Antimalarial Drugs: 8-Aminoquinolines and Primaquine SAR

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10 Questions

What is the mechanism of action of amodiaquine against Plasmodium parasites?

Causes fragmentation of the parasite's RNA and intercalates in its DNA

Which Plasmodium species is amodiaquine effective against at the erythrocytic stage?

P. falciparum

How does mefloquine act against Plasmodium parasites?

Binds to hemozoin, making a toxic complex for the parasite

Which of the following is NOT a known effect of amodiaquine?

Active against intrahepatic forms

What happens to haem in the parasite due to amodiaquine activity?

It builds up and kills the parasite by membranolytic action

How does amodiaquine concentrate in the parasite's lysosome?

Through a host-specific drug-concentrating mechanism

Which group reduces anti-malarial activity when introduced on the quinoline nucleus?

-Br group on the quinoline ring

'Mefloquine (Lariam)' belongs to which group of compounds?

-Quinoline methanols

'Amodiaquine is used in combination with an artemisinin derivative' primarily for what reason?

To treat uncomplicated malaria effectively

What is the main reason for Amodiaquine's rapid schizontocidal effect?

Inhibition of hemozoin polymerase enzyme

Learn about 8-Aminoquinolines including examples like Primaquine and the structure-activity relationship (SAR) of Primaquine. Explore how different substitutions on the quinoline nucleus can affect antimalarial activity and toxicity.

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