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Home > Drug Category > Immunosuppressive Agents > Rapamune and Equivalent

Rapamune Information

Rapamune (Sirolimus) is used for the prevention of organ rejection in people who have received a kidney transplant (typically in those with low-to-moderate rejection risk). It is typically used in combination with other immunosuppressant medications, such as cyclosporine and corticosteroids. It is also used to treat a lung disease called lymphangioleiomyomatosis (LAM). Its active ingredient is sirolimus, a macrolide known as MTOR (mechanistic target of rapamycin) inhibitors. Sirolimus works by blocking the response of T-lymphocytes to certain cytokines, thereby preventing cell proliferation that leads to organ rejection or abnormal tissue growth.

In a kidney transplant, the body's natural immune system may identify the new kidney as foreign and attempt to destroy it. Sirolimus suppresses this activation, allowing the newly transplanted organ to survive without being attacked by the host's immune system. Lymphangioleiomyomatosis, on the other hand, is a rare, progressive cystic lung disease seen almost exclusively in women, where abnormal cystic cells grow uncontrollably in the lungs, kidneys, and lymphatic system. These cells often harbor mutations in genes involved in tuberous sclerosis complex that keep the mTOR pathway permanently activated. By inhibiting this overactive pathway, sirolimus slows the growth of these cells, helping stabilize lung function and reduce the size of associated tumors, such as renal angiomyolipomas. It is worth noting that sirolimus has not been shown to be safe and effective in the prevention of organ rejection in people who have had liver or lung transplants.

Rapamune Side Effects

Common mild side effects of this medication include acne, constipation, diarrhea, headache, heartburn, increased growth of body hair, nausea, sleeping problems (insomnia), stomach pain, trembling, weakness, and weight gain.

Contact your doctor if these mild side effects persist or worsen. Stop taking this medicine and contact your doctor immediately if you experience any serious side effects, including the following:
• Allergic reactions such as breathing difficulties, body itching, body rash, skin blistering, swelling of the face, mouth, tongue, lips, or throat;
• Anemia (low red blood cells) with symptoms like dizziness, pale skin, unusual tiredness or weakness, shortness of breath;
• Bleeding problems with symptoms like unusual nosebleeds, bruising, blood in urine, coughing blood, bleeding gums;
• Electrolyte imbalances with symptoms like weakness, fatigue, muscle cramps, irregular heartbeat, and tingling in the hands and feet;
• High blood sugar;
• High cholesterol and triglycerides (hyperlipidemia);
• Impaired wound healing (incisions may take longer to heal or may reopen);
• Liver problems with symptoms like nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools;
• Lung infection or non-infectious lung inflammation (interstitial lung disease) with symptoms like cough, shortness of breath, coughing up blood, fever, chills, cold or flu-like symptoms;
• Ovarian cysts with symptoms like pelvic pain or heaviness, pain during intercourse, frequent need to urinate, changed menstrual periods, bloating;
• Pancreatitis with symptoms like abdominal pain on the upper left side, back pain, nausea, fever, chills, rapid heartbeat;
• Signs of infection such as fever or chills, severe diarrhea, shortness of breath, prolonged dizziness, headache, stiff neck, or weight loss;
• Skin changes such as the development of a new skin growth or enlargement of an existing skin growth, or changes in an existing mole;
• Urinary tract infection with symptoms such as difficult or painful urination, blood in the urine, or cloudy urine

Inform your doctor about any other side effects you notice that are not listed here.

Rapamune Precautions

Do not use this medicine if you are allergic to sirolimus or any other ingredients in Rapamune. Before using this medication, ensure you inform your doctor about any medical conditions you previously or currently have, including the following:
• Active infections, including viral, bacterial, fungal, or parasitic;
• Blood cell disorders such as anemia;
• Cancers;
• Diabetes;
• Electrolyte imbalances such as low blood levels of potassium, calcium;
• Gastrointestinal problems such as peptic ulcers;
• High blood cholesterol;
• Kidney disease;
• Liver disease;
• Obesity;
• Other lung diseases, such as lung inflammation;
• Upcoming surgeries (due to the risk of delayed wound healing).

It is worth noting that your doctor may perform some blood tests before and during treatment with this medication to monitor its effects in your body. Limit your skin's exposure to sunlight and undergo regular dermatological screenings, as this medication can increase the risk of skin cancer. Sirolimus can cause an overgrowth of the gum tissue. While taking this medication, it is important to maintain good oral hygiene and to visit a dentist regularly for a dental checkup. Avoid eating grapefruit or drinking grapefruit juice, as it can significantly increase the levels of Rapamune in your blood to dangerous levels. You should avoid live vaccines (such as MMR and yellow fever) while taking this medication, as a suppressed immune system may not be able to handle the weakened virus, and the vaccine may not be effective. Sirolimus is generally not recommended for use during pregnancy unless the benefit clearly outweighs the potential risk to the fetus. Animal studies have shown some toxicity to the fetus. Women of reproductive age group taking this medication must use highly effective contraception before starting, during, and for at least 12 weeks after stopping therapy. A decision must be made to either discontinue breastfeeding or discontinue this medication, depending on the mother's condition. Sirolimus is not suitable for use in children younger than 13 years for the prevention of kidney transplant rejection.

Caution is advised when using this medication in older adults, as they may be more prone to its side effects. Some medications like ketoconazole, voriconazole, clarithromycin, and ritonavir can cause Rapamune to build up to toxic levels. Therefore, it is important to tell your doctor about all medications, supplements, and herbal remedies you are using before starting sirolimus. Take Rapamune once daily at the same time, as directed by your doctor, to maintain steady blood levels. It is typically taken immediately after the transplant. Your doctor will determine the appropriate dose for you depending on your condition. Swallow the tablets whole; do not crush, chew, or split them. Avoid grapefruit juice entirely as it interferes with the drug’s metabolism. Check out the leaflet in the medication pack for more usage instructions. Store sirolimus tablets at room temperature (15°C to 30°C), protect them from light and moisture, and keep them out of the reach of children.

Do I need a prescription to order Rapamune?

Yes, a prescription is required from your physician to order Rapamune.