Clinical Use of Sulphonamides as Antimalarials
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Questions and Answers

What is the mechanism of action of amodiaquine?

  • Interference with the parasite's food vacuole transport system
  • Inhibition of haemozoin formation (correct)
  • Inhibition of DNA replication in the parasite
  • Disruption of sporozoite development

    • What differentiates amodiaquine from other 4-aminoquinolines?

  • Inhibition of intrahepatic forms of Plasmodium
  • Lack of schizontocidal activity
  • Increased toxicity but lower blood concentration
  • Gametocytocidal effect on P.vivax and P.falciparum gametocytes (correct)

    • How does mefloquine exert its anti-malarial effect?

  • Disruption of haemoglobin digestion in the parasite
  • Inhibition of DNA replication in the parasite
  • Inhibition of the parasite's RNA function
  • Interference with host-parasite metabolite transport (correct)

    • What is the role of haemozoin in the malaria parasite?

    <p>Converts toxic haem to harmless substance</p> Signup and view all the answers

    How does amodiaquine contribute to parasite death?

    <p>Prevents haemozoin formation</p> Signup and view all the answers

    What makes amodiaquine particularly advantageous in treating malaria?

    <p>Gametocytocidal effect against P.vivax and P.falciparum gametocytes</p> Signup and view all the answers

    How do sulphonamides act as antimalarials?

    <p>By competitively inhibiting dihydropteroate synthetase</p> Signup and view all the answers

    What is the mechanism of action of pyrimethamine?

    <p>Inhibits dihydrofolate reductase</p> Signup and view all the answers

    Which component of Fansidar acts as a folic acid inhibitor?

    <p>Sulphadoxine</p> Signup and view all the answers

    What enzyme do sulphonamides competitively inhibit?

    <p>Dihydropteroate synthetase</p> Signup and view all the answers

    How do sulphonamides contribute to the death of parasites?

    <p>By interfering with the incorporation of PABA into dihydropteroic acid</p> Signup and view all the answers

    Which other antimalarial agent is known to contain N' (5,6-dimethoxy-4-pyrimidinyl sulfanilamide) and 2,4-diamino-5-(p-chlorophenyl)-6-ethylpyrimidine?

    <p>Fansidar</p> Signup and view all the answers

    What is the role of DHFR inhibitors in antimalarial activity?

    <p>Selective inhibition of DHFR</p> Signup and view all the answers

    Which substitution on the quinoline nucleus tends to decrease both antimalarial activity and toxicity?

    <p>Addition of a 6-methyl group</p> Signup and view all the answers

    Which Biguanide has longer activity but becomes more toxic with a second chlorine at the meta position?

    <p>Chlorproguanil</p> Signup and view all the answers

    What type of substituent in the 5-position and the 6-position is required for the highest antimalarial activity in 2,4-diamino-pyrimidines?

    <p>Phenyl group in 5-position, alkyl group in 6-position</p> Signup and view all the answers

    Which compound started as an antibacterial agent but was later found to be active as an antimalarial?

    <p>Trimethoprim</p> Signup and view all the answers

    Where is the use of Artemisinin derivatives restricted?

    <p>To countries facing chloroquine resistance issues</p> Signup and view all the answers

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