Heme/Onc Flashcards
activation of anti-thrombin (decrease thrombin and factor Xa). use: immediate anti-coag for PE, acute coronary syndrome, MI, DVT. PRegnancy safe. effects PTT.
Heparin
act more on factor Xa, better bioavailability and 2-4 times longer half life than normal heparin
Low molecular weight heparins: enoxaparin, dalteparin
direct thrombin inhibitors. used instead of heparin in patients with heparin induced thrombocytopenia.
argatroban, bivalirudin
interferes with normal synthesis and gamma-carboxylation of K-dependent clotting factors (2, 7, 9, 10 and protein C ans S). metabolized by P450. measured by PT/INR. use: chronic coagulation, not during pregnancy.
Warfarin (coumadin)
Direct factor 10 inhibitors. treatment and prophylaxis of DVT and PE. stroke prophylaxis in patients w/a-fib.
Apixaban, riveroxaban
conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots. increase PTT and PT but no change in platelets. Early MI, ischemic stroke, and severe PE.
alteplase (tPA), reteplase (rPA), tenecteplase (TNK-tPA)
irreversibly inhibit COX-1 and 2). new platelets cannot be synthesized. increase bleed time, decrease TXA2 and prostaglandins. no effect on PT and PTT. antipyretic, analgesic, anti-inflamm, antiplatelet.
aspirin
ADP receptor inhibitor, inhibit platelet aggregation. prevents glycoprotein 2b/3a from binding fibrinogen. treat acute coronary syndrome, coronary stenting.
clopidogrel, ticlopidine, prasugrel, ticagrelor.
PDE3 inhibitor. increase cAMP in platelets, thus inhibiting aggregation. vasodilate. treat: intermitten claudication. coronary vasodilation, prevent stroke or TIA.
cilostazole, dipyridamole
GP2a/3b inhibitors. prevent aggregation. made from mAb fragments. treat unstable angina, percutaneous transluminal coronary angioplasty`
abciximab, eptifibatice, tirofiban
folic acid analog, inhibits dihydrofolate reductase, DNA and protein synth. treat both cancer and non-neoplastics. SE: myelosuppression (reversible with leucovorin (folinic acid)
Methotrexate
pyrimidine analog, covalently complexes folic acid. inhibits thymidylate synthetase, decrease DNA and protein synth. treat cancer. SE: myelosuppression, OD (rescue with uridine)
5-fluorouracil
Pyrimidine analog. inhibits DNA polymerase. treat leukemias and lymphomas. SE: pancytopenia.
Cytarabine (arabinofuranosyl cytidine)
Purine analog. decrease de novo purine synth. activated by HGPRT. PRevent organ transplant, RA, SLE, leukemia, IBD. toxic to bone marrow. metabolized by xanthine oxidase so allopurinol increases toxicity.
Azathioprine, 6-mercaptopurine, 6-thioguanine
anti-tumor antibiotic. intercalates in DNA. treat childhood tumors. SE: myelosuppression.
Dactinomycin (actinomycin D)
anti-tumor antibiotic. generates free radicals causing breaks in DNA. treat solid tumor, leukemia, lymphoma. SE: cardiotoxicity.
Doxorubicin and daunorubicin
anti-tumor antibiotic. free radical formation, breaks in DNA. treat: testicular cancer and hodgkin’s. SE: pulmonary fibrosis.
Bleomycin
Alkylating agent. Covalently X-link DNA at guanine N-7. cause myelosuppression, hemorrhagic cystitis (prevent w/mensa)
Cyclophosphamide, ifosfamide
Alkylating agent. Crosses BBB. cross link DNA. BRain tumors. SE: CNS toxicity.
Nitrosoureas: carmustine, lomustine, semustine, streptozocin
Alkylating agent. cross-link DNA. Treat CML and ablate BM before BM transplant. SE: severe myelosuppression, pulmonary fibrosis.
Busulfan
Microtubule inhibitor. bind Beta-tubulin, and inhibit polymerization into microtubules. treat solid tumors, leukemia, lymphoma.
Vinca alkaloids: vincristine (neurotoxicity) and vinblastine (Myelosuppression)
Microtubule inhibitor. Hyperstabilize polymerized tubules in M phase. Ovarian and breast cancer. SE: Myelosuppression.
Paclitaxel and other taxols
Cross link DNA. treat testicular, ovarian, bladder and lung cancer. Nephrotoxic and acoustic nerve damage.
Cisplatin, carboplatin
inhibit topoisomerase 2 causing DNA degradation. Treat: solid tumors, leukemias, lymphomas. SE: myelosuppression.
Etoposide, teniposide.
inhibit topoisomerase 1, preventing DNA unwinding and replication. treat colon, ovarian, and small cell lung cancers. SE: myelosuppression.
Irinotecan, topotecan
inhibits ribonucleotide reductase inhibiting DNA synth (S-phase). treat: Melanoma, CML, sickle cell (increase HbF). SE: bone marrow suppression.
hydroxyurea
triggers apoptosis, even in non-dividing cells. most commonly used GC in chemo. CLL and non-hodgkins. SE: cushing-like symptoms.
Prednisone, prednisolone.
SERM. estrogen receptor antagonists in breast and agonist in bone. Breast cancer and osteoporosis.
tamoxifen: BReast cancer. SE: endometrial cancer.
raloxifene: osteoporosis. SE: endometrial antagonist.
Tyrosine kinase inhibitor of bcr-abl gene and c-KIT. treat CML and GI stromal tumors. SE: fluid retention.
Imatinib (Gleevec)
mAb against CD20 (B-cells). treat: non-hodgkin’s, RA, Idiopathic thrombocytopenic purpura. SE: increase rick of PML
rituximab
inhibitor of B-Raf kinase w.the V600E mutation. treat metastatic cancers.
Vemurafenib
mAb against VEGF. inhibits angiogenesis. treat: solid tumors (colorectal and renal cell). SE: hemorrhage, impaired wound healing.
Bevacizumab