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  • Writer's pictureIkris Pharma

ALL YOU NEED TO KNOW ABOUT SIROLIMUS


sirolimus and its side effects

Sirolimus is a compound that is used to prevent organ transplant rejection or coating in coronary stents. This compound is also used in the treatment of a rare lung disease known as lymphangioleiomyomatosis. Sirolimus is used as an immunosuppressant that suppresses the immunity of the human body.

Sirolimus compound has an immunosuppressant activity that means it helps in preventing the rejection of transplant organs in the body it works by inhibiting the activation of B cell and T cell by reducing the sensitivity of interleukin 2 through mTOR inhibition.

Sirolimus was originally known as rapamycin and was used as an antifungal agent. It is basically produced by bacterium streptomyces hygroscopicus. After its regular use as an antifungal agent, it was discovered that it has immunosuppression as well as antiproliferative properties. This was now approved by the U.S food and drug administration in 1999 to be used as an immunosuppressive agent.

The main advantage of sirolimus is that it has a calcineurin inhibitor which has very low toxicity towards the kidney. Patients with transplant organs having calcineurin inhibitors may develop impaired kidney function; this situation can be avoided by using sirolimus.


Dosage and administration: Sirolimus is present in two different forms:

  • Tablet: 0.5mg, 1 my, 2mg

  • Oral solution: 60 mg per 60 ml

Sirolimus tablets should be taken once daily with or without food. Do Not Crush, split, or chew the tablet should be taken whole with water. Sirolimus medication should be taken at the same time of the day. The dosage of sirolimus is based upon patient weight, laboratory tests, medical condition, and response to treatment.

This medication should immediately be taken after organ transplantation or within 4 hours of organ transplantation. The concentration of sirolimus is decided by the patient having low or high immunologic risk. Patients having low to moderate in logic risk may have sirolimus and cyclosporine combination therapy for 2-4 months post-transplantation.

Patients having a high risk of immunologic therapy may have sirolimus and cyclosporine combination therapy for 12-month post-transplantation.

The dosage of sirolimus should be taken according to the doctor's prescription. The dose should not be altered as it will not improve the condition that it will increase the risk of side effects.

The optimal level of sirolimus is approximately 4-20ng/ml. The concentration of Sirolimus varies in accordance with the transplant type, protocol, and concentration.


Side effects:

The most common side effect of sirolimus are:

  • Hypertension

  • Hypertriglyceridemia

  • Peripheral edema

  • Hypercholesterolemia

  • Abdominal pain

  • Diarrhoea

  • Headache

  • Creatinine increase

  • Urinary tract infection

  • Fever

  • Nausea

  • Anemia

  • Pain

  • Constipation

  • Joint pain

  • Thrombocytopenia

Few severe adverse reactions of sirolimus 1 mg or 2 mg are mentioned below which when appear the patient should immediately consult your doctor. These are:

  • Renal function

  • Hyperlipidemia

  • Angioedema

  • Hypersensitivity

  • Fluid accumulation and wound healing

  • De novo use without cyclosporine

  • Intestinal lung disease

  • Latent viral infections

  • Proteinuria

  • Inhibitor-induced HUS

  • Rash

  • Itching

  • Swollen skins

  • Unusual bleeding

  • Swelling in the face, throat, tongue, and different parts of the body.

  • Hives

  • Hoarseness


Uses of sirolimus during pregnancy may lead to embryo-fetus damage thus it should only be used if it is highly patient. The sirolimus drug may pass through breast milk and may cause damage to the newborn babies. The patient suffering from hepatic impairment may decrease the dose of sirolimus.


Drug interaction

  • Avoid the use of concomitant with strong CYP3A4/P-gp inducers or strong CYP3A4/P-gp inhibitors that decrease or increase sirolimus concentrations.

  • Special attention should be paid with the drug-containing inhibitor or inducer of CYP3A4/P-gp.


Storage and disposal: Siromus 1 mg or Siromus 2 mg is stored at room temperature in a container away from light and children the container should be kept away from moisture and excess heat. The oral solution of sirolimus should be kept in the refrigerator.

Unused medication should be discarded after one month when the bottle opens. The medication should be disposed of in such a way that it does not cause any harm to children, animals, or any other person. It should be discarded carefully. The medication is discarded with proper SOP.


Price: It is very cost-friendly and economical. This medication is available at all registered pharmaceutical companies and can be bought by showing doctors prescriptions to the pharmacist. This medication is generally present when paid cash and is not covered in insurance plans.


Read:- Detailed info about tacrolimus - A transplant medication



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