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Chloroquine

Antiparasitic, Antivirals Chloroquine (Generic) Generic drugs, marketed without brand names, contain the exact same active ingredients used in their brand-name counterparts, but cost significantly less. The drugs are required to meet US Food and Drug Administration (FDA) standards for safety, purity and effectiveness.
Chloroquine

Generic chloroquine is a medication that is prescribed to patients in order to treat and prevent acute bouts of certain types of malaria as well as a specific form of parasite infection (extraintestinal amebiasis).

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Chloroquine is a medication primarily used to prevent and treat malaria in areas where malaria remains sensitive to its effects. It is also occasionally used for amebiasis that is occurring outside the intestines, rheumatoid arthritis, and lupus erythematosus. Chloroquine was discovered in 1934 by Hans Andersag and became widely used in the late 1940s. It is on the World Health Organization's List of Essential Medicines, the safest and most effective medicines needed in a health system.

Chemical Properties and Mechanism of Action

Chloroquine is a 4-aminoquinoline compound with a complex chemical structure that includes a quinoline ring and an amino side chain. Its chemical formula is C18H26ClN3, and it is typically administered as chloroquine phosphate or chloroquine sulfate. The drug works by accumulating in the food vacuoles of Plasmodium species, the parasites responsible for malaria. It inhibits the polymerization of heme to hemozoin, leading to the accumulation of toxic heme, which is lethal to the parasite. Additionally, chloroquine has immunomodulatory effects, which make it useful in autoimmune diseases like rheumatoid arthritis and lupus.

Pharmacokinetics

Chloroquine is well-absorbed from the gastrointestinal tract, with bioavailability ranging from 75% to 90%. It is widely distributed in body tissues, including the liver, spleen, kidney, and lungs, and has a large volume of distribution. The drug is metabolized in the liver by cytochrome P450 enzymes, primarily CYP3A4, and its metabolites are excreted in the urine. The half-life of chloroquine is long, ranging from 20 to 60 days, which allows for once-weekly dosing for malaria prophylaxis.

Clinical Uses

  1. Malaria: Chloroquine is used for the prevention and treatment of malaria caused by Plasmodium vivax, Plasmodium ovale, Plasmodium malariae, and some strains of Plasmodium falciparum. However, widespread resistance in P. falciparum has limited its use in many regions. For prophylaxis, it is typically taken once a week, starting 1-2 weeks before traveling to an endemic area and continuing for 4 weeks after leaving.

  2. Amebiasis: Chloroquine is used as an adjunct to other treatments for extraintestinal amebiasis, particularly amebic liver abscess.

  3. Rheumatoid Arthritis and Lupus Erythematosus: Chloroquine and its derivative hydroxychloroquine are used to manage symptoms of autoimmune diseases. They help reduce inflammation and modulate the immune response.

  4. COVID-19: During the COVID-19 pandemic, chloroquine and hydroxychloroquine were investigated as potential treatments. However, subsequent studies found them to be ineffective and associated with significant risks, leading to their disuse for this purpose.

Adverse Effects

Chloroquine is generally well-tolerated, but it can cause a range of adverse effects, particularly with long-term use or high doses. Common side effects include gastrointestinal disturbances (nausea, vomiting, diarrhea), headache, dizziness, and blurred vision. More serious adverse effects include retinopathy, which can lead to permanent vision loss, cardiomyopathy, and myopathy. Chloroquine can also cause hypoglycemia, especially in patients with diabetes, and can exacerbate psoriasis.

Contraindications and Precautions

Chloroquine is contraindicated in patients with known hypersensitivity to 4-aminoquinoline compounds. It should be used with caution in patients with pre-existing retinal or visual field changes, myopathy, or neurological disorders. Due to its potential to cause QT prolongation, it should be avoided in patients with known heart conditions or those taking other QT-prolonging drugs. Regular ophthalmological examinations are recommended for patients on long-term therapy.

Resistance

Resistance to chloroquine has become a significant problem, particularly in P. falciparum. Resistance is primarily due to mutations in the PfCRT (Plasmodium falciparum chloroquine resistance transporter) gene, which reduces the drug's accumulation in the parasite's food vacuole. This has led to the use of alternative antimalarial drugs, such as artemisinin-based combination therapies (ACTs), in many parts of the world.

Historical and Social Impact

Chloroquine played a crucial role in the global fight against malaria, particularly in the mid-20th century. It was a key component of malaria eradication campaigns and significantly reduced malaria-related morbidity and mortality. However, the emergence of resistance has diminished its effectiveness, highlighting the need for ongoing research and development of new antimalarial drugs.

Conclusion

Chloroquine remains an important drug in the medical arsenal, particularly for malaria prophylaxis and treatment in areas without resistance. Its immunomodulatory effects also make it valuable in managing autoimmune diseases. However, its use must be carefully monitored due to the risk of serious adverse effects, and its role in malaria treatment is increasingly limited by resistance. Ongoing research into new antimalarial therapies and strategies to combat resistance is essential to continue the fight against malaria and other diseases for which chloroquine has been historically significant.

Chloroquine Phosphate tablet What kind of medication is this? CHLOROQUINE can be used either as a treatment for malaria or as a preventative measure. Moreover, it is utilized in the treatment of amebiasis. Before I start using this medication, what should I discuss with my primary care physician? People have a right to know if you suffer from any of the following conditions: eye illness, vision difficulties glucose 6-phosphate dehydrogenase (G6PD) deficiency issues with hearing illness of the liver a history of epilepsy and an unusual or adverse reaction to chloroquine, hydroxychloroquine, or any other medications, foods, colors, or preservatives. psoriasis breastfeeding women who are either pregnant or attempting to conceive a child What is the correct way to take this medication? This medication should be taken orally with a full glass of water. To reduce your risk of contracting malaria, take this medication on the same day of each week beginning two weeks before you travel to an area where the disease is prevalent and continuing for eight weeks after you leave the area. Take your dosages at regular intervals. Do not take your medication more frequently than recommended by the label. Have a discussion with your child's physician about the possibility of giving them this medication. There are some circumstances in which this medication may be administered, but there are also certain warnings associated with its use. In the event that you believe you may have taken an excessive amount of this medication, you should immediately contact a poison control center or an emergency facility. PLEASE TAKE NOTE That no one else should use this medication. It is important that others not use this medication. What should I do if I forget a dose? If you forget to take a dosage, you should take it as soon as you remember it. Take only that dose if it is getting close to the time for your next scheduled dose. Do not take duplicate or additional dosages. What other substances could react with this medication? It is not safe to use this drug with any of the medicines listed below: arsenic trioxide chlorpromazine cisapride medications containing droperidol for the treatment of psychotic disorders, depression, or anxiety methadone and other medications for irregular heartbeats and rhythm pentamidine medications include erythromycin and levofloxacin, ranolazine, and others There is a possibility that this treatment will interact negatively with the following medications: ampicillin\santacids cimetidine cyclosporine\skaolin It's probable that this list doesn't cover all of the possible interactions. Provide your primary care physician with a list of all the medications, herbs, over-the-counter pharmaceuticals, and dietary supplements that you are currently using. Additionally let them know whether you are a smoker, a drinker, or if you take any illicit substances. It's possible that certain things might react badly with your medication. What side effects should I be on the lookout for when using this medication? If after a few days your symptoms do not begin to improve, you should consult a physician or another qualified health care expert. If you plan to use this medication for an extended period of time, you should schedule regular checkups with your primary care physician or another qualified medical expert. See your eye doctor for an examination if you've noticed any changes in the clarity of your vision. You should not treat yourself if you develop a fever while taking this medication or after you have started using it. Get in touch with a physician or other qualified health care provider right away. You may become tired or dizzy. Do not operate a motor vehicle, operate heavy machinery, or engage in any activity that requires mental attention until you have determined how this medication affects you. Take it easy when getting up, especially if you are an older patient who needs medical attention. This lowers the likelihood of experiencing periods of lightheadedness or fainting. While traveling through regions where malaria is prevalent, it is important to take precautions to avoid getting bitten by mosquitoes. This includes staying in air-conditioned or well-screened rooms to reduce human-mosquito contact, sleeping under mosquito netting, preferably one with pyrethrum-containing insecticide, wearing long-sleeved shirts or blouses and long trousers to protect arms and legs, applying mosquito repellents containing DEET to uncovered areas of skin, and using a flying insect spray containing pyrethrum to kill mosquitos. Other preventative measures include applying mosquito repellents containing IR This medication has the potential to increase your sensitivity to the sun. Stay out of the direct sunlight. Wear protective gear and be sure to apply sunscreen if you can't help but be outside in the sun. Avoid using sun lamps as well as tanning beds and booths. It is important to wait at least four hours before and after taking a dosage of this medication before consuming any items that include antacids or kaolin. What potential negative reactions may I have to this medication? You should report the following side effects to your physician or another qualified medical expert as soon as possible: Allergic reactions might include rashes, itching, or hives on the skin; swelling of the cheeks, lips, or tongue; and changes or hallucinations in eyesight. ringing in the ears, loss of hearing feelings of dizziness or fainting fever or infection a lack of muscular strength numbness, tingling seizures abnormal bruising or bleeding abnormally weak or exhausted than usual Adverse effects that, in most cases, do not need seeking medical attention (although you should let your doctor or another health care expert know if they persist or become bothersome): a coloring of the skin and nails that is blue-black, and the bleaching of the body hair diarrhea and a loss of hair headache lack of hunger and appetite nausea, vomiting cramping in the stomach It's conceivable that this list doesn't cover all of the potential negative consequences. Where should I store my medication, if you please? Be sure that youngsters can't get their hands on it. Even at very low dosages, this medication poses a risk of fatal overdose in youngsters. Keep at room temperature between 15 and 30 degrees C (59 and 86 degrees F). After the expiration date, any medicine that has been used but not finished should be thrown away.

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