雷帕鸣的作用和副作用

The main component of rapamycin is sirolimus. The mechanism of action of sirolimus is that sirolimus (rapamin) inhibits the activation and proliferation of T lymphocytes stimulated by antigens and cytokines (interleukin-2, IL-4? and IL-15) through a completely different mechanism from other immunosuppressants. Rapamin (sirolimus tablets, sirolimus) also inhibits the production of antibodies. In cells, sirolimus binds to the immunophilin, FK-binding protein-12 (FKBP-12), to generate an immunosuppressive complex.

Rapamin (sirolimus) and FK506 are structural homologs. Although they act on the same receptor, their immune action mechanisms are different. FK506 inhibits the proliferation of T lymphocytes from the G0 phase to the G1 phase, while sirolimus (rapamin) blocks signaling through different cytokine receptors, blocking the progression of T lymphocytes and other cells from the GI phase to the S phase. Compared with FK506, sirolimus can block the calcium-dependent and calcium-independent signaling pathways P1 of T lymphocytes and B lymphocytes.

Clinical trials explore the clinical efficacy and safety of rapamycin in kidney transplantation. The trial shows that rapamin (sirolimus tablets, sirolimus) has a significant therapeutic effect, but some side effects may also occur during treatment with rapamin (sirolimus tablets, sirolimus). The very common side effects of sirolimus (according to the frequency classification of the International Council of Medical Organizations, the incidence rate is 10%) include: lymphocele, peripheral edema, abdominal pain, diarrhea, hypokalemia, increased lactate dehydrogenase, acne, urinary tract infection; very common at higher doses: anemia, hypercholesterolemia, thrombocytopenia, hypertriesteremia (hyperlipidemia), etc.