Antiparistics Flashcards
Antimalarials
Chloroquine, primaquine, artemether
Prophylactic antimalarials
Chloroquine and primaquine
Treatment antimalarials
Artemether/lumefantrine
Chloroquine
Primaquine
Blood stage antimalarials
Chloroquine
Artemether
Liver stage antimalarials
Primaquine
3 characteristics of prophylactic agents
Low toxicity
Orally effective
Long half-life
Prophylaxis prevents what stage of malaria?
Blood stage
Chloroquine MOA
Weak base trapped in acidic parasite
Inhibits biocrystallization to increase heme concentration in food vacuole
Heme toxic to parasite
Chloroquine uses
Clinical cure & Prophylaxis against sensitive strains
Is chloroquine safe for pregnancy?
Yes
Chloroquine side effects
CV toxicity
Chloroquine resistance due to…
Mutated vacuole efflux transporter (PfRCT)
Chloroquine does not work for…
P. Falciparum in Asia, Africa, S. America
Artemether MOA
Maybe converted to toxic free radicals by heme
Artemether Uses
Fixed dose w/ lumefantrine
Oral drug for MDR falciparum
Artesunate (IV)
Artemether side effects
Neurotoxicity & embryotoxicity
Artemether PK (when not w/ lumefantrine)
Absorbed from GI tract —> short half-life
Does NOT work as prophylactic
Artemether Fun Fact
Inactive counterfeit to mimic drug
Liver Antimalarial
Primaquine
Primaquine MOA
Unknown
Primaquine Uses
Clinical & radical cure of vivax/ovale (take w/ chloroquine)
Terminal prophylaxis for vivax/ovale regions
Primary prophylaxis if other drugs inappropriate
Primaquine side effects
Mild cyanosis in normal G6PD
Hemolytic anemia in G6PD deficiency
Primaquine contraindications
G6PD deficiency
Pregnancy