SIROLIMUS

Description: Sirolimus is a potent immunosuppressant used for renal transplantation. It inhibits antibody production. It has been shown to possess antifungal and antineoplastic properties.

Pharmacokinetics:

Absorption: Rapidly absorbed in the GI tract after oral admin.

Distribution: Extensively bound to plasma proteins.

Metabolism: Metabolised by CYP3A4

Excretion: Mainly excreted via faeces; only about 2% excreted in the urine.

Indications:

Sirolimus is used with other medications to prevent rejection of a kidney transplant.

Sirolimus may also be used to treat a certain lung disease(lymphangioleiomyomatosis-LAM).

This may also be used to treat lymphangioleiomyomatosis.

OTHER USES: This medication may also be used to prevent rejection of a heart transplant.

Contraindications:

Should not be given to patients who had allergic reaction with this drug.

How to use sirolimus

Dosage: Take this medication by mouth as directed by your doctor, usually once daily.

  • Swallow this medication whole. Do not crush, chew, or split the tablets.
  • If you have nausea or an upset stomach, you may take this medication with food. However, it is important to choose one way (with food or without food) and take this medication the same way with every dose. Consult your doctor or pharmacist for more details.
  • If you are also taking cyclosporine, take sirolimus 4 hours after your cyclosporine dose. Consult your pharmacist for more information.
  • Avoid eating grapefruit or drinking grapefruit juice while using this medication it can increase the chance of side effects with this medicine.

If you are taking this medication to treat LAM, tell your doctor if your condition worsens.

Availability: This is a prescription only drug.

Please see Precautions section.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Common side effects:

  • diarrhea,
  • joint pain,
  • shaking,
  • acne, or
  • trouble sleeping

Tell your doctor right away if you have any serious side effects, including:

  • nausea/vomiting that doesn’t stop, yellowing eyes/skin, dark urine, muscle pain/cramps, bone pain, increased thirst/hunger, frequent urination, hearing problems (such as hearing loss, ringing in the ears), unusual tiredness, fast/slow/irregular heartbeat, easy bruising/bleeding, mental/mood changes, swelling ankles/feet, severe headache, dizziness, stomach/abdominal pain, missed/heavy/painful periods, change in the amount of urine, frothy urine, pain/redness/swelling of arms or legs, swelling abdomen.

Get medical help right away if you have any very serious side effects, including:

  • chest pain, shortness of breath.

This medication may increase your risk of getting a rare but very serious (possibly fatal) brain infection (progressive multifocal leukoencephalopathy-PML).

Get medical help right away if you have any of these side effects:

  • clumsiness, loss of coordination/balance, weakness, sudden change in your thinking (such as confusion, difficulty concentrating, memory loss), difficulty talking/walking, seizure, visionchanges.

Sirolimus may slow wound healing after surgery. The risk of poor wound healing is higher if you are obese.

Sirolimus may cause your cholesterol/triglycerides to increase.

Sirolimus can commonly cause a rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe reaction. Get medical help right away if you develop any rash.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Precautions:

General:

Sirolimus can make you more likely to get infections or may worsen any current infections. Wash your hands well to prevent the spread of infection. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.

Do not have immunizations/vaccinations without the consent of your doctor. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).

This medication may increase your risk of developing skin cancer. Avoid prolonged sun exposure, tanning booths, and sunlamps. Use a sunscreen with a high sun protection factor (SPF) and wear protective clothing when outdoors.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

  • Allergy: Before taking sirolimus, tell your doctor or pharmacist if you are allergic to it; or to temsirolimus; or if you have any other allergies.
  • Before using this medication, tell your doctor or pharmacist if you had: liver disease, high cholesterol/triglyceride levels, cancer, any recent/current infections.

Pregnancy Risk: Category C- It may harm an unborn baby.

Breastfeeding: This medication may pass into breast milk and may have undesirable effects on a nursing infant. Breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

Interactions:

  • Some products that may interact with this drug include: ACE inhibitors (such as benazepril, lisinopril), other drugs that weaken the immune system/increase the risk of infection (such as natalizumab, rituximab, tacrolimus).
  • Other medications can affect the removal of sirolimus from your body, which may affect how sirolimus works. Examples include azole antifungals (such as itraconazole, ketoconazole, voriconazole), enzalutamide, macrolide antibiotics (such as clarithromycin, erythromycin), mifepristone, rifamycins (such as rifampin, rifabutin), St. John’s wort, among others.
  • Sirolimus is very similar to temsirolimus. Do not use medications containing temsirolimus while using sirolimus.

Overdose:

If overdose is suspected, contact a poison control center or emergency room right away

Notes

Laboratory and/or medical tests (such as kidney/liver function, cholesterol/triglyceride levels, urine tests for protein, sirolimus trough level) will be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

If you had an organ transplant, attend a transplant education class or support group to learn more about the signs of organ rejection such as a feeling of being ill, fever, or tenderness/pain around the transplanted organ. Tell your doctor right away if you notice any of these signs.

Missed Dose

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

Storage

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Brands:

Available brands

  • Rapamune [ Pfizer ]

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