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