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Chapter 6 : Quinine to Mefloquine

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Quinine to Mefloquine, Page 1 of 2

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Abstract:

Malaria parasites have been toughened by decades of exposure to antimalarial drugs-conditions that promote their survival and resistance to the assault by “magic bullets.” Unlike malaria during the Korean War (1950-1953), the prevalent parasite in Vietnam was not but the deadly , and worse still, it was drug-resistant. In tests with malaria-infected mice, seven of the new quinoline methanols were found to be effective against parasites resistant to chloroquine; at an effective dose of 10 mg/kg, some were 8 times better than chloroquine and 64 times better than quinine. Twelve specially selected 4-quinoline methanols were tested with chloroquine-resistant and chloroquine-sensitive , and five were found to be at least as active as chloroquine against chloroquine-sensitive strains and equally effective against strains resistant to chloroquine, quinine, and pyrimethamine. The absence of cross-resistance to chloroquine by mefloquine was demonstrated in field studies as well as in an in vitro, quantitative, semi-automated micromethod that measured the uptake and incorporation of radioactive tracer. Mefloquine and quinine are both lipophilic ("lipid loving") and bind tightly to serum and high-density lipoproteins; this may facilitate entry into the parasite.

Citation: Sherman I. 2011. Quinine to Mefloquine, p 137-149. In Magic Bullets to Conquer Malaria. ASM Press, Washington, DC. doi: 10.1128/9781555816889.ch6

Key Concept Ranking

Long-Acting Sulfonamides
0.50860834
Amino Alcohols
0.46211445
Malaria
0.43221948
0.50860834
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Figures

Image of Figure 1
Figure 1

Structures of sulfadoxine, dapsone, pyrimethamine, and sulfanilamide.

Citation: Sherman I. 2011. Quinine to Mefloquine, p 137-149. In Magic Bullets to Conquer Malaria. ASM Press, Washington, DC. doi: 10.1128/9781555816889.ch6
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Image of Figure 2
Figure 2

Structures of quinine, SN-10275, WR-30090, and mefloquine.

Citation: Sherman I. 2011. Quinine to Mefloquine, p 137-149. In Magic Bullets to Conquer Malaria. ASM Press, Washington, DC. doi: 10.1128/9781555816889.ch6
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References

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