Chloroquine

Administration

• Type: Antimalarial
• Dosage Forms:
• Routes of Administration: Oral
• Common Trade Names: (Aralen)

Adult Dosing

Most malaria-endemic areas have high rates of chloroquine resistance. Per the CDC, chloroquine-sensitive areas include: Central America west of the Panama Canal, Haiti, the Dominican Republic, and most of the Middle East. See [CDC malaria information by country] for details

• Uncomplicated malaria treatment: 1000 mg PO, followed by 500mg PO at 6, 24, and 48 hours after first dose
• Malaria prophylaxis: 500 mg PO weekly beginning 1 to 2 weeks prior to travel to malarious area through 4 weeks after departure

Pediatric Dosing

• Uncomplicated malaria treatment: 16.6 mg/kg PO (max 1 g), followed by 8.3 mg/kg PO at 6, 24, and 48 hours after first dose
• Malaria prophylaxis: 8.3 mg/kg PO weekly beginning 1 to 2 weeks prior to travel to malarious area through 4 weeks after departure

Special Populations

• Pregnancy Rating: C
• Lactation risk: Infant risk minimal
• Renal dosing: reduce dose by 50% if CrCl < 10
• Hepatic dosing: may need serum drug level monitoring as 30-50% of dose modified by liver

Contraindications

• Allergy to class/drug
• Retinal or visual field changes

Adverse Reactions

Serious

• Prolonged QT, AV block
• Heart failure
• SJS
• Neutropenia
• Extrapyramidal disease
• Seizure
• Retinopathy

Pharmacology

• Half-life: 1-2 months
• Metabolism: Hepatic
• Excretion: Renal, fecal

Mechanism of Action

• Precise mechanism unknown, action thought to be due to interaction with DNA

See Also

• Antimalarials
• Malaria

References

• Lexicomp
• Akintonwa A, Gbajumo SA, and Mabadeje AF, "Placental and Milk Transfer of Chloroquine in Humans," Ther Drug Monit, 1988, 10(2):147-9. [PubMed 3381230]
• Anderson PO, Sauberan JB. Modeling drug passage into human milk. Clin Pharmacol Ther. 2016;100(1):42-52. doi: 10.1002/cpt.377. [PubMed 27060684]
• Aralen (chloroquine phosphate) [prescribing information]. Bridgewater, NJ: Sanofi-Aventis US LLC: October 2018.
• Aronoff GR, Bennett WM, Berns JS, et al, Drug Prescribing in Renal Failure: Dosing Guidelines for Adults and Children, 5th ed. Philadelphia, PA: American College of Physicians; 2007, p 73.
• ASHP. Standardize 4 Safety Initiative Compounded Oral Liquid Version 1.01. July 2017. https://www.ashp.org/-/media/assets/pharmacy-practice/s4s/docs/s4s-ashp-oral-compound-liquids.ashx?la=en&hash=4C2E4F370B665C028981B61F6210335AD5D0D1D6.
• Avina-Zubieta JA, Johnson ES, Suarez-Almazor ME, et al, “Incidence of Myopathy in Patients Treated With Antimalarials. A Report of Three Cases and a Review of the Literature,” Br J Rheumatol, 1995, 34(2):166-70. [PubMed 7704464]
• Bezerra EL, Vilar MJ, da Trindade Neto PB, et al. “Double-blind, randomized, controlled clinical trial of clofazimine compared with chloroquine in patients with systemic lupus erythematosus”. Arthritis Rheum, 2005;52(10):3073-8. [PubMed 16200586]
• Boelaert JR, Yaro S, Augustijns P, Meda N, Schneider YJ, Schols D, Mols R, De Laere EA, Van de Perre P. Chloroquine accumulates in breast-milk cells: potential impact in the prophylaxis of postnatal mother-to-child transmission of HIV-1. AIDS. 2001;15(16):2205-2207. [PubMed 11684948]
• Cappellini MD, Fiorelli G. Glucose-6-phosphate dehydrogenase deficiency. Lancet. 2008;371(9606):64-74. doi: 10.1016/S0140-6736(08)60073-2. Review. [PubMed 18177777]
• Centers for Disease Control and Prevention (CDC), "CDC Health Information for International Travel 2018," New York: Oxford University Press, 2018.