Table of contents
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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 (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 |
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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.) |
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