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Antimalarial drugs

Diploma in Pharmacy

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  • These are the drugs used for the treatment of malaria.
  • Malaria is a tropical life threatening disease caused by a member of protozoan genus Plasmodium.
  • Plasmodium species that cause malaria are:
    • Plasmodium vivax
    • Plasmodium ovale
    • Plasmodium malarie
    • Plasmodium falciparum

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Classification

  • Cinchona alkaloids:
    • Quinine, Quinidine
  • 4-aminoquinoline:
    • Chloroquine
  • 8-aminoquinoline:
    • Primaquine
  • Quinoline methanol:
    • Mefloquine, Halofantrine, Lumefantrine
  • Artemisin derivatives:
    • Artesunate, Artemether
  • Antifolates:
    • Diaminopyridine (pyrimethamine), biguanide (proguanil), sulphonamide (sulfadoxine)

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Chloroquine

  • Chemistry
    • It is a 4-aminoquinoline derivative.
    • Chloro group is present at position 7.
    • 4-diethyl amino, 1 methyl butyl amino group is attached at position 4 of quinoline ring.

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  • Physical properties
    • It is available as Chloroquine phosphate or sulfate.
    • Chloroquine sulfate is freely soluble in water and very slightly soluble in ethanol.
    • Chloroquine is very slightly soluble in water, soluble in most organic solvents.
    • It occurs as white or almost white crystalline powder.
    • It occurs as two polymorphs differing in their behavior. One of which melts at 195°C and the other melts at 218°C.
    • It is sensitive to light. It gets discolored on exposure to light.

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  • Stability/Storage
    • Store protected from light.

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  • Uses
    • Malaria (active against erythrocytic forms of P. vivax and P. malariae and most strains of P. falciparum)
    • Extraintestinal amoebiasis
    • Glioblastoma (aggressive cancer that begins in cells called astrocytes)
    • Porphyria cutanea ( rare disorder characterized by painful, blistering skin lesions that develop on sun-exposed skin (photosensitivity)

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Mefloquine

Chemistry:

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  • Derivative of quinoline.
  • Trifluoromethyl group attached at position 2 and 8
  • 2-piperidyl, hydroxy methyl group is attached at position 4.

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Physical properties

  • Exists as white colored powder.
  • Very slightly soluble in water. Freely soluble in methanol; soluble in ethanol, ethyl acetate.
  • Sensitive to high exposure of light, moisture and high temperature.
  • Melting point: 174-176 °C

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Stability and storage

  • Preserve in tight, light-resistant containers. Store between 15 and 30.

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Uses

  • Acute malarial infections
  • Malaria prevention