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69 Cards in this Set
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- Back
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MOA for heparin?
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catalyzes activation of Antithrombin III---> dec thrombin (IIa) and dec Xa
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half life for heparin?
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short
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Clinical Uses for Heparin?
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Immediate anticoagulation of PE's, strokes, acute coronary syndrome, MI, DVT
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Heparin and pregnancy?
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ok
doesn't cross placenta |
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How should we monitor Heparin Rx?
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Follow PTT
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Adverse Effects Heparin?
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Bleeding
Thrombocytopenia (HIT) Osteoporosis DDI's |
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How do you quickly reverse effects of heparin? mech?
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Protamine Sulfate
positively charged molecule--->binds negatively charged heparin |
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What is up with high vs low molecular weight heparin?
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HMWH is the old stuff
New LMWH acts more on Xa, has better bioavailability, and a half life 2-4 times longer. LMWH can also be given subcu w/o monitoring Only LMWH downside is its tough to reverse |
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What is HIT?
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Heparin-Induced Thrombocytopenia
heparin binds to platelets--->autoAb production that destroys the platelets and overactivates the remaining ones--->thrombocytopenic, hypercoagulable state |
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What are 2 Heparin derivatives?
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Lepirudin
Bivalirudin |
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MOA and Uses for Lepirudin and Bivalirudin?
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Directly inhibit Thrombin (IIa)
Alternate to heparin in pts w/ HIT |
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what is coumadin?
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WARFARIN
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MOA for Warfarin?
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Interferes w/ synthesis and gamma-carboxylation of Vit K-dependent factors (II, VII, IX, X, C, and S)
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Metabolism of Warfarin?
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by P450 pathway
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How to monitor Warfarin rx?
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It affects extrinsic pathway, so Inc PT
monitor w/ PT/INR values |
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half life of warfarin?
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long
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Clinical uses of warfarin?
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Chronic Anticoagulation
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Contraindications of Warfarin?
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pregnancy
it crosses placenta |
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Adverse effects of warfarin?
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Bleeding
Teratogenic Skin/Tissue necrosis DDI's |
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Heparin vs Warfarin
administration? |
H: IV or SC
W: PO |
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Heparin vs Warfarin
site of action? |
H: blood
W: liver |
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Heparin vs Warfarin
onset? |
H: seconds
W: slow |
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Heparin vs Warfarin
duration of ation? |
H: hours
W: days |
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Heparin vs Warfarin
Rx of acute OD? |
H: protamine sulfate
W: IV Vitamin K and fresh frozen plasma |
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Heparin vs Warfarin
monitoring? |
H: PTT (intrinsic pathway)
W: PT/INR (extrinsic pathway) \ |
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Who are the Thrombolytics?
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Streptokinase
Urokinase tPA (alteplase) APSAC (anistreplase) |
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MOA for the Thrombolytics?
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each aids in conversion of plasminogen to plasmin---> cleavage of thrombin and fibrin clots
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Lab values for Thrombolytics?
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Inc PT
Inc PTT no change in platelet count |
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Clinical uses for thrombolytics?
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Early MI
early Ischemic Stroke |
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Contraindications for Thrombolytics?
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Active bleeding
H/O intracranial bleeding Recent Surgery Known bleeding diastheses Severe HTN |
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Antidote to Thrombolytics?
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Aminocaproic Acid=inhibitor of fibrinolysis
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Who are the 4 receptors on platelet surfaces for adhesion and aggregation? what do they bind?
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GP Ia : exposed collage at site of wound
GP Ib : vWF at break GP IIIa/IIb : GP IIIa/IIb on another platelet via fibrinogen--> aggregation |
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How does Aspirin fxn as an antiplatelet drug?
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Acetylates and irreversibly inhibits COX1 and COX2---> dec TxA2 ---> decreased activation of platelets
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Aspirin effect on PT and PTT?
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no effect
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Clinical Uses of Aspirin?
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Antipyretic
Analgesic Anti-Inflammatory Anti-platelet drug |
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Adverse effects of Aspirin?
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Gastric ulcers
bleeding hyperventilation Reye's Tinnitus (CN VIII) |
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MOA for Clopidogrel and Ticlopidine?
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Irreversibly block ADP receptors on platelets--->dec GP IIb/IIIA expression---> inability of fibrinogen to bind---> dec aggregation
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Uses for Clopidogrel and Ticlopidine?
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Acute Coronary Syndrome
Coronary Stenting Decreases incidence or recurrence of thrombotic strokes |
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Adverse effects of Clopidogrel and Ticlopidine?
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Neutropenia (ticlopidine)
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MOA for Abciximab?
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Monoclonal Ab that binds to GP IIb/IIIa on activated platelets-->dec aggregation
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Clinical uses for abciximab?
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acute coronary syndrome
percutaneous transluminal coronary angioplasty |
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Adverse effects of abciximab
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bleeding
thrombocytopenia |
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Which cancer drugs are cell-cylce specific?
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Methotrexate (S)
5-Fluorouracil (S) 6-Mercaptopurine (S) Bleomycin (G2) Vincristine and Vinblastine (M) |
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Which cancer drugs are cell-cycle non-specific?
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Cisplatin
Cyclophosphamide Procarbazine Doxorubicin |
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Which drugs are alkylating agents? leads to?
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Cyclophosphamide
Cisplatin Procarbazine they all end up cross-linking DNA |
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MOA for Doxorubicin?
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Intercalator-->free radicals--->inhibits topoisomerase
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Which anti-cancer drugs are marrow sparing?
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Cisplatin
Bleomycin Vincristine |
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What are the DLT's for the marrow sparing drugs?
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Cisplatin: Nephro/Neuro (oto) toxic
Bleomycin: Pulmonary Fibrosis Vincristine: Neurotoxic (wrist/food drop) |
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Which anticancer drugs have cytoprotective drugs co-administered w/ them? what are the cytoprotective drug? what is it for?
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Cyclophosphamide: Mesna (traps acrolein) is given to prevent hemorrhagic cystitis
Cisplatin: Amifostine helps prevent Nephrotoxicity Doxorubicin: Dexrazoxane is an iron-chelator preventing formation of free-radicals--->no more Cardiomyopathy (CHF) Methotrexate: Leucovorin is given for a "rescue" |
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When do you have to "rescue the a patient being given methotrexate?
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Osteogenic sarcomas can be super sensitive to Methotrexate, but they can lack the Folic Acid transporter that MTX needs in order to get into the tumor cells. So to kill the tumor, so you just have overdose the patient on MTX...which would kill them if you didn't give them leucovorin to stop up all the normal cell's folic acid transporters.
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Besides BMS what else is a big time SE for Procarbazine?
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it can cause Leukemia
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MOA for Methotrexate?
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Inhibits DHF reductase (S phase)
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MOA for 5-fluorouracil?
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Pyrimidine antimetabolite (S phase) BIOACTIVATED to inhibit Thymidylate synthetase
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MOA for 6-mercaptopurine?
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Purine antimetabolite BIOACTIVATED by HGPR transferase (S phase)
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MOA for Bleomycin?
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Complexes w/ Fe and O2--->DNA strand scission (G2)
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MOA for Vincristine and Vinblastine?
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dec microtubular polymerization--->spindle poison (M phase)
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Why is Allopurinol used in anti-cancer drug regimens?
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To combat Tumor Lysis Syndrome = super increase in uric acid from tumor DNA breakdown
Allopurinol is a xanthine oxidase inhibitor |
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What metabolizes 6-mercaptopurine? significance?
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Xanthine Oxidase
allopurinol inhibits xanthine oxidase---> inc 6-MP toxicity**** |
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Who are the Nitrosoureas?
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Carmustine
Lomustine |
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What are the Nitrosoureas used for? why?
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Cross BBB so good for brain tumors (like glioblastoma mulitforme)
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What is Tamoxifen's MOA?
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SERM
Block the binding of estrogen to estrogen-receptor-positive cells |
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What is Tamoxifen's primary use?
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Premenopausal ER+ Breast Cancer
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What else can Tamoxifen be used for?
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Osteoporosis
its an AGONIST to the estrogen receptor on bone |
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Adverse effect of Tamoxifen?
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Inc risk of endometrial cancer
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Why is Tamoxifen on it's way out?
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Raloxifene has the same mechanism
AND it is an antagonist to the estrogen receptor on the uterus AND most importantly, it doesn't increase the risk of endometrial cancer |
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So what drug is used for Postmenopausal ER+ Breast Cancer? why?
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Anastrozole
aromatase inhibitor ---> dec estrogen synthesis this works well in post-menopausal but not in pre-menopausal, b/c estrogen synthesis is different in those two populations |
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Uses for Trastuzumab?
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Monoclonal Ab against ERB-B2 = HER-2
so it helps kill HER-2+ breast cancers (which is the most aggressive of all breast cancers) |
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What is Gleevac (Imatinib) used for? mech?
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Philadelphia Chromosome bcr-abl tyrosine kinase inhibitor
so its good for CML (and GI stromal tumors) |
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Mech for Paclitaxel and other taxols?
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screw up tubulin
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