Pharm

Chloroquine

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Chloroquine, Aralen

  • Indications
  1. Malaria Prophylaxis
    1. Travel to areas without Chloroquine resistance
  2. Discoid Lupus (off label)
  3. NOT indicated in COVID-19 outside of clinical trials as of May 2020
    1. Low efficacy in trials to date and risk of serious reactions (including QTc Prolongation)
    2. https://www.medrxiv.org/content/10.1101/2020.04.16.20065920v2
  1. General
    1. Indicated in Chloroquine sensitive regions only (few regions remain Chloroquine sensitive)
    2. Deaths have occurred when used in resistant regions
  2. Protocol
    1. Start 1-2 weeks before travel
    2. Continue through 4 weeks after return
  3. Adult: 300 mg base (500 mg salt) orally once weekly
  4. Child: Dose: 5 mg/kg base (8.3 mg/kg salt) up to 300 mg base orally once weekly
  1. General
    1. Indicated in Chloroquine sensitive regions only (other agents are preferred)
    2. Taking with food decreases gastric irritation
  2. Adults
    1. Load: 1000 mg salt (600 mg base) orally at start
    2. Maintenance: 500 mg salt (300 mg base) orally at 6 hours, 24 hours and 48 hours after initial dose
  3. Child
    1. Load: 16.7 mg/kg salt (10 mg/kg base) orally at start
    2. Maintenance: 8.3 mg/kg salt (5 mg/kg base) orally at 6 hours, 24 hours and 48 hours after initial dose
  • Adverse Effects
  1. Cardiovascular
    1. AV Block
    2. QTc Prolongation
      1. Risk of Ventricular Tachycardia including Drug-Induced Torsades de Pointes
  2. Dermatologic
    1. Hair, skin and Nail Discoloration
    2. Erythema Multiforme
    3. Psoriasis exacerbation
  3. Endocrine
    1. Hypoglycemia
  4. Ear (Ototoxicity)
    1. Tinnitus
    2. Hearing Loss
  5. Eye
    1. Blurred Vision
    2. Corneal disorders
    3. Retinopathy (more common than with Hydroxychloroquine)
  6. Gastrointestinal
    1. Nausea and Vomiting
    2. Diarrhea
    3. Abdominal Pain
  7. Hematologic (Bone Marrow toxicity)
    1. Agranulocytosis
    2. Neutropenia
    3. Pancytopenia
    4. Thrombocytopenia
  8. Musculoskeletal
    1. Myopathy
  9. Neurologic
    1. Confusion or Delirium
    2. Hallucination
    3. Psychosis
    4. Insomnia
    5. Extrapyramidal Side Effects
    6. Depressed mood and Suicidality
    7. Seizures
  • Safety
  1. Safe for children of all ages
  2. Considered safe in Lactation
  3. Pregnancy
    1. Safe in all trimesters of pregnancy (but Chloroquine does cross the placenta)
  • Drug Interactions
  1. Tamoxifen
    1. Increased risk of Retinopathy when combined with Chloroquine
  2. Antacids
    1. Reduced Chloroquine absorption
  • Pharmacokinetics
  1. Narrow safety range in children (fatal Overdoses have occurred at 1 g)
  • Efficacy
  1. Most world regions exhibit high Chloroquine resistance in Plasmodium Falciparum
  2. Limit use to only nonsevere infections from non-Chloroquine resistance regions
  • Resources
  1. Chloroquine Tablet (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=06c69e2b-211b-4746-9f3a-f86d36520570
  • References
  1. (2019) Drugs for Malaria Prophylaxis, Med Lett Drugs Ther, p. e104-5
  2. (2023) Presc Lett, Malaria Prophylaxis, Resource #350806
  3. (2020) LexiComp, Chloroquine, accessed 5/6/2020
  4. Shahbodaghi (2022) Am Fam Physician 106(3): 270-8 [PubMed]