- Spontocidal Prodrug hich is converted to active metabolite cycloguanil
- Used prophylactically for malaria (FALCIPARUM and VIVAX by selective inhibition of Dihydrofolate reductase and thus prevention of reproduction
- Proguanil + Atovaquone = Malarone : used for chloroquine resistant strains
- Used for latent tissue forms of OVALE and ViVAX in order to prevent relapse. MOA is by acting exo-erythrocytic schizonts. Gametocidal for all species.
- Do not give to pt's with G6Pdehydrogenase deficiency since it causes acute intravascular hemolysis and methemoglobinemia
- Blood Schizonticides which works in the asexual erythocytic cycle
- Tx for OVALE, VIVAX and MALARIAE, entamoeba histolytica. Not effective against exo-erythocytic forms. MOA is by preventing the polymerization of haem which is toxic to the plasmodium.
- AE is retinopathy and ototoxicity with high doses
- They are optical isomers. Quinidine is more potent but more toxic than Quinine. They come from Cinchona bark
- No effect on sporozites or preerythocytic forms. Tx is for chloroquinie resistant malaria forms. MOA is also preventing polymerization of haem
- Resistance occurs in falciparum by the pfmdr1 gene. AE is Cinochism which is tinnitus, visual disturbances, postural hypotension, N/V
Also hypoglycemia, hypotension and thrombocytopenia. CONTRAINDICATED in pregnancy
- Used to tx uncomplicated P.falciparum with quinine.
- MOA is inhibiting parasite DHFR
used in the tx for multidrug resistant malaria.
- Used for amebiasis and trichmonias and giaradias
- MOA is prodrug reduced by anerobic metabolism. acts as electron sink depriving anerobes of reducing capability.
- AE is nausea, headache and metallic aftertaste.
- Drug -drug interaction with Warfarin since the Warfarin effects are amplified. Dosage should be decreased of Warfarin
- Used to tx Chagras
- MOA is by intracllar reduction followed by auto oxidation yielding o2 free radicals. Prolonged use is required
- AE include n/v, abdominal pain, SEIZURES and POLYNEURITIS
- USed to tx Leishmanias which are transmitted by sandflies
- AE is cardiac toxicity