Tacrolimus and Other Immunosuppressive Macrolides in Clinical Practice
| Autor: | Ira D. Lawrence, Jun Hiroi, Tadahiro Amaya |
|---|---|
| Rok vydání: | 2003 |
| Předmět: |
medicine.medical_specialty
medicine.drug_class medicine.medical_treatment Antibiotics chemical and pharmacologic phenomena Immunosuppression Pharmacology Biology Cell cycle Organ transplantation Tacrolimus Calcineurin surgical procedures operative Immune system Sirolimus Immunology medicine medicine.drug |
| DOI: | 10.1016/b978-012526451-8/50010-2 |
| Popis: | Publisher Summary This chapter reviews tacrolimus and other immunosuppressive macrolides in clinical practice. Tacrolimus and rapamycin are classified as immunosuppressant drugs that are essentially macrolide derivatives. Tacrolimus inhibits T-cell activation at an early stage of the cell cycle through a calcium-mediated signal. It impedes the early phases of the immune signal transduction pathway in the cell by inactivating the dephosphatase activity of calcineurin. Tacrolimus is regarded as a significant agent in the treatment of a large number of immunologically mediated diseases. The role of tacrolimus-based primary immunosuppression in the prevention of rejection following solid organ transplants, especially liver and kidney transplants is well established. Its unique properties have led to its ability to rescue patients who have experienced rejection while on conventional cyclosporin-based immunosuppressive regimens. On the other hand, rapamycin (sirolimus) is another macrolide antibiotic that possesses potent immunosuppressant activity. Its chemical structure is partially similar to that of tacrolimus. The immunosuppressive effects of rapamycin result from its inhibition of T-cell and B-cell proliferation. The key effect on those cells results from the blocking of the signals of several cytokines, thus leading to interruption of the cell cycle from the G1 to the S phase. Rapamycin is investigated as an adjunctive immunosuppressant agent for prevention of rejection after organ transplantation in combination with cyclosporin and tacrolimus. |
| Databáze: | OpenAIRE |
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