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107 Cards in this Set
- Front
- Back
Heparin's effect on:
Antithrombin Thrombin Xa |
Activates
Decreases Decreases |
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Why is heparin used in pregnancy instead of warfarin?
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Cannot cross placenta
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Test to monitor for pts on heparin?
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PTT
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Test to monitor for pts on warfarin?
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INR
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Rapid reversal of heparin with?
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Protamine sulfate (positively charged)
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4 advantages of LMWH?
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Better bioavailability
Longer half-life Sub-Q administration No need for lab monitoring |
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Disadvantage of LMWH?
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Not easily reversible
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LMWHs have a greater effect on
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Xa
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Main toxicity of heparin?
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Heparin-induced thrombocytopenia (HIT)
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HIT ensues when heparin binds to ?
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Platelet factor IV
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Pathophys of HIT
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Heparin binds paltelet factor IV--> Ab production --> Abs bind and activate platelets --> platelets are cleared --> thrombocytopenic, hypercoagulable state
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Two direct thrombin inhibitors
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Lepirudin
Bivalirudin |
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Clinical utility of direct thrombin inhibitors
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Pts with HIT
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Four toxicities of warfarin
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Bleeding
Teratogenic Skin/ tissue necrosis Drug-drug interactions |
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Rapid reversal of warfarin overdose
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FFP
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Non-urgent reversal of warfarin overdose
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Vitamin K
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Advantage of warfarin administration over heparin?
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Available orally
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4 thrombolytics
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Streptokinase
Urokinase tPA (alteplase) APSAC (anistreplase) |
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Main toxicity of thrombolytics
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Bleeding
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Thrombolytic toxicity treated with
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Aminocaproic acid (inhibitor of fibrinolysis)
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6 toxicities of aspirin
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Gastric ulceration
Bleeding Hyperventilation Reye's Syndrome Tinnitus (CN VIII) Interstitial nephritis/ acute renal failure |
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Mechanism of ASA
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Acetylates and irreversibly inhibits cyclooxygenase to prevent conversion of arachidonic acid to TxA2
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Blood test affected by ASA
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Bleeding time
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2 mechanisms of clopidogrel and ticlopidine
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Irreversibly block ADP receptors --> inhibit platelet aggregation
Prevent glycoprotein IIb/IIIa expression --> inhibit fibrinogen binding |
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Toxicity of ticlopidine
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Neutropenia
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Abciximab is a monoclonal Ab that binds to ______ to prevent platelet aggregation
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Glycoprotein receptor IIb/IIIa
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Antimetabolites work in this phase of the cell cycle
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S phase
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Vinca alkaloids and taxols work in this phase of the cell cycle
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M phase
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Etoposide works in these 2 phases of the cell cycle
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S and G2
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Bleomycin works in this phase of the cell cycle
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G2
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MTX inhibits
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dihydrofolate reductase --> dTMP
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Drug for leukemias, lymphomas, choriocarcinoma, and sarcomas
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MTX
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Non-neoplastic uses of MTX
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Abortion
Ectopic pregnancy RA Psoriasis |
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Leucovorin rescue is used after toxicity from what drug?
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MTX
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Leucovorin rescue is used to decrease what toxicity of MTX?
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Myelosupression
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Another term for folinic acid
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Leucovorin
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Mechanism of leucovorin rescue
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Cofactor for thymidylate synthase (in lieu of THF)
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5 antimetabolites
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MTX, 5-FU, 6-MP, 6-TG, cytarabine (ara-C)
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4 toxicities of MTX
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Myelosuppression
Macrovesicular fatty change in liver Mucositis Teratogenic |
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How is leucovorin used with 5-FU?
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To increase cell kill, rather than to decrease toxicity
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5-FU overdose can be rescued with?
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Thymidine
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2 toxicities of 5-FU
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Myelosuppression
Photosensitivity |
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Mechanism of 5-FU
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Pyrimidine analog, bioactivated to 5F-dUMP, which complexes folic acid and inhibits thymidylate synthase
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MTX and 5-FU are
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Synergistic
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5-FU is used for
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Colon cancer and other solid tumors
Basal cell carcinoma (topical) |
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6-MP decreases
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De novo purine synthesis (is a purine analog)
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6-MP is used for leukemias and lymphomas except
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CLL
Hodgkin's |
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3 systems with toxicity from 6-MP
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BM
GI Liver |
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6-MP is metabolized by ?
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Xanthine oxidase (so toxicity is increased with allopurinol, which inhibits this enzyme)
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6-TG is used for
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ALL
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What distinguishes the drug interactions of 6-MP and 6-TG?
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6-TG can be given with allopurinol (and commonly is, to prevent uric acid stones from tumor lysis syndrome)
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Antimetabolite drug that is a pyrmidine analog
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Cytarabine (ara-C)
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Cytarabine inhibits ?
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DNA polymerase
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Another name for cytarabine?
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Ara-c
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Ara-C is used for
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AML
ALL High-grade non-Hodgkin's lymphoma |
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Toxicities of ara-C (3)
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Leukopenia
Thrombocytopenia Megaloblastic anemia |
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Drug used for childhood tumors
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Dactinomycin
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3 tumors treated with dactinomycin
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Ewing's sarcoma, Wilms' tumor, rhabdomyosarcoma
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Mechanism of dactinomycin
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Intercalates in DNA
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Toxicity of dactinomycin
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Myelosuppression
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Doxorubicin (adriamycin) and daunorubicin are in what class of antibiotics
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Anthracyclines
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Mechanism of anthracycline antibiotics
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Generate free radicals
Noncovalently intercalate in DNA |
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Clinical use of doxorubicin and daunorubicin
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Hodgkin's lymphoomas
Myelomas, sarcomas, and solid tumors |
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3 toxicities of doxorubicin and daunorubicin
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Cardiotoxicity
Myelosuppression Alopecia |
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Drug given to prevent cardiotoxicity from doxorubicin
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Dexrazoxane (iron-chelating agent)
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Mechanism of bleomycin
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Induces free radical formation --> breaks in DNA strands
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2 clinical uses of bleomycin
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Testicular cancer
Hodgkin's lymphoma |
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Two toxicities of bleomycin
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Pulmonary fibrosis
Skin changes |
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Mechanism of etoposide (and teniposide)
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Inhibits topoisomerase II --> DNA degradation
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Clinical use of etoposide
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Small cell carcinoma of lung and prostate
Testicular carcinoma |
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3 toxicities of etoposide
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Myelosuppression
GI irritation Alopecia |
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Mechanism of cyclophosphamide and ifosfamide
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Covalently X-link (interstrand) DNA at guanine-7
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Cyclophosphamide and ifosfamide must be bioactivated by
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Liver
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Use of cyclophosphamide and ifosfamide
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Hon-Hodgkin's lymphoma
Breast and ovarian carcinomas |
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2 toxicities of cyclophosphamide and ifosfamide
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Myelosuppression
Hemorrhagic cystitis |
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Prevention of hemorrhagic cystitis in cyclophosphamide and ifosfamide treatment with?
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Mesna (thiol group binds toxic metabolite)
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Which alkylating agent can be used for brain tumors?
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Nitrosoureas (cross BBB)
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Toxicity of nitrosoureas
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CNS (dizziness, ataxia)
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Busulfan is used for
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CML
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Busulfan toxicity
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Pulmonary fibrosis, hyperpigmentation
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4 antitumor antibiotics
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Dactinomycin
Doxorubicin/ daunorubici Bleomycin Etoposide/ teniposide |
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3 alkylating agents
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Cyclophosphamide/ ifosfamide
Nitrosoureas Busulfan |
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Mechanism of vincristine and vinblastine
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Bind tubulin and block polymerization of MTs so spindle cannot form
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Mechanism of paclitaxel and other taxols
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Hyperstabilize polymerized MTs in M-phase so mitotic spindle can't break down
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3 uses of vincristine/ vinblastine
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Hodgkin's lymphoma
Wilms' tumor Choriocarcinoma |
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2 uses of taxols
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Ovarian and breast carcinomas
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Toxicity of vincristine (2)
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Neurotoxicity (areflexia, peripheral neuritis)
Paralytic ileus |
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Toxicity of vinblastine
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BM suppression
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Toxicity of taxols (2)
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Myelosuppression
Hypersensitivity |
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Mechanism of cisplatin and carboplatin
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Cross-link DNA
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4 uses of cisplatin/ carboplatin
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Testicular, bladder, ovary, and lung carcinomas
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2 toxicities of cisplastin/ carboplatin
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Nephrotoxicity and acoustic nerve damage
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Prevent nephrotoxicity from cisplatin with
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Amifustine (thiol-based free radical scavenger) and hydration
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Hydroxyurea inhibits
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Ribonucleotide reductase
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Hydroxyurea is specific for
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(S-phase specific)
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3 uses for hydroxyurea
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Melanoma
CML SCD (increases HbF) |
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Toxicity of prednisone
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Cushing-like symptoms
Immunosuppression Cataracts, acne, osteoporosis, HTN, PUD, hyperglycemia, psychosis |
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2 SERMs
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Tamoxifen
Raloxifene |
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SERMs are receptor antagonists in ____ and agonists in ____
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Breast, bone
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Why is raloxifene preferred over tamoxifene?
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No increase in endometrial carcinoma b/c is an antagonist (whereas tamoxifen is a partial agonist)
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Trastuzumab is a monoclonal Ab against ?
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HER-2 (erb-B2)
|
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Toxicity of trastuzumab
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Cardiotoxicity
|
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Imatinib is a
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bcr-abl tyrosine kinase inhibitor
|
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2 clinical uses of imatinib
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CML
GI stromal tumors |
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Toxicity of imatinib
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Fluid retention
|
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Rituximab is a monoclonal Ab against ?
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CD20
|
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2 uses of rituximab
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Non-Hodgkin's lymphoma
RA (with MTX) |