ALPHACHYMOTRYPSIN Price

Overview

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Name

Chloroquine Phosphate

Precaution

Chloroquine phosphate is an antimalarial medication also used to treat and prevent malaria and certain autoimmune conditions such as rheumatoid arthritis and lupus. However, there are important precautions to consider when prescribing or using this drug: - **Pregnancy and breastfeeding**: Chloroquine is classified as a category C drug during pregnancy, meaning it should only be used if the benefits outweigh the risks. It is generally considered safe for use during pregnancy, especially for malaria prophylaxis or treatment, but should only be administered under medical supervision. In breastfeeding, chloroquine is excreted in small amounts into breast milk, but the risk to a nursing infant is minimal; nevertheless, careful monitoring is advised. - **Eye health**: Chloroquine may cause retinal toxicity with prolonged use, which can lead to irreversible damage to vision. Regular ophthalmologic exams are recommended for patients on long-term therapy, especially those on doses greater than 3.5 mg/kg/day. - **Renal and hepatic impairment**: Chloroquine should be used with caution in patients with pre-existing liver or kidney disease, as these conditions may impair the drug's clearance, increasing the risk of toxicity. Dosage adjustments may be required. - **G6PD deficiency**: Individuals with glucose-6-phosphate dehydrogenase (G6PD) deficiency may experience hemolytic anemia when using chloroquine. It is important to screen for G6PD deficiency in at-risk populations before starting treatment. - **Cardiac risks**: Chloroquine has been associated with QT interval prolongation, which may lead to serious arrhythmias. It should be used cautiously in patients with existing heart conditions or in combination with other drugs that prolong the QT interval. - **Drug interactions**: Chloroquine may interact with various medications, including antacids, other antimalarials, and certain antibiotics. Careful monitoring is required when combined with these agents to avoid additive toxicities.

Indication

Chloroquine phosphate is primarily used to treat and prevent malaria caused by Plasmodium species, particularly P. falciparum, the most common and severe form of malaria. It is effective in treating both acute malaria and for the prevention of malaria in regions where chloroquine resistance is not widespread. Key indications include: - **Malaria treatment**: Chloroquine is first-line therapy for treating uncomplicated malaria caused by P. falciparum in areas where resistance is low. It is also used to treat malaria caused by P. vivax, P. ovale, and P. malariae. - **Malaria prophylaxis**: It can be used for the prevention of malaria in travelers to areas where malaria is endemic, particularly in areas without chloroquine-resistant strains. - **Autoimmune conditions**: Chloroquine is also indicated in the management of autoimmune diseases such as rheumatoid arthritis, lupus erythematosus, and chronic discoid lupus. It helps to reduce inflammation and modulate immune system activity. - **Off-label uses**: Chloroquine has been studied and occasionally used off-label in the treatment of other conditions, such as amebiasis and certain skin disorders, though it is not FDA-approved for these purposes.

Contra indication

There are several conditions where chloroquine phosphate should not be used due to safety concerns: - **Hypersensitivity**: Patients with a known allergy or hypersensitivity to chloroquine or any related compounds should avoid this medication due to the risk of serious allergic reactions. - **Retinal or visual field changes**: Chloroquine should not be used in patients with pre-existing retinal or visual field changes, particularly those caused by chloroquine or hydroxychloroquine use in the past, as the drug can exacerbate retinal damage. - **Severe liver or kidney disease**: Chloroquine is metabolized in the liver and excreted by the kidneys, so patients with severe liver or renal impairment are at an increased risk of toxicity. Dosage adjustments or an alternative medication may be necessary. - **G6PD deficiency**: Individuals with G6PD deficiency are at risk of hemolytic anemia when taking chloroquine, and this condition should be screened for before starting therapy. - **Children under 6 years**: The use of chloroquine in children under 6 years is not recommended unless absolutely necessary, and the dose should be carefully adjusted based on weight.

Side Effect

Chloroquine phosphate, like many medications, can cause a range of side effects, which vary in severity: - **Common side effects**: - **Gastrointestinal disturbances**: Nausea, vomiting, and diarrhea are relatively common side effects, especially at the beginning of treatment. Taking the medication with food can help minimize these effects. - **Headache and dizziness**: Some patients may experience headaches or dizziness, which are generally mild and transient. - **Skin reactions**: Rashes and itching can occur, although they are typically mild. If a rash persists or worsens, it should be evaluated by a healthcare provider. - **Serious side effects**: - **Retinal toxicity**: Long-term use of chloroquine can lead to irreversible retinal damage, particularly with high doses, leading to blurred vision, difficulty reading, and eventually blindness. Regular eye exams are recommended for patients on long-term therapy. - **Cardiac effects**: Chloroquine may cause QT interval prolongation, leading to an increased risk of life-threatening arrhythmias, especially when used with other medications that prolong the QT interval. - **Hemolysis in G6PD deficiency**: Individuals with G6PD deficiency are at risk of hemolytic anemia when taking chloroquine. Symptoms of hemolysis include fatigue, pallor, jaundice, and dark urine. - **Less common side effects**: - **Myopathy or muscle weakness**: In rare cases, chloroquine can cause muscle weakness or damage, particularly with prolonged use. - **Hearing loss**: High doses of chloroquine have been linked to auditory toxicity, leading to hearing impairment. - **Management of side effects**: Reducing the dose, discontinuing the drug, or switching to a different therapy may be necessary if serious side effects occur. Regular monitoring and follow-up visits are recommended.

Pregnancy Category ID

3

Mode of Action

Chloroquine phosphate works by inhibiting the growth and replication of the malaria parasite, Plasmodium, in the body. Its mode of action involves: - **Inhibition of heme polymerization**: Chloroquine interferes with the parasite’s ability to digest hemoglobin in red blood cells. It accumulates in the food vacuole of the parasite, preventing the polymerization of heme into non-toxic forms. This leads to the accumulation of toxic free heme, which kills the parasite. - **Effect on the immune system**: In autoimmune diseases like lupus, chloroquine acts as an immunomodulator, suppressing the activity of the immune system. This helps to reduce inflammation and immune-mediated damage in conditions such as rheumatoid arthritis and lupus. - **Pharmacokinetics**: Chloroquine is absorbed from the gastrointestinal tract and distributed widely in tissues, including the liver, lungs, and spleen. It has a long half-life (approximately 30-60 days), which makes it effective for both acute treatment and long-term prophylaxis in malaria. - **Resistance**: Resistance to chloroquine has emerged in certain malaria-endemic regions, primarily due to mutations in the Plasmodium falciparum parasite. Resistance reduces the drug's effectiveness, leading to the use of alternative therapies like artemisinin-based combination treatments.

Interaction

Chloroquine phosphate can interact with several other medications, which may affect its efficacy or increase the risk of adverse effects: - **Antacids and laxatives**: The absorption of chloroquine can be reduced when taken concurrently with antacids containing aluminum or magnesium. This may lead to decreased effectiveness, especially in malaria treatment. It is recommended to separate the administration of chloroquine and these agents by at least 4 hours. - **Cimetidine**: Cimetidine may increase chloroquine levels by inhibiting its metabolism in the liver, leading to an increased risk of side effects. Monitoring of chloroquine levels is recommended if these drugs must be used together. - **Other antimalarials**: Combining chloroquine with other antimalarial drugs, particularly those that are also hepatically metabolized, can increase the risk of liver toxicity. Careful monitoring of liver function is needed. - **Cardiovascular drugs**: Chloroquine may interact with drugs that affect the heart’s rhythm, such as digoxin or other QT-prolonging agents, increasing the risk of serious arrhythmias. ECG monitoring may be necessary in patients receiving such combinations. - **Rifampicin**: Rifampicin can reduce the plasma levels of chloroquine, potentially reducing its effectiveness in the treatment of malaria.

Pregnancy Category Note

Information not available

Adult Dose

The adult dosage for chloroquine phosphate varies depending on the condition being treated: - **For malaria treatment**: - **Acute malaria**: The standard regimen is 600 mg (base) of chloroquine phosphate as an initial dose, followed by 300 mg after 6 hours and another 300 mg after 24 hours. - **Malaria prophylaxis**: 300 mg (base) once weekly, starting 1-2 weeks before travel to a malaria-endemic area and continuing for 4 weeks after leaving the area. - **For autoimmune diseases (e.g., lupus, rheumatoid arthritis)**: The initial dose is typically 200 mg to 400 mg daily, depending on the severity of the disease and the patient's response. The dose may be adjusted after several weeks of treatment. - **Dosage adjustments**: Dose reductions may be necessary in patients with renal or hepatic impairment or in those who experience side effects, especially retinal toxicity.

Child Dose

Chloroquine phosphate dosing in children is based on body weight: - **For malaria treatment**: - The dose is generally 10 mg/kg of chloroquine base for the initial dose, followed by 5 mg/kg after 6 hours and 5 mg/kg after 24 hours. - Prophylactic doses for children are typically 5 mg/kg once a week. - **For autoimmune conditions**: Dosing in children for conditions like lupus or rheumatoid arthritis is not as common but may involve 2.5 mg/kg daily. Children should be monitored for side effects, including visual changes, especially during prolonged therapy.

Renal Dose

Chloroquine phosphate is primarily excreted by the liver, and renal impairment does not require significant dosage adjustments. However, in cases of severe renal insufficiency, the drug’s clearance may be delayed, and there is a potential risk for accumulation and toxicity. Caution is advised in patients with renal disease, and these patients should be monitored closely for side effects, especially those related to cardiac and retinal toxicity.

Administration

Information not available