Immunosuppressants and biologics

  1. Name three anti-metabolite agents.
    Azathioprine, methotrexate and mycophenolate mofetil
  2. Azathioprine method of action?
    Gets converted to 6-mercaptopurine in the body.

    Purine synthesis inhibitor - prevents synthesis of adenine and guanine. Especially active in lymphocytes leading to apoptosis.

    Levels must be checked of an enzyme (TPMT) that converts 6MP to toxic products.
  3. Mycophenolate mofetil MOA?
    Salvage pathway - inhibits production of guanosine monophosphate. Lymphocytes cannot convert guanine back to guanine monophosphate therefore proliferation is inhibited.
  4. Methotrexate MOA and SE?
    Depletes folic acid (dihydrofolate -> tetrahydrofolate) - dihydrofolate inhibitor.
    Therefore inhibits generation of DNA building blocks

    SE - GI common, leucopenia, thrombocytopenia, transaminitis, pneumonitis (methotrexate lung)
  5. Ciclosporin MOA and SE?
    Inhibits calcineurin pathway (involved with calcium metabolism and influx).
    Inhibits nuclear transcription factor (NF-ATc) which activates T cells so transcription of IL-2 gene is prevented.

    SE - drug interactions, toxicity, hypertension, tremor
  6. Targets of biologic therapies and an example for each.
    * Cytokine targeting - e.g. Anti-TNF - infliximab
    * Anti cellular - e.g. Anti B cell - Rituximab
    * Receptor targeting - e.g. Herceptin
    * Endogenous product - e.g. Interferon alpha
  7. Which antibiotic should be used for MRSA skin infection?
  8. Where does cellulitis affect?
    Dermis and subcut
  9. Where does ersipelas affect?
  10. SE of biologics?
    • - Infections (esp first 6 months)
    • - Chronic inflammation
    • - Severe heart failure
    • - Viral reactivation e.g. TB
    • - Demyelination
    • - Infusion reaction (if chimaeric)
Card Set
Immunosuppressants and biologics
Immunosuppressants and biologics