Pharm One-Liners: Hematology/Oncology

Antineoplastic folic acid analog that inhibits dihydrofolate reductase

Methotrexate

Antineoplastic pyrimidine analog that inhibits thymidylate synthetase

5-fluorouracil (5-FU)

Antineoplastic pyrimidine analog that inhibits DNA polymerase

Cytarabine

Serious adverse effect associated with cytarabine

Pancytopenia

Antineoplastic purine analogs that inhibit purine synthesis (3)

Azathioprine, 6-mercaptopurine, 6-thioguanine

Drug used concurrently with antineoplastics to reduce renal precipitation of urates

Allopurinol

Antineoplastics that require dose-reduction in patients who are taking allopurinol

Azathioprine, 6-mercaptourine

Enzyme activates purine analogs

Hypoxanthine-guanine phosphoribosyltransferase (HGPRT)

Azathioprine is a prodrug for

6-mercaptopurine

Partial or complete deficiency of an enzyme can increase the toxicity of 5-FU

Dihydropyrimidine dehydrogenase (pharmacogenetic syndrome)

Inhibits microtubule formation by binding to β-tubulin; dose-limiting adverse effect is bone marrow suppression

Vinblastine

Inhibits microtubule formation by binding to β-tubulin; dose-limiting adverse effect is neurotoxicity

Vincristine

Hyperstabilizes microtubule polymer and prevents microtubule breakdown

Paclitaxel, -taxels

These classes of drugs are commonly associated with neurotoxicity (areflexia, peripheral neuritis) (2)

Vinca alkaloids (e.g., vincristine, vinblastine), taxanes (e.g., paclitaxel)

Vinca alkaloids cause excessive free water retention and euvolemic hyponatremia known as

Syndrome of inappropriate secretion of antidiuretic hormone (SIADH)

Prodrugs, that after hepatic bioactivation, bind to N7 nitrogen of guanine and cross-link DNA (2)

Cyclophosphamide, ifosfamide

Serious adverse effect of cyclophosphamide and ifosfamide due to geenration of acrolein

Hemorrhagic cystitis

Agent that is used to bind acrolein and prevent drug-induced hemorrhagic cystitis

Mesna

Nitrosureas that spontaneously form active intermediates that cross-link DNA; can cross blood-brain-barrier and is indicated for brain tumors

Carmustine, -mustines

Alkylating agent that has greater activity against myeloid cells than lymphoid cells; serious adverse effects include myelosuppression and pulmonary fibrosis

Busulfan

Alkylating drugs that cause disulfiram-like reaction to alcohol (2)

Dacarbazine, procarbazine

Anthracyclines that chelate DNA, form free radicals, and cause dose-limiting cardiotoxicity (2)

Daunorubicin; doxorubicin

Iron-chelator that is used to protect against anthracycline-induced cardio-toxicity

Dexarazoxane

Anthracycline-induced cardiotoxicity (dilated cardiomyopathy) is caused by

Increased production of free radicals within the myocardium

DNA intercalating agent useful for treatment of solid tumors in children

Dactinomycin (actinomycin D)

DNA intercalating agent with minimal myelosuppression that induces formation of free radicals; dose-limiting side effects include pulmonary fibrosis and mucocutaneous reactions

Bleomycin

Antineoplastic with G2 phase cell cycle selectivity

Bleomycin

Antineoplastic can be used as intravesical treatment for superficial bladder cancer and associated with hemolytic-uremic syndrome

Mitomycin

Ribonucleotide reductase inhibitor with S phase cell cycle selectivity that is used for management of sickle cell anemia

Hydroxyurea

Platinum-derivatives that form DNA intrastrand cross-links; causes dose-limiting nephrotoxicity, ototoxicity, and neurotoxicity (2)

Cisplatin, carboplatin

Agent that is used to detoxify reactive metabolites and savenge free radical and prevent drug-induced nephrotoxicity (Fanconi syndrome, acute tubular necrosis)

Amifostine

Antineoplastics that inhibit topoisomerase I (2)

Irinotecan, topotecan

Antineoplastics that inhibit topoisomerase II (4)

Etoposide, teniposide, anthracyclines, amsacrine

Irinotecan use is limited because of one severe adverse effect

Gastrointestinal toxicity (life-threatening diarrhea)

Inhibits BCR-ABL tyrosine kinase expressed by the Philadelphia chromosome in chronic myeloid leukemia

Imatinib

Inhibits BRAF kinase in melanomas with BRAF V600E mutation

Vemurafenib

Chimeric monoclonal antibody against CD20 antigen found on non-Hodgkin lymphomas and normal B lymphocytes

Rituximab

Recombinant humanized monoclonal antibody against vascular endothelial growth factor (VEGF)

Bevacizumab

Recombinant human monoclonal antibody against human epidermal growth factor-2 (HER2) receptor; useful for breast cancer cells that overexpress HER2

Trastuzumab

Human monoclonal antibody against CD52 that is used to treat chronic lymphocytic leukemia

Alemtuzumab

Gonadotropin-releasing hormone agonist that can be used to inhibit luteinizing hormone secretion and testosterone production in men with advanced prostate cancer when administered continuously

Leuprolide

Most commonly used glucocorticoids for cancer due to their lymphotoxic effects; may cause Cushing-like symptoms (2)

Prednisone, prednisolone

Increases activity of cytotoxic cells and indicated for hairy cell leukemia

Interferon alpha-2b

Agent used for hypochromic microcytic anemias

ferrous sulfate

Agent used for megaloblastic anemia (but does not reverse neurologic symptoms) and decrease neural tube defects during pregnancy

Folic acid

Agent used for megaloblastic anemia with neurological defects

Vitamin B12

Agent usef for pernicious anemia

Cyanocobalamin (Vit B12)

Agent used for anemias (especially with renal failure)

Erythropoietin

Agents used for neutropenia associated with cancer chemotherapy and bone marrow transplantation (2)

Filgrastim (granulocyte colony-stimulating factor) and sargramostim (granulocyte-macrophage colony-stimulating factor)