Immunosuppressants

Question 0

Tacrolimus (FK506)

Answer 0

• MOA: Binds FK-binding protein, inhibiting secretion of IL-2
• Use: organ transplant recipients
• Toxicity: nephrotoxicity, peripheral neuropathy, HTN, pleural effusion, hyperglycemia

Question 1

Cyclosporine

Answer 1

• MOA: Binds cyclophilins
  
  1. Blocks activation of T cells by inhibiting calcineurin
  2. Prevents production of IL-2 and its receptor
• Use: suppresses organ rejection after transplantation; some autoimmune disorders
• Toxicity: viral infections and lymphoma; nephrotoxic (prevent with mannitol diuresis); gout

Question 2

Sirolimus (Rapamycin)

Answer 2

• MOA: Inhibits mTOR- inhibits T cell proliferation in response to IL-2
• Use: Immune suppression after kidney transplantation
  
  1. Combo w/ cyclosporine & corticosteroids
  2. Also used w/ drug-eluting stents
• Toxicity: Hyperlipidemia, thrombocytopenia, leukopenia

Question 3

Daclizumab

Answer 3

• MOA: Monoclonal antibody w/ high affinity for IL-2 receptor on activated T cells
• Use: immunosuppression in organ transplants; MS
• Toxicity: HTN

Question 4

Azathioprine

Answer 4

• MOA: Antimetabolite precursor of 6-MP that interferes w/ metabolism & synth of nucleic acids
  
  1. Toxic to proliferating lymphocytes
• Use: Kidney transplant, autoimmune disorders (glomerulonephritis, and hemolytic anemia)
• Toxicity: Bone marrow suppression.
  
  1. MP is metabolized by xanthine oxidase- tox increased by allopurinol

Question 5

Muromonab-CD3 (OKT3)

Answer 5

• MOA: monoclonal antibody binds CD3 epsilon chain
  
  1. Blocks interaction w/ CD3 responsible for signal transduction
• Use: immunosuppression after kidney transplant
• Toxicity: cytokine release syndrome; hypersensitivity rxn

Question 6

Erythropoietin (epoetin)

Answer 6

• Recombinant epo analogue that stimulates RBC formation
• Use: Anemias esp in renal failure
• Toxicity: Stroke or CV effects

Question 7

Interferon alpha

Answer 7

• MOA: cytokine antagonists

- Use: Hep B, Hep C, Kaposi’s sarcoma, leukemia, melanoma

Question 8

Interferon beta

Answer 8

• MOA: cytokine antagonists

- Use: MS

Question 9

Interferon gamma

Answer 9

• MOA: cytokine antagonist

- Use: Chronic granulomatous disease

Question 10

Infliximab

Answer 10

• TNF alpha inhibitor

- Used for Crohn’s RA, psoriatic arthritis, and ankylosing spondylitis

Question 11

Adalimumab

Answer 11

TNF alpha antibody

Treats Crohns, RA, Psoriatic Arthritis

Question 12

Etanercept

Answer 12

• Anti TNF alpha antibody

- Tx crohn’s, RA, and psoriatic arthritis