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蚊子是全球最致命的動物,蚊媒疾病每年在全球導致數十萬人死亡。[1] 2015諾貝爾醫學獎3得主 對抗寄生蟲病有成

此類藥品的困難點在於寄生蟲人類一樣是真核生物,所以比起原核生物細菌較難找到有選擇性的藥品。

        課本說其實得寄生蟲病的人很多,但是藥廠的藥都往已開發國家的疾病為主。


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classification(分類[]

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Antiprotozoal drugs(抗原蟲藥[]

antimalaria(抗瘧藥: 治療瘧疾 的藥品。[]

2015NEJS抗瘧藥機轉圖

4-substituted quinolines=rapidly blood schizonticide[]
  • quinoline-4-menthanols(= methanoloquinolines)
    • 有quinoline
      • 天然生物鹼:quinine(奎寧:(+) isomer
      • 合成:mefloquine
    • 沒quinoline: 9-phenanthrene methanol
      • halofantrine—(M)→Desbutylhalofantrine(active)
      • —(似)→lumefantrine
  • 4-aminoquinolines
8-aminoquinolines=tissue schizonticide[]
  • pamaquine
  • primaquine
  • pentaquine
ubiquinone reductase inhibitor[]

atovaquone

Antifolate drug[]
2015諾貝爾醫學獎中國大陸的屠呦呦 Artemisinin(Qinghason) and its der.: often in combination therapy, often liposoluble except for one[]
  • 賽諾菲集團(Sanofi)和諾華集團(Novartis)的青蒿素藥物則是抗瘧利器。
  • active constituent of sweetworm wood(Artemisia annua)
  • liposoluble
  • water-soluble:Artesunate hemisuccinate salt
antibiotics[]
  • tetracycline
  • doxycycline
  • clindamycin

treatment of Amebiasis/Giardiasis/Trichomonias(阿米巴變形蟲/梨形蟲/滴蟲的治療[]

  • nitroimidazole
    • metronidazole first,
    • if resistence occurs, use tinidazole

giardiasis-associated diarrhea in children (age 1~11 years) or diarrhea caused by crytosporidiosis (protozoal infection caused by Crysporidium parvum) in patient with AIDS.[]

  • nitazoxanide(NTZ)—(M)→tazoxanide(TIZ): orphan drug, giardiasis-associated diarrhea in children (age 1~11 years) or diarrhea caused by crytosporidiosis (protozoal infection caused by Crysporidium parvum) in patient with AIDS.

treatment of Amebiasis(阿米巴變形蟲的治療[]

asymptomatic amebiasis[]
  • Diloxanide furoate: iodoquinol的替代物
treatment of intestinal Amebiasis(抗腸阿米巴變形蟲[]
  • iodoquinolDiloxanide furoate
    • 8-hydroxyquinoline der.
      • iodoquinol
      • iodochlorohydroxyquine
    • Diloxanide furoate(prodrug)→Diloxanide: iodoquinol的替代物
  • As der.
    • carbarsone(苯砷酸脲(卡巴宗
    • Acetarsol(乙醯胂酚
    • glycobiarsol
  • antibiotics
treatment of extraintestinal Amebiasis(抗肝阿米巴變形蟲[]
  • chloroquine(氯喹
treatment of intestinal and extraintestinal Amebiasis(抗腸阿米巴變形蟲和肝阿米巴變形蟲[]
  • emetine(吐根鹼dehydroemetine(Mebadin): faster elimination, thus less toxic
  • metronidazole first,
  • if resistence occurs, use tinidazole

treatment of Pneumocystis(卡氏肺囊蟲肺炎的治療[]

  • first-line:SMX-TMP: prophylaxis and treatment of of Pneumocystis in patients with AIDS
  • second-line:pentamidine: IV
  • trimetrexate(TMQ)
  • atovaquone
  • primaquine + clindamycin treat moderate to moderately severe Pneumocystis

treatment of Toxoplasmosis(弓漿蟲的治療[]

  • 2014研究:atypical neurleptics治療精神病的機轉可能和對Toxoplasmosis弓漿蟲感染的抑制效果有關。弓漿蟲與思覺失調症有關 bioforum.tw/modules/tadnews/index.php?nsn=2811
  • first-line:SMX-TMP
  • second-line:pentamidine
  • antifolate: pyrimithamine+sulfadiazine treat acute toxoplasmosis
  • antifolate: pyrimithamine+clindamycin treat AIDS-related toxoplasmosis of the brain

treatment of Trypanosomiasis(錐蟲病的治療[]

Trypanosoma brucei rhodesiense ( east African sleeping sickness )[]
  • suramin Sod. : early stage. bis-hexasulfonatednaphthylurea, non-CNS-associated African Trypanosomiasis (early stage of the disease)
  • pentamidine isethionate : early stage.
  • melasoprol: late stage
Trypanosoma brucei gambiense (west African sleeping sickness)[]
  • no suramin Sod. : bis-hexasulfonatednaphthylurea, non-CNS-associated African Trypanosomiasis (early stage of the disease)
  • no pentamidine isethionate
  • eflornithine: early stage and late stage
  • melasoprol: late stage
Trypanosoma cruzi ( American Trypanosomiasis = Chagas' disease ): 促使身體分泌的抗體會攻擊2nd extracellular loop of cardiac M2 muscarinic receptor造成 allosteric modulator而產生作用,所以用atropine治療[]
  • no suramin Sod.
  • no pentamidine isethionate
  • Nifurtimox
  • Benznidazole

treatment of Leishmaniasis(利什曼原蟲的治療[]

  • Sod. stibogluconate:五價Sb

antihelmintic drugs(抗蠕蟲藥[]

成藥基準表甲類成藥(五)驅蟲劑:蛔蟲、蟯蟲、十二脂腸蟲、絛蟲之驅除。[]

  • 海人酸(Kainic Acid)
  • 山道年(Santonin)
  • 二乙烯二胺(Piperazine)
  • 海人草(Digenea)
  • 使君子(Combretaceae)
  • 石榴皮(Granatum)

drugs to nematodes(抗線蟲藥、抗圓蟲藥(Aschelminth)(nematodes)(roundworms)[]

Intestinal nematodes(腸內線蟲[]
  • round worm/hook worm/pin worm
    • round worm(蛔蟲
    • hook worm(鉤蟲
    • pin worm(蟯蟲(threadworm)
  • whipworm(鞭蟲
  • benzimidazoles:廣效抗寄生蟲藥,可以同時對付多種Intestinal nematodes(腸內線蟲
    • mebendazole
    • tiabendazole
    • albenadazole
  • niridazole
  • levamisole
  • bithionol
  • metrifonate
  • oxamniquine
  • tetrachloroethylene:hook worm(鉤蟲
  • arecoline檳榔鹼: 促進cholinergic activity而使蟲體痙攣, round worm(蛔蟲
  • pyrantel pamoate: treat round worm(蛔蟲、hook worm(鉤蟲、pin worm(蟯蟲(threadworm), 促進cholinergic activity而使蟲體痙攣
  • pyrvinium pamoate: 在體內因為類似ACh而因為抗膽鹼使蟲體麻痺
  • piperazine: 在體內因為類似ACh而因為抗膽鹼使蟲體麻痺, round worm(蛔蟲
tissue nematodes(組織內線蟲:(血)絲蟲[]
  • ivermectin: 促進GABA Cl-通道的傳導而使蟲體麻痺。2015年諾貝爾醫學獎愛爾蘭的康貝爾(William C. Campbell)和日本的大村智(Satoshi Omura)研究來自土壤細菌的化合物後,從而發現藥物阿維菌素avermectin )。河盲症淋巴絲蟲病(又名象皮病)現已接近根除。默克藥廠(Merck & Co)生產阿維菌素的衍生物伊維菌素(Ivermectin)在全世界被用來對抗蛔蟲寄生。
  • diethylcarbamazine

drugs to platyhelminth抗扁蟲門藥(flatworms):antihelmintic drugs抗蠕蟲藥中的praziquantel(PZQ)是窄效,只對platyhelminth(扁蟲門有效[]

Trematode(flukes or schistosomes)(血吸蟲[]
  • praziquantel(PZQ)
Cestode(tapeworms)(絛蟲[]
  • praziquantel(PZQ)
  • niclosamide—(-)→mitochondrion的氧化功能
  • pelletierine石榴鹼(l): from Punicaceae Punica granatum
  • arecoline檳榔鹼:因其所具有的cholinergic direct agonist activity 使得蟲體肌肉因為收縮而麻痹因而被排出體外

常用中藥[]

  • 驅蟲:檳榔種子(Arecae Semen)-生物鹼 (Alkaloids)

drugs for parasites of cells(some antibacterials and antiviral agents)[]

重點[]

antihelmintic drugs(抗蠕蟲藥[]

成藥基準表甲類成藥(五)驅蟲劑:蛔蟲、蟯蟲、十二脂腸蟲、絛蟲之驅除。[]

  • 海人酸(Kainic Acid)
  • 山道年(Santonin)
  • 二乙烯二胺(Piperazine)
  • 海人草(Digenea)
  • 使君子(Combretaceae)
  • 石榴皮(Granatum)

drugs to nematodes(抗線蟲藥、抗圓蟲藥(Aschelminth)(nematocles)(roundworms)[]

Intestinal nematodes(腸內線蟲[]
  • benzimidazoles:廣效抗寄生蟲藥,可以同時對付多種Intestinal nematodes(腸內線蟲
    • mebendazole
    • tiabendazole
    • albenadazole
  • niridazole

drugs to platyhelminth(抗扁蟲門藥(flatworms):antihelmintic drugs(抗蠕蟲藥中的praziquantel(PZQ)是窄效,只對platyhelminth(扁蟲門有效[]

常用中藥[]

  • 驅蟲:檳榔種子(Arecae Semen)-生物鹼 (Alkaloids)

drugs for parasites of cells(antiviral agents)[]

see Antiviral agents抗病毒藥物

reference[]

延伸學習[]

Parasite

電視上常見的parasite-米奇

20180927-044134 U3792 M456708 99b6

extraterrestrial parasite will make you a Venom.

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