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(Rapamune®)

(should not be prescribed as rapamycin)

Indication

As an adjunct to or substitute to a calcineurin phosphatase inhibitor for immunosuppression in patients in whom ciclosporin/tacrolimus have been implicated in allograft pathology.

Contraindications

Hypersensivity to Sirolimus and its derivatives.
Pregnancy and breast feeding.
 

Presentation - 1mg and 2mg tablets

Dosage and Administration
Doses should be given on an empty stomach
Day 1    6mg daily
Day 2    6mg daily
Day 3 onwards 2mg daily adjusted according to levels
 

Monitoring

Target range 5-15ng/ml depending on whether it is an adjunct to or substitute for a CNI.
As an adjunct to CNI: CNI levels with concurrent sirolimus should be lower eg. Tacroimus levels 3-5

Switch from tacrolimus to sirolimus

If clinically indicated, patients may be switched from tacrolimus to sirolimus. This can be performed abruptly.

Tacrolimus is stopped the night before giving 8mg sirolimus on day 1, 4mg on day 2, then 2mg and levels are measured.
 

Side Effects





  • Raised triglycerides & cholesterol
  • Thrombocytopeania
  • Mouth Ulceration
  • Anaemia
  • Neutropenia
  • Proteinuria
  • Hypokalaema
  • Arthralgia
  • Epistaxis
  • Delayed wound healing
  • Lymphocele
  • Rash
  • Oedema
  • Infections
  
  • PTLD
  • Diarhoea
  


Drug Interactions

Compounds which modulate CYP3A4 activity may effect Sirolimus levels.
Drugs which may increase sirolimus levels


  • Diltiazem
  • Bromocriptine
  • Azole antifungals
  • Cimetidine
  • Macrolide antibiotics
  • Danazol
  • Prokinetic agents
  • Protease inhibitors
  • Grapefruit juice
  

 

Drugs which may decrease Sirolimus levels

  • Rifampicin
  • Anticonvulsants


Caution should be exercised with concomitant administration of nephrotoxic drugs.

 

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Archive of Nov 2006 version of Rapamycin Jul 23 2009 0 kB 213

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