Sirolimus (rapamycin)

What is Sirolimus

Sirolimus (rapamycin) is an immunosuppressant. Sirolimus is a macrolide produced by Streptomyces hydroscopicus, a streptomycete that was isolated from a soil sample from Easter Island.

Sirolimus has antifungal, antitumor, and immunosuppressive activities. 

Brand Name

Rapamune

Indications & Dosage

  • heart transplant rejection prophylaxis
  • kidney transplant rejection prophylaxis
  • lymphangioleiomyomatosis

For kidney transplant rejection prophylaxis

Side Effects

  1. abdominal pain
  2. acne vulgaris
  3. acneiform rash
  4. alopecia
  5. amenorrhea
  6. anaphylactic shock
  7. anaphylactoid reactions
  8. anemia
  9. angioedema
  10. arthralgia
  11. ascites
  12. azoospermia
  13. BK virus-associated nephropathy
  14. bronchiolitis obliterans
  15. cardiac tamponade
  16. chest pain (unspecified)
  17. constipation
  18. cough
  19. cystitis
  20. diabetes mellitus
  21. diarrhea
  22. dizziness
  23. dyspnea
  24. dysuria
  25. edema
  26. elevated hepatic enzymes
  27. encephalopathy
  28. epistaxis
  29. exfoliative dermatitis
  30. fatigue
  31. fever
  32. folliculitis
  33. gingivitis
  34. headache
  35. hematuria
  36. hemolytic-uremic syndrome
  37. hepatic necrosis
  38. hypercholesterolemia
  39. hyperglycemia
  40. hyperlipidemia
  41. hypertension
  42. hypertrichosis
  43. hypertriglyceridemia
  44. hypokalemia
  45. hypophosphatemia
  46. hypoxia
  47. immunosuppression
  48. impaired wound healing
  49. infection
  50. leukoencephalopathy
  51. leukopenia
  52. lymphocele
  53. lymphoma
  54. menorrhagia
  55. myalgia
  56. nausea
  57. nephrotic syndrome
  58. neutropenia
  59. new primary malignancy
  60. oligospermia
  61. onycholysis
  62. oral ulceration
  63. pancreatitis
  64. pancytopenia
  65. pericardial effusion
  66. peripheral edema
  67. pharyngitis
  68. pleural effusion
  69. pneumonitis
  70. post-transplant lymphoproliferative disorder (PTLD)
  71. proteinuria
  72. pruritus
  73. pulmonary embolism
  74. pulmonary fibrosis
  75. pulmonary hypertension
  76. rash
  77. sinus tachycardia
  78. stomatitis
  79. thrombocytopenia
  80. thromboembolism
  81. thrombosis
  82. thrombotic thrombocytopenic purpura (TTP)
  83. vasculitis
  84. wound dehiscence
  85. xerosis

Monitoring Parameters

  • CBC
  • serum cholesterol profile
  • serum creatinine/BUN
  • serum lipid profile
  • serum potassium
  • sirolimus concentrations

Contraindications

  • accidental exposure
  • Black patients
  • breast-feeding
  • cardiac arrhythmias
  • cardiac disease
  • children
  • contraception requirements
  • coronary artery disease
  • diabetes mellitus
  • dialysis
  • heart failure
  • hepatic disease
  • hypercholesterolemia
  • hyperlipidemia
  • hypertriglyceridemia
  • immunosuppression
  • infants
  • infection
  • infertility
  • liver transplant
  • lung transplant
  • lymphoma
  • neonates
  • new primary malignancy
  • ocular exposure
  • pregnancy
  • proteinuria
  • renal failure
  • renal impairment
  • reproductive risk
  • requires a specialized care setting
  • requires an experienced clinician
  • soya lecithin hypersensitivity
  • sunlight (UV) exposure
  • surgery
  • vaccination
  • wound dehiscence

Interactions

  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Alpelisib
  • Amiodarone
  • Amlodipine
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amobarbital
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amprenavir
  • Angiotensin-converting enzyme inhibitors
  • Apalutamide
  • Aprepitant, Fosaprepitant
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Pravastatin
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atorvastatin
  • Atorvastatin; Ezetimibe
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Azathioprine
  • Barbiturates
  • Basiliximab
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Blinatumomab
  • Boceprevir
  • Bosentan
  • Brigatinib
  • Butabarbital
  • Cabozantinib
  • Canakinumab
  • Capmatinib
  • Carbamazepine
  • Carboplatin
  • Carvedilol
  • Caspofungin
  • Cenobamate
  • Ceritinib
  • Chlorambucil
  • Chloramphenicol
  • Cimetidine
  • Cisapride
  • Clarithromycin
  • Clofazimine
  • Cobicistat
  • Conivaptan
  • Crizotinib
  • Cyclosporine
  • Dabrafenib
  • Daclatasvir
  • Daclizumab
  • Dalfopristin; Quinupristin
  • Danazol
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Daunorubicin
  • Delavirdine
  • Dexamethasone
  • Diltiazem
  • Doxorubicin
  • Dronedarone
  • Duvelisib
  • Echinacea
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elagolix
  • Elagolix; Estradiol; Norethindrone acetate
  • Elbasvir; Grazoprevir
  • Elexacaftor; tezacaftor; ivacaftor
  • Eliglustat
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Emapalumab
  • Encorafenib
  • Enzalutamide
  • Erdafitinib
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Eslicarbazepine
  • Etravirine
  • Ezetimibe; Simvastatin
  • Fedratinib
  • Flibanserin
  • Fluconazole
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fluvastatin
  • Fluvoxamine
  • food
  • Fosamprenavir
  • Fosphenytoin
  • Fostamatinib
  • Glecaprevir; Pibrentasvir
  • Glycerol Phenylbutyrate
  • grapefruit juice
  • Ibrutinib
  • Idelalisib
  • Imatinib
  • Indinavir
  • Infliximab
  • Isavuconazonium
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Istradefylline
  • Itraconazole
  • Ivacaftor
  • Ivosidenib
  • Ixabepilone
  • Ketoconazole
  • Lapatinib
  • Larotrectinib
  • Ledipasvir; Sofosbuvir
  • Lefamulin
  • Letermovir
  • Live Vaccines
  • Lomitapide
  • Lopinavir; Ritonavir
  • Lorlatinib
  • Lovastatin
  • Lovastatin; Niacin
  • Lumacaftor; Ivacaftor
  • Lumacaftor; Ivacaftor
  • Melphalan
  • Mephobarbital
  • Methohexital
  • Metoclopramide
  • Metreleptin
  • Metronidazole
  • Micafungin
  • Mifepristone
  • Mitotane
  • Mycophenolate
  • Natalizumab
  • Nefazodone
  • Nelfinavir
  • Neratinib
  • Nevirapine
  • Niacin; Simvastatin
  • Nicardipine
  • Nilotinib
  • Ombitasvir; Paritaprevir; Ritonavir
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Amoxicillin; Rifabutin
  • Oritavancin
  • Osilodrostat
  • Osimertinib
  • Ozanimod
  • Pazopanib
  • Pentobarbital
  • Perindopril; Amlodipine
  • Phenobarbital
  • Phenytoin
  • Pitavastatin
  • Ponatinib
  • Posaconazole
  • Pravastatin
  • Primidone
  • Protease inhibitors
  • Ranolazine
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Rimegepant
  • Ritonavir
  • Rolapitant
  • Rucaparib
  • Rufinamide
  • Sapropterin
  • Saquinavir
  • Sarilumab
  • Secobarbital
  • Selpercatinib
  • Siltuximab
  • Simeprevir
  • Simvastatin
  • Simvastatin; Sitagliptin
  • Sofosbuvir; Velpatasvir
  • Sofosbuvir; Velpatasvir; Voxilaprevir
  • Sorafenib
  • St. John’s Wort, Hypericum perforatum
  • Streptogramins
  • Tacrolimus
  • Talazoparib
  • Tazemetostat
  • Teduglutide
  • Telaprevir
  • Telithromycin
  • Telotristat Ethyl
  • Temozolomide
  • Temsirolimus
  • Tezacaftor; Ivacaftor
  • Thiopental
  • Tinidazole
  • Tipranavir
  • Tocilizumab
  • Tofacitinib
  • Topotecan
  • Trandolapril; Verapamil
  • Tucatinib
  • Ubrogepant
  • Upadacitinib
  • Vemurafenib
  • Venetoclax
  • Verapamil
  • Voriconazole
  • Voxelotor
  • Zanubrutinib
  • Zileuton
  • Zonisamide
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