Sirolimus

Immunomodulator · Immunosuppressant

Indications

Prophylaxis of organ rejection in adults at low to moderate immunological risk receiving a renal transplant. It is recommended that sirolimus be used initially with cyclosporin microemulsion and corticosteroids for 2-3 months. Continue Sirolimus as maintenance therapy with corticosteroids only if cyclosporin can be progressively discontinued.

Dosage

Initial therapy: Adults: 6 mg oral loading dose followed by 2 mg/day the Astlimus dose should be individualized to obtain 4-12 mg/mL over 4-8 wk whole blood trough levels. Maintenance therapy: Adults: Progressively discontinue cyclosporin and adjust Sirolimus dose to obtain 12-20 mg/mL whole blood trough levels.

Adverse Effects

Hyper cholesterolaemia, hypokalaemia, hyperlipidaemia, thrombocytopenia, anaemia, acne, abdominal pain, urinary tract infection, arthralgia, diarrhoea, lymphocele, peripheral oedema, including lactic dehydrogenase.

Risk Factor (Pregnancy/Lactation)

Contraindications: Pregnancy, lactation. Precautions: Co-administration of cyclosporin and Sirolimus as maintenance therapy is not recommended. The use of live vaccines should be avoided during treatment with sirolimus whole blood trough levels should be closely monitored in hepatically impaired patients. Monitor whole blood trough levels in patients taking or discontinuing strong inducers or inhibitors of CYP3A4 and in patients where cyclosporin is being markedly reduced or discontinued. Antibiotics for pneumocystis carinii should be administered for 12 months, following transplant.

Interactions

CYP3A4 inhibitors and inducers, GI prokinetic agents, grapefruit juice.

Pharmacokinetics

Absorption: Rapid. Metabolism: Hepatic and intestinal. Half-life elimination: 57-63 hrs. Time to peak: 1-2 hrs. Excretion: Faeces (91%). Urine (2.2%).

Brands with this active ingredient

• Astlimus
• Cymusi Oral
• Rapamune

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.