Rapamune Sirolimus 1 mg/mL Oral Solution

Description

What is Rapamune sirolimus 1 mg/mL oral solution?

Rapamune sirolimus 1 mg/mL is a prescription immunosuppressant supplied as a pale-yellow oral solution in a 60 mL amber bottle. Sirolimus inhibits the mammalian target of rapamycin (mTOR), reducing activation and proliferation of immune cells. Treatment must be initiated and monitored by a transplant or other appropriately qualified specialist, with regular whole-blood sirolimus trough measurements.

The pack contains one 60 mL bottle, a syringe adapter, 30 amber dosing syringes and a syringe carry case. Each millilitre contains 1 mg sirolimus. The solution also contains soya-derived ingredients, propylene glycol, polysorbate 80 and a small amount of ethanol.

Rapamune sirolimus quick facts

• Active ingredient: sirolimus.
• Strength and pack: 1 mg/mL oral solution; 60 mL bottle.
• Drug class: mTOR-inhibitor immunosuppressant.
• Route: oral use only; it is not an injection.
• Monitoring: whole-blood trough concentration plus clinical and laboratory review.
• Food: take consistently either with or without food.
• Storage: refrigerate at 2–8°C and protect from light.
• Prescription status: prescription-only specialist medicine.

Approved uses and an important local-label distinction

The Turkish prescribing information lists Rapamune for prevention of organ rejection in adults at low to moderate immunological risk receiving a kidney transplant. It recommends initial use with ciclosporin microemulsion and corticosteroids for two to three months, followed by maintenance with corticosteroids only when ciclosporin can be progressively withdrawn.

Current European product information also includes treatment of sporadic lymphangioleiomyomatosis (S-LAM) with moderate lung disease or declining lung function. Approved indications can differ between countries. Rapamune must therefore be used only for an indication and regimen authorised locally and selected by the treating specialist. It is not established as immunosuppressive therapy for liver or lung transplantation.

How sirolimus works

Sirolimus binds to the intracellular protein FKBP-12. The resulting complex blocks mTOR, a central regulator of cell growth and immune-cell proliferation. In kidney transplantation, this reduces T-lymphocyte responses that can attack the transplanted organ. In S-LAM, excessive mTOR signalling contributes to abnormal proliferation of LAM cells; mTOR inhibition can slow this process. Suppressing immune activity also increases susceptibility to infection and some malignancies, so benefit and risk must be reviewed continuously.

Specialist dosing and blood-level targets

Never calculate, start or change a Rapamune dose from online information. Sirolimus has a long half-life, major interactions and a narrow therapeutic range. Dose changes should normally be based on more than one appropriately timed trough result together with symptoms, laboratory tests and, in transplant patients, graft assessment.

Kidney-transplant rejection prophylaxis

The usual initial licensed regimen is a single 6 mg oral loading dose as soon as possible after transplantation, followed by 2 mg once daily until therapeutic-monitoring results are available. The dose is then individualised to a whole-blood trough concentration of 4–12 ng/mL by chromatographic assay while used with ciclosporin. Rapamune should be taken four hours after the ciclosporin dose.

When ciclosporin is progressively withdrawn over four to eight weeks, the recommended sirolimus trough target is 12–20 ng/mL by chromatographic assay. Continued combined use of ciclosporin and Rapamune beyond three months after transplantation is not recommended. Assay methods are not interchangeable, and the treating team must interpret results using the method employed by the laboratory.

Sporadic lymphangioleiomyomatosis

In current European product information, the initial dose for S-LAM is 2 mg once daily. A whole-blood trough concentration is measured after 10–20 days and the dose is adjusted to maintain 5–15 ng/mL. The long-term benefit should be reassessed periodically. This indication may not appear in every national label.

How to measure, dilute and take the oral solution

1. Use only the supplied dosing syringe and adapter. Confirm the prescribed amount in millilitres, not just milligrams.
2. Withdraw the exact prescribed volume from the bottle. Do not use a household spoon.
3. Empty the syringe into a glass or plastic container containing at least 60 mL of water or orange juice.
4. Stir vigorously and drink immediately.
5. Refill the same container with at least 120 mL more water or orange juice, stir vigorously and drink immediately so the full dose is taken.
6. Do not dilute Rapamune in grapefruit juice or any liquid other than water or orange juice.

Take Rapamune at the same time each day and in a consistent relationship to food. Switching unpredictably between fed and fasting conditions can change exposure. If ciclosporin is prescribed, keep the instructed four-hour separation.

9 essential safety checks

1. Therapeutic drug monitoring: check sirolimus trough levels after initiation, dose changes, formulation switches, relevant interaction changes and as scheduled once stable.
2. Infection review: report fever, persistent cough, painful urination, wounds, shingles, severe diarrhoea, confusion or new neurological symptoms promptly. Opportunistic and sometimes fatal infections can occur.
3. Blood counts and chemistry: monitor platelets, haemoglobin, white cells, potassium, phosphate, glucose, liver tests and kidney function.
4. Lipids: cholesterol and triglycerides frequently rise and may require diet, exercise or medicine under clinical supervision.
5. Kidney and urine protein: monitor creatinine and quantitative urinary protein, especially when ciclosporin is used or a calcineurin inhibitor is changed.
6. Wound healing and fluid: sirolimus can delay healing and cause lymphocele, peripheral oedema, pleural or pericardial fluid. Discuss surgery or a non-healing wound urgently.
7. Lung symptoms: new or worsening dry cough, breathlessness or fever needs assessment for infection and sirolimus-associated interstitial lung disease.
8. Skin and malignancy: immunosuppression raises lymphoma and skin-cancer risk. Limit UV exposure, use high-protection sunscreen and report new lumps or changing skin lesions.
9. Vaccines and reproduction: avoid live vaccines. Effective contraception is required during treatment and for 12 weeks after stopping; breast-feeding should be discontinued during therapy.

Critical interactions and foods to avoid

Sirolimus is metabolised by CYP3A4 and transported by P-glycoprotein. Strong inhibitors such as ketoconazole, voriconazole, itraconazole, telithromycin and clarithromycin can greatly increase sirolimus levels; strong inducers such as rifampicin or rifabutin can markedly reduce them. St John’s wort, carbamazepine, phenytoin and phenobarbital may also lower exposure. Grapefruit juice must be avoided.

Tell the transplant team about every prescription medicine, antibiotic, antifungal, antiviral, seizure medicine, cannabinoid product, herbal product and supplement before it is started or stopped. ACE inhibitors can increase angioedema-type reactions. Statins and fibrates require monitoring for muscle toxicity. Never compensate for an interaction by changing the Rapamune dose yourself.

Who must not use this oral solution?

Do not use Rapamune oral solution if there is hypersensitivity to sirolimus or any excipient. Because this formulation contains soya oil, patients allergic to peanut or soya must not take it. The safety and efficacy in children and adolescents under 18 have not been established sufficiently for a dosing recommendation in the current European information. Severe hepatic impairment generally requires a specialist reduction of the maintenance dose and closer monitoring; the loading dose is not automatically changed.

Side effects and urgent warning signs

Very common or common effects include low platelets, anaemia, fever, high blood pressure, low potassium or phosphate, urinary infection, raised cholesterol, glucose or triglycerides, abdominal pain, diarrhoea, constipation, nausea, headache, acne, joint pain, swelling, lymphocele and increased creatinine. The risk of adverse reactions may rise with higher trough concentrations.

Seek urgent medical advice for swelling of the face or throat, difficulty breathing, severe rash, high fever, signs of sepsis, new neurological changes, unexplained bruising or bleeding, severe weakness, chest pain, sudden leg swelling, jaundice, marked reduction in urine, a non-healing wound or new/worsening breathlessness. Do not stop transplant immunosuppression without immediate direction from the specialist because abrupt changes can endanger the graft.

Storage and expiry checks

• Store unopened and opened bottles in a refrigerator at 2–8°C in the original bottle to protect from light.
• If necessary, a bottle may be held at up to 25°C for a short period of 24 hours.
• Use an opened bottle within 30 days.
• A filled dosing syringe may be stored for up to 24 hours at room temperature not exceeding 25°C.
• After dilution, drink the preparation immediately.
• Check the expiry dates on the medicine and supplied adapter. A 2025 European safety communication restricted specific EU-market lots because the adapter expired earlier than the solution; the listed notice did not include Turkey.

Frequently asked questions

Is Rapamune oral solution an injection?

No. The syringe is an oral dosing syringe used to measure the solution. The medicine is diluted in water or orange juice and swallowed.

Can I mix Rapamune with any juice?

No. Use only water or orange juice as instructed. Never use grapefruit juice because it can alter sirolimus metabolism.

Can I take it with food?

It may be taken with or without food, but it must be taken consistently the same way to reduce variation in blood levels.

What if I miss a dose or vomit?

Contact the transplant or specialist team for instructions. Do not double a dose or repeat a dose after vomiting unless the treating team specifically advises it.

Can Rapamune be used for anti-ageing?

Rapamune is a potent prescription immunosuppressant with serious infection, interaction and monitoring risks. This product page does not support unlicensed self-use for longevity, anti-ageing or cosmetic purposes.

Official medical sources

• European Medicines Agency: Rapamune EPAR
• Rapamune 1 mg/mL oral solution SmPC
• Pfizer Turkey: Rapamune oral solution
• Pfizer Turkey: official Kısa Ürün Bilgisi

Browse more health information on No Style Like. Medical disclaimer: This page is educational and does not replace the package leaflet, local prescribing information or personal advice from the transplant team, physician or pharmacist. Never start, stop, dilute differently or change the dose of Rapamune sirolimus without specialist instruction.

Safe Use Checklist for Rapamune Sirolimus

Rapamune sirolimus must be taken exactly as the specialist prescribes, with the same relationship to food each day and every monitoring appointment kept. Never change or stop Rapamune sirolimus because of a missed dose, side effect or new medicine without contacting the transplant or respiratory team.