1. AFSAR FATHIMA
M.Pharm

2. DEFINITION:
Malaria is a mosquito-borne infectious disease of humans and other animals caused by parasitic protozoan's.

3. Species of malaria
Plasmodium vivax
Plasmodium ovale
Plasmodium falciparum
Plasmodium malariae
Plasmodium knowlesi

5. LIFE CYCLE OF MALARIA

7. DIAGNOSIS OF MALARIA

9. Classification of anti-malarial drugs

10. Therapeutic classification
Chemical classification

11. Therapeutic classification
Causal prophylaxis: (Primary tissue schizonticides)
Destroy parasite in liver cells and prevent invasion of erythrocytes
Primaquine, proguanil
Supressives Prophylaxis:
Supress the erythrocytic phase and thus attack of malarial fever can be used as prophylactics
Chloroquine, proguanil, mefloquine, doxycycline
Clinical cure: erythrocytic schizonticides
used to terminate an episode of malarial fever

12. Fast acting high efficacy :
Chloroquine, quinine, mefloquine, atovaquone, artemisinin
Slow acting low efficacy drugs:
Proguanil, pyrimethamine, sulfonamides, tetracyclines

13. Therapeutic classification
Radical curatives: Eradicate all forms of P.vivax & P.ovale from the body.
Suppressive drugs + hypnozoitocidal drugs For vivax: Primaquine 15 mg daily for 14 days
Gametocidal: Destroy gametocytes and prevent transmission
Primaquine, artemisinin – against all plasmodia
Chloroquine, quinine – Pl Vivax
Proguanil, pyrimethamine – prevent development of sporozoites

14. Chemical classification
4 aminoquinolines:
Chloroquine, Hydroxychloroquine, Amodiaquine, Pyronaridine
8 aminoquinolines:
Primaquine, Tafenoquine, Bulaquine
Cinchona alkaloids:
Quinine, Quinidine
Quinoline methanol:
Mefloquine
Biguanides:
Proguanil, Chlorproguanil

15. Sesquiterpene lactones:
Diaminopyrimidines:
Pyrimethamine
Sulfonamides:
Sulfadoxine, dapsone
Tetracycline's:
tetracycline, doxycycline
Naphthoquinone:
Atovaquone
Sesquiterpene lactones:
Artesunate, artemether, arteether

16. Chloroquine Hemoglobin Globin utilized by malarial parasite
Heme (highly toxic for malaria parasite)
Chloroquine , Quinine,
mefloquine (-)
Hemozoin (Not toxic to plasmodium)

17. Pharmacokinetics: Well absorbed, 60 % protein bound, Concentrated in liver , spleen, kidney, lungs , leucocytes .Selective accumulation in retina: ocular toxicity.
Adverse drug reactions: Nausea, vomiting, anorexia, skin rashes, angioneurotic edema, photosensitivity, pigmentation, exfoliative dermatititis
Therapeutic uses: Hepatic amoebiasis, Giardiasis, Clonorchis sinensis Rheumatoid
arthritis, Discoid Lupus Erythematosus, Control manifestation of lepra reaction, Infectious mononucleosis.
Hydroxy chloroquine: Less toxic, properties &uses similar
Amodiaquine: As effective as chloroquine, Chloroquine resistant strains may be effective
Adverse events: GIT, headache , photosensitivity, rarely agranulocytosis
Pyronaridine: effective in resistant cases

18. Quinine: In 1820 Pelletier & caventou isolated quinine from cinchona bark.
Erythrocytic forms of all malarial parasites including resistant falciparum strains Gametocidal for vivax & malariae.
Adverse effects: Cinchonism, Tinnitus, nausea & vomiting. Headache mental confusion, vertigo, difficulty in hearing & visual disturbances Diarrhoea , flushing, respiratory depression , cyanosis.
Primaquine:
Primaquine
Converted to electrophiles
Generates reactive oxygen species

19. Adverse effects: epigastric distress, abdominal cramps, mild anemia, methaemoglobinemia, cyanosis, hemolytic anemia in G6PD deficiency .
Tafenoquine: More active slowly metabolized analog of primaquine, has advantage that it can be given on weekly basis.
Bulaquine: Partly metabolized to primaquine , Better tolerated in G6PD deficiency .