Heme-onc Pharmacology Flashcards
Heparin toxicity
Bleeding, duh. Also, HIT.
Use protamine.
Heparin-MOA
Cofactor for activation antithrombin. Decreases thrombin, Xa.
Monitor PTT.
Warfarin-MOA
Interferes with gamma carboxylation of vit k dependent clotting factors II, VII, IX, X, protein C and protein S.
Extrinsic pathway. Increases PT.
Warfarin-toxicity
Bleeding.
Teratogenic (“don’t wage WAR on the baby”)
Thrombolytics (streptokinase, urokinase, tPA=alteplase, APSAC)
Aids conversion plasminogen to plasmin.
Plasmin cleaves thrombin and fibrin clots.
Thrombolytics, clinical use
Early MI, early CVA
Aspirin, MOA
Irreversibly inhibits COX.
Increases bleeding time, no effect on PT, PTT
Aspirin, clinical use
Antipyretic, analgesic, anti inflammatory, antiplatelet
Aspirin, toxicity
Gastric ulceration, bleeding, hyperventilation, Reye’s syndrome (kids), tinnitus
Clopidogrel, MOA
Blocks ADP irreversibly
Clopidogrel, clinical use
ACS, coronary stenting
Abciximab, MOA
Binds GpIIb/IIIa on platelets, inhibiting aggregation
Abciximab, clinical use
ACS, PTCA
Abciximab, toxicity
Bleeding, thrombocytopenia
Antimetabolites
Act on S phase of cell cycle
Methotrexate 5-FU 6-MP 6-TG Cytarabine
Methotrexate, MOA
Folic acid analog, inhibits dihydrofolate reductase.
Methotrexate, clinical use
Cancer-leukemia, lymphomas, choriocarcinomas, sarcomas
Other-abortion, ectopic pregnancy, RA, psoriasis
Methotrexate, toxicity
Myelosuppression-reversible with leucovorin
Fatty liver, mucositosis, teratogenic
5-FU (fluorouracil), MOA
Pyramiding analog, inhibits thymidylate synthase
5-FU, clinical use
Colon cancer and other solid tumors, BCC.
5-FU, toxicity
Myelosuppression
Photosensitivity
Tx OD with thymidine
6-mercaptopurine (MP), MOA
Purine analog, decreases de novo purine synthesis
6-MP, clinical use
Leukemias, lymphomas
6-MP, toxicity
Bone marrow, GI, liver.
Metabolized by Xanthine oxidase so increased toxicity if used with allopurinol.
6-thioguanine (TG), MOA
Purine analog, decreases de novo purine synthesis
6-TG, clinical use
ALL
6-TG, toxicity
Bone marrow depression, liver. Can be given with allopurinol.
Cytarabine, MOA
Pyrimidine analog
Cytarabine, clinical use
AML, ALL, high grade NHL.
Cytarabine, toxicity
Leukopenia, thrombocytopenia, megaloblastic anemia
Dactinomycin, MOA
DNA intercalating agent
Dactinomycin, clinical use
Wilms tumor, Ewing’s sarcoma, rhabdomyosarcoma.
I.e. Kids tumors
Doxorubicin, daunorubicin, MOA
Generates free radicals
Noncovalently intercalates in DNA
Doxorubicin, duanorubicin, clinical use
Hodgkins
Myelomas, a sarcomas, solid tumors (breast, ovary, lung)
Doxorubicin, daunorubicin, toxicity
Cardiotoxicity (DCM), myelosuppression, alopecia.
Dexrazoxane used to prevent cardiotoxicity
Bleomycin, MOA
Induces ROS, which cause strand breaks
Bleomycin, clinical use
Testicular cancer, Hodgkins
Bleomycin, toxicity
Pulmonary fibrosis
Skin changes
Minimal myelosuppression
Etoposide, MOA
Inhibits topoisomerase II
Etoposide, clinical use
Small cell of lung and prostate, testic carcinoma
Etoposide, toxicity
Myelosuppression, GI irritation, alopecia
Cyclophosphamide, MOA
Alkylation agent. Requires bioactivation by liver.
Cyclophosphamide, clinical use
NHL, breast and ovarian carcinoma. Also, immunosuppression
Cyclophosphamide, toxicity
Myelosuppression Hemorrhagic cystitis (partially prevented it with mesna)
Nitrosoureas, MOA
Alkylating agent that crosses BBB
Nitrosoureas, clinical use
Brain tumors
Nitrosoureas, toxicity
CNS toxicity (dizziness, ataxia)
Busulfan, MOA
Alkylates DNA
Busulfan, clinical use
CML. Also to ablate pt’s bone marrow before transplant
Busulfan, toxicity
Pulmonary fibrosis, hyper pigmentation
Vincristine, Vinblastine, MOA
Bind to Tubulin in M phase to prevent microtubule polymerization
Vincristine, Vinblastine, clinical use
Hodgkins, Wilms tumor, choriocarcinoma, ALL
Vincristine, vinblastine, toxicity
Vincristine-neurotoxicity, paralytic ileus
Vinblastine-bone marrow suppression
Paclitaxel, taxols, MOA
Prevent mitotic spindle breakdown
Paclitaxel, taxols, clinical use
Ovarian and breast carcinomas
Paclitaxel, taxols, toxicity
Myelosuppression, hypersensitivity
Cisplatin, carboplatin, MOA
Cross link DNA
Cisplatin, carboplatin, clinical use
Testicular, bladder, ovary, lung carcinoma
Cisplatin, carboplatin, toxicity
Nephrotoxicity and acoustic nerve damage.
Prevent nephrotoxicity with amifostine (free radical scavenger
Hydroxyurea, MOA
Inhibits ribonucleotide reductase thus inhibits S phase
Also increases HbF
Prednisone MOA
May trigger apoptosis
Prednisone clinical use
CLL, Hodgkins, immunosuppressant in AI diseases
Prednisone toxicity
Cushing like sxs
Tamoxifen, MOA
SERM-receptor antagonist in breast, agonist in bone.
Tamoxifen toxicity
Increases risk endometrial carcinoma. Hot flashes.
Trastuzumab (herceptin), MOA
Monoclonal Ab against HER-2, a tyrosine kinase.
Trastuzumab, toxicity
Cardio toxicity
Imantinib, MOA
Bcr-abl tyrosine kinase inhibitor
Imantinib, clinical use
CML, GI stromal tumors
Imantinib, toxicity
Fluid retention
Rituximab, MOA
Monoclonal Ab against CD20, which is found on most B cell neoplasms
Rituximab, clinical use
NHL, RA
Aminocaproic acid
Reverses tPA
Protamine sulfate
Reverses heparin
Filgramstim
Granulocyte stimulating factor