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Writer's pictureMohammed A Rashad

A Comprehensive Guide on Methotrexate

Updated: Jul 22

Methotrexate Guide by TMMT

Imagine navigating the complexities of a medication that has transformed the treatment landscape for several severe health conditions. Methotrexate, a drug introduced in the 1950s, initially gained fame for its effectiveness in cancer therapy but has since become a cornerstone in managing autoimmune diseases like rheumatoid arthritis and psoriasis. Its versatility in medical use is matched by the depth of considerations required for safe and effective use.


This blog explores Methotrexate, the scientific mechanism behind its effects and practical advice for those it impacts most. Whether you're a patient seeking clarity on your treatment options or a carer looking to understand more about this potent drug, our comprehensive exploration will equip you with the knowledge you need to navigate its benefits and challenges effectively. Read on!


Key Takeaways


What is Methotrexate?


Methotrexate is a chemotherapy agent and immune system suppressant. It is classified as an antimetabolite, specifically a folic acid antagonist, inhibiting folic acid metabolism, vital for DNA synthesis and cell replication. This action makes it highly effective in treating diseases characterized by rapid cell division.


History

The development of Methotrexate dates back to the 1940s when it was first synthesized as part of efforts to identify compounds that could compete with folic acid. Initially used in the 1950s to treat certain types of cancer, its application was later expanded to autoimmune diseases due to its ability to modulate the immune system. 


Over the decades, Methotrexate has been extensively studied, leading to a well-established efficacy and safety profile, making it a mainstay in the treatment protocols for various conditions.


Mechanism of Action

Methotrexate operates primarily by inhibiting dihydrofolate reductase (DHFR), an enzyme critical in the folate pathway. This pathway is essential for the synthesis of nucleotides required for DNA and RNA synthesis. By blocking this pathway, Methotrexate effectively slows down cell replication, particularly in rapidly dividing cells such as those found in malignant tumors and inflammatory responses characteristic of autoimmune disorders.


Methotrexate Uses


Methotrexate serves a dual role in the medical field, acting as a chemotherapeutic and a disease-modifying antirheumatic drug (DMARD). Its uses span various diseases, reflecting its versatility and effectiveness.


  1. Cancer Treatment

Methotrexate is a cornerstone drug in oncology, used primarily to treat leukaemia, breast cancer, and osteosarcoma. It is often administered at high doses in cancer therapy, where its ability to inhibit cell multiplication can effectively destroy cancer cells.

  1. Autoimmune Disorders

In lower doses, Methotrexate is used to treat autoimmune conditions such as rheumatoid arthritis. It helps reduce joint damage and enhance physical function by suppressing the immune system's abnormal activity. It is also prescribed for psoriasis, where it can reduce the rapid skin cell turnover associated with the disease.

  1. Ectopic Pregnancy


In specific cases, Methotrexate is used to treat ectopic pregnancies. This application utilises the drug's cytotoxic effects to stop the growth of the embryo in a non-viable pregnancy, thus preserving the mother's health and future fertility.


Administration of Methotrexate


Forms of Methotrexate

Methotrexate is available in several forms, catering to different treatment requirements and patient preferences. The most common forms include oral tablets and subcutaneous or intramuscular injections. 


Oral tablets are often used for long-term treatment of conditions like rheumatoid arthritis, while injections are preferred in cancer chemotherapy to ensure higher bioavailability and quicker therapeutic effects.


Recommended Methotrexate Dose


The dosage of Methotrexate varies widely depending on the condition being treated, the patient's overall health, and their response to therapy. For rheumatoid arthritis, a typical starting dose might be low, gradually increasing based on patient tolerance and clinical response. 


In contrast, higher doses are often necessary for cancer treatment. A healthcare professional must manage dosing to avoid toxicity.


Tips on Administration and Adherence


Adherence to the prescribed Methotrexate regimen is vital for its effectiveness. Patients are advised to follow a consistent schedule, particularly with oral forms, to maintain stable drug levels in the body. It is also important to monitor for any side effects and communicate with healthcare providers about any concerns. 


Regular blood tests are required to monitor liver function and blood cell counts to adjust dosing and prevent complications.


Methotrexate Side Effects

Methotrexate  Guide by TMMT


Methotrexate can cause a range of side effects, which vary in severity and are influenced by the dosage and duration of treatment. Understanding these side effects can help patients and caregivers manage them effectively.


Common Side Effects

The most frequently encountered side effects include nausea, fatigue, and dizziness. These are generally mild and can often be managed with supportive care or dosage adjustments. Oral ulcers, mild hair loss, and headaches are also common but usually reversible upon cessation of therapy or dosage reduction.


Serious Adverse Effects

More severe side effects include liver toxicity, which can be life-threatening. Regular liver function tests are essential to monitor health and adjust treatment as needed. Methotrexate can also cause pulmonary toxicity, presenting as a cough or shortness of breath, which requires immediate medical attention.


Long-term Risks

Due to its immunosuppressive effects, long-term use of methotrexate can increase the risk of infections. Patients may also experience bone marrow suppression, leading to anaemia, leukopenia, or thrombocytopenia. Regular monitoring through complete blood counts is critical to detect these effects early and manage them appropriately.


Conclusion

Methotrexate is a key treatment for various severe health conditions, offering significant benefits when managed correctly. Despite its potential side effects, with careful oversight, it can greatly improve patient outcomes. Ensuring a deep understanding and meticulous management of Methotrexate is essential for both healthcare providers and patients.


Enhance Methotrexate management in your practice or PCN with The Medicines Management Team (TMMT). Our experienced team of clinical practitioners and GPs is dedicated to delivering efficient medicines management services, easing the burdens of primary care. 


Contact us today to improve your processes and patient care.


FAQs


What is methotrexate used for?

Methotrexate is primarily used to treat certain types of cancer, such as leukaemia, breast cancer, and osteosarcoma. It is also widely prescribed for autoimmune diseases like rheumatoid arthritis and psoriasis, where it helps control inflammation and slow disease progression.

Why is methotrexate high risk?

What is the most common complication of methotrexate?

Is methotrexate a steroid or chemotherapy?


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