西罗莫司片是什么？

What is it? Many patients don’t know what sirolimus tablets are and what they treat. Let’s find out together. The main ingredient of sirolimus tablets is sirolimus. Sirolimus tablets are suitable for patients aged 13 or above who have received kidney transplants to prevent organ rejection. Recommended for use in combination with cyclosporine and corticosteroids.

In stable renal transplant recipients, the mean (± standard deviation) blood/plasma ratio of sirolimus after administration of sirolimus tablets was 36 ± 18, indicating that sirolimus is widely distributed into the formed components of the blood. The average volume of distribution (Vss/F) of sirolimus tablets is 12±8L/kg. Sirolimus tablets are extensively bound to human plasma proteins (approximately 92%). Sirolimus Tablets In men, sirolimus tablets are bound primarily to serum albumin (97%), alpha 1-acid glycoprotein, and lipoproteins. Sirolimus tablets are extensively metabolized via O-demethylation and/or hydroxylation. Sirolimus tablets can detect seven major metabolites in whole blood, including hydroxylation, demethylation and hydroxydemethylation metabolites.

Sirolimus tablets are substrates of CYP3A4 and P-gp. Sirolimus tablets are extensively metabolized by CYP3A4 isoenzymes in the intestinal wall and liver, and can be reversely transported from the intestinal epithelial cells into the intestinal lumen by the P-gp drug efflux pump. Inhibitors of CYP3A4 and P-gp may increase sirolimus concentrations. Inducers of CYP3A4 and P-gp can reduce sirolimus concentrations. Some sirolimus tablets can also be detected in plasma, feces, and urine. Sirolimus tablets are the main component in human whole blood, and their immunosuppressive activity accounts for more than 90% of the total activity.

Adverse reactions of sirolimus tablets: Very common (incidence >10% according to frequency classification of the International Council of Medical Organizations): lymphocele, peripheral edema, abdominal pain, diarrhea, hypokalemia, increased lactate dehydrogenase, acne, urinary tract infection; very common at higher doses: anemia, hypercholesterolemia, thrombocytopenia, hypertriesteremia (hyperlipidemia). Store in a cool, dry, dark environment.

The above is the drug introduction provided by our Medical Companion Overseas Medical Consulting Service Company. Patients should read it carefully and use the drug rationally.