Malaria Pharmacology

  1. Drugs that work at the schizont stage (in the liver)/ used for prophylaxis:
    • Primaquine
    • Tafenoquine
    • Atovaquone
  2. Artemisinin MOA:
    Production of free radicals
  3. Artemisinin combination therapy agents:
    • Artesunate-amodiaquine
    • Artemether-lumefantrine
    • Artesunate-mefloquine
  4. T/F: artemisinin is used in combination with a longer acting agent and together they are the standard therapy in endemic areas for ovale/vivax malaria
    False; Artemisinin is standard therapy for falciparum malaria
  5. Adverse effects of artemisinin:
    n/v/d and dizziness
  6. For severe falciparum malaria, what is the preferred route of administration for artemisinin?
  7. MOA of Chloroquine?
    Prevent the detoxification of heme into hemozoin
  8. Chloroquine therapeutic indications?
    • Uncomplicated nonflaciparum and sensitive falciparum malaria
    • Drug of choice for treatment and prophylaxis
  9. Adverse effects of chloroquine?
    • High fever!
    • Not so much GI complaints
    • At high enough dose can lead to suicide
  10. Contraindications for chloroquine?
    Psoriasis or porphyria
  11. MOA of quinine and quinidine?
  12. Therapeutic indications for quinine and quinidine?
    • Severe uncomplicated falciparum malaria
    • Babesiosis
  13. Which drug can be used to treat babesiosis as well as falciparum malaria?
    Quinine and quinidine
  14. Which drug, if given too fast intravenously, could lead to arrhythmia and have cardiotoxic effet?
    Quinine and quinidine
  15. What are adverse effects of quinine and quinidine?
    • Cinchonism- tinnitus, headache, nausea, dizziness, flushing
    • Visual disturbances
    • GI upset
  16. Contraindications for quinine/ quinidine?
    Underlying visual and auditory problems (do not want to exacerbate these sxs since these are potential side effects of quinine/ quinidine
  17. MOA of mefloquine?
  18. Therapeutic indication for mefloquine?
    • For chloroquine resistance falciparum malaria, and vivax malaria
    • Also used as chemoprophylaxis
  19. Adverse effects of mefloquine?
    • n/v. dizziness.
    • Neuropsychiatric toxicity: seizure, depression (black box warning)
  20. Contraindications or precautions for mefloquine?
    • Epilepsy
    • Psych disorders
    • Arrhythmia (like quinine, so not to be used with quinine/ quinidine)
  21. Which of the malarial drug comes with a black box warning for adverse neuropsychiatric reaction?
  22. Which malarial drugs could lead to arrhythmia?
    • Quinine and mefloquine.
    • These two so never be taken at the same time
  23. MOA of primaquine?
  24. Indication for primaquine use?
    • Vivax and ovale malaria (in addition with chloroquine use, primaquine kills the hypnozoite)
    • Terminal prohpylaxis of vivax and ovale malaria
    • Gametocidal action
  25. Adverse effect of primaquine?
    Hemolysis due to G6PD deficiency. Because primaquine uses oxidative stress to kill the parasite
  26. Contraindications for primaquine?
    • G6PD deficient individuals
    • Pregnancy
  27. Atovaquone-Proguanil MOA:
    • Atovaquone: Disrupts electron transport chain which in turn affects nucleotide synthesis
    • Proguanil: inhibiting dihydrofolate reductase
  28. Trade name for atovaquone-proguanil?
  29. Therapeutic indications for atovaquone-proguanil (malarone):
    Chemoprophylaxis and treatment of falciparum malaria
  30. Adverse effects of atovaquone-proguanil:
    • n/v/d
    • headache and insomnia
  31. precautions for atovaquone-proguanil:
  32. which malarial drugs should be avoided when pregnant?
    • Atovaquone-proguanil
    • Primaquine
  33. Atovaquone-doxycycline MOA:
    • Atovaquone- disrupts ETC
    • Doxycycline- blocks 30S ribosomal subunit (a tetracycline antibiotic); prevent tRNA from binding to mRNA
  34. Doxycycline is used in combination with _____, ____ and _____
    • Quinine
    • Artesunate
    • Atovaquone
Card Set
Malaria Pharmacology
HemeOnc Midterm