Sirolimus is a Medicine belongs to Immunosuppressants group whose information about Brand can be referenced from   Book : Martindale    Page : 1968   Edition : 38,

  ►   Brandname : Rapamune, Rui Pa Ming

  ►  Strength : Oral solution with   ,

Reference of this Medicine for its Strength can be taken from   Book : Martindale    Page : 1968   Edition : 38,
A Route of administration in pharmacology and toxicology is the path by which a drug, fluid, poison, or other substance is taken into the body. Routes of administration are generally classified by the location at which the substance is applied. Common examples include oral and intravenous administration.

  ►  Route of administration : Oral,
Reference :-   Book : Martindale    Page : 1966   Edition : 38,

Dosing of Medicine differ in Adult & Pediatrics ↓


Adult Dose

S.No Ailment   Route   Dose Min   Dose Max   Unit   Dosage Form   Frequency   Additional Info
1 For the prevention of graft rejection in kidney transplantation Oral It is given with ciclosporin and corticosteroids as soon as possible after transplantation. A loading dose of 6 mg is given orally, followed by a maintenance dose of 2 mg daily, 4 hours after ciclosporin.

Ref :-  Book : Martindale    Page : 1966   Edition : 38,




Pediatric Dose

S.No Ailment   Age Min   Age Max   Weight ( Kg ) Route   Dose Min   Dose Max   Unit   Dosage Form   Frequency  Additional Info  
1 For the prevention of graft rejection in kidney transplantation 13 or above Year less than 40 kg Oral Solution
2 The prevention of graft rejection in kidney transplantation patients at high immunological risk Oral Solution

Ref :- Book : Martindale    Page : 1966   Edition : 38,
►  Side Effect : Common adverse effects:, peripheral oedema, hypokalaemia, hypophosphataemia, hyperlipidaemia, hypercholesterolaemia, hypertriglyceridaemia, Hyperglycaemia, lymphocele, tachycardia, venous thromboembolism, Gastrointestinal disturbances, stomatitis, arthralgia, epistaxis, acne, Rashes, bone necrosis, fever, hypertension, headache, Pain, anaemia, thrombocytopenia, neutropenia, leucopenia, treatment is associated with an increased incidence of lymphoma and other malagnancies, particularly of the skin, and excess exposure to UV light should be avoided during treatment, increased risk of infection including activation of latent viral infections, these include JC virus-associated progressive multifocal leukoencephalopathy (pml) and BK virus-associated nephropathy that can lead to renal graft loss, thrombotic thrombocytopenic purpura, and haemolytic-uraemic syndrome may occur, anaphylactic reactions, angioedema, exfoliative dermatitis, hypersensitivity vasculitis, there are reports of , lymphoedema, pleural effusion, pericardial effusion, renal impairment, proteinuria, focal glomerulosclerosis, or nephrotic syndrome may develop, , reports of hepatotoxicity, interstitial lung disease, azoospermia and infertility have been reported,
Ref :-   Book : Martindale    Page : 1967   Edition : 38,

►  Drug Interaction : Drug interaction of Sirolimus is with , Hiv Protease Inhibitors, , , , , Angiotensin conveting enzyme inhibitors ,  Ketoconazole , Delavirdine, Diltiazem , Nevirapine, Rifampicin , Cyclosporine ,
Ref :-   Book : Martindale    Page : 1968   Edition : 38,


  ►    Mechanism of Drug Drug Interaction :  Inhibitors of the cytochrome P450 isoenzyme CYP3A4, such as ketoconazole, HIV-protease inhibitors, the NNRTI delavirdine, and diltiazem may increase plasma concentrations of sirolimus. Conversely, inducers of this isoenzyme, such as nevirapine and rifampicin, may reduce plasma concentrations of sirolimus. Use of sirolimus with strong inhibitors or inducers of CYP3A4 and/or P-glycoprotein is not recommended. Grapefruit juice should not be taken with sirolimus. Ciclosporin can affect the rate and extent of sirolimus absorption and it is recommended that these drugs be given 4 hours apart. Use of sirolimus with a calcineurin inhibitor may also increase the risk of calcineurin inhibitor-induced haemolytic uraemic syndrome, thrombotic thrombocytopenic purpura, or thrombotic microangiopathy. Use of sirolimus with an ACE inhibitor may increase the risk of developing angioedema.,
Ref :-   Book : Martindale    Page : 1968   Edition : 38,


►  Contraindication : Excess mortality, graft loss, and hepatic artery thrombosis has been associated with the use of sirolimus in immunosuppressive regimens in liver transplant recipients and therefore not used in such patients.,
Ref :-   Book : Martindale    Page : 1967   Edition : 38,
  ►  Mechanism of Action :   Sirolimus binds to a protein (FK binding protein-12; FKBP-12; FKPB-12) and this complex inhibits the activation of the mammalian target of rapamycin (mTOR), a key regulatory kinase for cell cycle progression thus suppressing cytokine-driven T-cell proliferation.,
Ref :-   Book : Martindale    Page : 1966   Edition : 38,

Pathway of Dietry Product


​   ► Act.Comp / Nutrient / Food / Herb as follows :- NA


Dietry Substance Interactions


​   ► This Medicine interact with :- NA



ContraIndication Dietry Substance


​   ► This Medicine contraindicate with :- NA

►   Route of Elimination :   Faecal,
Ref :-   Book : Martindale    Page : 1968   Edition : 38,


►    Plasma Half-life :
  Min value :-   terminal half-life in stable renal transplant patients after multiple oral doses is about 62 hours,    Max value :-   NA
Ref :-   Book : Martindale    Page : 1968   Edition : 38,

►    Peak Plasma Concentration :   Min value :-   about 2 hours,    Max value :-   NA
Ref :-   Book : Martindale    Page : 1968   Edition : 38,