Rapamycin or Rapacan (Sirolimus)

Drug Info

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

Rapamycin (Rapacan) and its active substance Sirolimus

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

After you take the tablet, the active substance Sirolimus gets into the blood and has these effects:

• Blocking cell growth;
• Blocking cell reproduction;
• Suppressing the immune system.

ATTENTION! Overdosing on Rapamycin may lead to hazardous results. Don't take the drug without a doctor's prescription.

Indications for use

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

• Preventing donor organ rejection after kidney transplantation in adults;
• Treating sporadic lymphangioleiomyomatosis with moderate lung damage.

Treatment regimens and dosages

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

• After transplantation, a single dosage of 6 mg is usually prescribed. After that, you switch to a daily dosage of 2 mg until the required therapeutic level of the active substance in the blood is achieved. Next, the dosage is calculated individually, and the treatment duration 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 depending on individual characteristics.

Before adjusting the drug dosage, you should have 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 response of people over 65 years to the drug may differ from that of younger people. The drug's safety for children and people under 18 has also yet to be proven. So, a doctor should decide on dosage adjustments based on individual characteristics and the advisability of using Rapamycin in each particular case.

Recommendations for use

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

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

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

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

Missed Dose

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

Precautions

In some cases, using Rapamycin may have 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 ingredient;
• You had a liver or lung transplantation.

Considering 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) may increase the risk of bleeding and slow wound healing. Be careful when using sharp objects and seek immediate medical attention if you have symptoms such as:

• Bruises;
• Black stool;
• Blood in 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 medication reduces the effect of vaccinations. Moreover, Sirolimus may increase skin sensitivity to the sun. So, always use sunscreen during treatment.

Use of Rapamycin (Rapacan) during pregnancy

Usually, doctors don't prescribe the drug to pregnant women because there is no data on its safety for them. Animal studies confirm fetal toxicity of Rapamycin. A doctor should decide on the possible use of the medicine during pregnancy if it is absolutely necessary.

There is also no evidence that Sirolimus gets into women's breast milk due to the lack of relevant studies. However, according to some studies, the drug gets into the milk of animals. So, its use by breastfeeding women can be dangerous for the child. If you are breastfeeding, avoid using Rapamycin and consult a doctor.

Possible side effects

Like any other drug, Rapamycin may cause side effects. To reduce the likelihood of side effects, follow the doctor’s instructions and don't exceed the prescribed dosage. The most common (in 10% of cases) side effects of the medicine are as follows:

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

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

As a rule, overdosing on the drug causes increased side effects. See a doctor if you exceed the prescribed dosage, and your condition worsens.

Rapamycin (Rapacan): interaction with other drugs

Rapamycin may interact with other medicines. So, you should inform a doctor about all the drugs you take. When combined with CYP3A4 inhibitors, the medication may increase the active substance in the blood and cause side effects. At the same time, CYP3A4 inhibitors reduce Sirolimus levels. Don't use 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 about possible Rapamycin interactions, consult a doctor or pharmacist.

Storage

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

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