Methotrexate

What is it?

Composition

Methotrexate contains the active substance methotrexate, which determines the main action of the drug. Depending on the dosage form, the composition may vary slightly, but the main components remain unchanged.

• Methotrexate (active substance) is the main active substance that inhibits the enzyme dihydrofolate reductase.
• Fillers are auxiliary substances that ensure stability and correct dosage of the drug. In tablet forms, these can be lactose, starch, talc and magnesium stearate.
• Solvents - in injection forms of methotrexate, various solutions are used to create the necessary concentration and facilitate the administration of the drug.

Each dosage form of methotrexate, be it tablets or injections, contains optimal proportions of the active substance and auxiliary components that ensure the effectiveness and safety of the drug.

How to use?

Methotrexate can be used in different forms and dosages depending on the disease, the patients age and other individual factors. Typically, the drug is prescribed by a doctor and requires strict adherence to the dosing regimen.

1. Tablets: Taken by mouth, usually once a week. It is important to take methotrexate on the same day of the week to avoid overdose and minimize the risk of side effects.
2. Injections: The drug can be administered subcutaneously, intramuscularly or intravenously, depending on the indication and the patients condition. Injections are also often prescribed once a week and can be administered by either a healthcare professional or the patient themselves after appropriate training.
3. Concomitant therapy: In some cases, methotrexate is taken with folic acid to reduce the risk of toxicity. Folic acid is usually prescribed the day after taking methotrexate.

It is important to remember that the dosage of methotrexate should be strictly individual and prescribed by a doctor. Self-medication or changing the dosage without consulting a specialist can lead to serious health consequences.

How does it work?

Methotrexate works by inhibiting the enzyme dihydrofolate reductase, which plays a key role in the synthesis of DNA, RNA, and proteins. This enzyme is involved in converting dihydrofolate into tetrahydrofolate, which is necessary for the synthesis of purines and thymidylate, which are essential components for cell growth and division.

When methotrexate blocks this process, it slows down or completely stops cell division. This is especially important in the context of treating malignant neoplasms, where it is necessary to suppress the proliferation of cancer cells. In the case of autoimmune diseases such as rheumatoid arthritis, methotrexate reduces inflammation and suppresses excessive activity of the immune system, reducing the autoimmune attack on the bodys own tissues.

Thus, methotrexate acts at the cellular level, controlling the processes of cell division and activity, which makes it effective both in oncology and in the treatment of autoimmune diseases.

Indications

Methotrexate is used to treat a wide range of conditions, mostly related to excessive cell division or abnormal immune system activity. This drug is often prescribed for the following conditions:

• Oncology: Methotrexate is used to treat various forms of cancer, including acute lymphoblastic leukemia, breast cancer, ovarian cancer, and lymphomas. It helps slow the growth of malignant cells and can be used either as a monotherapy or in combination with other chemotherapy agents.
• Autoimmune diseases: The drug is widely used in the treatment of rheumatoid arthritis, where it helps reduce inflammation and slow the progression of the disease. Methotrexate is also used in psoriasis and psoriatic arthritis to reduce skin manifestations and joint pain.
• Ectopic pregnancy: In some cases, methotrexate is used to terminate an ectopic pregnancy in the early stages, which allows avoiding surgical intervention.

This drug has many indications, and its effectiveness is due to the ability to control cell division and modulate immune activity, which makes it useful in a variety of diseases that require suppression of abnormal cell growth.

Contraindications

Despite its widespread use and effectiveness, methotrexate has a number of contraindications that must be taken into account before starting treatment. Incorrect use of the drug can lead to serious complications, so it is important to know in which cases its use is prohibited.

• Pregnancy and lactation: Methotrexate is strictly contraindicated during pregnancy, as it can cause teratogenic effects and lead to miscarriage or birth defects. Also, the drug is not recommended for breastfeeding, as it can be transmitted through milk and negatively affect the child.
• Liver and kidney failure: The drug is contraindicated in patients with severe liver and kidney dysfunction, since methotrexate is metabolized and excreted mainly through these organs, which increases the risk of toxicity.
• Infectious diseases: In case of active infections, especially those caused by viruses, bacteria or fungi, methotrexate is contraindicated due to its immunosuppressant effect, which can worsen the condition and slow recovery.
• Hypersensitivity: If the patient has previously had allergic reactions to methotrexate or its components, the use of the drug is prohibited.

Side effects

Methotrexate, despite its effectiveness, can cause a number of side effects that vary depending on the dosage, duration of treatment and individual patient characteristics. Most side effects are related to the drugs effect on rapidly dividing cells in the body.

• Digestive system: Methotrexate can cause nausea, vomiting, diarrhea and abdominal pain. Sometimes there is inflammation of the mucous membrane of the mouth and throat, which can lead to ulcers and discomfort.
• Hematopoietic system: The drug can cause a decrease in the level of white blood cells, platelets and red blood cells, which increases the risk of infections, bleeding and anemia. Therefore, it is important to regularly monitor blood counts during treatment.
• Liver and kidneys: Long-term use of methotrexate can lead to impaired liver and kidney function, which requires regular monitoring of these organs. Changes in blood chemistry tests, such as increased liver enzymes, may occur.
• Immune system: The immunosuppressant effect of the drug increases the risk of developing infections, including opportunistic infections that do not usually cause disease in healthy people.
• Skin and mucous membranes: Skin reactions such as rash, redness, itching, and hair loss (alopecia) are possible, especially at high doses of the drug.