Updated: 9/8/2019

Anti-Malarial Drugs

Topic
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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-Malarial 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 metabolism, making 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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