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Part-2: Anti-protozoal Agents

Protozoal infections: Amoebiasis, Giardiasis, Trichomonas, Trypanosomiasis, Leishmaniasis

These infections are transmitted by insect vectors or directly from other mammalians.

Protozoa multiply rapidly in hosts because:

 Unavailability of effective vaccines.


 Chemotherapy is only practical way to treat infected part & reduce transmission.

Classification of Anti-protozoal agents

 Chemical Classification (Main)

Anti-protozoal Agents

Nitro-
Miscellaneous
imidazoles

Pentamidine
Metronidazole Tinidazole Ornidazole Iodoquinol Diloxanide Atovaquone Eflornithine
isethionate

MOA of Nitro-imidazoles: Broad spectrum bactericidal drugs activated by reduction of nitro group to
anion radical  this highly reactive radical forms adjuncts with protein & DNA leading to strand
breakage  loss of function  cell death.

MOA of Iodoquinol & Diloxanide: Destroy trophozoites of E. histolytica

MOA of Pentamidine isethionate: Interferes with DNA replication & its function

MOA of Atovaquone & Eflornithine: Decrease pyrimidine synthesis, preventing DNA synthesis 
protozoal death by blocking mitochondrial electron transport complex-III of respiratory chain of
protozoa.

Anti-protozoal
Agents

Luminal amoebicide
Tissue amoebicide (Agents that treat asymptomatic
(Agents that destroy amoeba having tissue) or mild intestinal form so
amoebiasis

Pentamidine
Metronidazole Tinidazole Ornidazole Iodoquinol Diloxanide Atovaquone Eflornithine
isethionate
Atovaquone

Eflornithine

Diloxanide

Iodoquinol
Pentamidine isethionate

Synthesis of Metronidazole

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