Clinical Use of Sulphonamides as Antimalarials

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What is the mechanism of action of amodiaquine?

Inhibition of haemozoin formation

What differentiates amodiaquine from other 4-aminoquinolines?

Gametocytocidal effect on P.vivax and P.falciparum gametocytes

How does mefloquine exert its anti-malarial effect?

Interference with host-parasite metabolite transport

What is the role of haemozoin in the malaria parasite?

Converts toxic haem to harmless substance

How does amodiaquine contribute to parasite death?

Prevents haemozoin formation

What makes amodiaquine particularly advantageous in treating malaria?

Gametocytocidal effect against P.vivax and P.falciparum gametocytes

How do sulphonamides act as antimalarials?

By competitively inhibiting dihydropteroate synthetase

What is the mechanism of action of pyrimethamine?

Inhibits dihydrofolate reductase

Which component of Fansidar acts as a folic acid inhibitor?

Sulphadoxine

What enzyme do sulphonamides competitively inhibit?

Dihydropteroate synthetase

How do sulphonamides contribute to the death of parasites?

By interfering with the incorporation of PABA into dihydropteroic acid

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

Fansidar

What is the role of DHFR inhibitors in antimalarial activity?

Selective inhibition of DHFR

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

Addition of a 6-methyl group

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

Chlorproguanil

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

Phenyl group in 5-position, alkyl group in 6-position

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

Trimethoprim

Where is the use of Artemisinin derivatives restricted?

To countries facing chloroquine resistance issues

Explore the clinical use of medium and long-acting sulphonamides as antimalarials, including examples like Sulphadiazine and Sulphadoxine. Learn about their mechanism of action, particularly how they competitively inhibit dihydropteroate synthetase enzyme.

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