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27 Cards in this Set
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heparin
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activation of antithrombin III, decreases thrombin (IIa) and Xa. short half life.
antithrombin inhibits factors 9-12 use: immediate anticoaglation for PE, stroke, acute coronary syndrome, MI, DVT. used during pregnancy. follow with PTT. toxicity: bleeding, thrombocytopenia (HIT), osteoporosis, drug-drug interactions. reverse with protamine sulfate. lower mc weight heparin (enoxaparin) act more on Xa, with better bioavailabity and 2-4 times longer 1/2 life. HIT: heparin bind platelets, cause autoab production that kill platelets and overactivate the rest; thrombocytopenia, hypercoagulable state. |
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lepirudin, bivalirudin
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hirudin derivatives; direct inhibition of thrombin. alternative to heparin for anticoagulating patients with HIT
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warfarin (coumadin)
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interferes with normal synthesis and g-carboxylation of vit K-dependent clotting factors (II, VII, IX, X, proteins C, S). metabolized by p450. effects extrinsic pathway, increased PT. long 1/2 life.
use: chronic anticoagulation. not used in pregnant women b/c it crosses the placenta. follow with PT/INR. toxicity: bleeding, teratogenic, skin/tissue necrosis due to decreased protien C, drug-drug interactions. reverse with vit k and fresh frozen plasma. |
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thrombolytics
streptokinase, urokinase, tPA, APSAC |
directly/indirectly aid convrseion of plasminogen to plasmin which cleaves thrombin and fibrin clots. increased PT, PTT, doesn't change platelet count.
use: early MI, early ischemic stroke, DVT, PE. toxicity: bleeding; CI in patients with active bleeding, history of intracranial bleeding, recent surgery, known bleeding diathesis, or sever hypertension. reverse with aminocaproic acid. |
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aspirin
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acteylates and irreversibly inhibit COX 1&2. prevents conversion of arachidonic acid to TXA2 in platelets.
increased bleeding time. no change in PT/PTT since coag. factors not affected. use: antipyretic, analgesic, anti-inflammatory, antiplatelet toxicity: gi ulcers, bleeding, hyperventilation, reye's syndrome (encephalopathy), tinnitus. |
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clopidogrel, ticlopidine
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irreversibly block ADP receptors to prevent platelet activation and expression of glycoprotein IIb/IIIa, which inhibits fibrinogen binding and eventual platelet aggregation.
use: acute coronary syndrome; coronary stenting. decreased incidence or recurrence of thrombi stroke. toxicity: neutropenia. |
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abciximab
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monoclonal AB that bind glcoprotein receptors Iib/IIIA on activated platelets, prevents aggregation.
use: actue coronary syndromes, percutaneous transluminal coronary angioplasty. toxicity: bleeding, thrombocytopenia. |
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antimetabolites
methotrexate (MTX) |
folic acid analog that inhibits dihydrofolate reductase: decreased dTMP, decraesed DNA and protein synthesis
use: cancer: leukemias, lymphomas, choriocarcinoma, sarcoma non-neoplastic: abortion, ectoptic pregnancy, RA, psoriasis. toxicity: myelosupression, reversible with leucovorin (folinic acid). fatty change in liver; mucositis (infllammation of mucous lining the GI tract), teratogenic. |
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antimetabolites
5-fluorouracil (5-FU) |
pyrimidine analog bioactivated to 5F-dUMP, covalently complexes with folic acid. inhibits thymidylate synthase, decreased dTMP, DNA, protein synthesis.
use: colon cancer and solid tumors, basal cell carcinoma (topical). synergy with MTX toxicity: myelosuppression, not reversible with leucovorin. rescue with thymidine. photosensitivity. function like flucytosine, which gets converted into 5-FU to kill fungi. |
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antimetabolites
6-mercaptopurine (6-MP) |
purine (thiol) analog: decreases de novo purine synthesis. activated by HGPRTase.
use: leukemias, lymphomas (not CLL or Hodgkin's) toxicity: BM, GI, liver. metabolized by xanthine oxidase, thus increased toxicity with allopurinol (xanthine oxidase inhibitor). prodrug is azathioprine. |
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antimetabolites
6-thioguanine (6-TG) |
purine (thiol) analog: decdreases de novo purine synthesis. acxtivated by HGPRTase.
use: acute lymphoid leukemia (ALL) toxicity: BM depression, liver. can be given with allupurinol. |
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antimetabolites
cytarabine (ara-C) |
pyrimidine antagonist: inhibit DNA polymerase
use: AML, ALL, high grade non-hodgkin's lymphoma. toxicity: leukopenia, thrombocytopenia, megaloblastic anemia. |
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antitumor antibiotics
dactinomycin (ACTinomycin D) |
intercalates in DNA.
use: wilm's tumor, ewing's sarcoma, rhabdomyosarcoma. used for chilhood tumors (children ACT out). toxicity: myelosuppression. |
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antitumor antibiotics
doxorubicin (Adriamycin), daunorubicin |
generate free radicals. noncovalently intercalte in DNA: breaks in DNA: decreased replication.
use: part of the ABVD combination regimen for hodgkin's lymphomas. also for myelomas, sarcomas, and solid tumors (breast, ovary, lung). toxicity: cardiotoxicity, also myelosuppression and marked alopecia. toxic to tissue with extravasation. |
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antitumor antibiotics
bleomycin |
g2 phase specific. induces formation of free radicals, causing DNA strand breaks.
use: testicular cancer, hodgkin's lymphoma (ABVD). toxicity: pulmonary fibrosis, skin changes, minimal myelosuppression. |
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antitumor antibiotics
etoposide (VP-16), teniposide |
late s to g2 phase specific. inhibits topoisomerase II: increased DNA degradation.
use: small cell carcinoma of lung and prostate, testicular carcinoma. toxicity: myelosuppression, GI irritation, alopecia. |
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alkylating agents
cyclophosphamide, ifosfamide |
covalently x-link (interstrand) dna at guanine n-7. require bioactivation by liver.
use: non-hodgkin's lymphoma, breast and ovarian carcinomas. also ummunosuppressants. toxicity: myelosuppressoin; hemorrhagic cystitis; prevent with mesna |
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alkylating agents
nitrosoureas (carmustine, lomustine, semustine, streptozocin) |
require bioactivation. cross bbb: enter cns
use: brain tumors (including glioblastoma multiforme). toxicity: cns toxicity: dizziness, ataxia |
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alkylating agents
busulfan |
alkylates DNA.
use: CML, ablating BM in hematopoietic stem cell transplant. toxicity: pulmonary fibrosis, hyperpigmentation. |
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microtubule inhibitors
vincristine, vinblastine |
alkaloids that bind to tubulin in M phase and block polymerzation of microtubules so that mitotic spindle cannot form. microtubules are the vines of your cells functions like griseofulvin for fungi.
use: part of the MOPP (Oncovin [vincristine]) regiment for hodgkin's lymphoma, wilms' tumor, choriocarcinoma. toxicity: vincristine-neurotoxicity (areflexia, periphral neuritis, paralytic ileus. vinbalstine BLASTs BM (suppression) |
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paclitaxel, other taxoles
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hyperstabilze polymerized microtubules in M phase so that mitotic spindle can't break down, anaphase can't occur.
its TAXing to stay polymerized. use: ovarian and breast carcinomas. toxicity: myelosuppression and hypersensitivity. |
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cisplatin, carboplatin
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cross link DNA
use: testicular bladder, ovary and lung carcinomas. toxicity: nephrotoxicity and acoustic nerve damage. |
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hydroxyurea
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inhibits ribonucleotide reductase: decreased DNA synthesis (S phase specific).
use: melanoma, CML, sickle cell disease (increases HbF) toxicity: BM suppression, GI upset |
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prednisone
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may trigger apoptosis. may work on non-dividing cells
use: most comonly used glucocorticoid in cancer chemotherapy. used in CLL, hodgkin's lymphomas (MOPP regimen). also immunosuppressant used in autoimmune sieases. toxicity: cushing like symptoms, immunosuppression, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis. |
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tamoxifen, raloxifene
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SERMs - receptor antagonist in breast, agonst in bone; block binding of estrogen to estrogen receptor positive cells.
use: breast cancer, prevents osteoporsis toxicity: tamoxifen may incrase teh risk of endometrial cracinoma via partial agonist effets; hot flashes. raloxifene does not cause endometrial cracinoma b/c it is an endometrial antagonist. |
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trastuzumab (herceptin)
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monoclonal AB against HER-2 (erb-B2). helps kill breast cancer cells that overexpress HER-2, possibly through antibody dependent cytotoxicity.
use: metastatic breast cancer toxicity: cardiotoxicity |
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imatinib (gleevec)
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philadelphia chromosome bcr-abl tyrosine kinase inhibitor
use: CML, GI stromal tumors. toxicity: fluid retention. |
