This medication is primarily used as an immunosuppressant and plays a crucial role in preventing rejection of transplanted organs in kidney transplant patients. Additionally, it can be used to treat certain autoimmune diseases. The mechanism of action of the drug is to inhibit the activation of T cells, thereby reducing the immune response. This helps the patient's immune system better accept the transplanted organ.
Rapamune(sirolimus), Side effects, Drug Interactions
Index
- A. Key Information
- A.1. Ingredients
- A.2. Appropriate Users
- A.3. Side Effects
- A.4. Dosage Instructions
- B. Drug Interactions
- B.1. Diltiazem
- B.2. Ketoconazole
- B.3. Rifampin
- B.4. Erythromycin
- B.5. Verapamil
A. Key Information
This medication is primarily used as an immunosuppressant and plays a crucial role in preventing rejection of transplanted organs in kidney transplant patients. Additionally, it can be used to treat certain autoimmune diseases. The mechanism of action of the drug is to inhibit the activation of T cells, thereby reducing the immune response. This helps the patient's immune system better accept the transplanted organ.
The medication can also interact with other drugs, particularly those affecting CYP enzymes and P-glycoprotein. Such interactions can influence the blood concentration of the drug, potentially increasing the likelihood of its effects or side effects. Therefore, caution is needed when using this medication in combination with other drugs.
The medication can also interact with other drugs, particularly those affecting CYP enzymes and P-glycoprotein. Such interactions can influence the blood concentration of the drug, potentially increasing the likelihood of its effects or side effects. Therefore, caution is needed when using this medication in combination with other drugs.
| Category | Details |
|---|---|
| Product Name | Rapamune Tab. 2mg |
| Ingredients | Sirolimus 2mg (Sirolimus Dispersible Tablet 13.3mg) |
| Form | Tablet |
| Company | Pfizer |
| ATC Code | L04AH01: SIROUMUS |
| Dosage & Administration |
2mg orally once daily |
| How to Take | Oral administration (can be taken with or without food) |
| Packaging Unit | 100 tablets (10 tablets per blister pack x 10) |
A.1. Ingredients
• Rapamycin (Sirolimus)
- Role -
Rapamycin is primarily used as an immunosuppressant and plays a crucial role in preventing organ rejection in transplant patients. It inhibits the activation of T cells and modulates the immune response, helping the body not to attack the transplanted organ. Additionally, rapamycin is used in the treatment of certain types of cancer, inhibiting cell growth and division to impede tumor growth. This drug contributes to the regulation of cellular metabolism and growth signals by inhibiting the mTOR (mechanistic Target Of Rapamycin) pathway.
Rapamycin is primarily used as an immunosuppressant and plays a crucial role in preventing organ rejection in transplant patients. It inhibits the activation of T cells and modulates the immune response, helping the body not to attack the transplanted organ. Additionally, rapamycin is used in the treatment of certain types of cancer, inhibiting cell growth and division to impede tumor growth. This drug contributes to the regulation of cellular metabolism and growth signals by inhibiting the mTOR (mechanistic Target Of Rapamycin) pathway.
- Characteristics -
Rapamycin has unique features in terms of its chemical structure and mechanism of action. The drug has low solubility and strongly binds to plasma proteins, affecting its distribution and metabolism within the body. Rapamycin can interact with various drugs, particularly acting as a substrate for CYP450 enzymes and P-glycoprotein, thereby influencing the metabolism of other medications. Patients taking rapamycin need to carefully monitor potential drug interactions. Lastly, rapamycin poses a risk of toxicity to the fetus when used during pregnancy, so it should be avoided during this period.
Rapamycin has unique features in terms of its chemical structure and mechanism of action. The drug has low solubility and strongly binds to plasma proteins, affecting its distribution and metabolism within the body. Rapamycin can interact with various drugs, particularly acting as a substrate for CYP450 enzymes and P-glycoprotein, thereby influencing the metabolism of other medications. Patients taking rapamycin need to carefully monitor potential drug interactions. Lastly, rapamycin poses a risk of toxicity to the fetus when used during pregnancy, so it should be avoided during this period.
A.2. Appropriate Users
This drug is an immunosuppressant primarily used in organ transplant patients. It is specifically not recommended for use in liver transplant patients. Studies in patients receiving their first liver transplant have shown that concomitant administration of this drug with tacrolimus is associated with excess mortality and graft failure.
A.3. Side Effects
Potential side effects of this drug include increased susceptibility to infections, the development of lymphoma and other malignancies. Other reported side effects include hepatotoxicity, azoospermia, and Clostridium difficile enterocolitis. Hepatotoxicity can be severe, including fatal hepatic necrosis.
A.4. Dosage Instructions
This medication should be taken consistently with or without food. It should be swallowed whole with water and not chewed or crushed. If symptoms such as rash, redness, or itching occur, consult a healthcare professional. It is important to notify a healthcare professional immediately if any signs of infection appear.
B. Drug Interactions
B.1. Diltiazem
Diltiazem is known as both a substrate and an inhibitor of CYP3A4 and P-glycoprotein. Co-administration with sirolimus can significantly alter the bioavailability of sirolimus, necessitating monitoring and dose adjustment.
B.2. Ketoconazole
Ketoconazole is a potent CYP3A4 inhibitor, which can increase the concentration of sirolimus when used together. This may require adjusting the dosage of sirolimus.
B.3. Rifampin
Rifampin is a strong inducer of CYP3A4 and can decrease the blood levels of sirolimus. Therefore, the combination of sirolimus with rifampin is not recommended.
B.4. Erythromycin
Erythromycin is a CYP3A4 inhibitor and can increase the concentration of sirolimus when used together. Monitoring and dose adjustment are necessary in this case as well.
B.5. Verapamil
Verapamil can affect the bioavailability of sirolimus, and co-administration of sirolimus and verapamil can increase the AUC of sirolimus. Hence, this combination also requires caution.
