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30 Cards in this Set

  • Front
  • Back
Heparin:
- mechanism
- clinical use
- toxicity
- HIT
- LMWH
MECH: heparin activates antithrombin III, inhibits thrombin and Xa. short half-life.
USE: immediate anticoag for PE, stroke, acute coronary syndrome, MI, DVT. Can be used during preg (does not cross placenta). Follow PTT.
TOXICITY: bleeding, HIT, osteoporosis, drug intxns. For rapid reversal of heparinization, use PROTAMINE SULFATE (pos charged molecule that binds neg charged heparin).
New LMWH (enoxaparin) act more on Xa, have better availability, and 2-4 x longer halflife. can be admin subQ w/out lab monitoring. not easily reversible, however.
HIT: heparin binds to plts, causing IgG autoAb production that binds to PF4/heparin and destroys platelets and overactivates the remaining ones --> thrombocytopenic, hypercogulable state.
Lepirudin, bivalirudin.
Directly inhibit thrombin. used as alternative to heparin for anticoagulating pts w/ HIT. Mech is independent of antithrombin III.
Warfarin (Coumadin)
interferes w/ nl synthesis and gamma carboxylation of vit D depending clotting factors; metabolized by cyt P450. long half-life. watch PT/INR.
USE: chronic anticoagulation (warfarin crosses the placenta).
TOXICITY: bleeding, teratogenic, skin/tissue necrosis, drug-drug intxns.
What are the differences between heparin and warfarin in terms of structure, route of administration, site of action, onset of action, mechanism of action, duration of action, treatment of acute overdose, monitoring, and placental crossing and inhibition of coag in vitro?
HEPARIN: large, anionic, acidic polymer. Parenteral (IV, SC). Works in blood, w/ rapid (seconds) onset. Activates antithrombin III, which decreases the action of IIa (thrombin) and Xa. Lasts for hours (acute). Inhibits coagulation in bitro. Treatment of acute overdose is w/ protamine sulfate. Monitoring: PTT (intrinsic pathway). Does not cross placenta.
WARFARIN: small, lipid soluble molecule. Oral. Site of action is in liver. Onset of action slow, limited by half-lives of nl clotting factors. Impairs synthesis of vitamin K dependent clotting factors. Lasts for days. Does not inhibit coagulation in vitro. Treatment of acute OD is IV vit K and FFP. Monitor PT/INR (extrinsic pathway). Crosses placenta and is teratogenic.
What are streptokinase, urokinase, tPA (altepase), APSAC (anistreplase)?
Thrombolytics. They directly or indirectly aid the conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots. increase PT, PTT. no change in plt ct.
USE: early MI, early ischemic stroke
TOXICITY: bleeding. contraindicated in pts w/ active bleeding, hx of intracranial bleeding, recent surg, known bleeding diathesis, or severe HTN. treat toxicity w/ aminocaproic acid (inhibitor of fibrinolysis).
Clopidogrel, ticlopidine
MECH: inhibit platelet aggregation by irreversibly blocking ADP receptors. Inhibit fibrinogen binding by preventing glycoprotein IIb/IIIa expression.
USE: acute coronary syndrome; coronary stenting. decreased incidence or recurrence of thrombotic stroke.
AE's: neutropenia (ticlopidine)
Abciximab
monoclonal Ab that binds to glycoprotein receptor IIB/IIIa on activated platelets, preventing aggregation.
USE: acute coronary syndromes, percutaneous transluminal coronary angioplasty.
TOXICITY: bleeding, thrombocytopenia.
On what part of the cell cycle do vinca alkaloids and taxols work?
M
On what part of the cell cycle does bleomycin work?
G2 (synthesiss of components needed for mitosis).
On what part of the cell cycle does Etoposide work?
G2 and S
Which part of the cell cycle do antimetabolites work on?
S phase
Methotrexate
MECH: S-phase specific antimetabolite. Folic acid analog that inhibits DHFR, --> decreased dTMP and therefore decreased DNA and protein synthesis
USE: leukemia, lymphoma, choriocarcinoma, sarcoma. abortion, ectopic pregnancy, RA, psoriasis.
TOXICITY: myelosuppression (reversible w/ LEUCOVORIN - FOLINIC ACID - RESCUE. macrovesicularfatty change in liver. mucositis.
5-fluorouracil (5-FU)
MECH: S-phase specific antimetabolite. pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes folic acid. this complex inhibits thymidylate synthase --> decrease in dTMP and same effects as MTX.
USE: colon cancer, other solid tumors, topically for basal cell carcinoma. synergy w/ MTX.
TOXICITY: myelosuppression, which is NOT reversible w/ leukovorin; photosensitivity; can "rescue" with THYMIDINE.
6-mercaptopurine (6-MP)
MECH: blocks de novo purine synthesis. activated by HGPRTase.
USE: leukemias, lymphomas (not CLL or Hodgkins)
TOXICITY: bone marrow, GI, liver. metabolized by xanthine oxidase, so increased toxicity w/ allopurinol.
Cytarabine (ara-C)
MECH: inhibits DNA polymerase
USE: AML,ALL, high grade non-Hodgkin's lymphoma.
TOXICITY: leukopenia, thrombocytopenia, megaloblastic anemia.
Cyclophosphamide, Ifosfamide
Alkalating agents; covalently x-link (interstrand) DNA at guanine N-7. Require bioactivation by liver.
USE: NHL, breast and ovarian carcinomas, immunosuppression.
TOXICITY: myelosuppression; hemorrhagic cystitis - can be partially prevented w/ MESNA.
Nitrosoureas (carmustine, lomustine, semustine, streptozocin)
alkylate DNA; require bioactivation; cross BBB --> CNS. used for brain tumors (including glioblastoma multiforme). Toxicity: CNS (dizziness, ataxia).
Cisplatin/carboplatin
Cross-link DNA.
USE: testicular, bladder, ovary, lung carcinomas.
TOXICITY: nephrotoxicity and acoustic nerve dmg.
Busulfan
alkylates DNA
Used in CML, as well as for ablating bone marrow in hematopetic stem cell transplants.
TOXICITY: pulmonary fibrosis, hyperpigmentation
Doxorubicin (Adriamycin), daunorubicin
anthracycline ABX that generate free radicals and noncovalently intercalate in DNA (creating breaks in DNA strand --> decreased replication).
USE: part of ABVD combo regimin for Hodgkin's lymphomas; also for myelomas, sarcomas, and solid tumors.
TOXICITY: cardiotoxicity; also myelosuppression and alopecia. toxic extravasation.
Dactinomycin (actinomycin D)
intercalates in DNA; used in childhood tumors (Wilms' tumor, Ewing's sarcoma, rhabdomyosarcoma)...

Children ACT out...use ACTinomycin D.
Bleomycin
induces formation of free radicals, which cause breaks in DNA strands.
USE: testicular CA, Hodgkins (ABVD regimin).
TOXICITY: pulmonary fibrosis, skin changes, BUT minimal myelosuppression!
Hydroxyurea
inhibits ribonucleotide reductase --> decrease DNA synthesis (S-phase specific).
USE: melanoma, CML, sickle cell dz (increases HbF).
Etoposide (VP-16)
G2-phase specific agent that inhibits topoisomerase II and increases DNA degradation.
USE: small cell carcinoma of lung and prostate, testicular carcinoma.
TOXICITY: melosuppression, GI irritation, alopecia.
Prednisone
MECH: may trigger apoptosis. may work on nondividing cells! most commonly used glucocorticoid in cancer chemo. used in CLL, Hodgkins lymphomas (part of MOPP) regimen).
Tamoxifen, raloxifen
SERMs - receptor antagonists in breast, agonists in bone; block binding of estrogen to estrogen-receptor pos cells.
USE: breast cancer. also useful to prevent osteoporosis.
TOXICITY: tamoxifen may increase risk of endometrial carcinoma via partial agonist effects; "hot flashes." Raloxifene does not cause endometrial carcinoma b/c it is an endometrial antagonist.
Trastuzumab (Herceptin)
mech:monoclonalAb against HER-2 (erb-B2). helps kill breast cancer cells that overexpress HER-2, possibly through Ab-depenent cytotoxicity.
USE: metastatic breast CA
TOXICITY: cardiotoxicity.
Imatinib (GLeevec)
Philadelphia chromosome bcr-abl tyrosine kinase inhiibitor
USE: CML, GI stromal tumors.
TOXICITY: fluid retention.
Vincristine/vinblastine
M phase specific alkaloids that bind tubulin and block polymerization of microtubules so that mitotic spindle cannot form. microtubules are the VINES of your cells.
USE: part of MOPP (oncovin/vincristine) regimen for Hodgkins, Wilm's tumor, choriocarcinoma.
TOXICITY VINCRISTINE: neurotox (areflexia, peripheral neuritis, paralytic ileus)
TOXICITY VINBLASTINE: BONE MARROW SUPPRESSION
Paclitaxel, other taxels
M-phase specific agents that bind to tubulin, and hyperstabilize polymerized microtubules so that spindle cannot break down (anaphase cannot occur).
USE: ovarian and breast carcinomas
TOX: myelosuppression and hypersensitivity.