雷帕鸣适用于治疗哪些病症?
What conditions is (Rapamune) used to treat? Let’s find out together below. Rapamune was approved by the FDA on May 30, 2007 for the treatment of advanced kidney disease and kidney transplantation. It has now entered clinical phase 4 for the treatment of mantle cell lymphoma.
As mentioned in the efficacy and role of Rapamune, Rapamune is suitable for patients receiving kidney transplants to prevent organ rejection. Recommended for use in combination with cyclosporine and corticosteroids. Sirolimus, the main component of Rapamune, inhibits the activation and proliferation of T lymphocytes stimulated by antigens and cytokines (interleukins IL-2, IL-4 and IL-15). It also inhibits the production of antibodies.
In cells, rapamune binds to the immunophilin, FK-binding protein-12 (FKBP-12), to generate the FKBP-12 immunosuppressive complex. This complex binds to the mammalian sirolimus BA molecule (mTOR, a key regulatory kinase) and inhibits its activity, thereby inhibiting the progression from the G1 phase to the S phase in the cell cycle. Rapamune is an oral medication and is recommended to be taken once daily. It should be started as soon as possible after transplantation. For new transplant recipients, the loading dose that should be taken for the first time is three times the maintenance dose. The recommended loading dose for kidney transplant patients is 6 mg and the maintenance dose is 2 mg/day.
Rapamune adverse reactions are common (incidence >10% according to International Council of Medical Organization frequency classification): lymphocele, peripheral edema, abdominal pain, diarrhea, hypokalemia, increased lactate dehydrogenase, acne, urinary tract infection; common at higher doses: anemia, hypercholesterolemia, thrombocytopenia, hypertriesteremia (hyperlipidemia). Store in a cool, dry, dark environment.
When taking Rapamune, patients should note that grapefruit juice cannot be used to deliver or dilute Rapamune. Because grapefruit juice can slow down the metabolism of sirolimus tablets and reduce its efficacy.
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