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AFSAR FATHIMA M.Pharm. DEFINITION: Malaria is a mosquito-borne infectious disease of humans and other animals caused by parasitic protozoan's. Species of malaria Plasmodium vivax Plasmodium ovale Plasmodium falciparum Plasmodium malariae Plasmodium knowlesi. LIFE CYCLE OF MALARIA.
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AFSAR FATHIMA M.Pharm
DEFINITION: Malaria is a mosquito-borne infectious disease of humans and other animals caused by parasitic protozoan's.
Species of malaria • Plasmodium vivax • Plasmodium ovale • Plasmodium falciparum • Plasmodium malariae • Plasmodium knowlesi
Therapeutic classification • Chemical classification
Therapeutic classification • Causal prophylaxis: (Primary tissue schizonticides) • Destroy parasite in liver cells and prevent invasion of erythrocytes • Primaquine, proguanil • SupressivesProphylaxis: • 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
Fast acting high efficacy : • Chloroquine, quinine, mefloquine, atovaquone, artemisinin • Slow acting low efficacy drugs: • Proguanil, pyrimethamine, sulfonamides, tetracyclines
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
Chemical classification • 4 aminoquinolines: • Chloroquine, Hydroxychloroquine, Amodiaquine, Pyronaridine • 8 aminoquinolines: • Primaquine, Tafenoquine, Bulaquine • Cinchona alkaloids: • Quinine, Quinidine • Quinolinemethanol: • Mefloquine • Biguanides: • Proguanil, Chlorproguanil
Diaminopyrimidines: • Pyrimethamine • Sulfonamides: • Sulfadoxine, dapsone • Tetracycline's: • tetracycline, doxycycline • Naphthoquinone: • Atovaquone • Sesquiterpene lactones: • Artesunate, artemether, arteether
Chloroquine Hemoglobin Globin utilized by malarial parasite Heme (highly toxic for malaria parasite) • Chloroquine , Quinine, • mefloquine (-) • Hemozoin (Not toxic to plasmodium)
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, Clonorchissinensis Rheumatoid arthritis, Discoid Lupus Erythematosus, Control manifestation of leprareaction, 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
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:
Adverse effects: epigastricdistress, 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 .