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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.

I. DRUGS THAT INFLUENCE THE IMMUNE RESPONSE

CLASSIFICATION OF IMMUNOMODULATORS

II. IMMUNOSUPPRESSANTS

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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