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Immunosupressives

  1. Calcinurin inhibition
    1. Cyclosporine        
    2. Tacrolimus 

1. Cyclosporine

  1. Glycopeptide                
  2. Obtained from soil        
  3. Macrolide antibiotic      
  4. Short acting        
  5. Food reduces absorption      
  6. Poor oral bioavailability due to two main reasons:
    1. ABC proteins (MDRP-1, MDRP 2)
    2. Rapid metabolism (CYP 3A5 mediated)
  7. Combined routinely with verapamil/diltiazem
  8. Use GVHD
  9. S/e
    1. Hypertension
    2. Hyperlipidemia  Most common side effects
    3. Hyperglyecemia (More with tacrolimus)
    4. Hypomagnesimia
    5. Hyperkalemia
    6. Hirsutism (not with tacrolimus)
    7. Gum enlargement (not with tacrolimus)
    8. Psychosis, seizures (Overdose)
    9. Hepato & nephrotoxicity
    10. Secondary cancers
  10. MAO
     
    Cyclosporine binds to calcineurine, binding is aided by cyclophillins---inhibits transcription of IL2---CD4 cell proliferation  

2. Tacrolimus does not bind to cyclophillins; instead binds to FKBP-12

No gum enlargement or hirsutism 

  1. mTOR inhibitors
    1. Sirolimus        
    2. Everolimus
      1. useful for organ transplantation, GVHD and autoimmune disorders
      2. sirolimus also has antifibrotic properties so added to cardiac stents to avoid occlusion
      3. main side effect is dyslipidemia
  2. Mycophenolate Mofetil
    1. Prodrug
    2. Short acting
    3. GI irritant
    4. Inhibits inosine monophosphate dehydrogenase
    5. Blocks T cell proloferation
    6. Poorly tolerated
    7. Bone marrow depression occurs
    8. Used in refractory patients
    9. Given as a component of triple therapy
    10. PAC: prednisolone, azathioprine and cyclosporine was used originally  

D. Thalidomide :

 Immunomodulator,not immunosuppressant

 

Use:

  1. HIV aphthous ulcer
  2. HIV wasting disease
  3. Type 2 lepra reaction
  4. SLE
  5. Sjogren syndrome
  6. Amyloidosis
  7. IBD
  8. Multiple myeloma

Side effects:

  1. Hypothyroidism
  2. Constipation
  3. Peripheral neuropathy
  4. Rashes
  5. Teratogenecity
  6. DVT
  7. Sedation 

P/K: metaboloised by Hoffmann elimination(enenatiomer formation)

  1. Glucocorticoids
  2. Azathioprine
  3. Misc drugs
    1. Chloroquine  
    2. Leflunomide
    3. Basiliximab
    4. Daclizumab        
    5. Muromonab  





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