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44 Cards in this Set

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mechanism of heparin?
catalyzes the activation of antithrombin III, decreases thrombin and Xa
which can be used during pregnancy - heparin or warfarin?
heparin
what drug can be used for rapid reversal of heparin?
protamine sulfate - positively charged molecule that acts by binding negatively charged heparin
what do you follow with heparin?
PTT
mechanism of warfarin?
interferes with normal synthesis and gamma-carboxylation of vitamin K-dependent clotting factors II, VII, IX, and X and proteins C and S
what pathway does warfarin affecct?
extrinsic - increases PT
how do you reverse warfarin?
vitamin K of FFP
what do you follow with warfarin?
PT or INR
onset of action of heparin? warfarin?
heparin - fast
warfarin - slow (limited by half-lives of vitamin K-dependent clotting factors)
how do thrombolytics work?
directly or indirectly aid conversion of plasminogen to plasmin, the major fibrinolytic enzyme, which cleaves thrombin and fibrin clots
how do you treat thrombolytic toxicity?
aminocaproic acid, an inhibitor of fibrinolysis
mechanism of aspirin?
acetylates and irreversibly inhibits cyclooxygenase to prevent conversion of arachidonic acid to prostaglandins
how does aspirin affect bleeding time, PT, PTT
increases bleeding time, no effect on PT or PTT
these inhibit platelet aggregation by irreversibly blocking ADP receptors; inhibit fibrinogen binding by preventing glycoprotein IIb/IIIa expression
clopidogrel, ticlopidine
toxicity of ticlopidine?
neutropenia
monoclonal antibody that binds to the glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation
abciximab
folic acid analog that inhibits dihydrofolate reductase, resulting in decreased dTMP and therefore decreased DNA and protein synthesis
methotrexate
toxicity of methotrexate? what can reverse it?
myelosuppression - leucovorin (folinic acid) rescue
this is an S-phase specific antimetabolite
5-FU
pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes folic acid - this complex inhibits thymidylate synthase, resulting in decreaed dTMP and inhibition of DNA synthesis
5-FU
toxicity of 5-FU?
myelosupression - nor reversible with leucovorin
blocks de novo purine synthesis; activated by HGPRTase
6-mercaptopurine
cancer drug that is metabolized by xanthine oxidase
6-mercaptopurine - thus increased toxicity with allopurinol
inhibits DNA polymerase; used in AML
cytarabine
alkylating agents that covalently x-link (interstrand) DNA at guanine N-7
cyclophosphamide, ifosfamide
the hemorrhagic cystitis that can be seen with cyclophosphamide & ifosfamide can be partially prevented with what?
mesna
carmustine, lomustine, semustine, and streptozocin are what kind of drug?
nitrosureas
clinical use of nitrosureas?
brain tumors
mechanism of nitrosureas?
alkylate DNA; require bioactivation
these drugs act like alkylating agents and are used for testicular, bladder, ovary, and lung carcinomas
cisplatin, carboplatin
drug that alkylates DNA and is used for CML
busulfan
toxicity of busulfan?
pulmonary fibrosis, hyperpigmentation
drugs that generate free radicals and noncovalently intercalate in DNA (creating breaks in DNA strand to reduce replication)
doxorubicin, daunorubicin
toxicity of doxorubicin, daunorubicin
cardiotoxicity; myelosuppression and marked alopecia
drug used for Wilms' tumor, Ewing's sarcoma, rhabdomyosarcoma?
dactinomycin (actinomycin D) - used for childhood tumors - children ACT out
toxicity of bleomycin?
pulmonary fibrosis, skin changes, but minimal myelosuppression
toxicity of vincristine?
neurotoxicity (areflexia, peripheral neuritis), paralytic ileus
toxicity of vinblastine?
vinBLASTine BLASTs bone marrow (suppression)
what is the most commonly used glucocorticoid used in cancer chemo?
prednisone
monoclonal antibody against HER-2 (erb-B2)
trastuzumab (Herceptin)
M-phase-specific alkaloids that bind to tubulin and block polymerization of microtubules so that mitotic spindle cannot form
vincristine, vinblastine - arrest cell at metaphase
estrogen receptor mixed agonist/antagonists that block the binding of estrogen to estrogen receptor-positive cells
tamoxifen, raloxifene
G2-phase-specific agent that inhibits topoisomerase II and increases DNA degradation
etoposide
monoclonal antibody agains the Philadelphia chromosome bcr-abl tyrosine kinase
imatinib (Gleevec)