Anti-amebiasisdrugs（amebicides）
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Pyrimethamine+ Primaquine
PHARMACOLOGY
Anti-amebiasis drugs and anti-trichomoniasis drugs
The life cycle of amebae
amebic cysts (包囊)
small trophozoite(小滋养体)
large trophozoite(大滋养体)
intestinal wall
liver, brain, lung
Amebic dysentery
(阿米巴痢疾)
evacuating amebic cyst
Systemic amebiasis
(肠外阿米巴病 )
amebic cysts (包囊)
and various gametocytes(配子体) of subtertian malaria.
Owing to fast elimination, the effects are not lasting.
2. Drugs controlling relapse and transmission
1. Drugs controlling symptoms
Mechanism of anti-malarial action: 1. Alkalinization of food vacuole 2. Damage mediated by accumulated heme 3. Decreased DNA synthesis
Adverse reactions: • GI reaction, occasionally serum GPT↑, Teratogenesis.
2. Drugs controlling relapse and transmission
Primaquine(伯氨喹)
Anti-malarial activity: • Kill dormancytes(休眠子) of tertian malaria
Adverse reactions: 1. Inducing acute hemolytic anemia in patients
with genetically low levels of G-6-PD. 2. GI and CNS reactions
3. Drugs for etiological prevention
3. Drugs for etiological prevention
Anti-malarial activity: • Primethamine inhibits development of sporophytes
(孢子体) in mosquito, can’t kill gametocytes(配子体).
• Single large dose can cause acute toxication.
Summarization
Selection of antimalarial drugs
1. Symptom control: Chloroquine; 2. Cerebral malaria: Artemisinin, im.
Folate is synthesized from 3 basic building blocks, GTP, p-aminobenzoic acid (pABA), and glutamate, in a pathway involving 5 enzymes.
•DHPS dihydropteroate synthase;DHFR dihydrofolate reductase
1. Drugs controlling symptoms
Quinine (奎宁)
Anti-malarial activity :
• Kill the schizonts(裂殖体) in erythrocytic stage • A gametocide(杀配子体) for P. vivax(间日疟原虫) and P.
性疟) • Curing subtertian malaria(恶性疟); • Symptomatic prevention in epidemic area.
1. Drugs controlling symptoms
2. Treatment of amebiasis(阿米巴病): • treating systemic amebiasis(肠外阿米巴病), such
dizziness, tinnitus(耳鸣), dysphoria(烦躁), skin itching, and GI reaction. 2. In high dose, visual disturbance can occur 3. Quinidine-like effects 4. Teratogenesis
as amebic hepatitis(阿米巴肝炎) and amebic hepatic abscess(阿米巴肝脓肿).
3. Immunosuppression.
1. Drugs controlling symptoms
Adverse Reactions: 1. Be less in anti-malarial dose, occasionally
Life cycle of malarial parasite
Anti-malarial Drugs
1. Drugs controlling symptoms -Chloroquine (氯喹), quinine(奎宁), artemisinin (青蒿素)
2. Drugs controlling relapse and transmission -primaquine(伯氨喹)
美国拉斯克奖将2011年临床研究奖授予中国中医科学院终身研究员屠呦呦，以表彰 她发现了青蒿素。
1. Drugs controlling symptoms
Clinical uses: • Chloroquine-resistant subtertian malaria, and benign
malaria. – But its recurrence rate is high(30%).
(抗血吸虫病和抗丝虫病药) 4. Anthelmintic drugs (抗肠蠕虫药)
Anti-malarial Drugs
Malarial parasite (plasmodium, 疟原虫)
1. P.falciparum(恶性疟原虫) 2. P.vivax (间日疟原虫) 3. P.malariae(三日疟原虫) 4. P.ovale (卵形疟原虫)
malariae(三日疟原虫), but not for P. falciparum(恶性疟 原虫).
1. Drugs controlling symptoms
Clinical uses: • Treatment of the chloroquine- and
multidrug-resistant subtertian malaria (恶性 疟) and severe cerebral malaria(脑型疟).
3. Drugs for etiological prevention -primethamine(乙胺嘧啶)
1. Drugs controlling symptoms
Chloroquine (氯喹)
Anti-malarial activity:
• Kill the schizonts(裂殖体) in erythrocytic stage – The effects are fast and lasting. – The clinical symptoms will vanish after administration of chloroquine in 24-48 h, blood malarial parasites disappear in 48-72 h.
Anti-malarial activity: • Kill the schizonts(裂殖体) in erythrocytic
stage.
– The effects are faster than that of chloroquine, and effective to chloroquine-resistant subtertian malaria, especially to cerebral malaria.
Clinical uses: 1. Treating benign malaria radically, at
combination with chloroquine； 2. Preventing transmission of subtertian
malaria.
2. Drugs controlling relapse and transmission
Quinine dihydrochloride, iv 3. Chloroquine-resistant subtertian malaria:
Quinine, Artemisinin. 4. Resting stage: Pyrimethamine+ Primaquine 5. Prevent transmission: Pyrimethamine 6. Combined administration: Chloroquine+ Primaquine
hypotension, arrhythmias 3. Idiosyncrasy(特异质反应) : acute hemolytic
reaction. 4. Stimulating womb(兴奋子宫): abortion
1. Drugs controlling symptoms
Artemisinin (青蒿素)
ne(乙胺嘧啶)
Anti-malarial activity: 1. Killing schizonts(裂殖体) of subtertian
malarial parasites and benign malarial parasites in exo-erythrocytic stage; 2. Killing immature schizonts of erythrocytic stage.
1. Drugs controlling symptoms
Adverse reactions: 1. Cinchonism(金鸡纳反应): tinnitus(耳鸣),
headache, nausea, disturbed vision, etc. 2. Myocardial depression(心肌抑制作用):
PHARMACOLOGY
Anti-parasitic drugs
Contents
1. Anti-malarial drugs (抗疟药) 2. Anti-amebiasis and anti-trichomoniasis drugs
(抗阿米巴病和抗滴虫病药) 3. Anti-schistosomiasis and anti-filariasis drugs
Chloroquine (CQ) accumulates in the food vacuole of the parasite.
1. Drugs controlling symptoms
Clinical Uses: 1. Treatment of malaria: • Controlling the symptoms of benign malaria(良
3. Drugs for etiological prevention
Clinical uses: prevent malaria
Adverse reactions:
• Administration in large dose or in long time, megaloblastic anemia (巨红细胞贫血) can occur→ treated with formyl tetrahydrofolic acid(甲酰四氢叶酸).
PHARMACOLOGY
Anti-amebiasis drugs and anti-trichomoniasis drugs
The life cycle of amebae
amebic cysts (包囊)
small trophozoite(小滋养体)
large trophozoite(大滋养体)
intestinal wall
liver, brain, lung
Amebic dysentery
(阿米巴痢疾)
evacuating amebic cyst
Systemic amebiasis
(肠外阿米巴病 )
amebic cysts (包囊)
and various gametocytes(配子体) of subtertian malaria.
Owing to fast elimination, the effects are not lasting.
2. Drugs controlling relapse and transmission
1. Drugs controlling symptoms
Mechanism of anti-malarial action: 1. Alkalinization of food vacuole 2. Damage mediated by accumulated heme 3. Decreased DNA synthesis
Adverse reactions: • GI reaction, occasionally serum GPT↑, Teratogenesis.
2. Drugs controlling relapse and transmission
Primaquine(伯氨喹)
Anti-malarial activity: • Kill dormancytes(休眠子) of tertian malaria
Adverse reactions: 1. Inducing acute hemolytic anemia in patients
with genetically low levels of G-6-PD. 2. GI and CNS reactions
3. Drugs for etiological prevention
3. Drugs for etiological prevention
Anti-malarial activity: • Primethamine inhibits development of sporophytes
(孢子体) in mosquito, can’t kill gametocytes(配子体).
• Single large dose can cause acute toxication.
Summarization
Selection of antimalarial drugs
1. Symptom control: Chloroquine; 2. Cerebral malaria: Artemisinin, im.
Folate is synthesized from 3 basic building blocks, GTP, p-aminobenzoic acid (pABA), and glutamate, in a pathway involving 5 enzymes.
•DHPS dihydropteroate synthase;DHFR dihydrofolate reductase
1. Drugs controlling symptoms
Quinine (奎宁)
Anti-malarial activity :
• Kill the schizonts(裂殖体) in erythrocytic stage • A gametocide(杀配子体) for P. vivax(间日疟原虫) and P.
性疟) • Curing subtertian malaria(恶性疟); • Symptomatic prevention in epidemic area.
1. Drugs controlling symptoms
2. Treatment of amebiasis(阿米巴病): • treating systemic amebiasis(肠外阿米巴病), such
dizziness, tinnitus(耳鸣), dysphoria(烦躁), skin itching, and GI reaction. 2. In high dose, visual disturbance can occur 3. Quinidine-like effects 4. Teratogenesis
as amebic hepatitis(阿米巴肝炎) and amebic hepatic abscess(阿米巴肝脓肿).
3. Immunosuppression.
1. Drugs controlling symptoms
Adverse Reactions: 1. Be less in anti-malarial dose, occasionally
Life cycle of malarial parasite
Anti-malarial Drugs
1. Drugs controlling symptoms -Chloroquine (氯喹), quinine(奎宁), artemisinin (青蒿素)
2. Drugs controlling relapse and transmission -primaquine(伯氨喹)
美国拉斯克奖将2011年临床研究奖授予中国中医科学院终身研究员屠呦呦，以表彰 她发现了青蒿素。
1. Drugs controlling symptoms
Clinical uses: • Chloroquine-resistant subtertian malaria, and benign
malaria. – But its recurrence rate is high(30%).
(抗血吸虫病和抗丝虫病药) 4. Anthelmintic drugs (抗肠蠕虫药)
Anti-malarial Drugs
Malarial parasite (plasmodium, 疟原虫)
1. P.falciparum(恶性疟原虫) 2. P.vivax (间日疟原虫) 3. P.malariae(三日疟原虫) 4. P.ovale (卵形疟原虫)
malariae(三日疟原虫), but not for P. falciparum(恶性疟 原虫).
1. Drugs controlling symptoms
Clinical uses: • Treatment of the chloroquine- and
multidrug-resistant subtertian malaria (恶性 疟) and severe cerebral malaria(脑型疟).
3. Drugs for etiological prevention -primethamine(乙胺嘧啶)
1. Drugs controlling symptoms
Chloroquine (氯喹)
Anti-malarial activity:
• Kill the schizonts(裂殖体) in erythrocytic stage – The effects are fast and lasting. – The clinical symptoms will vanish after administration of chloroquine in 24-48 h, blood malarial parasites disappear in 48-72 h.
Anti-malarial activity: • Kill the schizonts(裂殖体) in erythrocytic
stage.
– The effects are faster than that of chloroquine, and effective to chloroquine-resistant subtertian malaria, especially to cerebral malaria.
Clinical uses: 1. Treating benign malaria radically, at
combination with chloroquine； 2. Preventing transmission of subtertian
malaria.
2. Drugs controlling relapse and transmission
Quinine dihydrochloride, iv 3. Chloroquine-resistant subtertian malaria:
Quinine, Artemisinin. 4. Resting stage: Pyrimethamine+ Primaquine 5. Prevent transmission: Pyrimethamine 6. Combined administration: Chloroquine+ Primaquine
hypotension, arrhythmias 3. Idiosyncrasy(特异质反应) : acute hemolytic
reaction. 4. Stimulating womb(兴奋子宫): abortion
1. Drugs controlling symptoms
Artemisinin (青蒿素)
ne(乙胺嘧啶)
Anti-malarial activity: 1. Killing schizonts(裂殖体) of subtertian
malarial parasites and benign malarial parasites in exo-erythrocytic stage; 2. Killing immature schizonts of erythrocytic stage.
1. Drugs controlling symptoms
Adverse reactions: 1. Cinchonism(金鸡纳反应): tinnitus(耳鸣),
headache, nausea, disturbed vision, etc. 2. Myocardial depression(心肌抑制作用):
PHARMACOLOGY
Anti-parasitic drugs
Contents
1. Anti-malarial drugs (抗疟药) 2. Anti-amebiasis and anti-trichomoniasis drugs
(抗阿米巴病和抗滴虫病药) 3. Anti-schistosomiasis and anti-filariasis drugs
Chloroquine (CQ) accumulates in the food vacuole of the parasite.
1. Drugs controlling symptoms
Clinical Uses: 1. Treatment of malaria: • Controlling the symptoms of benign malaria(良
3. Drugs for etiological prevention
Clinical uses: prevent malaria
Adverse reactions:
• Administration in large dose or in long time, megaloblastic anemia (巨红细胞贫血) can occur→ treated with formyl tetrahydrofolic acid(甲酰四氢叶酸).