Rapasin
Generic Name
Sirolimus
Manufacturer
Hypothetical Pharma Ltd.
Country
Bangladesh
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Price Details
Current market pricing information
| Variant | Unit Price | Strip Price |
|---|---|---|
| rapasin 8 mg capsule | ৳ 25.00 | ৳ 250.00 |
Description
Overview of the medicine
Rapasin (Sirolimus) is an immunosuppressant medication used primarily to prevent organ rejection in patients who have received a kidney transplant. It is also approved for the treatment of lymphangioleiomyomatosis (LAM), a rare progressive lung disease.
Uses & Indications
Dosage
Adults
For kidney transplant rejection prophylaxis: Initially, a loading dose of 6 mg is given on Day 1, followed by a maintenance dose of 2 mg once daily. Dosage is adjusted based on therapeutic drug monitoring to achieve target trough levels (e.g., 4-12 ng/mL). For LAM: 2 mg once daily. Adjust dosage to achieve trough levels of 5-15 ng/mL.
Elderly
No specific dosage adjustment is generally recommended for elderly patients, but monitoring of renal function and sirolimus trough levels is crucial due to potential age-related physiological changes and increased susceptibility to adverse effects.
Renal_impairment
No dosage adjustment is needed for patients with mild to moderate renal impairment. For severe renal impairment, close monitoring of sirolimus trough levels and dose adjustment may be required.
How to Take
Take Rapasin orally once daily, at the same time each day, consistently with or without food. Do not crush, chew, or split the capsule; swallow it whole. Administer Sirolimus oral solution consistently with water or orange juice, but never with grapefruit juice or other beverages.
Mechanism of Action
Sirolimus inhibits the mammalian target of rapamycin (mTOR), a protein kinase critical for cell growth, proliferation, and differentiation. By inhibiting mTOR, it suppresses T-lymphocyte activation and proliferation, thereby preventing the immune response that leads to organ rejection. It also has anti-proliferative effects beneficial in LAM.
Pharmacokinetics
Onset
Therapeutic effects are not immediate; steady-state concentrations and optimal immunosuppression typically require several days to weeks to achieve.
Excretion
The primary route of elimination is via feces (approximately 91% of an oral dose). Only a small fraction (approximately 2.2%) is excreted in urine.
Half life
The elimination half-life is long, ranging from approximately 57 to 62 hours, supporting once-daily dosing.
Absorption
Rapidly absorbed after oral administration, but with low and variable oral bioavailability (approximately 14%). Peak plasma concentrations are typically reached within 1-3 hours. High-fat meals can increase bioavailability, so consistent administration with or without food is recommended.
Metabolism
Extensively metabolized in the liver and intestinal wall, primarily by the cytochrome P450 3A4 (CYP3A4) enzyme system. Multiple metabolites exist, some with minimal immunosuppressive activity.
Side Effects
Contraindications
- Known hypersensitivity to sirolimus or any component of the formulation.
- Not recommended for use in liver or lung transplant patients due to increased risk of mortality and complications.
Drug Interactions
Ciclosporin
Concurrent use with ciclosporin can increase sirolimus levels. It is recommended to administer sirolimus at least 4 hours after ciclosporin to minimize interaction.
Live Vaccines
Avoid live vaccines during sirolimus therapy due to immunosuppression, which may impair immune response to vaccination.
Strong CYP3A4 inhibitors (e.g., ketoconazole, diltiazem, voriconazole)
These agents can significantly increase sirolimus blood levels, potentially leading to toxicity. Sirolimus dose reduction and close monitoring are often necessary.
Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John's wort)
These agents can decrease sirolimus blood levels, reducing its efficacy. Sirolimus dose increase and close monitoring are often necessary.
Storage
Store at controlled room temperature (20°C to 25°C), with excursions permitted to 15°C to 30°C. Protect from light and moisture. Keep out of reach of children.
Overdose
Limited experience exists with sirolimus overdose. Symptoms may include an exacerbation of known side effects. Management involves general supportive measures, including monitoring blood sirolimus levels and initiating symptomatic treatment. Sirolimus is not significantly removed by hemodialysis.
Pregnancy & Lactation
Pregnancy Category C. Sirolimus should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Women of childbearing potential should use effective contraception during treatment and for 12 weeks after discontinuation. Sirolimus is excreted into human milk, therefore, breastfeeding is not recommended.
Side Effects
Contraindications
- Known hypersensitivity to sirolimus or any component of the formulation.
- Not recommended for use in liver or lung transplant patients due to increased risk of mortality and complications.
Drug Interactions
Ciclosporin
Concurrent use with ciclosporin can increase sirolimus levels. It is recommended to administer sirolimus at least 4 hours after ciclosporin to minimize interaction.
Live Vaccines
Avoid live vaccines during sirolimus therapy due to immunosuppression, which may impair immune response to vaccination.
Strong CYP3A4 inhibitors (e.g., ketoconazole, diltiazem, voriconazole)
These agents can significantly increase sirolimus blood levels, potentially leading to toxicity. Sirolimus dose reduction and close monitoring are often necessary.
Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John's wort)
These agents can decrease sirolimus blood levels, reducing its efficacy. Sirolimus dose increase and close monitoring are often necessary.
Storage
Store at controlled room temperature (20°C to 25°C), with excursions permitted to 15°C to 30°C. Protect from light and moisture. Keep out of reach of children.
Overdose
Limited experience exists with sirolimus overdose. Symptoms may include an exacerbation of known side effects. Management involves general supportive measures, including monitoring blood sirolimus levels and initiating symptomatic treatment. Sirolimus is not significantly removed by hemodialysis.
Pregnancy & Lactation
Pregnancy Category C. Sirolimus should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Women of childbearing potential should use effective contraception during treatment and for 12 weeks after discontinuation. Sirolimus is excreted into human milk, therefore, breastfeeding is not recommended.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
Typically 24 to 36 months from the date of manufacture.
Availability
Hospitals, pharmacies
Approval Status
FDA approved (for Sirolimus)
Patent Status
Patent expired for generic Sirolimus; generic versions available
WHO Essential Medicine
YesClinical Trials
Sirolimus has been extensively studied in numerous clinical trials establishing its efficacy and safety for kidney transplant rejection prophylaxis and LAM treatment. Ongoing research explores its potential applications in other autoimmune diseases and various cancers.
Lab Monitoring
- Sirolimus whole blood trough levels (regularly to ensure therapeutic range and avoid toxicity).
- Complete blood count (CBC) with differential (to monitor for anemia, leukopenia, thrombocytopenia).
- Renal function tests (serum creatinine, BUN) to monitor kidney function.
- Liver function tests (ALT, AST, bilirubin) to assess hepatic health.
- Lipid profile (total cholesterol, HDL, LDL, triglycerides) due to risk of hyperlipidemia.
- Fasting blood glucose (to monitor for hyperglycemia).
Doctor Notes
- Crucial to perform regular therapeutic drug monitoring (TDM) of sirolimus blood trough levels to maintain the therapeutic window and prevent toxicity, especially in transplant recipients.
- Educate patients thoroughly on the importance of strict adherence to the dosing regimen, consistent administration, and avoidance of grapefruit products.
- Be vigilant for early signs of infection, skin abnormalities, and metabolic disturbances (e.g., hyperlipidemia, hyperglycemia), and manage proactively.
Patient Guidelines
- Take your Rapasin-8-mg-capsule exactly as prescribed by your doctor, at the same time each day, to maintain consistent drug levels.
- Do not stop taking Rapasin suddenly without consulting your doctor, as this may lead to serious complications like organ rejection.
- Avoid consuming grapefruit or grapefruit juice, as it can dangerously increase sirolimus levels in your blood.
- Report any signs of infection (fever, chills, sore throat), unusual bleeding or bruising, or new skin growths to your doctor immediately.
Missed Dose Advice
If you miss a dose, take it as soon as you remember. If it is almost time for your next dose (e.g., within 4 hours), skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one.
Driving Precautions
Rapasin may cause dizziness or visual disturbances in some patients. If you experience these effects, exercise caution when driving or operating machinery until you know how the medication affects you.
Lifestyle Advice
- Practice good hygiene, including frequent hand washing, to reduce your risk of infections.
- Avoid close contact with people who are sick or have active infections, and avoid crowded places.
- Use sun protection (sunscreen with high SPF, protective clothing) as you have an increased risk of skin cancer.
- Avoid live vaccines while taking Rapasin, as your immune system is suppressed.
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