Week 3: Antimalarial drugs Flashcards
What are the three main species of Malaria?
Plasmodium flaciparum, P. vivax, P. ovale
What are the most persistent hepatic forms of malaria?
P. vivax and P. ovale
What is the most extreme form of malaria?
P. falciparum
What drug targets and kills the hepatic form?
primaquine
What forms readily become resistant to malaria?
P. vivax and P. falciparum
When do most deaths occur from malaria?
within the first 24-48 hours of infection
What drug is used for suppressive prophylaxis?
chloroquine, low dose
What is the first line treatment for acute attack?
chloriquine
What is the treatment for chloroquine-resistant P. falciparum and P. vivax?
Quinine sulfate + doxycycline
What is the treatment of parenteral treatment for severe diseases?
Qunidine + doxycyline
What are the alternative treatments for prevention of malaria?
atovaquone/proguanil
What is the alternative treatment for prevention of chloroquine resistant malaria?
Doxycyline or mefloquine
What is the radical cure of prevention of relapse drug?
primaquine
T/F: there are no drugs that target the sporozoite form of malaria?
True
What form of malaria do all malarial drugs target besides primaquine?
Red blood cell stage
How does chloroquine become more selective?
concentrates in parasitized 25 fold more
What is the MOA of chloroquine?
binds to FPIX and doesn’t allow the parasite to turn it into hemozoin from its parasite heme polymerase
What are the adverse effects of chloroquine?
severe eye damage and blindness
T/F: quinine and quinidine are more toxic than chloroquine?
True
What is quinine and quinidine used for?
chloroquine resistant P. falciparum
What are adverse effects of quinine/quinidine?
Cinchonism; permanent damage to vision, balance and hearing
What other thing is quinidine used to treat?
anti-arrhymic, blocks Na and K channels
What are adverse effects of quinidine?
cardiac issues
What are side effects of mefloquine?
neuropsychiatric reactions
What is indicated for the prevention of chloroquine resistant P. falciparum?
mefloquine
What is the MOA of atovaquone?
depolarizes parasitic mitochondria and inhibits electron transport
What is MOA of proguanil?
inhibits malarial dihydrofolate reductase
Is atovaquone/proguanil quick or slow onset?
Slow
What is MOA of artemisinins (2 MOAs)?
Heme iron in malarial pigment acts on drug to produce free radicals, inhibitions calcium ion ATPases of P. falciparum
Are artemisinins fast or slow?
Very rapid
Do you use artemisinins alone?
no, to avoid selection of resistant organisms
What stage of malaria is lumefantrine effective against?
erythrocytic state
Why do you treat with lumefantrine?
Helps clear remaining viable parasites
What pt population can primaquine cause hemolytic anemia?
G6PD deficiency
