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What are immunosuppressive agents?

Jul 23, 2025 Source: Cainiu Health
Dr. Yang Ziqi
Introduction
Under normal circumstances, immunosuppressants are a class of drugs that suppress the body's immune response. They are commonly used in organ transplantation to prevent rejection and in the treatment of autoimmune diseases. Commonly used medications include cyclosporine, tacrolimus, mycophenolate mofetil, methotrexate, and glucocorticoids. It is recommended to follow medical advice when using these drugs, selecting either monotherapy or combination regimens according to the specific condition, and to regularly monitor drug blood levels as well as liver and kidney function.

Generally, immunosuppressants are a class of drugs that suppress the immune response. They are commonly used in organ transplantation to prevent rejection and in the treatment of autoimmune diseases. Commonly used drugs include cyclosporine, tacrolimus, mycophenolate mofetil, methotrexate, and glucocorticoids. A detailed analysis is as follows:

1. Cyclosporine

Cyclosporine works by inhibiting cytokines required for T lymphocyte activation. It is widely used in kidney and liver transplantation to prevent rejection, as well as in autoimmune diseases such as psoriasis and rheumatoid arthritis. It is incompletely absorbed orally, so therapeutic drug monitoring is necessary to adjust the dosage. Common side effects include nephrotoxicity and hypertension.

2. Tacrolimus

Tacrolimus has a mechanism of action similar to cyclosporine but exhibits stronger immunosuppressive activity. It is suitable for liver and kidney transplantation and atopic dermatitis. It can be administered orally or topically. Systemic use requires caution regarding neurotoxicity, such as tremors, headache, and hyperglycemia, while topical formulations have higher safety profiles.

3. Mycophenolate Mofetil

Mycophenolate mofetil inhibits purine synthesis in lymphocytes, selectively suppressing the proliferation of B and T cells. It is often used in combination with cyclosporine to prevent transplant rejection and is also used in systemic lupus erythematosus. The main side effects are gastrointestinal reactions and bone marrow suppression.

4. Methotrexate

Methotrexate inhibits nucleic acid synthesis by blocking dihydrofolate reductase, thereby suppressing the proliferation of immune cells. It is a first-line medication for rheumatoid arthritis and psoriatic arthritis and is also used in cancer treatment. Administered as a low weekly dose, folic acid supplementation is needed to reduce side effects such as mucosal damage and bone marrow suppression.

5. Glucocorticoids

Glucocorticoids nonspecifically suppress immune responses by inhibiting inflammatory cell infiltration and cytokine release. They are used in various autoimmune diseases, such as systemic lupus erythematosus, ulcerative colitis, and acute episodes of transplant rejection. Long-term use requires attention to side effects such as osteoporosis, hyperglycemia, and central obesity.

When using immunosuppressants, it is recommended to follow medical advice, selecting monotherapy or combination regimens based on the condition. Regular monitoring of drug levels and liver and kidney function is necessary to avoid self-adjustment of dosage. Side effects are related to dose and duration of treatment; appropriate medication use can balance efficacy and safety.

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