Sirolimus

Drug #1492

Sirolimus is a potent non-calcineurin inhibiting immunosuppressant. Sirolimus is given after kidney transplant to keep body from rejecting the new kidney. It can cause hyperlipidemias. It has been shown to possess antifungal and antineoplastic properties. Sirolimus is often given in conjunction with cyclosporin.<br><b>Everolimus </b>A derivative of the natural macrocyclic lactone sirolimus with immunosuppressant and anti-angiogenic properties. In cells, everolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of the mammalian Target of Rapamycin (mTOR), a key regulatory kinase. Inhibition of mTOR activation results in the inhibition of T lymphocyte activation and proliferation associated with antigen and cytokine (IL-2, IL-4, and IL-15) stimulation and the inhibition of antibody production. Check for active clinical trials or closed clinical trials using this agent.

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Primary Characteristics

Sirolimus is also known as Everolimus.

Molecular Weight: 914.2 · Non-proprietary name: Sirolimus.

Pharmacokinetics

Distribution: Sirolimus has a volume of distribution is 12(7.4-16.6)l/kg. plasma protein binding is 40%.

Elimination: plasma half-life is 46.1-78.5hr.

Indications

Sirolimus is primarily indicated in conditions like Autoimmune disease, Rejection of organ transplants.

Sirolimus is also indicated for secondary conditions like Prophylaxis of organ rejection in kidney allograft recipients.

Contraindications

Sirolimus is contraindicated in conditions like Hypersensitivity to the drug.

Dosage

None recorded.

Drug Interactions

Unknown1 interaction

2 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Sirolimus in overdosage may give rise to further complications which include Blood disorders .

Sirolimus is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Constipation , Diarrhea, GI disturbance, Hypersensitivity reactions, Nausea and vomiting.

Warnings / Precautions

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly and to check for unwanted effects. While you are taking sirolimus, it is important to maintain good dental hygiene and see a dentist regularly for teeth cleaning. Sirolimus may lower your body's resistance and there is a chance you might get the infection the immunization is meant to prevent. In addition, other persons living in your household should not take or have recently taken oral polio vaccine since there is a chance they could pass the polio virus on to you. Also, avoid other persons who have taken the oral polio vaccine. Do not get close to them, and do not stay in the same room with them for very long. If you cannot take these precautions, you should consider wearing a protective face mask that covers the nose and mouth.

Interference in Pathology

Sirolimus may interfere in the diagnosis of Abnormal LFTs , Increased Alkaline Phosphatase Levels.

Available Brands

Click on a strength to view available brands.

Single Ingredient

Tabs

0.25 mg 0.75 mg 10 mg 5 mg

Storage Conditions

Sirolimus should be stored Tabs.

Drug Classification

1.8.1 — Immunomodulators

Manufacturers

Manufacturers of Sirolimus in Pakistan:

Novartis