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Learn about the life cycle, diagnosis, and treatment of malaria, including therapeutic and chemical classifications, drug options, adverse reactions, and therapeutic uses. Understand the pharmacokinetics and adverse effects of commonly used anti-malarial drugs.
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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 .