Chloroquine (Aralen Generic) for Malaria Prevention
Chloroquine is a part of malaria treatment protocol with the exception of the Plasmodium falciparum strain, and is also used in systemic diseases like lupus erythematous or rheumatoid arthritis. Chloroquine evokes few to no adverse reactions and is widely used in anticipation of travels to regions where malaria is spread.
Chloroquine (Aralen) appeared in 1934, but it did not enter the clinical practice until 1947. This medication is well-documented; it has been around for quite a while and still plays an important role. 1950s saw the advance of a drug closely related to it, hydroxychloroquine. Extensive research yielded the conclusion that this latter is safer in long term therapies.
Chloroquine prices in Canadian Pharmacies
Chloroquine prices can vary considerably depending on the retailer. According to a popular price aggregator, prices for 12 tablets of chloroquine 500mg start at $75, with an average price of around $200. However, generic chloroquine is available in Canadian pharmacies as cheap as $1.5 per tablet.
Mechanism of action
Chloroquine is a derivative of 4-aminoquinoline. This multipurpose drug has immunomodulatory, anti-inflammatory, analgesic, antiplatelet, lysosomotropic, hypoglycemic, hypolipidemic, and antimicrobial effects.
As an antimalarial drug, it acts against malaria parasites, Plasmodium, at the stage when they enter the red blood cells. It causes an acidic environment in parasites, which interferes with their basic life processes.
Chloroquine can easily penetrate cell membranes. Getting into the cell and interacting with hydrogen ions, it is not able to leave and accumulates inside. As a result of retaining hydrogen ions, intracellular pH rises, which leads to important consequences: synthesis of some proteins, including autoantibodies, is reduced, interaction with some receptors is disrupted, and the production of cytokines is lowered. This might explain the immunomodulatory, anti-inflammatory, analgesic, antiplatelet, hypoglycemic, hypolipidemic, and antimicrobial effects of chloroquine. Its photoprotective effect on skin lesions in systemic lupus erythematosus is also known. This effect is probably more related to the antioxidant effect of the drug.
In the treatment of rheumatoid arthritis, it has a delayed clinical effect, occurring 4–12 weeks after the start of the drug.
Indications
Chloroquine is taken as prescribed by a doctor. It is commonly used in the treatment of the following diseases:
Malaria. Chloroquine is used for the treatment and prevention of malaria. Because chloroquine has been widely used around the world since the mid-20th century, malaria parasites have become resistant to the drug in some regions.
Rheumatic diseases. Chloroquine is used to treat autoimmune diseases such as rheumatoid arthritis and lupus erythematosus.
Amoebiasis. Amebiasis is an infectious disease that affects the large intestine (intestinal form) and sometimes invades other tissues and organs (extraintestinal form). Chloroquine may be used in cases where amoebiasis occurs outside the intestines. In amoebic liver abscess, it is used as an additional remedy.
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Doses and administration
The highest daily dose of chloroquine is 1.5 g. The highest single dose is 1 g.
Use in children
- 1–6 years: 1st day — 125 mg, 2–3 days — 50 mg each
- 6–10 years: 1st day — 250 mg, 2–3 days — 125 mg each
- 10–15 years: 1st day — 500 mg, 2–3 days — 250 mg each
For the treatment of extraintestinal amebiasis: 6 mg/kg per day for 2 weeks, followed by a dose reduction by half.
Use in adults
- For malaria prevention: 500 mg 2 times per week, then 500 mg 1 time per week.
- For malaria treatment: 1st day — 1 g once, after 6–8 hours — 500 mg, 2nd and 3rd day — 750 mg once.
- For amoebiasis: 1st week — 500 mg 3 times a day, 2nd week — 250 mg 3 times per day, after that — 750 mg 2 times per week for 2–6 months.
- For rheumatoid arthritis: 1st week — 250 mg 2 times per day. Then 250 mg daily for 12 months.
- For systemic lupus erythematosus: 250–500 mg 1 time per day.
- For photodermatosis: 1st week — 250 mg per day, then 500–750 mg per week.
Contraindications and precautions
Inhibition of cerebral circulation, renal and hepatic insufficiency, psoriasis, neutropenia, cardiac arrhythmias, individual intolerance, children under 12 months of age.
Use with caution: epilepsy, deficiency of glucose-6-phosphate dehydrogenase, retinopathy, myasthenia gravis, diseases of the gastrointestinal tract, hypersensitivity.
Pregnancy and lactation: category C according to FDA. Use with caution during pregnancy and lactation in cases where the intended benefit outweighs the risk to the fetus and newborn.
When using chloroquine, certain precautions should be taken, such as regular monitoring of blood count, blood electrolytes, blood glucose, as well as liver and kidney function. Since the drug can increase the QTc interval, a standard electrocardiogram (ECG) should be performed before administration. Avoid simultaneous use of other drugs that increase QTc (antiarrhythmics, antihistamines, antidepressants, antipsychotics, teneligliptin, etc.). Finally, caution should be exercised in terms of visual impairment and mental disorders development.
Side effects
Common side effects occur due to overdose, allergic reactions to the components of the drug, contraindications, and interactions with other drugs. They can range from mild to extremely severe. This includes:
- Common and mild side effects: nausea, vomit, abdominal pain, headaches, diarrhea, loss of appetite, skin rash, muscle cramps, pain, and atrophy.
- Rare side effects: blurred vision, swelling of the ankles and legs, shortness of breath, pale skin/nails/lips, muscle weakness, hearing impairment, mental problems, mood swings, behavior changes, depression, withdrawal symptoms, hallucinations.
- Serious signs of infection include high fever, severe chills, persistent sore throat, and low blood cell count.
- Itchy skin, especially in Africans, with symptoms of discoloration of the skin, hair loss, and skin rash. This is not common among other races, and its effects increase with age.
- Long-term use of chloroquine can cause retinopathy. Retinal damage may be irreversible.
- Irreversible electrocardiographic changes may occur causing cardiomyopathy.
- There may be a decrease in the number of red blood cells (pancytopenia), aplastic anemia, in which the bone marrow cannot produce red blood cells, which leads to a deficiency, a decrease in the number of granulocyte cells in the blood (agranulocytosis), a decrease in platelets, and neutropenia (a decrease in neutrophils).
- Overdose is responsible for at least 20% of chloroquine deaths.
Summary
Chloroquine is an old and well-studied drug with a wide range of uses. However, to this day, research is being carried out to reveal its new, yet undiscovered properties in the field of fighting viruses and oncological diseases. Chloroquine remains the drug of first choice for malaria (except for its resistant strains). Despite its high safety profile, it can cause mild to serious and even fatal side effects associated with misuse. Chloroquine is not recommended by WHO and FDA for the treatment and prevention of COVID-19. Before use, it is highly advisable to consult a healthcare specialist.
The information we provide on this page is not intended to substitute a physical examination and a consultation in your doctor’s office followed with the prescription of the best-suited medicating. Furthermore, this information may appear incomplete, partial, non-specific and otherwise unfitted to be used as the recommendation basis for any type of treatment. We try to create scientifically accurate copies that go through multiple checkpoints and are curated by professionals, but we reserve the right for occasional errors. Seek doctor’s advice before commencing, renewing or discontinuing any drug. The same concerns recommendations and best practices for drug application, effects, caution and adverse reactions.
