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 in antimalarial therapy for decades. Beyond its antimalarial properties, chloroquine also exhibits immunomodulatory effects, 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, interfering with critical processes like hemoglobin degradation and antigen presentation. This product card provides a comprehensive overview for healthcare professionals regarding its appropriate use, safety profile, and clinical considerations.
Features
- Active ingredient: Chloroquine phosphate
- Available formulations: Oral tablets (250 mg, 500 mg), injection solution
- Chemical class: 4-Aminoqunoline derivative
- Half-life: Approximately 20-60 days
- Metabolism: Hepatic (partial)
- Excretion: Renal (50-70% as unchanged drug)
Benefits
- Provides effective chemoprophylaxis against malaria in endemic regions
- Offers rapid clinical response in acute malarial attacks when caused by susceptible parasites
- Demonstrates anti-inflammatory properties beneficial for autoimmune disease management
- Shows in vitro activity against some viral pathogens through pH-dependent mechanisms
- Presents well-established dosing protocols with extensive clinical experience
- Maintains cost-effectiveness compared to newer antimalarial alternatives
Common use
Chloroquine is primarily prescribed for:
- Prophylaxis of malaria in geographic regions where chloroquine-sensitive Plasmodium species exist
- Treatment of acute attacks of malaria caused by P. vivax, P. malariae, P. ovale, and susceptible strains of P. falciparum
- Extraintestinal amebiasis treatment (as an adjunct to other amebicides)
- Management of rheumatoid arthritis unresponsive to first-line agents
- Treatment of discoid and systemic lupus erythematosus
- Off-label uses in certain photodermatoses and porphyria cutanea tarda
Dosage and direction
Malaria Prophylaxis (adults): 500 mg 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 followed by 500 mg after 6-8 hours, then 500 mg daily for 2 days (total 2.5 g over 3 days)
Rheumatoid Arthritis (adults): Initial dose 400-600 mg daily, reducing to maintenance dose of 200-400 mg daily
Note: Dosage must be adjusted for children based on body weight and specific indication. All dosing should be determined by a healthcare provider considering individual patient factors.
Precautions
- Regular ophthalmologic examinations required (baseline and every 6-12 months during long-term therapy)
- Complete blood counts recommended periodically during prolonged treatment
- Use with caution in patients with hepatic impairment or alcoholism
- May exacerbate psoriasis or porphyria
- Caution in patients with neurological disorders or history of seizures
- Requires careful monitoring in patients with G6PD deficiency due to hemolysis risk
- Not recommended during pregnancy unless potential benefit justifies potential risk
Contraindications
- Hypersensitivity to chloroquine or other 4-aminoquinoline compounds
- Retinal field changes attributable to any 4-aminoquinoline compound
- Psoriasis (unless benefits outweigh risks and psoriasis is not exacerbated)
- Porphyria
- Combination with other drugs known to cause retinal damage
- History of ventricular arrhythmias or QT prolongation
- Severe hepatic impairment
Possible side effect
Common (≥1%):
- Gastrointestinal disturbances (nausea, vomiting, diarrhea, abdominal cramps)
- Headache
- Pruritus (especially in dark-skinned patients)
- Visual disturbances (blurring, difficulty focusing)
- Dermatological reactions (rash, hair loss, pigmentary changes)
Serious (<1%):
- Irreversible retinopathy with long-term use
- Cardiomyopathy leading to cardiac failure
- Blood dyscrasias (aplastic anemia, agranulocytosis, thrombocytopenia)
- Severe hypoglycemia
- Neuropsychiatric reactions (psychosis, seizures)
- Ototoxicity (nerve deafness, tinnitus)
- Extrapyramidal disorders
Drug interaction
- May increase digoxin levels (monitor serum concentrations)
- Enhances effects of insulin and oral hypoglycemics (hypoglycemia risk)
- Cimetidine may increase chloroquine levels
- May antagonize effects of neostigmine and pyridostigmine
- Concurrent use with hepatotoxic drugs increases toxicity risk
- May increase cyclosporine levels
- Ampicillin absorption reduced when taken with chloroquine
- QT prolongation risk when combined with other QT-prolonging agents
Missed dose
If a weekly prophylactic dose is missed, take it as soon as remembered, then resume the regular weekly schedule. Do not double the dose. For daily regimens, take the missed dose when remembered unless it’s almost time for the next dose, in which case skip the missed dose and continue regular schedule. Patients should contact their healthcare provider for specific guidance based on their treatment regimen.
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 with gastric lavage, activated charcoal, and intensive supportive care including respiratory support and management of hypotension. Diazepam may reduce cardiotoxicity. Serum potassium should be monitored closely as hypokalemia is common.
Storage
Store at controlled room temperature (20-25°C/68-77°F) in original container. Protect from light and moisture. Keep tightly closed and out of reach of children. Do not use if discolored or if tablets show signs of deterioration. Properly discard any unused medication after treatment completion or expiration.
Disclaimer
This information is intended for healthcare professionals and should not replace professional medical advice, diagnosis, or treatment. Always consult appropriate prescribing information and clinical guidelines before administration. The prescriber should verify current susceptibility patterns for malaria in specific geographic regions. Patients should be fully informed of risks and benefits, particularly regarding long-term ophthalmologic monitoring requirements.
Reviews
“Chloroquine remains an essential tool in our antimalarial arsenal, particularly for vivax malaria and in specific geographic regions. Its well-characterized safety profile, when monitored appropriately, makes it valuable despite resistance concerns.” - Infectious Disease Specialist, 15 years experience
“The immunomodulatory effects provide significant benefit in refractory rheumatoid arthritis cases. However, the retinal toxicity risk requires diligent monitoring and patient education.” - Rheumatologist, 12 years experience
“While resistance has limited its utility in many regions, chloroquine continues to serve important roles in both travel medicine and autoimmune therapy when used judiciously with proper monitoring protocols.” - Clinical Pharmacologist, 20 years experience