This page contains brief details about the drug , it's indication, dosage & administaration, mechanism of action, related brands with strength, warnings and common side effects.

Background and Date of Approval

Methotrexate is an anti-metabolite and immunosuppressant drug. The FDA approved this for its medical use on 26th February 1999.

Mechanism of Action of undefined

Methotrexate inhibits dihydrofolic acid reductase. Therefore, methotrexate interferes with DNA synthesis, repair, and cellular replication. Actively proliferating tissues such as malignant cells, bone marrow, fetal cells, buccal and intestinal mucosa, and urinary bladder cells are, in general, more sensitive to this medicine. Blocking these slows down how fast cancer cells grow and spread. In treating rheumatoid arthritis, methotrexate is thought to stop or reduce inflammation in the joints by altering the body's defense mechanism in the immune system.

Uses of undefined

It treats certain types of cancer, such as acute lymphocytic leukemia (ALL), meningeal leukemia, non-hodgkin’s lymphoma, osteosarcoma, cutaneous T-cell lymphoma, breast cancer, and head and neck cancer in adults. It is also used to treat severe psoriasis in adults (a skin disease in which red, scaly patches form on some body areas). It is also indicated to treat rheumatoid arthritis in adults.  

undefined Drug administaration and Dosage available

Methotrexate is available as an injection and tablet. Always use this medicine as exactly prescribed by your doctor. Depending on the condition being treated, your physician decides the dose, dosage, and frequency of this injection. Methotrexate is injected into a vein (intravenously) or into muscle (intramuscularly). Do not self-administer this medicine. 

If you are prescribed with tablets, do not chew, crush or dissolve the tablets. The score line is only there to help you break the tablet if you have difficulty swallowing it whole.  Swallow the tablets whole with water. 

Warnings, Precautions and Side Effects of undefined

Warnings

This drug is indicated to cause serious infections such as bacterial, fungal infections, hepatitis B reactivation, tuberculosis, and pneumonia. This medicine can cause neurotoxicity and increase your chances of developing secondary malignancies (tumors). Immunization with live vaccines is not recommended during the treatment because it can cause infections. This medicine can cause impairment of fertility in males and females. Discuss with your physician if you are trying for pregnancy. 

Precautions

Do not use this medicine if you are allergic to methotrexate or any of the other ingredients of this medicine. Do not take this medicine if you have kidney or liver problems, blood disorders, weakened immune system, pregnant, or breastfeeding. Inform your physician immediately if you experience any symptoms of spitting and coughing up blood, general muscle weakness, vision disturbance, changes in thinking, memory, and orientation problems. Avoid getting pregnant during the treatment and for six months after the last dose. 

Tell your doctor if you have a stomach ulcer, active infection, or mild kidney problems and about any recent vaccinations before starting the treatment. This medicine can cause serious side effects even with low doses; hence, regular follow-ups and routine laboratory tests will be necessary as a precaution. Inform your healthcare provider about all the medicines you take, including prescription, over-the-counter, vaccines, nutritional or vitamin supplements, and herbal products. Certain medications interact with methotrexate and reduce their effectiveness by causing undesirable side effects.

Side Effects

The common side effects of methotrexate are hair loss, photosensitivity, rash, diarrhea, nausea, vomiting, decreased WBC and platelet count, dizziness, tiredness, fever, and shivering, and blurred vision. Serious side effects of this medicine are severe allergic reactions, spitting or coughing blood, chest pain, weakness on one side of the body, and muscle weakness.

Word Of Advice

Do not store above 25°C. Do not freeze. Protect the medicine from light and excessive moisture. Keep the medicine out of reach of children and pets. If you forgot to take the tablet, take it as soon as you remember. However, skip the missed dose if it is nearly time for the next dose. Avoid getting vaccines while using this medicine because it increases your risk of getting infections. This drug can cause sun sensitivity, so use sunscreen when going outdoors. Methotrexate affects male and female infertility; consult your doctor before initiating the treatment if this concerns you.

Male patients with female partners with reproductive potential should use an effective form of birth control during the treatment and 3 months after the last dose. Do not consume alcohol while receiving this medicine because this may increase the risk of liver damage. This medicine may make you bleed, bruise, or get infections more easily. Take precautions to prevent illness and injury. Wash your hands often. Your doctor will do lab tests at regular visits to check on the effects of this medicine. Keep all appointments. Inform your physician if you develop sores or white patches on your lips, mouth, or throat while using this medicine.

Frequently Asked Question

References

  1. Methotrexate tablet - Patient Information Leaflet (PIL) - (emc) [Internet]. www.medicines.org.uk. [Revised March 2022] [cited 2023 Jun 2]. Available from: https://www.medicines.org.uk/emc/product/511/smpc
  2. Hospira, Methotrexate Tablet, Food and drug administration. acess.fda.gov. [Revised August 2020] [cited 2023 Jun 2]. Available from: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/040054s015,s016,s017.pdf
  3. Goodman & Gilman’s, The Pharmacological Basis of Therapeutics, Pharmacotherapy of inflammatory bowel disease, 12th edition, 2011, 1358.
  4. KD Tripathi, Essentials of Medical Pharmacology, Antirheumatoid and antigout drugs, 7th edition, 2013, 211.

Disclaimer

The drug information on this page is not a substitute for medical advice. It is meant for educational purposes only. For further details, consult your doctor about your medical condition to know if you can receive this treatment.