II. 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

III. Dosing: Malaria Prophylaxis

  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

IV. Dosing: Malaria Treatment

  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

VI. 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)

VII. Drug Interactions

  1. Tamoxifen
    1. Increased risk of Retinopathy when combined with Chloroquine
  2. Antacids
    1. Reduced Chloroquine absorption

VIII. Pharmacokinetics

  1. Narrow safety range in children (fatal Overdoses have occurred at 1 g)

IX. Efficacy

  1. Most world regions exhibit high Chloroquine resistance in Plasmodium Falciparum
  2. Limit use to only nonsevere infections from non-Chloroquine resistance regions

XI. 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]

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Ontology: Chloroquine (C0008269)

Definition (NCI) A 4-aminoquinoline with antimalarial, anti-inflammatory, and potential chemosensitization and radiosensitization activities. Although the mechanism is not well understood, chloroquine is shown to inhibit the parasitic enzyme heme polymerase that converts the toxic heme into non-toxic hemazoin, thereby resulting in the accumulation of toxic heme within the parasite. This agent may also interfere with the biosynthesis of nucleic acids. Chloroquine's potential chemosensitizing and radiosensitizing activities in cancer may be related to its inhibition of autophagy, a cellular mechanism involving lysosomal degradation that minimizes the production of reactive oxygen species (ROS) related to tumor reoxygenation and tumor exposure to chemotherapeutic agents and radiation.
Definition (MSH) The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.
Definition (CSP) antiamebic and antimalarial; chloroquine phosphate is also listed by USP as a suppressant of lupus erythematosus.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D002738
SnomedCT 330034001, 324890009, 14728000, 373468005
LNC LP16070-2, MTHU014870
English Chingamin, Chlorochin, Chloroquine, Khingamin, chloroquine, 1,4-Pentanediamine, N4-(7-chloro-4-quinolinyl)-N1,N1-diethyl-, Chloroquine [anti-malarial], Chloroquine [musculo-skeletal], chloroquine (medication), Chloroquine [Chemical/Ingredient], chloroquine products, Chloroquine [musculo-skeletal] (product), Chloroquine [anti-malarial] (product), CHLOROQUINE, Chloroquine (product), Chloroquine (substance), Chloroquine [anti-malarial] (substance), Chloroquine [musculo-skeletal] (substance)
Swedish Klorokin
Czech chlorochin, chloroquin
Finnish Klorokiini
Russian KHLOROKHIN, KHINGAMIN, ХИНГАМИН, ХЛОРОХИН
Japanese リン酸クロロキン, クロロキン
Polish Arechina, Resochina, Chlorochina
Spanish cloroquina [antipalúdico] (producto), cloroquina [uso musculoesquelético] (producto), cloroquina [antipalúdico], cloroquina [uso musculoesquelético], cloroquina (producto), cloroquina (sustancia), cloroquina, Cloroquina
Croatian Klorokin
French Chloroquine
German Chlorochin
Italian Clorochina
Portuguese Cloroquina

Ontology: Aralen Phosphate (C0718643)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
English Aralen Phosphate