Regal Malaria IHO Week 3 Flashcards
Name the drug with the basis for selectivity is that the RBC concentrates it at least 25x more than unparasitized RBC to accumulate in the acid pH of the food vacuole
Chloroquine
MOA is intercalates between base pairs in DNA thus inhibiting nucleic acid synthesis
Chloroquine MOA
parasite eats host hgb in the acidic food vaculoe to get lots of ferriprotoporphyrin IX which is toxic to the parasite and so is converted to hemozoin via heme polymerase. How does Chloroquine stop this?
Chloroquine binds to FPIX and prevents its conversion to hemozin and this is toxic to the plasmodium
AE of Chloroquine in low doses?
None
AE of Chloroquine in acute attack doses
-dizziness, headache, itching, vomiting, skin rashes-difficulty with visual accommodation-large doses for prolonged periods can cause severe eye damage and even blindness
Are Qunine and Quinidine more or less toxic than chloroquine
Quinine and Quinidine are more toxic than chloroquine, but less resistance
When do you use Quinine and Quinidine
in chloroquine resistant P. falciparum
AE of Quinine and Quinidine
cinchonism-tinnitus, blurred vision, nausea, headache, decreased hearing acuity, permanent damage to vision, balance and hearing can result, cardiac problems
Uses of Quinidine
-anti-arrhythmic drug that blocks Na and K, IV for severe malaria,
When to use Mefloquine
for treatment and prevention of Chloroquine resistant P. falciparum
AE of Mefloquine
disorientation, hallucinations, depression, n/v, dizziness, visual or auditory disturbances
MOA of Mefloquine
similar to chloroquine
MOA of Atovaquone
depolarizes parasitic mitochondria and inhibits their electron transport
Proguanil MOA
metabolite inhibits dihydrofolate reductase, selective for the plasmodial enzyme, enhances the mitochondrial toxicity of atovaquone and reduces the frequency of resistance, NOT acitve against hepatic stage of vivax or ovale, concentrated in the erythrocytes
What is replacing mefloquine for prophylaxis?
atovaquone-proguanil
Which malaria med will cause GI disturbances?
atovaquone-proguanil
What are 2 combinations of malaria meds?
artesunate plus mefloquine and artemether plus lumefantrine
MOA of Artemisinins
heme iron in the marlarial pigment acts on the drug to produce free radicals that damage parasite proteins; inhibits a calcium ion ATPase in P. falciparum
What has RAPID and potent activity against even multi-drug resistant organisms (not hepatic forms)
Artemisinins
unkown MOA, effective in erythrocyte stage, rapid initial reduction of parasite biomass afforded by artemether and subsequent clearance of remaining viable parasites by more slowly eliminated what
Lumefantrine
Radical Cure to eliminate hepatic forms of P. vivax and P.ovale
Primaquine
MOA of Primaquine
unkown, thought to be generation of ROS or by interfering with electron transport in the parasite
Ae of Primaquine
occasional GI distress, nausea, headache, pruritis, leukopenia, hemolytic anemia in ppl with G6PDH deficiency
