Antimalarial Drugs: 8-Aminoquinolines and Primaquine SAR
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Questions and Answers

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

  • Causes fragmentation of the parasite's RNA and intercalates in its DNA (correct)
  • Interferes with the transport of sporozoites
  • Inhibits the transport of haemoglobin and other products of metabolism
  • Inhibits the conversion of haem to haemozoin

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

  • P. vivax
  • P. malariae
  • P. ovale
  • P. falciparum (correct)

How does mefloquine act against Plasmodium parasites?

  • Binds to hemozoin, making a toxic complex for the parasite (correct)
  • Causes fragmentation of the parasite's RNA
  • Inhibits the conversion of haemoglobin to haemozoin
  • Interferes with the parasite's DNA replication

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

<p>Active against intrahepatic forms (B)</p> Signup and view all the answers

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

<p>It builds up and kills the parasite by membranolytic action (C)</p> Signup and view all the answers

How does amodiaquine concentrate in the parasite's lysosome?

<p>Through a host-specific drug-concentrating mechanism (C)</p> Signup and view all the answers

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

<p>-Br group on the quinoline ring (A)</p> Signup and view all the answers

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

<p>-Quinoline methanols (A)</p> Signup and view all the answers

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

<p>To treat uncomplicated malaria effectively (B)</p> Signup and view all the answers

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

<p>Inhibition of hemozoin polymerase enzyme (B)</p> Signup and view all the answers

Flashcards

Amodiaquine's mechanism vs Plasmodium

Amodiaquine fragments Plasmodium RNA and intercalates into its DNA.

Amodiaquine, erythrocytic stage

Effective against P. falciparum at the erythrocytic stage.

Mefloquine's mechanism

Mefloquine binds to hemozoin, creating a toxic complex for the parasite.

Amodiaquine's non-effect

Not active against intrahepatic forms of malaria.

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Amodiaquine and haem

Amodiaquine causes haem buildup, leading to membranolytic action, killing the parasite.

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Amodiaquine lysosome concentration

Amodiaquine concentrates in the parasite's lysosome by a host-specific mechanism.

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Quinoline ring, anti-malarial reduction

Adding a bromine group to the quinoline ring reduces anti-malarial activity.

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Mefloquine compound type

Mefloquine is a quinoline methanol.

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Amodiaquine combination therapy

Used in combination with artemisinin derivatives to effectively treat uncomplicated malaria.

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Amodiaquine's schizontocidal speed

Amodiaquine's rapid schizontocidal effect is primarily due to inhibition of hemozoin polymerizing enzyme.

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