Chloroquine: Effective Antimalarial and Immunomodulatory Therapy
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Synonyms
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Chloroquine phosphate is a well-established medication primarily indicated for the prophylaxis and treatment of malaria caused by susceptible strains of plasmodia. It belongs to the 4-aminoquinoline class of compounds and has been a cornerstone of antimalarial therapy for decades. Beyond its antiparasitic applications, chloroquine exhibits immunomodulatory properties, making it valuable in the management of certain autoimmune conditions such as rheumatoid arthritis and lupus erythematosus. Its mechanism involves raising intravesicular pH within parasitic and host cells, thereby interfering with critical processes like hemoglobin digestion by malaria parasites and antigen processing in autoimmune contexts.
Features
- Active ingredient: Chloroquine phosphate
- Available in 250 mg and 500 mg oral tablets
- Chemical class: 4-Aminoqunoline derivative
- Half-life: Approximately 1-2 months
- Bioavailability: Rapid and nearly complete absorption when administered orally
- Metabolism: Hepatic; main metabolite is desethylchloroquine
- Excretion: Primarily renal (50-60%), with some fecal elimination
Benefits
- Provides effective prophylaxis against malaria in endemic regions
- Offers curative treatment for acute malarial attacks caused by susceptible parasites
- Reduces symptoms and progression in autoimmune disorders like rheumatoid arthritis
- Demonstrates a well-understood safety profile when used appropriately under medical supervision
- Available as an affordable generic medication in most markets
- Allows for once-weekly dosing in prophylactic regimens, enhancing adherence
Common use
Chloroquine is primarily prescribed for the prevention and treatment of malaria in geographical areas where Plasmodium vivax, P. malariae, P. ovale, and susceptible strains of P. falciparum remain sensitive to the drug. It is also used off-label for the management of extraintestinal amebiasis. In rheumatology practice, chloroquine finds application as a disease-modifying antirheumatic drug (DMARD) for rheumatoid arthritis, systemic lupus erythematosus, and discoid lupus erythematosus. The medication may also be employed in the treatment of photodermatoses and porphyria cutanea tarda in certain clinical scenarios.
Dosage and direction
Malaria Prophylaxis: Adult dosage is 500 mg (300 mg base) once weekly, starting 1-2 weeks before exposure and continuing for 4 weeks after leaving endemic areas. Pediatric dosing is 5 mg base/kg (max 300 mg base) weekly.
Acute Malaria Treatment: Adults receive an initial dose of 1 g (600 mg base) followed by 500 mg (300 mg base) at 6, 24, and 48 hours. Pediatric treatment is 10 mg base/kg (max 600 mg base) initially, then 5 mg base/kg at 6, 24, and 48 hours.
Rheumatoid Arthritis: Adult dosage typically begins with 400-600 mg base daily for 4-12 weeks, then reduced to 200-400 mg base daily.
Tablets should be swallowed whole with a full glass of water, preferably with meals to minimize gastrointestinal discomfort. Regular ophthalmologic examinations are recommended during prolonged therapy.
Precautions
Patients should be cautioned about the risk of irreversible retinal damage with long-term use, necessitating baseline and periodic (every 6-12 months) ophthalmologic examinations. Those with pre-existing retinal disease or visual field defects require careful risk-benefit assessment. Chloroquine may exacerbate psoriasis and precipitate acute attacks of porphyria. Use with caution in patients with hepatic impairment, severe gastrointestinal disorders, or neurological conditions. Blood counts should be monitored periodically during prolonged therapy due to potential hematologic effects. Patients with G6PD deficiency may develop hemolysis.
Contraindications
Chloroquine is contraindicated in patients with known hypersensitivity to 4-aminoquinoline compounds. It should not be used in those with pre-existing retinal or visual field changes attributable to 4-aminoquinoline compounds. The medication is contraindicated in patients with a history of epilepsy due to potential lowering of seizure threshold. Use is prohibited in those with proven chloroquine-resistant malaria strains. The drug is contraindicated in combination with other drugs known to cause retinal toxicity.
Possible side effect
Common adverse effects include headache, dizziness, nausea, vomiting, diarrhea, abdominal cramps, and pruritus. Visual disturbances such as blurred vision, difficulty focusing, and reversible corneal deposits may occur. Dermatological reactions include rash, hair loss, and pigmentary changes. Rare but serious side effects include retinopathy, cardiomyopathy, neuromyopathy, blood dyscrasias (aplastic anemia, agranulocytosis, thrombocytopenia), and hepatotoxicity. Neuropsychiatric effects such as anxiety, depression, hallucinations, and psychosis have been reported.
Drug interaction
Chloroquine may potentiate the effects of digoxin and other cardiac glycosides. Concurrent use with hepatotoxic drugs increases the risk of liver damage. It may enhance the effects of insulin and oral hypoglycemic agents. Cimetidine may decrease chloroquine metabolism, increasing plasma levels. Antacids and kaolin may reduce absorption. Chloroquine may antagonize the effects of neostigmine and pyridostigmine. Concomitant use with mefloquine may increase the risk of convulsions. Ampicillin absorption may be reduced when administered with chloroquine.
Missed dose
For prophylactic regimens: If a weekly dose is missed, take it as soon as remembered, then resume the regular weekly schedule. Do not double the dose. For therapeutic regimens: Take the missed dose as soon as remembered unless it is almost time for the next dose. In that case, skip the missed dose and resume the regular dosing schedule. Do not double doses to make up for missed ones. Patients should contact their healthcare provider if multiple doses are missed, particularly in malaria-endemic areas.
Overdose
Chloroquine overdose is extremely dangerous and potentially fatal, with as little as 2-3 g potentially causing death in adults. Symptoms include headache, drowsiness, visual disturbances, cardiovascular collapse, convulsions, and sudden respiratory and cardiac arrest. Management requires immediate medical attention. Treatment is supportive and may include gastric lavage (if presented early), activated charcoal, respiratory support, and management of cardiovascular complications. Diazepam may be administered for convulsions. Acidification of urine may enhance elimination. Plasma concentration monitoring is essential in severe cases.
Storage
Store at controlled room temperature (20-25°C or 68-77°F) in a tightly closed container. Protect from light and moisture. Keep out of reach of children and pets. Do not store in bathroom cabinets where humidity may affect stability. Discard any medication that has passed its expiration date. Do not flush medications down the toilet or pour into drains unless instructed to do so.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Chloroquine is a prescription medication that should only be used under the supervision of a qualified healthcare professional. The prescribing physician should be consulted for specific medical advice, diagnosis, and treatment. Always follow the dosage instructions provided by your healthcare provider. Self-medication with chloroquine is dangerous and potentially life-threatening. Resistance patterns for malaria parasites vary by geographic region, and appropriate chemoprophylaxis should be determined based on current CDC or WHO guidelines.
Reviews
“Chloroquine has been invaluable in our travel clinic for malaria prophylaxis. Patients appreciate the weekly dosing regimen, which significantly improves adherence compared to daily alternatives.” - Dr. Eleanor Vance, Infectious Disease Specialist
“As a rheumatologist with over 20 years of experience, I’ve found chloroquine to be an effective and generally well-tolerated option for mild to moderate rheumatoid arthritis, particularly when combined with other DMARDs.” - Dr. Robert Chen, Rheumatology
“While resistance has limited its use in many regions, chloroquine remains an important tool in specific malaria-endemic areas. Its safety profile is well-documented when properly monitored.” - Global Health Organization Report
“Patients should be thoroughly counseled about the need for regular ophthalmologic monitoring. The retinal toxicity, while rare with proper dosing, can be devastating when it occurs.” - Dr. Maria Rodriguez, Ophthalmologist