Sirolimus (also referred as rapamycin) is a macrocyclic lactone-based mTOR (mammalian target of rapamycin) inhibitor that is authorized to prevent graft rejection in solid organ transplant patients. It is currently approved for renal transplant patients to prevent rejection in certain other solid organ transplant recipients as well as to treat graft-versus-host disease in hematopoietic stem cell transplant patients. Sirolimus is supplied as a tablet or liquid. The liquid strength of Sirolimus is 1mg/mL.
The immunomodulating properties of sirolimus tablets 1mg are due to its potential in order to inhibit the effects of interleukin-2 on T-lymphocyte activation and proliferation. Sirolimus binds to FKPB-12, an intracellular cytoplasmic protein that exists in T-cells. The sirolimus-FKPB complex then binds to the mammalian target of rapamycin, which blocks the reaction of the T-cell to interleukin-2 binding to its outer cell wall. This mechanism helps in preventing T-cell proliferation and progression of the cell cycle.
Because certain calcineurin inhibitors (such as tacrolimus) are nephrotoxic, sirolimus is used by various transplant centers as part of calcineurin inhibitor avoidance regimens or calcineurin inhibitor conversion protocols to avoid drug-induced renal damage.
Dosage & Administration
Follow your health specialist's instructions carefully. The proposed dosage of Sirolimus should be taken once daily at the persistent time each day in order to maintain a steady blood level. Most patients typically take it in the morning between 7 & 9 am. Dosage may be taken on an empty stomach or with meals for reducing stomach irritation. The most crucial thing to remember is to take your dose, in the same way, every day, either with or without a meal as the meal can affect the medicine's absorption. The pills should be swallowed whole, without crushing or chewing. There is an oral solution of Sirolimus available for such individuals who need very low doses or those who are not capable of swallowing the Sirolimus tablets. The oral solution is typically drawn into an oral syringe from the bottle. Empty the syringe into a glass or plastic cup that contains at least 2 ounces (1/4 cup, 60 mL) of water or orange juice, stir vigorously for 1-minute and drink promptly. The container should be refilled with a minimum of 4 ounces (1/2 cup, 120 mL) of water or orange juice, stir vigorously again, and drink the rinse solution. Avoid the consumption of apple juice, grapefruit juice, or any other liquids. In order to dilute the oral solution, only glass or plastic cups should be used. Store your bottle of oral solution in the refrigerator. In case you need to pre-draw a Sirolimus dose you can store a single dose in the oral syringe outside of the refrigerator for 24 hours only.
NOTE: Deets mentioned in this article about "DOSAGE AND ADMINISTRATION of Sirolimus" is for informational or educational purposes only, and does not substitute professional medical advice or consultations with health specialists.