Sirolimus: Your Guide to a Vital Immunosuppressant Medication

Sirolimus is an immunosuppressant (available as a tablet and solution) used with other drugs to help prevent the rejection of a transplanted kidney. It’s also available as a topical sirolimus gel used to treat a skin condition.

What Is Sirolimus?

Sirolimus (Rapamycin) is an immunosuppressant medication, meaning it lowers the activity of your immune system.  It’s available as an oral version (Rapamune) and topical version (Hyftor). Both Rapamune and Hyftor are available as generic versions. 

What Is Sirolimus Used to Treat?

Rapamune (sirolimus tablet and liquid) is FDA-approved to prevent the body from rejecting a transplanted kidney in individuals 13 years or older. It’s also used to treat a lung disease called lymphangioleiomyomatosis (LAM), which is a rare disease that causes abnormal growth of smooth muscle cells in your lungs and lymphatic system. 

Hyftor (sirolimus topical gel) is a prescription topical medication that treats a condition called facial angiofibroma, which is a specific type of facial lesion, in adults and children 6 years and older. 

How Does Sirolimus Work?

Sirolimus lowers the activity of your immune system to help lower inflammation. In terms of transplants, lowering the activity of your immune system prevents your body from rejecting the transplanted organ. 

How Is Sirolimus Supplied and Used?

Oral sirolimus products come in the following forms and strengths:

• Բանավոր դեղահաբեր: 0.5 mg, 1 mg, and 2 mg 
• Oral solution: 1 mg/ml 

Proper Use, Storage, and Disposal 

• Read the instructions for use carefully, and take this medication exactly as directed. 
• Never stop taking any medication without talking to your doctor. Continue taking it even if you feel better. 
• You can take the medication with or without food. If it’s hurting your stomach, try taking it with food to help.
• If you also take cyclosporine, take sirolimus 4 hours after cyclosporine because they interact with each other.
• Your provider will occasionally order a blood test to check the medication’s level in your blood. Based on the results, your provider might change your dose.
• Swallow the entire tablet; do not crush, chew, or split it. Tell your provider if you cannot swallow the tablets. They will likely give you the liquid preparation. 
• Use the syringe that comes with the sirolimus solution to measure out your dose. Never use household spoons to measure your dose because they aren’t accurate. Using them can cause you to take the wrong dose.
• Do not take oral sirolimus products with grapefruit or grapefruit juice because they can interact with the medication and raise your risk for side effects.
• If your skin comes in contact with the solution, wash the exposed area with soap and water. If your eye is exposed, rinse it with water. 
• Store the oral solution in a refrigerator (36°F to 46°F). You can also store it at room temperature (up to 77°F) for up to 15 days, protected from light. Once the bottle is opened, use it within one month. Store the tablets at room temperature (68°F to 77°F).
• Keep all your medicines out of the reach of children. 
• Dispose of unused, unneeded, or expired medicine through a medicine take-back program. Ask your pharmacist or local garbage department to learn more about the program. 
• If such programs are not accessible, read the FDA’s guidelines for safely disposing of medicines here. 

What Should You Know Before Taking Sirolimus?

Before receiving your first dose, inform your provider if you have:

• Liver disease
• Skin cancer or a family history of skin cancer
• High cholesterol or triglycerides in your blood

Also, since sirolimus can interact with a lot of commonly used medications, make sure to tell your provider about all of the medications you take, including prescription and over-the-counter medications as well as vitamins and dietary supplements. Some examples of medications that interact with sirolimus include: 

• Cholesterol-lowering medicine
• Cyclosporine, tacrolimus, or other immunosuppressants
• Antibacterial or antifungal medicines
• Medications to lower blood pressure 
• Heart disease drugs
• Medicines for seizures
• HIV drugs
• St. John’s Wort
• Cannabidiol 

What Should You Avoid While Using Oral Sirolimus Products?

• Don’t get vaccinated with live vaccines while taking this medication. Because sirolimus weakens your immune system, it’s possible that receiving live vaccines while taking sirolimus can cause you to get sick. You should be brought up to date on all of your vaccines before starting sirolimus.
• Limit sun exposure. Wear protective clothing and apply broad-spectrum sunscreen because sirolimus can make your skin sensitive to light.

Oral Sirolimus Dosage

Prevention of Kidney Transplant Rejection

You should receive your first dose as soon as possible after transplantation. This medication is typically used with cyclosporine and corticosteroids.

Your provider will calculate the starting dose based on your body weight or body surface area and the estimated risk of rejection of the transplanted kidney. Then, they will adjust the dose (maintenance dose) to achieve the desired blood concentration of sirolimus. The maximum dose is 40 mg per day. 

Treatment of Lymphangioleiomyomatosis (LAM)

The initial dose is 2 mg/day. Your provider will determine the trough level, usually between days 10 and 20. Then, they will adjust the dosage accordingly based on the level in your blood.

Sirolimus Side Effects

Side effects can be mild or severe. Furthermore, they may vary depending on the condition for which the drug is being used. 

Հաճախակի կողմնակի ազդեցություններ

• High blood pressure
• Միզուղիների վարակ
• Ստամոքսի ցավ
• Հոդերի ցավ
• Կրծքավանդակի ցավ
• Low red blood cell count
• Լուծ
• Սրտխառնոց
• Գլխացավ
• Թրոմբոցիտների ցածր քանակ 
• Ջերմություն
• High blood sugar 
• Բերանի խոցեր
• Վերին շնչառական համակարգի վարակ
• Գլխապտույտ
• Կոկորդի ցավ

Talk to your provider or pharmacist if any side effect worsens or persists. 

Լուրջ կողմնակի ազդեցություններ

Call your provider immediately or seek emergency care if you have:

• Swelling of your hands or feet
• Poor wound healing
• Unusual bleeding or bruising
• New or worsening cough
• Շնչառության դժվարություն
• Շնչառության դժվարություն
• Signs of viral infection, including confusion, altered consciousness, and weakness on one side of your body

Allergic Reactions

Seek emergency medical help if you experience the following:

• Կրծքավանդակի ցավ
• Մեղվափեթակներ
• Շնչառության դժվարություն
• Բարձր կամ ցածր արյան ճնշում
• Ջերմություն
• Սառնություն

Օգտագործել հղիության և կրծքով կերակրման ժամանակ

Taking sirolimus during pregnancy should be avoided because it can harm the unborn baby. Thus, use effective contraception (birth control) during treatment, and for 12 weeks after the last dose of sirolimus. 

Additionally, avoid breastfeeding while using sirolimus due to the risk of serious side effects to your baby.

Sirolimus might also affect fertility in men and women. Ask your doctor for more information. 

How Much Does Sirolimus Cost?

Cost can vary depending on your insurance plan, location, and pharmacy. Contact your insurance provider to find out if your plan covers this medication or if you need prior authorization. Also, be sure to get in touch with us if you need financial assistance for sirolimus.