Anti-protozoals

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Author:
sumo
ID:
225120
Filename:
Anti-protozoals
Updated:
2013-06-26 15:34:39
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anti-P
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  1. Proguanil
    • Antimalarial 
    • 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 
  2. Primaquine
    • Antimalarial
    • 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
  3. Chloroquine
    • 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
  4. Quinine/Quinidine
    • 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
  5. Pyrimethamine
    • Antifolate
    • Used to tx uncomplicated P.falciparum with quinine. 
    • MOA is inhibiting parasite DHFR
  6. Artemisinin
    used in the tx for multidrug resistant malaria.
  7. Metronidazole
    • 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 
  8. Nifurtimox
    • 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
  9. Sodium Stibogluconate
    • USed to tx Leishmanias which are transmitted by sandflies
    • AE is cardiac toxicity

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