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 (C)</p> Signup and view all the answers

How does amodiaquine contribute to parasite death?

<p>Prevents haemozoin formation (B)</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 (C)</p> Signup and view all the answers

How do sulphonamides act as antimalarials?

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

What is the mechanism of action of pyrimethamine?

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

Which component of Fansidar acts as a folic acid inhibitor?

<p>Sulphadoxine (C)</p> Signup and view all the answers

What enzyme do sulphonamides competitively inhibit?

<p>Dihydropteroate synthetase (C)</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 (D)</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 (B)</p> Signup and view all the answers

What is the role of DHFR inhibitors in antimalarial activity?

<p>Selective inhibition of DHFR (B)</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 (A)</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 (C)</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 (D)</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 (C)</p> Signup and view all the answers

Where is the use of Artemisinin derivatives restricted?

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

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