Antimalarial Drugs Flashcards
What is cinchonism?
(cause by quinine or quinidine): h/a, vertigo, blurry vision, tinnitus, GI distress
MoA of Quinine?
complexes w/ double stranded DNA and prevents strand separation -> preventing DNA replication and mRNA synthesis
Mechanism of resistance to chloroquine?
decreased intracellular accumulation via increased activity of membrane pumps. resistance in falciparum can also result from decreased intravascular accumulation of chloroquine via a transporter encoded by pfert gene
Which antimalarial may cause folate deficiency?
pyrimethamine
Which antimalarial can cause Blackwater fever?
Quinine (it is a form of intravascular hemolysis that is a sometimes fatal adverse effect in quinine-sensitized people)
MoA of Primaquine?
quinolone-quinone metabolites, which are electron-transferring redox compounds acting as cellular oxidants
Adverse effects of mefloquine?
cardiac conduction defects, psychiatric problems, seizures and neurologic problems
Adverse effects of chloroquine?
peripheral neuropathy, retinal damage, auditory impairment, psychosis. skin lesions and mycardial depression
Mechonism of Artesunate?
metabolized in food vacuole to form free radicals
Malaria prophylaxis?
Chloroquine (weekly) where possible (but this isn’t much)… Mefloquine (weekly) in places where chloroquine resistance is present…… In places w/ multi-drug resistance, use either doxycycline or atovaquone-proguanil (Malarone)
Combo sulfadoxine/pyrimethamine?
sulfadoxine is an antimetabolite of PABA, pyrimethamine blocks dihydrofolate reductase. together they create sequential blockade
Don’t use which antimalarials in people w/ G6PD deficiency?
Primaquine, Quinidine