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101 Cards in this Set

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What enzyme(s) do NSAIDs, acetaminophen, aspirin block? Which are reversible and irreversible?
COX-1, COX-2
Aspirin - irreversible
NSAIDs - reversible
Acetominophen - reversible
Zafirlukast
Montelukast MOA?
Blocks leukotrienes (LTC4, LTD4, LTE4)
Aspirin: Adverse effects
GI Upset and bleeding
Analgesic Nephropahy
Reye's syndrome
Ketorolac: Drug Class and MOA
NSAIDS - block COX-1 and COX-2
Celecoxib: Class and MOA
COX-2 inhibitor (reversible)
Celecoxib: adverse effects
increased risk of thrombosis
Use this drug instead of aspirin to prevent Reye's syndrome
Acetaminophen
Etidronate: Class and MOA
Bisphosphonate - inhibit osteoclastic activity
Pamidronate: Class and MOA
Bisphosphonate - inhibit osteoclastic activity
ALendronate: Class and MOA
Bisphosphonate - inhibit osteoclastic activity
Colchicine: Class and MOA
It's own class - depolymerzies microtubules, impairing leukocyte chemotaxis
Colchicine: Use
Chronic gout
Probenecid: Class and MOA
Inhibits reabsorption of uric acid in PCT
Probenecid: Use
Chronic Gout
Allopurinol: Class and MOA
Xanthine Oxidase inhibitor. Prevents the formation of plasma uric acid
Allopurinol: Use
Chronic Gout
What should be used in an acute flare of gout?
Indomethacin
Allopurinol: Drug interactions
Increases azathioprine and 6-MP (both normally metabolized by xanthine oxidase)
Etanercept: Class and MOA
Recombinant TNF receptor. binds TNF
Etanercept: USes
Rheumatoid arthritis, psoriasis, ankylosing spondylitis
Infliximab: Class and MOA
Monoclonal antibody that Binds TNF.
Infliximab: Uses
Crohn's disease, Rheumatoid arthritis, ankylosing spondylitis.
Infliximab: Toxicity
Infection predisposition (TB reactivation)
Heparin: Class and MOA
Anticoagulant. Catalyzes the activation of antithrombin III (decreases thrombin and Xa)
Heparin: Use
Immediate anticoagulation for PEs, strokes, MI, etc.
How do you monitor Heparin use?
Monitor PTT
Heparin: Adverse effects
Bleeding, Thrombocytopenia (via HIT), osteoporosis
Reversal of Heparin OD?
Protamine sulfate
Lepirudin, bivalirudin: class and MOA
Anticoagulants. Hirudin derivatives that directly inhibit thrombin.
Lepirudin, bivalirudin: Use
Replacement of heparin in HIT
Warfarin: Class and MOA
Anticoagulant. inhibits factor synthesis and γ-carboxylation of K-dependant factors (II, VII, IX, X and Proteins C and S)
How do you monitor Warfarin use?
PT
Warfarin: Use
Chronic anticoagulation
What would you use in a pregnant woman, Warfarin or heparin?
Heparin. Warfarin crosses the placenta
Warfarin: adverse effects
Bleeding, Warfarin-induced tissue necrosis, teratogen
tPA: Class and MOA
Thrombolytic. Activator of plasminogen -> breakdown of fibrin and fibrinogen
tPA: Use
Early MI, Ischemic Stroke
tPA: Adverse Effects
Bleeding, Contrai'ed in pts with bleeding.
tPA: Toxicity Tx
Aminocapric acid (inhibits plasminogen)
Streptokinase, urokinase: Class and MOA
Thrombolytic. Activate plasminogen
Clopidogrel, ticlopidine: Class and MOA
Anticoagulant. Inhibits platelet aggregation by blocking ADP receptors -> Inhibition of fibrinogen bdnding by prevention of gpIIb/IIIa
Clopidogrel, ticlopidine: Use
Acute coronary syndrome, coronary stenting
ticlopidine: toxicity
Neutropenia
Abciximab: class and MOA
Monoclonal antibody that binds the gpIIb/IIIa receptor on activated platelets, preventing aggregation
Abciximab: Use
Acute coronary syndromes, percutaneous transluminal coronary angioplasty
Abciximab: adverse effects
Bleeding, thrombocytopenia
Methotrexate: Class and MOA
DHF reductase inhibitor. No production of Thymidine.
Methotrexate: Use
Cancer, Rheumatoid Arthritis, Psoriasis
Methotrexate: Adverse effects (and how to reverse)
Myelosuppression, reverisble with leucovorin (folinic acid) rescue
5-fluorouracil: Class and MOA
Thymidylate synthase inhibitor (no production of dTMP)
5-fluorouracil: Use
Cancer. Synergistic with MTX
5-fluorouracil: Adverse effects (and how to reverse)
Myelosuppression. Thymidine rescue
6-mercaptopurine: class and MOA
Block of de novo purine synthesis. Needs activated by HGPRTase.
6-mercaptopurine:Use
Cancer
6-mercaptopurine: Adverse Effects
Bone marrow, GI, Liver. Metabolized with xanthine oxidase...toxicity with allopurinol
Cytarabine (ara-c): Class and MOA
Inhibits DNA polymerase
Cytarabine (ara-c): Use
Cancer (A__Ls and non-hodgkin's)
Cytarabine (ara-c): Adverse Effects
Leukopenia, thrombocytopenia, Megaloblastic anemia
Cyclophosphamide, Ifosfamide: Class and MOA
Alkylating agents. Colvalently link DNA at guanine. Both require activation by liver
Cyclophosphamide, Ifosfamide: USe
Cancer and immunosuppression
Cyclophosphamide, Ifosfamide: Adverse effects (and reversibility)
Myelosuppression, HEMORRHAGIC CYSTITIS (reversible with mesna)
Nitrosureas: Names
Carumustine, lomustine, semustine, streptozocin
Nitrosureas: Class and mOA
DNA Alkylating agents. Require activation. Cross BBB.
Nitrosureas: Use
Brain tumors
Nitrosureas: Adverse effects
CNS toxicity
Cisplatin, carboplatin: Class and MOA
Crosslink DNA
Cisplatin, carboplatin: Use
Cancer
Cisplatin, carboplatin: Adverse effects
NEPHROTOXIC and acoustic nerve damage
Busulfan: Class and MOA
Alkylates DNA
Busulfan: Use
Cancer and Bone marrow ablation
Busulfan: Adverse effects
Pulmonary Fibrosis, hyperpigmentation
Doxorubicin: Class and MOA
Generates free radicals
Doxorubicin: Adverse Effects
Cardiotoxic
Dactinomycin: Class and MOA
Intercalates DNA
Dactinomycin: Use
Childhood cancers
Dactinomycin: Adverse Effects
Myelosuppression
Bleomycin: Class and MOA
Free radical induction
Bleomycin: Use
Cancer (testicular), ABVD Hadgkin's regimen
Bleomycin: Adverse Effects
Pulmonary fibrosis, skin changes
Hydroxyurea: Class and MOA
Inhibits Ribonucleotide Reductase, decreased DNA synthesis
Hydroxyurea: Use
Cancer
Hydroxyurea: Adverse Effects
BM Suppresion, GI upset
Etoposide (VP-16): Class and MOA
G2 specific agent taht inhibits topo II and enhances DNA degradation
Etoposide (VP-16): USe
cancer
Etoposide (VP-16): Adverse effects
Myelosuppression, GI irritation, alopecia
Prednisone: Class and MOA
Apoptosis trigger.
Prednisone: Use
Most common glucocorticoid in cancer, CLL, Lymphomas (MOPP), immunosuppressant
Prednisone: Adverse Effects
Cushing-like, cataracts, acne, osteoporosis, HTN, peptic ulcers, hyperglycemia, psychosis
Tamoxifen, reloxifene: Class and MOA
SERMs. Estrogen receptor agonsits in estrogen sensitive cancers
Tamoxifen, reloxifene: Uses
Breast cancer. Osteoporosis prevention
Tamoxifen, reloxifene: adverse effects
tamoxifen may increase risk of endometrial carcinoma.
Trastuzumab: Class and MOA
monoclonal Ab to HER-2 in breast cancer cells that overexpress this molecule.
Trastuzumab: Use
Breast Cancer
Trastuzumab: Toxicity
Cardiotoxic
Imatinab (Gleevec): Class and MOA
Philadelphia chromosome bcr-abl tyrosine kinase inhibitor
Imatinab (Gleevec): USE
CML, GI stromal tumors
Vincristine, vinblastine: Class and MOA
Microtubule polymerization blockers. M-phase-specific
Vincristine, vinblastine: Use
Hodgkin's (MOPP), other cancers
Paclitaxel: Class and MOA
Binds tubulin, preventing microtubule formation. (no anaphase). M-phase-specific
Paclitaxel: Use
Ovarian and breast carcinomas
Paclitaxel: Adverse Effects
Myelosuppression and hypersensitivity