Rx Chemotherapeutics

    .

     

     

    Cytotoxic Therapy:

     

    Drug Class Use Notes
    Cytarabine Anti-metabolite

    - AML

    - Non-Hodghkin's Lymphoma

     
    Anthracycline
     - Daunorubicin (Daunomycin)
     - Daunorubicin (liposomal)
     - Doxorubicin (Adriamycin)
     - Doxorubicin (liposomal)
     - Epirubicin
     - Idarubicin
     - Valrubicin, used only
        to treat bladder cancer
     - Mitoxantrone, anthracycline
       analog

    Anthracycline

    - Derived from streptomyces

    - Intercalating agent (stops

    DNA replication, leading to 

    strand breaks etc..

    - AML

    - ALL

     

    Thalidomide

    Lenalidomide

       

    - High risk of VTE!!! especially when
      used with corticosteroids 

      (Hyperviscocity)

    - Recommend Low Dose ASA (at least)

    - Teratogenic

    Bortezomib

    Proteosome inhibitor

    - Proteosome is a cellular

    garbage collector (removing

    misfolded proteins). 

    - Pro-apoptotic factors get

    removed by proteosome

    preventing cancer apoptosis.

    - Multiple Myeloma  
    Melphalan Alkylating Agent    
    Vincristine

    Binds tubulin dimers, arrests

    mitosis in metaphase

    - ALL  
    Fludarabine Nucleoside analogue - CLL

    - Toxicity: low blood counts

    - Need PCP and anti-HSV prophylaxis

    Cladribine   - Hairy Cell Leukemia

    Highly effective therapy, if doesn't

    respond, consider other dx.

     

    Thalidomide and Lenalidomide

    Indications:

    Multiple Myeloma

    ...

    Mechanism:

    Thalidomide Side Effects:

    - Somnolence

    - Constipation

    - Peripheral Neuropathy

    Lenalidomide Side Effects:

    - Myelosuppression

    Cautions:

    - Teratogenic

    - High risk of VTE (esp if used with steroids)

      Recommend at least low-dose ASA for prophylaxis

     

    Bortezomib

    Indications:

    Multiple Myeloma

    Mantle Cell Lymphoma

    Mechanism:

    - Proteosome inhibitor

    (proteosome is like a 

    "garbage disposal")

    - When inhibited cells

    undergo apoptosis.

    Side Effects:

    - Peripheral Neuropathy

    - Thrombocytopenia

    Cautions:

    - Teratogenic

    - High risk of VTE (esp if used with steroids)

      Recommend at least low-dose ASA for prophylaxis

     

    Melphalan

    Indications:

    Multiple Myeloma

     

    Mechanism:

    - Alkylating Agent

    - Old drug for MM

    Side Effects:

    - Myelosuppression

    - Stem cell toxicity

    Cautions:

    - Not used in induction for pts that are candidates for autologous HSCT


    Myelosuppression

    Drug Class Use Notes
    Hydroxyurea

    Inhibits ribonucleotide

    reductase (decr. ribonucleotides)

    - Sickle Cell Disease

    - Essential Thrombocythemia

    - Polycythemia Vera

    - Monitor CBCs q2w

    - Terratogenic (need contraception)

    - Increases MCV - can monitor compliance

     
         

     

    Anti-Rejection Drugs

     

     

    Anti-Rejection Drugs

    Mycophenylate Mofetil

    (Cellcept)

    Mycophenylate Mofetil = prodrug to

    improve bioavailability (converts to

    mycophenolic acid)

    Use:

    - Renal Transplant

    - Also liver, heart, lung transplants

    - Autoimmune Diseases (Behcets,

      pemphigus, refractory SLE

      small vessel vasculitis, psoriasis)

    Mechanism: Inhibits B and T-cell

      proliferation.

    - Increases cholesterol levels

    - Monitor BUN, Lytes, Ext-Lytes

    NOTE: Typically azathioprine

      preferred in autoimmune cond

      b/c lower incidence of diarrhea.

    Tacrolimus

    (Prograf, Advagraf)

    Use: Allogeneic organ transplant

    - Liver Transplants (first use in 1994)

    - Kidney, heart, small bowel, pancreas

      lung, trachea, skin, cornea, bone

      marrow, limb transplants

    - Topical: atopic dermatitis

    First macrolide immunosuppressant

    was sirolimus (rapamycin), this was

    second.  Produced by Streptomyces

    tsukubaensis in soil.

    Mechanism: Macrolide calcineurin

    inhibitor.  Inhibits calcineurin (activated

    by high Ca2+ levels in activated T-cells)

    Prevents phosphorylation of NF-AT,

    nuclear factor for activated T-cells,

    thereby preventing transcription of

    T-cell signaling and IL-2.

     

    - Renal monitoring (Tacrolimus

      Nephrotoxicity)

    - Note: mechanism similar to 

      ciclosporin but tacro shown to have

      lower acute rejection rates.

    - Interacts with grapefruit and

      antifungals

    - Topical preparations used for

      atopic

    Ciclosporin

    (calcineurin inh.)

    Use: Allogeneic organ tarnsplant.

     

    Mechanism: It is a cyclic non-ribosomal

    peptide that inhibits T-cell inhibitor.

    - Binds cyclophilin -> inhibits calcineurin

    (calcineurin allows transcr. of IL2, etc.)

       
    Tag page (Edit tags)
    • No tags
    Page statistics
    8038 view(s), 11 edit(s) and 8200 character(s)

    Comments

    You must login to post a comment.

    Attach file

    Attachments