Antiparasitics Flashcards
Most common and severe form of malaria
Falciparum malaria
Milder form of malaria that can remain dormant in liver and relapse
Vivax malaria
Drugs for malaria prophylaxis
Chloroquine
Primaquine
Drugs for treatment of active or latent malarial infection
Artemether/lumefantrine
Chloroquine
Primaquine
Blood stage antimalarials (produce clinical cure)
Chloroquine
Artemisinins
Liver stage antimalarials (produce radical cure of relapsing malaria)
Primaquine
____ stage antimalarials are ineffective against ____ stage parasites
Blood
Liver
Prophylactic drugs must be ____ effective, ____ half lives, and ____ toxicity
Orally effective
Long half-lives
Low toxicity
Chloroquine MOA
Inhibits biocrystallization of toxic hematin (product of hemoglobin digestion) by ion trapping of drug in parasite food vacuole
Clinical uses of chloroquine
Clinical cure and prophylaxis against sensitive strains (ineffective against most strains of P. falciparum in Africa, Asia, and S. America)
Can be used during pregnancy
Chloroquine adverse effects
Prophylactic doses- none
Curative doses- pruritus, headaches, CV toxicity
Artemether MOA
Unclear; may produce free radicals in presence of heme
Why is Artemether not useful for prophylaxis?
Short half-life (1-3 hr)
What drug is Artemether usually combined with?
Lumefantrine
Why is lumefantrine added to Artemether?
Has a long half life to sustain antimalarial activity so it’s more useful for prophylaxis