primaquine （伯氨喹）,Mechanism of actionsAntimalari,红细胞外期,红细胞内期,按蚊有性繁殖,Antimalarial drugs Pyrimethamine （乙胺嘧啶）,病因预防Pyrimethamine(乙胺嘧啶) 速发,Pyrimethamine(乙胺嘧啶),红细胞外期红细胞内期按蚊有性繁殖Antimalarial,Pharmacological effectsInhibition of proliferation of sporozoite (子孢子) to s

14、chizont (裂殖体)Prophylaxis of infectionsMechanism of actionsDihydrofolate reductase inhibitorAdverse effectsFolate metabolism disturbtance,Antimalarial drugs Pyrimethamine （乙胺嘧啶）,Pharmacological effectsAntimal,symptom？,symptom？,复发？,传播？,控制症状Chloroquine（氯喹）Quinine（奎宁）Mefloquine（甲氟喹）Artemisinin（青蒿素）,复发？传

15、播？控制症状,病因预防？,控制复发Primaquine（伯氨喹） 迟发,阻止传播Primaquine （伯氨喹） Chloroquine （氯喹）Quinine （奎宁）（恶性疟无效）,病因预防？控制复发阻止传播,病因预防Pyrimethamine(乙胺嘧啶) 速发,阻止传播Pyrimethamine（乙胺嘧啶）,病因预防阻止传播,用于控制症状的抗疟药 Chloroquine （氯喹）、Quinine （奎宁）、 Mefloquine （甲氟喹）、Pyronaridine (咯萘啶)、Artemisinin (青蒿素) 、 Artemether and artesunate (蒿甲醚和青蒿琥酯

16、) 用于控制复发和传播的抗疟药 Primaquine （伯氨喹）用于病因性预防的抗疟药 Pyrimethamine （乙胺嘧啶）,用于控制症状的抗疟药,Antiamebiasis drugs,Antiamebiasis drug,Amebiasis is infection with Entamoeba histolytica.（溶组织内阿米巴原虫 ）Classification of amebiasisAsymptomatic intestinal infection;Mild to moderate colitis;Severe intestinal infection (dysenter

17、y);Extraintestinal infections: ameboma, liver abscess.,Antiamebiasis drugs -Amebiasis,Amebiasis is infection with En,Amebiasis is infection with Entamoeba histolytica, A tiny, one-celled organism.,Antiamebiasis drugs -Amebiasis,Amebiasis is infection with En,Intestinal Amebiasis,Extraintestinal Ameb

18、iasis,Features of Amebiasis,Intestinal AmebiasisExtraintes,Multiplication and life cycle of E histolytica,Antiamebiasis drugs -Amebiasis,Multiplication and life cycle,Clinical Manifestations Acute or chronic diarrhea, which may progress to dysentery. Extraintestinal disease may be present as a compl

19、ication or as a primary problem (e.g., liver, lung or brain abscess, or skin or perianal infection).,Antiamebiasis drugs -Amebiasis,Clinical Manifestations Antiam,Antiamebiasis drugs - Metronidazole 甲硝唑,Pharmacological effectsAntibiotic effective against anaerobic bacteria. Anti-giardia lamblia （贾第氏

20、鞭毛虫）effectAnti-ameba effects （肠内、肠外） The treatment of all tissue infections with E histolytica4. Anti-infusorian （滴虫）effects,Antiamebiasis drugs - Metronid,Mechanism of actionsThe methyl group of metronidazole is chemically reduced in anaerobic bacteria and sensitive protozoans. （原生动物）Reactive reduc

21、tion products appear to be responsible for antimicrobial activity.Rapidly absorbed and has a bioavailability of approximately 90%,Antiamebiasis drugs - Metronidazole,Mechanism of actionsAntiamebia,Adverse effectsSerious side effects of metronidazole are rare; and include seizures and damage of nerve

22、s resulting in numbness and tingling of extremities (peripheral neuropathy). Minor side effects include nausea, headaches, loss of appetite, a metallic taste, and rarely a rash.,Antiamebiasis drugs - Metronidazole,Adverse effectsAntiamebiasis d,Emetine依米丁& dehydroemetine去氢依米丁Amebicide effects : spor

23、adin (滋养体)Mechanism of actions: protein synthesis inhibitor.Clinic uses: Amebic liver abscess , Acute amebic dysenteryUsed in case of resistance to metronidazole.,Emetine依米丁& dehydroemetine去氢依米,Emetine依米丁& dehydroemetine去氢依米丁Adverse effectsNausea, vomiting and diarrhoea. Palpitations, tachycardia, r

24、etrosternal pain, hypotension, dyspnoea, ECG changes (ST depression, QT prolongation, T-wave inversion). Tremor, myasthenia and paralysis including respiratory paralysis.,Antiamebiasis drugs - Other amebicides,Emetine依米丁& dehydroemetine去氢依米,Diloxanide furoate is slowly absorbed from the gastrointest

25、inal tract and can therefore provide an adequate concentration of the medication in the intestinal lumen for a long period of time.,Antiamebiasis drugs - Diloxanide 二氯尼特,Diloxanide furoate is slowly a,Mechanism of actionsLuminal amebicide. Destroys the trophozoites of E. histolytica that eventually

26、form into cysts. (包囊)The cysts are then excreted by persons infected with asymptomatic amebiasis. (无症状的阿米巴病),Antiamebiasis drugs - Diloxanide,Mechanism of actionsAntiamebia,Adverse effectsNot commonly seen with this medication unless the patient is taking especially high doses. Minor side effects in

27、clude nausea, headaches, and rarely a rash.,Antiamebiasis drugs - Diloxanide,Adverse effectsAntiamebiasis d,Antiamebiasis drugs - Other amebicides,Paromomycin 巴龙霉素Aminoglycosides antibiotics. Not significantly absorbed from the gastrointestinal tract Mechanism of actions: Acts by inhibition protein

28、synthesis.Direct and indirect action of amebicideClinical usage: Amebic dysentery (阿米巴痢疾)No effect against extraintestinal amebic infections.,Antiamebiasis drugs - Other am,Extraintestinal amebiasisAmoeba trophozoite amebic liver abscess,Antimalarial drugs - Chloroquine,Antimalarial drugs - Chloroqu

29、i,Anti-bilharziasis & filariasis Drug,Anti-bilharziasis & fila,Bilharziasis急性发热过敏反应腹痛、腹泻肝脾肿大,Bilharziasis,Anthelmintic ActionsSchistosomiasis (血吸虫病)Clonorchiasis, Opisthorchiasis (支睾吸虫病), and Paragonimiasis (肺吸虫病)Taeniasis (绦虫病)、Diphyllobothriasis (裂头绦虫病） H Nana （缩小膜壳绦虫） Neurocysticercosis （脑囊虫病）Hyd

30、atid Disease （包虫囊病）Other Parasites： fasciolopsiasis, metagonimiasis, and other forms of heterophyiasis. fascioliasis,Praziquantel 吡喹酮,Anthelmintic ActionsPraziquant,Mechanism of actionsIncrease the permeability of cell membranes to calcium, resulting in paralysis, dislodgement, and death.In schistos

31、ome infections, praziquantel is effective against adult worms and immature stages Prophylactic effect against cercarial （尾蚴）infection.,Praziquantel 吡喹酮,Mechanism of actionsPraziquant,Adverse effectsMost frequent are headache, dizziness, drowsiness, and lassitude;Others include nausea, vomiting, abdo

32、minal pain, pruritus, urticaria, arthralgia, myalgia, and low-grade fever.Mild and transient elevations of liver enzymes,Praziquantel 吡喹酮,Adverse effectsPraziquantel 吡喹,Filariasis淋巴管炎、淋巴结炎橡皮肿、乳糜尿,Filariasis,Diethylcarbamazine 乙胺嗪,Anthelmintic ActionsDiethylcarbamazine immobilizes microfilariae （微丝蚴）

33、and alters their surface structure, displacing them from tissues and making them more susceptible to destruction by host defense mechanisms.,Clinical Uses Wuchereria Bancrofti, Brugia Malayi, Brugia Timori, and Loa LoaAdverse effectsGenerally mild and transientInclude headache, malaise, anorexia, we

34、akness, nausea, vomiting, and dizziness.,Diethylcarbamazine 乙胺嗪Anthelm,Anthelmintic Drugs 驱(蠕)虫药,Anthelmintic Drug,Anthelmintic Drugs Albendazole （阿苯达唑）,Anthelmintic Drugs Albendazol,Pharmacological effectsA broad-spectrum oral anthelmintic, is the drug of choice for treatment of hydatid disease （包虫

35、病）and cysticercosis. （囊虫病）Also used for the treatment of pinworm （蛲虫）and hookworm infections, ascariasis（蛔虫病） , trichuriasis（鞭虫病）and strongyloidiasis（类圆线虫病）,Anthelmintic Drugs -Albendazole,Pharmacological effectsAnthelm,Adverse effectsMild and transient epigastric distress, diarrhea, headache, nause

36、a, dizziness, lassitude, and insomnia can occur. Abdominal distress, headaches, fever, fatigue, alopecia, increases in liver enzymes, and pancytopenia in long-term use,Anthelmintic Drugs -Albendazole,Adverse effectsAnthelmintic Dr,A synthetic benzimidazole that has a wide spectrum of anthelmintic activity,Anthelmintic Drugs - Mebendazole,Anthelmintic Drugs - Mebendazo,Piperazine （哌嗪）:蛔虫、绦虫Levamisole （左旋咪唑）：蛔虫、钩虫、绦虫Pyrantel （噻嘧啶）：蛔虫、钩虫、绦虫Niclosamide （氯硝柳胺）：绦虫Praziquantel （吡喹酮）：吸虫、绦虫,Anthelmintic Drugs - Other Anthelmintic Drugs,Piperazine （哌嗪）:蛔虫、绦虫Ant,