Updated: 10/17/2020

Immunosuppressive Drugs

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Overview
 

 
Snapshot
  • A 36-year-old woman presents to the emergency department with worsening weakness and decreased visual acuity of the right eye. She reports that her symptoms progressively worsened over the course of a week and after developing an upper respiratory infection. Medical history is significant for multiple sclerosis (MS) treated with rituximab. Physical examination is significant for 2/5 strength in the lower extremities and an afferent pupillary defect appreciated in the right eye. Magnetic resonance imaging of the brain and spine shows new enhancing lesions when compared to prior imaging. After further evaluation, it was determined she had an MS exacerbation. She is started on intravenous methylprednisolone.
Immunosuppressants
 
Immunosuppressants
Medication
Clinical Use
Mechanism of Action Adverse Effects
Cyclosporine
  • Rheumatoid arthritis
  • Psoriasis
  • Transplant rejection prophylaxis
  • Calcineurin inhibitor which
    • impairs IL-2 production and release
    • impairs IL-2-induced T-cell activation
  • Nephrotoxicity 
  • Neurotoxicity
  • Hirsutism
  • Gingival hyperplasia
  • Hypertension
  • Hyperlipidemia
Tacrolimus (FK506) 
  • Transplant rejection prophylaxis
  • Calcineurin inhibitor via binding with intracellular FKBP-12 protein which
    • impairs IL-2 production and release
    • impairs IL-2-induced T-cell activation
  • Nephrotoxicity
  • Neurotoxicity
  • ↑ risk of diabetes
Sirolimus (Rapamycin)
  • Lymphangioleiomyomatosis
  • Renal transplantation prophylaxis
  • mTOR inhibitor via binding with intracellular FKBP-12 protein which
    • ↓ cytokine-induced T-cell proliferation
  • Pancytopenia
  • Hyperlipidemia
  • Edema
  • Insulin resistance
Basiliximab
  • Renal transplantation prophylaxis
  • Targets the α-chain of the IL-2 receptor complex which
    • is expressed on activated T-cells
  • Edema
  • Tremor
  • Hypertension
Azathioprine 
  • Rheumatoid arthritis
  • Renal transplantation
  • Inflammatory bowel disease
  • precursor of 6-mecaptopurine which
    • inhibits purine nucleotide synthesis 
    • incorporates itself into the cell's DNA and halts replication
  • Pancytopenia 
Mycophenolate mofetil
  • Organ transplantation
  • Lupus nephritis
  • Inosine monophosphate dehydrogenase (IMPDH) inhibitor which 
    • impairs guanosine nucleotide synthesis
  • Gastrointestinal upset
  • Pancytopenia
  • Hypertension
Corticosteroids
  • A number of autoimmune and inflammatory disorders
  • NF-κB inhibitor
  • Induces T-cell apoptosis
  • Hyperglycemia
  • Osteoporosis
  • Cushing syndrome
  • Adrenocortical atrophy
  • Peptic ulcers
  • Cataracts
  • Avascular necrosis
  • Psychosis
 

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(M1.IM.13.59) A 31-year-old female receives a kidney transplant for autosomal dominant polycystic kidney disease (ADPKD). Three weeks later, the patient experiences acute, T-cell mediated rejection of the allograft and is given sirolimus. Which of the following are side effects of this medication?

QID: 101013
1

Nephrotoxicity, hypertension

12%

(39/320)

2

Pancreatitis

7%

(22/320)

3

Hyperlipidemia, thrombocytopenia

55%

(177/320)

4

Cytokine release syndrome, hypersensitivity reaction

9%

(29/320)

5

Nephrotoxicity, gingival hyperplasia

13%

(42/320)

M 3 E

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Evidence (4)
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EXPERT COMMENTS (7)
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