Primaquine

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Generic Name of Primaquine - Learn More

Primaquine

Primaquine Precaution - What You Need to Know

Before using Primaquine, patients should always consult their healthcare provider, as there are several important precautions to consider:

- Glucose-6-phosphate dehydrogenase (G6PD) deficiency: Primaquine can cause hemolytic anemia in individuals with G6PD deficiency. Testing for G6PD deficiency should be conducted before prescribing this medication. If G6PD deficiency is present, Primaquine is generally contraindicated or must be used under careful medical supervision with lower doses.
- Pregnancy and breastfeeding: Primaquine is classified as a Category D drug during pregnancy, meaning it may cause harm to the fetus, particularly if taken in high doses. It should only be used during pregnancy if the benefits outweigh the risks, typically in cases of malaria. Pregnant women, especially in the first trimester, should consult their healthcare provider about the potential risks. Primaquine also passes into breast milk, so it should be used cautiously during breastfeeding.
- Liver disease: People with liver dysfunction may experience altered metabolism and clearance of Primaquine. In such cases, the dose may need adjustment, and close monitoring for side effects is advised.
- Heart disease: Primaquine can potentially cause QT interval prolongation, so caution is needed for patients with heart disease, particularly those with arrhythmias or those on other drugs that affect the QT interval.
- Bone marrow suppression: Pregnant women or patients with a history of bone marrow suppression or blood disorders should use Primaquine with caution, as it can cause hematological side effects, including leukopenia and thrombocytopenia.
- Use with other medications: Patients should inform their healthcare provider of any other medications, including over-the-counter drugs and herbal supplements, as Primaquine can interact with other treatments and increase the risk of adverse effects.

Primaquine Indication - Uses and Benefits

Primaquine is primarily indicated for the treatment and prevention of malaria, particularly for the following:

- Plasmodium vivax and Plasmodium ovale malaria: Primaquine is used to target the dormant liver stage (hypnozoites) of these parasites, helping to prevent relapse after initial treatment with other antimalarial drugs, such as chloroquine.
- Prevention of malaria relapse: It is used as a radical cure in combination with other antimalarial medications to eliminate the liver stages of Plasmodium vivax and Plasmodium ovale, thus preventing relapses.
- P. falciparum malaria: Although not first-line therapy for acute malaria caused by Plasmodium falciparum, Primaquine may be used in certain cases for treating the gametocytes of P. falciparum, helping to reduce transmission of the parasite.
- Malaria prophylaxis: In some cases, Primaquine is used as part of a preventive regimen to reduce the risk of malaria in travelers to regions where malaria is endemic, though it is often not the primary medication for prevention.

Primaquine Contraindications - Important Warnings

Primaquine is contraindicated in the following situations:

- G6PD deficiency: Patients with G6PD deficiency should not take Primaquine unless absolutely necessary, as the drug can induce hemolysis (destruction of red blood cells), leading to severe anemia and other complications.
- Pregnancy: Primaquine should generally be avoided in pregnancy, particularly during the first trimester, due to potential teratogenic effects. It is also contraindicated during breastfeeding, as the drug passes into breast milk and could potentially harm the infant.
- Liver disease: In patients with severe liver impairment, Primaquine should be avoided, as it is metabolized in the liver and altered liver function could lead to toxicity or reduced efficacy.
- History of blood disorders: Patients with a history of hemolytic anemia or other blood disorders should avoid Primaquine, particularly if they have G6PD deficiency or other conditions that predispose them to blood cell damage.
- Severe cardiac disease: In patients with heart arrhythmias or other serious heart conditions, Primaquine may be contraindicated due to the risk of QT prolongation.

Primaquine Side Effects - What to Expect

Common and severe side effects of Primaquine include:

- Common side effects:
- Nausea and vomiting: Some individuals may experience gastrointestinal disturbances, including nausea, vomiting, and stomach discomfort.
- Headache: Headaches are a frequently reported side effect, particularly when starting treatment.
- Dizziness: Dizziness and lightheadedness may occur, especially when standing up quickly.
- Rash: Mild skin reactions, such as rashes, may occur, but these are usually not serious.
- Abdominal pain: Some patients may experience abdominal discomfort or cramping.

- Serious side effects:
- Hemolytic anemia: Particularly in individuals with G6PD deficiency, Primaquine can cause the breakdown of red blood cells, leading to severe anemia, jaundice, and fatigue. Regular screening for G6PD deficiency should be done before initiating treatment.
- Bone marrow suppression: In rare cases, Primaquine may cause a reduction in white blood cells or platelets, leading to infections or bleeding.
- QT prolongation: Primaquine has been associated with QT interval prolongation on the electrocardiogram (ECG), which can lead to arrhythmias and potentially fatal heart issues, particularly when combined with other drugs that affect the QT interval.
- Liver toxicity: Rarely, Primaquine can cause liver toxicity, particularly in individuals with pre-existing liver conditions.
- Severe allergic reactions: Though rare, severe allergic reactions, including difficulty breathing, swelling of the face or throat, and anaphylaxis, can occur.

Patients should promptly report any side effects, particularly signs of hemolytic anemia (e.g., fatigue, jaundice) or heart problems (e.g., palpitations, irregular heartbeats), to their healthcare provider.

Primaquine Pregnancy Category ID - Safety Information

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Primaquine Mode of Action - How It Works

Primaquine is an antimalarial drug that works by targeting the liver stages of certain species of malaria-causing parasites, specifically Plasmodium vivax and Plasmodium ovale. Its mechanism of action involves:

- Inhibition of parasite metabolism: Primaquine interferes with the metabolic processes of the malaria parasite, particularly by disrupting the parasite's ability to utilize oxygen and other vital compounds.
- Targeting the liver stage (hypnozoites): Primaquine is unique in its ability to target the dormant liver stage (hypnozoites) of Plasmodium vivax and Plasmodium ovale. This helps prevent relapse and reactivation of malaria, which can occur months or years after the initial infection.
- Inhibition of gametocytes: Primaquine also acts on the gametocytes of Plasmodium falciparum, the sexual form of the parasite that is responsible for transmitting the disease to mosquitoes. This action helps reduce the transmission of malaria.

The drug’s specific effects on the liver stages and its ability to eliminate dormant forms of the parasite are key in ensuring a radical cure for malaria and preventing relapses.

Primaquine Drug Interactions - What to Avoid

Several drug interactions may alter the effectiveness or safety of Primaquine:

- Other antimalarial drugs: Combining Primaquine with other antimalarial medications, such as chloroquine, quinine, or artemisinin derivatives, may increase the risk of side effects or reduce the effectiveness of one or both medications.
- CYP450 enzyme inhibitors or inducers: Primaquine is metabolized by the liver enzymes, particularly CYP2D6 and CYP3A4. Drugs that inhibit or induce these enzymes may alter the metabolism of Primaquine, leading to higher or lower blood concentrations of the drug.
- CYP450 inhibitors (e.g., fluoxetine, quinine, ritonavir) can increase the levels of Primaquine in the blood, leading to an increased risk of toxicity.
- CYP450 inducers (e.g., rifampin, phenytoin) may decrease the drug's effectiveness by accelerating its metabolism.
- Medications that prolong the QT interval: Since Primaquine may cause QT interval prolongation, concurrent use with other medications that also prolong the QT interval (such as antiarrhythmics, antipsychotics, and macrolide antibiotics) should be avoided, as this increases the risk of serious heart arrhythmias.
- Blood pressure medications: There is a possibility that Primaquine, in combination with certain antihypertensive drugs, may increase the risk of orthostatic hypotension or fainting episodes due to its vasodilation effects.
- Sulfonylureas: Primaquine may potentiate the hypoglycemic effects of sulfonylureas (used to treat diabetes), increasing the risk of low blood sugar.

Primaquine Adult Dose - Recommended Dosage

The dosing of Primaquine in adults depends on the condition being treated:

- For radical cure of Plasmodium vivax and Plasmodium ovale: The typical dose is 30 mg daily for 14 days. This dose is used to target the dormant liver stage of the parasite.
- For gametocidal therapy in P. falciparum: 45 mg daily for 7 days.
- For prevention of relapse: The dosing regimen may vary based on the severity of the infection and other patient factors, but it typically involves 30 mg daily for 14 days.

Patients should follow the healthcare provider’s instructions regarding duration and dosage adjustments, as long-term use or incorrect dosing may lead to adverse effects.

Primaquine Child Dose - Dosage for Children

For pediatric patients, Primaquine dosing is based on weight and the specific condition being treated:

- For radical cure of Plasmodium vivax and Plasmodium ovale: The dose is typically 0.5 mg/kg/day for 14 days, not

exceeding the adult dose of 30 mg daily.
- For gametocidal therapy in P. falciparum: The dose is usually 0.5 mg/kg/day for 7 days.

Pediatric dosing may vary depending on specific clinical needs, and healthcare providers should carefully monitor for side effects in children due to the risk of toxicity, especially if G6PD deficiency is present.

As always, dosing and treatment plans should be individualized by a healthcare provider based on the patient’s age, weight, and medical history.

Primaquine Renal Dose - Dosage for Kidney Conditions

Primaquine is primarily metabolized in the liver and excreted in the urine. In patients with renal impairment, dose adjustments may be necessary:

- Mild to moderate renal impairment: No significant dose adjustment is usually required, but the patient should be monitored for side effects.
- Severe renal impairment: In patients with severe kidney disease (e.g., creatinine clearance < 30 mL/min), the use of Primaquine should be avoided or the dose may need to be reduced. Close monitoring is required for potential toxicity.