Rapamycin
Rapasim (Sirolimus) – a lipophilic macrolide immunosuppressant, which was isolated from a strain of fungus called Streptomyces hygroscopicus in 1972 September. The compound was originally named rapamycin – an antifungal agent. It was approved by the US Food and Drug Administration as an immunosuppressant in September 1999.
Rapasim (Sirolimus) is used in combination with other medications to prevent rejection of kidney transplants.
Rapasim (Sirolimus) is in a class of medications called immunosuppressants. It works by suppressing the body’s immune system. For the prophylaxis of organ rejection in patients receiving renal transplants.
COMPOSITION:
Rapamycin 1mg
MODE OF ACTION:
- In cells, Rapasim 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.
- This results in inhibition of T lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (IL-2, IL-4, and IL-15) stimulation and inhibition of antibody production.
- Rapasim is macrocyclic antibiotic with potent immunosuppressive activity that is used alone or in combination with calcineurin inhibitors and corticosteroids to prevent cellular rejection after renal transplantation.
- Potent inhibitor of B-cell proliferation and immunoglobulin production (humor immunity)
- Rapasim does not affect IL-2 production, unlike Cyclosporine & Tacrolimus, rather inhibits T-cell response to it (Blocks cytokine-stimulated cell proliferation)
- Rapasim substantially inhibits T & B cell proliferation
INDICATIONS
- Prophylaxis of organ rejection in patients aged 13 years or older receiving renal transplants.
Dosage
- Prophylaxis of Renal Transplant Rejection
High immunologic risk
<40 kg: 3 mg/m² loading dose
≥40 kg: 15 mg PO loading dose
Maintenance: 5 mg/day PO if >40 kg and 1 mg/m²/day if <40 kg on day 2 and thereafter; obtain trough levels between days 5 and 7
- Low-to-moderate immunologic risk
<40 kg: 3 mg/m² loading dose
≥40 kg: 6 mg PO loading dose
Maintenance: 2 mg/day PO if ≥ 40 kg and 1 mg/m²/day if <40 kg on day 2 and thereafter; obtain trough levels between days 5 and 7
Disclaimer:
This information is for registered medical practitioner only. Anyone other than medical practitioner should consult medical practitioner before using this product.
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