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Antimalarials
• Malaria is also known as ague fever, Periodic fever or Paludism, it is a communicable
mosquito borne disease caused by the protozoan parasite belonging to the genus
plasmodium.
• Out of the hundred species of plasmodium available only four are known to show
devasting effects on human beings.
• The three species of plasmodium that cause mild malaria include p.vivax,p.ovale,and
plasmodium malariae.
• They cause malaria by destructing the red blood cells present in the peripheral capillaries.
• The most complicated species of plasmodium that might even lead to death of an
individual is plasmodium falciparum.
• These species infect red blood cells and makes them sticky , there by arrest the
circulation.
• These parasites undergo asexual phase in man and sexual phase in female anaopheles
mosquito, whose bites infect man and transmits malaria.
Life cycle of malaria parasite
Classification of antimalarials
1. Chinchona Alkaloids
2. 4-Amino quinolines
3. 8-Amino quinolines
4. 9-Amino Acridine
5. Biguanides
6. Pyrimidine analogues
7. Polycyclics
8. Miscellaneous
9. Newer antimalarial agents
10.Combination
Anti malarials are divided in to 10 types
Site of antimalarial agents
Actually there are four sites for drug therapy for anti malarial agents
• Kill the sporozoites injected by the mosquito
• Kill the schizonts present in the hepatocytes or prevent them to form merozoites
Eg: Quinine, Chloroquine, Amodoquine, Pyremethamine
• Kill the merozoites in the blood or prevent them from developing in to gametocytes
Eg: Chloroquine, Amodoquine.
• Kill the gametocytes before they enter in to the mosquito and reproduce in to zygote
Eg: Primaquine
1. Kill the sporozoites injected by the mosquito
2. Kill the schizonts present in the hepatocytes or prevent them to form merozoites
Eg: Quinine, Chloroquine, Amodoquine, Pyremethamine
3. Kill the merozoites in the blood or prevent them from developing in to gametocytes
Eg: Chloroquine, Amodoquine.
4. Kill the gametocytes before they enter in to the mosquito and reproduce in to zygote
Eg: Primaquine
Quinine
• It is a quinoline derivative
• What is quinoline : Quinoline is the fusion of two six membered rings.
One is benzene ring and the other one is Pyridine ring
• It also contains another ring called quinclidine
• What is meant by quiniclidine: It is a bicyclo amine ring or it is also called as 1-aza bicyclo octane
ring
• So quinine is having two rings one is Quinoline ring and the other is quiniclidine
ring
• These both the rings are connected with hydroxy methyl group
• In the case of quinoline ring it is having
methoxy group at 6th position
• In the case of Quinuclidine ring there is
a vinyl group at 5th position
• What is meant by vinyl it means CH=CH2
Or it is also called as ethenyl.
• It is called as 4-quinoline methanol
derivative.(At 4th position methanol is
attached )
• So it is available as salt of
• HCl
• Dihydrochloride
• Sulphate
• Bisulphate
• Gluconate
Source of Quinine
 Quinine is an alkaloid and it is obtained from the bark of Chinchona
From this cinchona we are getting 4 alkaloids they are
• Quinine
• Quinidine
• Cinchonine
• Cinchonidine
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C0-2.pptx

  • 2. • Malaria is also known as ague fever, Periodic fever or Paludism, it is a communicable mosquito borne disease caused by the protozoan parasite belonging to the genus plasmodium. • Out of the hundred species of plasmodium available only four are known to show devasting effects on human beings. • The three species of plasmodium that cause mild malaria include p.vivax,p.ovale,and plasmodium malariae. • They cause malaria by destructing the red blood cells present in the peripheral capillaries.
  • 3. • The most complicated species of plasmodium that might even lead to death of an individual is plasmodium falciparum. • These species infect red blood cells and makes them sticky , there by arrest the circulation. • These parasites undergo asexual phase in man and sexual phase in female anaopheles mosquito, whose bites infect man and transmits malaria.
  • 4.
  • 5. Life cycle of malaria parasite
  • 6.
  • 7.
  • 8.
  • 9.
  • 10.
  • 11.
  • 12.
  • 13.
  • 14.
  • 16. 1. Chinchona Alkaloids 2. 4-Amino quinolines 3. 8-Amino quinolines 4. 9-Amino Acridine 5. Biguanides 6. Pyrimidine analogues 7. Polycyclics 8. Miscellaneous 9. Newer antimalarial agents 10.Combination Anti malarials are divided in to 10 types
  • 17. Site of antimalarial agents Actually there are four sites for drug therapy for anti malarial agents • Kill the sporozoites injected by the mosquito • Kill the schizonts present in the hepatocytes or prevent them to form merozoites Eg: Quinine, Chloroquine, Amodoquine, Pyremethamine • Kill the merozoites in the blood or prevent them from developing in to gametocytes Eg: Chloroquine, Amodoquine. • Kill the gametocytes before they enter in to the mosquito and reproduce in to zygote Eg: Primaquine
  • 18. 1. Kill the sporozoites injected by the mosquito
  • 19. 2. Kill the schizonts present in the hepatocytes or prevent them to form merozoites Eg: Quinine, Chloroquine, Amodoquine, Pyremethamine
  • 20. 3. Kill the merozoites in the blood or prevent them from developing in to gametocytes Eg: Chloroquine, Amodoquine.
  • 21. 4. Kill the gametocytes before they enter in to the mosquito and reproduce in to zygote Eg: Primaquine
  • 22. Quinine • It is a quinoline derivative • What is quinoline : Quinoline is the fusion of two six membered rings. One is benzene ring and the other one is Pyridine ring
  • 23. • It also contains another ring called quinclidine • What is meant by quiniclidine: It is a bicyclo amine ring or it is also called as 1-aza bicyclo octane ring
  • 24. • So quinine is having two rings one is Quinoline ring and the other is quiniclidine ring • These both the rings are connected with hydroxy methyl group
  • 25. • In the case of quinoline ring it is having methoxy group at 6th position • In the case of Quinuclidine ring there is a vinyl group at 5th position • What is meant by vinyl it means CH=CH2 Or it is also called as ethenyl. • It is called as 4-quinoline methanol derivative.(At 4th position methanol is attached ) • So it is available as salt of • HCl • Dihydrochloride • Sulphate • Bisulphate • Gluconate
  • 26. Source of Quinine  Quinine is an alkaloid and it is obtained from the bark of Chinchona From this cinchona we are getting 4 alkaloids they are • Quinine • Quinidine • Cinchonine • Cinchonidine