Methotrexate Drugs: Overview of Mechanism, Uses and Side Effects

Methotrexate is a drug that was originally developed and continues to be used for chemotherapy treatment of cancer, with particularly high efficacy in treating breast cancer, head and neck cancers, lymphoma, and lung cancer.

However, over the past few decades it has also found increasing application for the treatment of autoimmune disorders due to its anti-inflammatory and immunosuppressive effects.

Methotrexate Drugs: Mechanism of Action

Methotrexate works by inhibiting the enzyme dihydrofolate reductase (DHFR) which is involved in DNA synthesis and cellular replication. By blocking the action of DHFR, methotrexate affects the synthesis of nucleic acids like DNA, RNA, and proteins that are required for cellular growth and division. This antimetabolite property of methotrexate allows it to be effectively employed against rapidly dividing cancer cells as well as immune cells involved in inflammatory responses.

Uses of Methotrexate Drugs

Some of the major uses of methotrexate include:

Treatment of cancer: Methotrexate Drugs Due to its disruptive effects on cellular replication, methotrexate is used as a chemotherapy drug against various cancers including breast, head and neck, lung, lymphoma etc. It is often combined with other chemotherapy drugs in multiple dose regimens to enhance anticancer effects.

Rheumatoid arthritis: Methotrexate has become a first line treatment for rheumatoid arthritis in doses lower than those used for cancer chemotherapy. By suppressing inflammatory immune responses, it provides effective relief from joint pain, swelling and stiffness associated with RA.

Psoriatic arthritis: The anti-inflammatory properties of methotrexate are also utilized in the treatment of psoriatic arthritis, which involves inflammation of joints along with psoriasis of the skin.

Juvenile idiopathic arthritis: Children with persistent arthritis are often prescribed methotrexate to control disease activity and hinder joint damage at a young age.

Inflammatory bowel disease: Some studies have shown benefits of methotrexate for inducing and maintaining remission in ulcerative colitis and Crohn's disease.

Side Effects of Methotrexate Drugs

While methotrexate can prove highly effective clinically, it also has several potential side effects which must be kept in mind:

Nausea and vomiting: Nausea is a common complaint experienced by around 30% of patients taking methotrexate, which can often be managed with anti-emetics.

Stomatitis: Mouth sores and ulcerations may occur in about 10-20% of patients due to mucosal reactions to the drug.

Liver toxicity: Methotrexate can cause mild to moderate increases in liver enzymes and even potential liver damage at higher doses if monitoring is inadequate.

Lung toxicity: Rarely methotrexate may lead to interstitial pneumonitis causing cough and breathing difficulty.

Bone marrow suppression: Low white blood cell or platelet counts requiring treatment holds can result from methotrexate's effects on proliferation of blood cell precursors.

Folic acid supplements: Taking folic acid supplements 5 days a week can reduce the gastrointestinal side effects linked to methotrexate therapy. Close monitoring under medical supervision is recommended when using this medication.

methotrexate remains one of the most commonly prescribed disease-modifying anti-rheumatic and anti-cancer drugs owing to its good efficacy profile against rapidly dividing cells. However, appropriate patient education regarding potential side effects and need for regular monitoring is important when pursuing methotrexate therapy. With care and precautions, it can provide effective disease control for various indications.

 

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