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Updated: Sep 22 2019

Anti-Malarial Drugs

5.0

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(1)

  • Snapshot
    • A 32-year-old man presents to urgent care after returning from a trip to sub-Saharan Africa, where he did a safari tour and suffered from many bug bites. He reports feeling intermittently feverish since then and having a persistent headache. On physical exam, he has left upper quadrant tenderness and splenomegaly. Laboratory evaluation reveals anemia. Due to high index of suspicion for malaria, a peripheral blood smear is conducted, which shows trophozoite ring forms within the red blood cells, suggestive of malaria. He is started on atovaquone/proguanil.
  • Introduction
    • Drugs
      • chloroquine
      • hydroxychloroquine
      • quinidine
      • quinine
      • artemether/lumefantrine
      • atovaquone/proguanil
      • artesunate
      • mefloquine
      • primaquine
      • doxycycline
    • Clinical use
      • malaria
        • treatment
        • prophylaxis
      • P. falciparum and, increasingly, P. vivax may be resistant to chloroquine, hydroxychloroquine, and mefloquine
      • Anti-Protozoal Medications
      • Drug
      • Mechanism of Action
      • Adverse Effects
      • Indications
      • Chloroquine
      • Blocks heme polymerase, which causes heme accumulation 
      • Heme is toxic to plasmodia
      • Retinopathy
      • Pruritus
      • Gastrointestinal upset
      • Myopathy
      • All plasmodial species
        • however, there is increasing resistance to P. falciparum and recently P. vivax
      • Hydroxychloroquine
      • Unknown, but impairs neutrophils and chemotaxis and may interfere with lysosomal degradation of hemoglobin
      • Retinopathy
      • Bleaching of hair
      • Gastrointestinal upset
      • All plasmodial species
        • however, there is increasing resistance to P. falciparum 
      • Quinidine
      • A class IA antiarrhythmic drug
      • Diarrhea
      • QTc prolongation
      • Palpitations
      • Life-threatening/severe malaria due to P. falciparum
        • drug is discontinued in the US
      • Quinine
      • Disrupts plasmodial DNA transcription and replication
      • Hemolytic anemia in G6PD deficiency
      • Gastrointestinal upset
      • Flushing
      • Chloroquine-resistant P. falciparum and P. vivax
      • Artemether/lumefantrine
      • Inhibits nucleic acid and protein synthesis
      • Gastrointestinal upset
      • Headache
      • QTc prolongation
      • Chloroquine-resistant P. falciparum and P. vivax
      • Atovaquone/proguanil
      • Unknown, may interfere with cell membrane permeability and cause paralysis in the helminth
      • Gastrointestinal upset
      • Dizziness
      • P. falciparum
      • Babesia (used with azithromycin)
      • Chemoprophylaxis
      • Artesunate
      • Inhibits arachidonic acid metabolismmaking the helminth more susceptible to the host's innate immune system
      • Hemolytic crisis in patients with G6PD deficiency
        • test for G6PD deficiency prior to starting
      • First-line for life-threatening malaria due to P. falciparum
      • Mefloquine
      • Inhibits oogenesis and spermatogenesis
      • Central nervous system toxicity: dizziness, hallucinations, altered mental status
      • Gastrointestinal upset
      • P. falciparum
      • Also has increasing resistance
      • Primaquine
      • Interferes with electron transport chain in plasmodial mitochonrdia
      • Gastrointestinal upset
      • Hemolytic crisis in patients with G6PD deficiency
        • test for G6PD deficiency prior to starting
      • Adjuvant for P. vivax/ovale to eradicate hypnozoites
      • Chemoprophylaxis
      • Doxycycline
      • Inhibits 30S ribosomal subunit
      • Gastrointestinal upset
      • Esophagitis
      • Photosensitivity
      • Chemoprophylaxis
      • Adjuvant therapy with chloroquine, quinine, or primaquine
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