Rapamycin or Rapacan (Sirolimus)

Rapamycin (Rapacan) is an immunosuppressant with antifungal and antitumor effects. It has a suppressive effect on the immune system. It is effective in cases where it is necessary to suppress its activity to prevent certain diseases or donor organ rejection.

According to some data, the active ingredient of the drug, Sirolimus, and the Rapamycin supplement may have a positive effect on the health of older people, helping to prolong life, but confirmation of this requires further studies.

Drug Information

• Brand: Rapamune, Rapamycin, Rapacan;
• Active substance: Sirolimus;
• Manufacturer: Pfizer, Biocon.

Rapamycin (Rapacan) and its active substance Sirolimus

Rapamycin (or Rapacan) is a tablet containing the active substance Sirolimus. For treatment with the drug to be effective, you must follow the instructions or the doctor's recommendations.

After taking the tablet, the active substance Sirolimus enters the blood and has these effects:

• Blocks cell growth;
• Blocks cell reproduction;
• Suppresses the immune system.

ATTENTION! An overdose of Rapamycin can lead to dangerous consequences. Do not take the drug without a prescription.

Indications for use

The main indications for Rapamycin (Rapacan) are the treatment of tumors and the elimination of the risk of donor organ rejection. The EMA approved the use of the drug in the following cases:

• Prevention of donor organ rejection after kidney transplantation in adults;
• Treatment of sporadic lymphangioleiomyomatosis with moderate lung lesions.

Treatment regimens and dosages

Rapamycin treatment regimens and dosages depend on the purpose of its use. The drug is available in 1 mg dosage. A doctor may prescribe more than one tablet at a time.

• After transplantation, a single dose of 6 mg is usually prescribed. Then, you switch to a daily dosage of 2 mg until the required therapeutic level of the active substance in the blood is reached. The dosage is then calculated individually, and the duration of treatment is 2-3 months.
• For the treatment of sporadic lymphangioleiomyomatosis, the usual starting dosage is 2 mg per day. After 10-20 days, when the therapeutic level of the active substance is reached in the blood, the dosage should be adjusted according to individual characteristics.

Before adjusting the dosage of the drug, you should perform special tests to determine the level of the active substance in the blood. Dosage adjustments are also necessary for:

• Black people due to high immunological risk;
• People with liver dysfunction.

Currently, there is not enough data to confirm that the reaction of people over 65 to the drug may differ from that of younger people. The safety of the drug for children and people under 18 has also not yet been proven. Thus, a doctor should decide on dosage adjustments based on individual characteristics and the appropriateness of using Rapamycin in each particular case.

Recommendations for use

Rapamycin (Rapacan) 1 mg is available in tablet form. To get the most out of Rapamycin treatment, follow these rules:

• Take the drug at the same time each day;
• Take the tablet with plenty of water;
• Take the drug before or after meals;
• Avoid grapefruit juice.

Although data on the combination of alcohol and Rapamycin are insufficient, to prevent adverse effects, we recommend avoiding alcohol throughout the entire period of treatment with the drug.

In addition, when using the Rapamycin supplement, you should avoid fatty foods. This is because fats reduce the absorption rate of the active ingredient of the drug. St. John's wort can decrease the blood concentration of the active substance. Avoid medications containing St. John's wort during treatment.

Missed dose

If you miss a dose of Rapamycin, take it as soon as possible. If the time for your next dose is near, skip the previous dose and continue treatment as scheduled.

Precautions

In some cases, the use of Rapamycin may present a higher risk and be contraindicated. A doctor will not prescribe the drug in the following cases:

• You are pregnant or breastfeeding;
• You have an increased sensitivity to the active substance;
• You have had a liver or lung transplant.

Due to the immunosuppressive effect of Rapamycin, the risk of contracting various types of infections increases during its use. Avoid contact with sick people to protect yourself. The immunosuppressive effect of the drug can persist for 6 months after the end of treatment.

Rapamycin (Rapacan) can increase the risk of bleeding and slow wound healing. Be careful when using sharp objects and consult a doctor immediately if you experience symptoms such as:

• Bruising;
• Black stools;
• Blood in the urine.

According to some data, people with a body mass index greater than 30 kg/m² may have an increased risk of impaired wound healing when taking Rapamycin.

The drug reduces the effect of vaccinations. In addition, Sirolimus can increase the skin's sensitivity to the sun. So always use sunscreen during treatment.

Use of Rapamycin (Rapacan) during pregnancy

In general, doctors do not prescribe the drug to pregnant women because there is no data on its safety for them. Animal studies confirm the fetal toxicity of rapamycin. A doctor should decide on the possible use of the drug during pregnancy if absolutely necessary.

There is also no evidence that Sirolimus enters breast milk in women due to the lack of relevant studies. However, according to some studies, the drug enters animal milk. Therefore, its use by breastfeeding women may be dangerous for the child. If you are breastfeeding, avoid using Rapamycin and consult a doctor.

Possible side effects

Like any other drug, Rapamycin can cause side effects. To reduce the likelihood of side effects, follow the doctor's instructions and do not exceed the prescribed dosage. The most common side effects (in 10% of cases) of the drug are:

• Anemia;
• High blood pressure;
• Urinary tract infections;
• Hypokalemia;
• Abdominal pain;
• Swelling;
• Headaches;
• Diarrhea;
• Constipation;
• Nausea.

Most often, the severity of side effects depends on individual characteristics and the dosage of the drug. If you have severe side effects or if they worsen over time, consult a doctor.

As a rule, an overdose of the drug causes an increase in side effects. Consult a doctor if you exceed the prescribed dosage and your condition worsens.

Rapamycin (Rapacan): interaction with other drugs

Rapamycin can interact with other drugs. Therefore, you should inform a doctor of all medications you are taking. When combined with CYP3A4 inhibitors, the drug can increase the active substance in the blood and cause side effects. At the same time, CYP3A4 inhibitors reduce Sirolimus levels. Do not take Rapamycin with these drugs:

• Rifampicin;
• Ketoconazole;
• Voriconazole;
• Diltiazem;
• Erythromycin;
• Cyclosporine.

Grapefruit juice affects CYP3A4-mediated metabolism. So avoid it in any form. For more information on possible Rapamycin interactions, consult a doctor or pharmacist.

Storage

Store Rapamycin at room temperature 20 - 25°C in a dark place, out of reach of children and animals. Do not use the drug if the expiration date has passed or the packaging is damaged.

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