Methotrexate

💊 What is Methotrexate used for?

• •Acute lymphoblastic leukemia (ALL), as part of a combination chemotherapy maintenance regimen, in adults and children
• •Mycosis fungoides (cutaneous T-cell lymphoma) in adults
• •Relapsed or refractory non-Hodgkin lymphoma in adults, as part of a metronomic combination chemotherapy regimen
• •Rheumatoid arthritis in adults
• •Polyarticular juvenile idiopathic arthritis (pJIA) in children
• •Severe psoriasis in adults

How it works

The label describes methotrexate as a dihydrofolate reductase inhibitor. It is a folate-blocking medicine, and the label does not describe its effects in more detail than this.

How it is usually taken

• •Methotrexate is taken by mouth. Many of its uses involve a dose taken once weekly, and the label says that a once-weekly dose is to be taken as a single dose, not once daily. Mistakenly taking a weekly dose once daily has led to fatal reactions. The label says patients and caregivers must take the recommended dose as directed. It should not be given to people who cannot swallow a tablet. The label says the tablets are a cytotoxic drug and require special handling and disposal. Follow the instructions from your prescriber or pharmacist.

Comes as

• •2.5 mg tablets, pale yellow to yellow, round, uncoated, scored, and marked 'C7' on one side
• •Supplied in bottles of 36 and 100 tablets with child-resistant closures

⚠️ Methotrexate side effects

🛑 Who should not take Methotrexate, and who should be careful

The label says not to take it if

• 🚨You are pregnant and are being treated for a condition other than cancer (non-neoplastic disease).
• 🚨You have a history of severe allergic reactions to methotrexate, including anaphylaxis.
• 🚨You are unable to swallow a tablet, according to the dosage section of the label.

Tell your doctor before taking it if

• •Females who could become pregnant should have a pregnancy test before starting. The label says the healthcare provider should verify pregnancy status first.
• •Use effective birth control during treatment and for 6 months after the final dose (females). Males with female partners who can become pregnant should use effective birth control during treatment and for 3 months after the final dose.
• •Tell your healthcare provider right away if you become pregnant or think you might be pregnant.
• •Tell your healthcare provider about all medicines you take, including prescription drugs, over-the-counter drugs, vitamins, and herbal products.
• •Live vaccines are not recommended during treatment. Follow current vaccination guidelines.
• •The label says methotrexate may impair fertility.

🔀 Methotrexate with other medicines, food and alcohol

The label says to discuss these with your doctor or pharmacist

• •Aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs)
• •Oral antibiotics (including neomycin) and penicillin or sulfonamide antibiotics
• •Antifolate drugs such as dapsone, pemetrexed, pyrimethamine, and sulfonamides
• •Proton pump inhibitors
• •Probenecid
• •Hepatotoxic (liver-affecting) or nephrotoxic (kidney-affecting) products
• •Highly protein-bound drugs, such as oral anticoagulants, phenytoin, salicylates, sulfonylureas, and tetracyclines
• •Nitrous oxide anesthesia: the label says to avoid it in patients receiving methotrexate
• •Folic acid or folinic acid: the label says to take these only as directed by your healthcare provider, because they can reduce methotrexate's effectiveness in neoplastic diseases
• •Live vaccines are not recommended

Alcohol and food

The label says the risk of liver damage (hepatotoxicity) increases with heavy alcohol consumption. The label does not give specific food instructions in the text provided.

🤰 Methotrexate in pregnancy and breastfeeding

Pregnancy

The label says methotrexate is contraindicated in pregnant women with non-neoplastic diseases. It says methotrexate can cause embryo-fetal toxicity and fetal death. Exposure during pregnancy is associated with an increased risk of miscarriage and developmental problems. Women with cancer are advised about the potential risk to a fetus, and the label says the treatment decision is made by the patient and healthcare provider. Use effective birth control during treatment and for 6 months after the final dose.

Breastfeeding

The label says not to breastfeed during treatment with methotrexate and for 1 week after the final dose.

🗓️ Storage, missed doses and taking too much

Storage

Store at 20°C to 25°C (68°F to 77°F). Short excursions to 15°C to 30°C (59°F to 86°F) are permitted, according to the label. The tablets are a cytotoxic drug, so follow special handling and disposal procedures. Keep out of reach of children, since the bottles have child-resistant closures.

If a dose is missed

The label does not say.

If too much is taken

The label says overdose, including fatal overdose, has occurred with methotrexate. Symptoms can include low blood counts, bleeding in the stomach or intestines, mouth sores, nausea, and vomiting. Some cases reported sepsis, kidney failure, and aplastic anemia. The label says leucovorin or levoleucovorin is used to diminish the adverse reactions of an overdose. If you think someone has taken too much, contact emergency services or a poison control center right away.

🗒️ Questions to ask about Methotrexate

• Why is a pregnancy test needed before I start this medicine?
• How will you check my blood counts and liver tests during treatment?
• Is my dose meant to be taken once a week? How should I keep track of my dosing day?
• Should I avoid NSAIDs, aspirin, or other pain relievers while taking this medicine?
• What birth control method should I use, and for how long after my last dose?
• What should I do if I have a fever, infection symptoms, or unusual bleeding?
• Can I still take my folic acid or other vitamins?

❓ Methotrexate: frequently asked questions