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Malaria
Protozoal disease
Plasmodium
infected female anopheles mosquito
WHO estimates
300-500 million cases year
> 1 million death
5
Classification of Anti Malarial Agents: 1
Chemical Structure
4-Aminoquinolines : Chloroquine, Amodiaquine
6
Life Cycle of the Malarial Parasite
Antimalarial Therapy
Causal prophylaxis
Suppressive prophylaxis
Clinical cure
Radical cure
Gametocidal
Classification- Stage of Parasite affected
Stage Drugs
Blood schizonticidal drugs Erythrocytic phase Chloroquine,
Terminates clinical illness Artemissin,
Quinine,
Atovaquone,
Oral administration.
Visual Disturbances
abnormalities.
Black water fever
rare severe illness
marked hemolysis ,
hemoglobinuria
Proguanil & Pyrimethamine
Proguanil is cyclized in the body to a triazine
derivative(cycloguanil) which inhibits
plasmodial DHFRase.
Half life: 16-20hr
Pyrimethamine is a directly acting inhibitor of
plasmodium DHFRase.
High affinity for plasmodial enzyme(-2000 times
greater than for the mammalian enzyme)
Proguanil and Pyrimethamine
Sulfonamide-Pyrimethamine Combination
Analogs are:
Artesunate (water-soluble; oral, IM, IV and rectally),