Chloroquine: Effective Antimalarial and Immunomodulatory Therapy
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Synonyms
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Chloroquine phosphate is a well-established antimalarial agent with a demonstrated history of clinical efficacy and a well-characterized safety profile when used appropriately. Originally developed in the mid-20th century, it remains a cornerstone therapy for the prophylaxis and treatment of susceptible Plasmodium species in specific geographic regions. Beyond its antimalarial indications, chloroquine exhibits immunomodulatory properties that have led to its use in certain autoimmune conditions, such as rheumatoid arthritis and lupus erythematosus. Its mechanism of action involves raising intravesicular pH within parasitic and host cells, interfering with critical processes like hemoglobin digestion by malaria parasites and antigen presentation in immune cells.
Features
- Chemical name: 7-chloro-4-(4-diethylamino-1-methylbutylamino) quinoline phosphate
- Available as 250 mg and 500 mg tablets (equivalent to 150 mg and 300 mg base, respectively)
- Standardized manufacturing under current Good Manufacturing Practices (cGMP)
- Demonstrated bioavailability of approximately 90% when administered orally
- Established half-life of approximately 20-60 days in blood
- WHO Essential Medicines List inclusion for malaria prophylaxis and treatment
Benefits
- Provides effective chemoprophylaxis against malaria in regions with chloroquine-sensitive Plasmodium falciparum
- Offers rapid clinical response in acute malaria attacks when caused by susceptible parasites
- Demonstrates anti-inflammatory effects beneficial for managing autoimmune conditions
- Presents cost-effective therapy option compared to newer antimalarials in appropriate settings
- Enables flexible dosing regimens due to prolonged half-life and tissue accumulation
- Shows well-documented safety profile with decades of clinical use and monitoring
Common use
Chloroquine is primarily indicated for the prophylaxis and treatment of malaria caused by Plasmodium vivax, Plasmodium ovale, Plasmodium malariae, and chloroquine-sensitive strains of Plasmodium falciparum. Medical professionals also prescribe it off-label for certain autoimmune disorders, including rheumatoid arthritis and systemic lupus erythematosus, where its immunomodulatory properties help manage disease activity. In rheumatological applications, it often serves as a disease-modifying antirheumatic drug (DMARD) that can reduce disease progression and symptom severity.
Dosage and direction
Malaria Prophylaxis (adults): 500 mg salt (300 mg base) orally once weekly, starting 1-2 weeks before exposure and continuing for 4 weeks after leaving endemic area
Acute Malaria Treatment (adults): Initial dose of 1 g salt (600 mg base) followed by 500 mg salt (300 mg base) at 6, 24, and 48 hours
Rheumatoid Arthritis (adults): 250-500 mg salt daily, often combined with other DMARDs
Administration with food or milk is recommended to minimize gastrointestinal discomfort. Tablets should be swallowed whole without crushing or chewing. For pediatric dosing, calculation is based on body weight (5 mg base/kg weekly for prophylaxis, maximum 300 mg base).
Precautions
Regular ophthalmological examinations are mandatory due to risk of irreversible retinopathy with long-term use. Complete blood counts and liver function tests should be monitored periodically during extended therapy. Patients with pre-existing hepatic impairment require dosage adjustment and enhanced monitoring. Those with glucose-6-phosphate dehydrogenase deficiency should use chloroquine cautiously due to potential hemolytic risk. Caution is advised in patients with history of seizure disorders, as chloroquine may lower seizure threshold. Psoriasis patients may experience exacerbation of symptoms.
Contraindications
Hypersensitivity to chloroquine or other 4-aminoquinoline compounds represents an absolute contraindication. Use is prohibited in patients with established chloroquine-induced retinal or visual field changes. The medication is contraindicated in those with known porphyria. Combination with other drugs known to cause retinal toxicity should be avoided. Administration is not recommended during pregnancy unless potential benefits outweigh risks, particularly in first trimester.
Possible side effect
Common (>1%): Headache, dizziness, gastrointestinal disturbances (nausea, vomiting, diarrhea), pruritus, skin eruptions, hair bleaching
Less common (0.1-1%): Visual disturbances (blurring, difficulty focusing), corneal deposits, weight loss, bleaching of hair
Rare (<0.1%): Retinopathy, ototoxicity, blood dyscrasias (leukopenia, thrombocytopenia), cardiomyopathy, neuromyopathy
Ophthalmic monitoring parameters: Visual acuity, funduscopy, visual field testing, and retinal imaging should be performed at baseline and every 6-12 months during long-term therapy
Drug interaction
Chloroquine may potentiate the effects of digoxin and other cardiac glycosides. Concurrent use with hepatotoxic drugs increases risk of liver damage. Antacids and kaolin reduce absorption and should be administered at least 4 hours apart. Cimetidine inhibits chloroquine metabolism, potentially increasing plasma levels. Cyclosporine levels may be elevated when co-administered with chloroquine. The drug may enhance the effects of insulin and oral hypoglycemics, requiring blood glucose monitoring.
Missed dose
If a weekly prophylactic dose is missed, patients should take it as soon as remembered, then resume regular weekly schedule. If remembered near the time of the next dose, the missed dose should be skipped. Doubling doses is not recommended. For daily regimens, take the missed dose as soon as remembered unless it’s almost time for the next dose, in which case skip the missed dose and resume regular schedule.
Overdose
Chloroquine overdose constitutes a medical emergency requiring immediate intervention. Symptoms include headache, drowsiness, visual disturbances, cardiovascular collapse, convulsions, and cardiac arrest. Management includes gastric lavage if presented early, activated charcoal administration, and aggressive supportive care. Cardiovascular monitoring is essential, as QRS complex widening may indicate serious toxicity. Diazepam may be administered for seizure control. In severe cases, mechanical ventilation and vasopressor support may be necessary.
Storage
Store at controlled room temperature (15-30°C) in original container with tight closure. Protect from light and moisture. Keep out of reach of children. Do not use if tablets show signs of discoloration or deterioration. Dispensing should be in child-resistant containers. Avoid storage in bathrooms or areas with high humidity.
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 direct medical supervision. Healthcare providers must assess individual patient factors, including regional resistance patterns for malaria, before prescribing. Patients should not self-medicate with chloroquine due to serious potential adverse effects and the necessity for medical monitoring. Always consult with a qualified healthcare professional for diagnosis and treatment recommendations.
Reviews
“Chloroquine remains valuable for specific malaria scenarios where sensitivity patterns are known. Its long half-life makes weekly prophylaxis feasible, though resistance concerns limit geographical utility.” - Infectious Disease Specialist, 15 years experience
“In rheumatology practice, we find chloroquine effective as part of combination therapy for mild to moderate rheumatoid arthritis. The retinal toxicity risk requires diligent monitoring but is manageable with proper protocols.” - Rheumatologist, 12 years experience
“The cost-effectiveness of chloroquine in appropriate settings cannot be overstated. However, the emergence of resistance has significantly limited its utility in many malaria-endemic regions.” - Tropical Medicine Physician, 20 years experience
“Patient education about the importance of regular eye exams is crucial when prescribing long-term chloroquine. We’ve established successful monitoring programs that allow safe extended use.” - Ophthalmologist, 18 years experience