Pyrimethamine NEW

Pyrimethamine Cas 58-14-0

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Pyrimethamine is a prescription medication used primarily to treat and prevent certain serious parasitic infections. It belongs to a class of drugs known as antimalarials and antiprotozoals.

Its most common brand name is Daraprim.

How Does It Work?

Pyrimethamine works by inhibiting a key enzyme in parasites called dihydrofolate reductase.

• Folate is Essential: Parasites need folate to create DNA and RNA, which are essential for their growth and reproduction.

  Blocking the Process: By blocking this enzyme, pyrimethamine stops the parasite from using folate.

  Stopping Reproduction: This effectively halts the growth and multiplication of the parasite, allowing the body's immune system to clear the infection.

It's important to note that pyrimethamine is bacteriostatic (stops growth) rather than bactericidal (directly kills) against the parasites.

Primary Medical Uses

Pyrimethamine is almost always used in combination with other medications to enhance its effect and prevent parasite resistance.

1. Toxoplasmosis

This is one of its most critical uses. Toxoplasmosis is an infection caused by the parasite Toxoplasma gondii.

• Who needs it: It is a first-line treatment, used in combination with a sulfonamide antibiotic (like sulfadiazine) and folinic acid (leucovorin).

  At-Risk Populations: It is crucial for:

• People with HIV/AIDS, where toxoplasmosis can cause life-threatening brain infections.

  Pregnant women who have acquired the infection (to prevent transmission to the fetus, though this requires careful risk-benefit analysis by a doctor).

  Individuals with weakened immune systems, such as organ transplant recipients.

2. Malaria

Pyrimethamine is used for both prevention and treatment of malaria, but it is never used alone due to widespread resistance.

• In Combination: It is combined with sulfadoxine in a well-known medication called Fansidar.

  Use Case: This combination is used for:

• Intermittent Preventive Therapy (IPT) in pregnant women and infants in high-risk areas.

  Treatment of uncomplicated malaria caused by Plasmodium falciparum in specific regions where the parasite is still sensitive.

3. Isosporiasis

It is also used, in combination with other drugs, to treat Isospora belli infections, which can cause severe diarrhea in immunocompromised individuals.

Important Considerations and Side Effects

1. Black Box Warning

Pyrimethamine carries a Black Box Warning from the FDA, its strongest safety alert. This is primarily due to:

• Bone Marrow Suppression: The drug can cause a severe decrease in blood cells (anemia, low white blood cells, low platelets), which can lead to infections, bleeding, and fatigue.

2. Folinic Acid (Leucovorin) is Essential

To mitigate the bone marrow toxicity, patients must take folinic acid (also called leucovorin) concurrently.

• Why? Folinic acid is a form of folic acid that the human body can use, but the parasite cannot. It "rescues" the human bone marrow from the effects of pyrimethamine, reducing the risk of dangerous side effects, without helping the parasite survive.

3. Common Side Effects

• Bone marrow suppression (see above)

  Loss of appetite, vomiting, or diarrhea

  Headache, dizziness, or insomnia

  Skin rashes

Key Takeaways

• What it is: A powerful antiparasitic drug.

  Main Use: Treating toxoplasmosis, especially in immunocompromised patients, and malaria (in combination).

  Key Mechanism: Stops parasites from using folate to grow.

  Critical Safety Note: It requires close medical supervision and must be taken with folinic acid to prevent severe bone marrow toxicity.

  Availability: It is a prescription-only medication, famously known by the brand name Daraprim.

Disclaimer: This information is for educational purposes only. Always consult a qualified healthcare professional for diagnosis and treatment of medical conditions. Do not self-prescribe pyrimethamine.

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