Chloroquine: Effective Antimalarial and Immunomodulatory Therapy
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Synonyms
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Chloroquine phosphate is a well-established antimalarial agent with additional applications in the management of certain autoimmune conditions. As a 4-aminoquinoline compound, it demonstrates both antiprotozoal and immunomodulatory properties through distinct mechanisms of action. This medication has been a cornerstone of tropical medicine for decades and continues to play a role in specific therapeutic protocols when appropriately prescribed. Proper patient selection and monitoring are essential for optimal therapeutic outcomes and risk mitigation.
Features
- Contains chloroquine phosphate as the active pharmaceutical ingredient
- Available in 250 mg and 500 mg tablet formulations (equivalent to 150 mg and 300 mg base respectively)
- Demonstrated activity against chloroquine-sensitive Plasmodium species
- Exhibits immunomodulatory effects through lysosomal pH alteration
- Long elimination half-life (approximately 20-60 days)
- High volume of distribution with tissue accumulation
Benefits
- Provides rapid clinical response in acute malaria attacks when caused by sensitive parasites
- Offers chemoprophylaxis against malaria in specific geographical regions
- Reduces symptom severity in autoimmune conditions like rheumatoid arthritis and lupus erythematosus
- Demonstrates cost-effectiveness compared to newer antimalarial alternatives
- Established safety profile with decades of clinical use documentation
- Convenient oral administration with once-weekly dosing for prophylaxis
Common use
Chloroquine is primarily indicated for the prevention and treatment of malaria caused by Plasmodium vivax, P. malariae, P. ovale, and susceptible strains of P. falciparum. Its use requires confirmation of regional sensitivity patterns due to widespread resistance development. Additionally, it is FDA-approved for extraintestinal amebiasis and certain autoimmune disorders including rheumatoid arthritis and systemic lupus erythematosus. Off-label applications include Q fever prophylaxis and photodermatosis management, though evidence supporting these uses varies in quality.
Dosage and direction
Malaria prophylaxis: 500 mg (300 mg base) orally once weekly, starting 1-2 weeks before exposure and continuing for 4 weeks after leaving endemic area
Acute malaria treatment: Initial dose of 1 g (600 mg base) followed by 500 mg (300 mg base) at 6, 24, and 48 hours
Rheumatoid arthritis: 250-500 mg (150-300 mg base) daily initially, with maintenance doses typically ranging from 125-250 mg daily
Administration with food or milk minimizes gastrointestinal discomfort. Tablets should be swallowed whole without crushing or chewing. Regular ophthalmologic examinations are mandatory during long-term therapy.
Precautions
Regular ophthalmologic monitoring is essential due to potential retinal toxicity, particularly with prolonged use exceeding five years or cumulative doses greater than 1000 grams. Hematologic parameters should be periodically assessed as bone marrow suppression may occur. Patients with hepatic impairment require dosage adjustment and careful monitoring. Neurologic and neuromuscular function should be evaluated periodically. Psoriasis may be exacerbated, and porphyria may be precipitated. Glucose-6-phosphate dehydrogenase deficiency increases hemolysis risk.
Contraindications
Hypersensitivity to 4-aminoquinoline compounds constitutes an absolute contraindication. Retinal field changes attributable to chloroquine or related compounds prohibit use. Pre-existing maculopathy presents a relative contraindication requiring careful risk-benefit assessment. The medication is contraindicated in patients with known porphyria. Concomitant use with hepatotoxic drugs requires extreme caution. Pregnancy category C status necessitates careful consideration of maternal versus fetal risks.
Possible side effects
Common: Nausea, vomiting, diarrhea, abdominal cramps, headache, pruritus (particularly in black patients)
Ophthalmic: Vortex keratopathy, retinal pigmentary changes, visual field defects, blurred vision
Dermatologic: Hair bleaching, alopecia, skin eruptions, photosensitivity
Neurologic: Dizziness, vertigo, tinnitus, nerve deafness, neuromyopathy
Hematologic: Leukopenia, thrombocytopenia, agranulocytosis
Cardiac: Cardiomyopathy, conduction defects (particularly with pre-existing cardiac conditions)
Psychiatric: Emotional changes, psychosis, depression
Drug interaction
Chloroquine may potentiate the effects of digoxin and other cardiac glycosides. Concomitant use with hepatotoxic agents increases the risk of liver damage. Antacids and kaolin reduce absorption when administered simultaneously. Cimetidine inhibits chloroquine metabolism, potentially increasing plasma levels. Cyclosporine concentrations may be elevated when co-administered. Ampicillin absorption may be reduced. Mefloquine co-administration increases seizure risk. The drug may antagonize the effects of anticonvulsants.
Missed dose
For weekly malaria prophylaxis: Take the missed dose as soon as remembered, then resume the regular weekly schedule. Do not double the dose. For daily regimens: Take the missed dose unless it is almost time for the next scheduled dose. Do not take extra medication to make up for the missed dose. Consistent adherence is particularly crucial for malaria prophylaxis to maintain therapeutic blood levels.
Overdose
Chloroquine overdose constitutes a medical emergency with rapid onset of severe toxicity. Symptoms include headache, drowsiness, visual disturbances, cardiovascular collapse, convulsions, and hypokalemia. Cardiac manifestations include QRS widening, QT prolongation, and ventricular arrhythmias. Fatality may occur within hours of ingestion. Management requires immediate gastric lavage, activated charcoal administration, and intensive supportive care. Intravenous diazepam may reduce cardiovascular toxicity. Potassium supplementation should be guided by frequent monitoring.
Storage
Store at controlled room temperature (20-25°C/68-77°F) in the original container with the lid tightly closed. Protect from light and moisture. Keep out of reach of children and pets. Do not transfer to other containers. Discard any medication that has expired or shows signs of deterioration. Proper disposal through medication take-back programs is recommended to prevent environmental contamination.
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 dosage recommendations and treatment duration. Regional resistance patterns must be considered for malaria treatment and prophylaxis. Regular monitoring is essential during therapy to detect potential adverse effects.
Reviews
Clinical studies demonstrate chloroquine’s efficacy against sensitive malaria strains with cure rates exceeding 95% when properly administered. Rheumatology applications show significant symptom improvement in approximately 60-70% of patients with autoimmune conditions. The drug maintains favor in specific geographical regions where resistance patterns remain favorable. Ophthalmologic monitoring protocols have significantly reduced the incidence of serious retinal complications with long-term use. Cost-effectiveness analyses support its continued use in appropriate clinical scenarios despite the development of newer agents.