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1、1,Fang Sanhua,Anti-parasite drugs,2,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,3,Antimalarial drugs,4,The malarial parasite, Plasmodium, is a very small, single-cell organism. It lives as a parasite in other o
2、rganisms, namely man and mosquito. The parasite is the cause of the tropical or subtropical disease malaria.,Antimalarial drugs -Malarial parasite,5,6,Four species of plasmodium can produce the disease in its various forms: Plasmodium falciparum （恶性疟原虫） Plasmodium vivax （间日疟原虫） Plasmodium ovale （卵形疟
3、原虫） Plasmodium malaria （三日疟原虫）,7,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,8,No one available agent can reliably effect a radical cure, ie, eliminate both exo-erythrocytic and erythrocytic stages. Few available agents are causal prophylactic drugs, ie, capable of preventing
4、erythrocytic infection.,Antimalarial drugs,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 Pyrimethamine （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,10,Antimalarial drugs Chloroquine
5、 （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,11,Pharmacological effects 1. Antimalarial effects Rapid schizonticidal activity （裂殖体杀灭剂） against all infections of malaria species . Also gametocytocidal（杀配子体）against P. vi
6、vax, P. malariae and P. ovale . It is not active against exo-erythrocytic form, and should therefore be used with primaquine（伯氨喹）to effect radical cure of P. vivax.,Antimalarial drugs - Chloroquine,12,Pharmacological effects 2. Immune inhibition Treatment of rheumatoid arthritis, lupus erythematosus
7、 3. Extraintestinal amebiasis Amoeba trophozoite amebic liver abscess,Antimalarial drugs - Chloroquine,13,Mechanism of actions Accumulation in erythrocytepH malarial pigment synthesis heme Heme-quinoline compound heme accumulate in plasmodium Insert in the double stranded DNA helix DNA replication a
8、nd RNA transcription ,Antimalarial drugs - Chloroquine,14,Adverse effects Rare at the usual antimalarial dosages Pruritus (瘙痒症) common among dark-skinned people. Transient headaches, nausea, vomiting, gastrointestinal symptoms and “blurred vision”. Others: aplastic blood and neurological disorders,
9、such as polyneuritis (多发性神经炎), seizures and neuromyopathy.,Antimalarial drugs - Chloroquine,15,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,16,控制复发 Primaquine (伯氨喹) 迟发,阻止传播 Primaquine (伯氨喹) Chloroqui
10、ne (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,Antimalarial drugs Primaquine （伯氨喹）,17,Pharmacological effects Highly 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 currently used for the
11、 treatment of relapsing malaria,Antimalarial drugs Primaquine （伯氨喹）,18,Mechanism of actions Inhibition of coenzyme Q Inhibition of reduction of NADP Adverse effects Transient dizziness , nausea, vomiting, gastrointestinal symptoms Acute hemolytic anemia, methemoglobinemia (高铁血红蛋白血症),Antimalarial dru
12、gs Primaquine （伯氨喹）,19,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),20,Pharmacological effects Inhibition of proliferation of sporozoite (子孢子) to schizont (裂殖体) Prophylaxis of infections Mechanism of actions Dihydrofolate reductase inhi
13、bitor Adverse effects Folate metabolism disturbtance,Antimalarial drugs Pyrimethamine （乙胺嘧啶）,symptom？,复发？,传播？,控制症状 Chloroquine（氯喹） Quinine（奎宁） Mefloquine（甲氟喹） Artemisinin（青蒿素）,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 Pyrimethamine (乙胺嘧啶) 速发,阻止传播
14、 Pyrimethamine （乙胺嘧啶）,25,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) 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）,26,Antiamebiasis drugs,27,Amebiasis is infection with Entamoeba histolytica.
15、 （溶组织内阿米巴原虫 ） Classification of amebiasis Asymptomatic intestinal infection; Mild to moderate colitis; Severe intestinal infection (dysentery); Extraintestinal infections: ameboma, liver abscess.,Antiamebiasis drugs -Amebiasis,28,Amebiasis is infection with Entamoeba histolytica, A tiny, one-celled
16、organism.,Antiamebiasis drugs -Amebiasis,29,Intestinal Amebiasis,Extraintestinal Amebiasis,Features of Amebiasis,30,Multiplication and life cycle of E histolytica,Antiamebiasis drugs -Amebiasis,31,Clinical Manifestations Acute or chronic diarrhea, which may progress to dysentery. Extraintestinal disease may be present as a complication or as a primary problem (e.g., liver, lung or brain abscess, or
