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TERMS TO LEARN

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Aplastic Anemia Low blood count due to defective regeneration of cells.
Erythema Nodosum Leprosum Painful erythematous subcutaneous nodules seen in patients with a high level of mycobacterial antigens.
Hirsutism Excessive body and facial hair in women.
Kawasaki Disease Medium to large vessel vasculitis seen in children; symptoms include conjunctivitis, rash, erythema of the palms and soles, coronary aneurysms, and strawberry tongue.
Malignant Osteopetrosis Increased skeletal density due to osteoclastic failure.

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I. DRUGS THAT INFLUENCE THE IMMUNE RESPONSE

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CLASSIFICATION OF IMMUNOMODULATORS

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II. IMMUNOSUPPRESSANTS

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IMMUNOSUPPRESSANTS: DRUG FACTS

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Drug Pharmacokinetics Mechanism of Action Clinical Uses Side Effects
Fungal Cyclic Peptide Antibiotic
Cyclosporine (Neoral, Gengraf, Sandimmune)
  • A: PO or IV

  • M: Hepatic (P450)

  • E: Metabolites excreted in feces

  • Binds to cyclophilin to form a complex that inhibits calcineurin

  • Highly selective inhibition of T cell activation by blocking cytokine production (especially IL-2)

  • Prophylaxis for organ rejection following transplant (ie, kidney, heart, liver, BMT, lung, and pancreas)

  • Treatment of graft versus host reactions (often in combination with corticosteroids)

  • Autoimmune disorders (ie, RA and severe psoriasis)

  • Gingival hyperplasia

  • GI distress

  • Increased risk of infections and malignancies

  • Hirsutism

  • Hypertension

  • Nephrotoxicity

  • Neurologic effects (seizures and tremor)

Macrolide Antibiotics
Sirolimus (Rapamune)
  • A: PO

  • M: Metabolized in intestinal wall and hepatic (P450)

  • E: Metabolites excreted in feces

  • Binds to FK-binding protein, inhibiting the response of T cells to cytokines without affecting cytokine production

  • Liver and kidney transplantation

  • Potentially useful in conjunction with cyclosporine with which it acts synergistically

  • Blood dyscrasias

  • Hepatic artery thrombosis

  • Increased risk of infections and malignancies

  • Hyperlipidemia

  • Hypertension

  • Rash

  • Peripheral edema

  • Inhibits P450 enzymes

Tacrolimus/FK-506 (Prograf, Hecoria)
  • A: PO or IV

  • M: Hepatic (P450)

  • E: Metabolites excreted in feces

  • Binds to FK-binding protein and forms a complex that inhibits calcineurin

  • Calcineurin regulates the T cells ability to produce interleukins

  • 10–100 times more potent immunosuppression than cyclosporine

  • Liver, cardiac, and kidney transplantation

  • Asthenia

  • Blood dyscrasias

  • GI (diarrhea, nausea, abdominal pain)

  • Hyperglycemia due to new onset diabetes

  • Increased risk of infections and malignancies

  • Nephrotoxicity

  • Neurotoxicity

  • Hyperkalemia

  • Inhibits P450 enzymes

Glucocorticoid
Prednisone
  • A: PO

  • M: Metabolized in multiple tissues including the liver (P450 minor)

  • E: Metabolites excreted in urine

  • Impaired release of cytokines from macrophages and granulocytes

  • Suppression of T cell proliferation and activation

  • Suppression of antibody production

  • Reduction of accumulation of macrophages

  • Seems to spare B cell population under normal conditions

  • Inhibit migration of cells that cause acute rejection of an organ, which is an inflammatory response

  • Administered before, during, and after transplant surgery (always used in combination with other immunosuppressants, such as cyclosporine, for organ transplantation)

  • Autoimmune diseases (eg, RA, SLE, and dermatomyositis)

  • Treatment of acute graft versus host rejection (suppress secondary [antibody] ...

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