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57 Cards in this Set
- Front
- Back
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Heparin MOA and Clinical Use....
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Catalyzes the activation of antithrombin III, decreases thrombin and Xa. Short half life.
Used for immediate anticoagulation in the following... Pulmonary embolism Stroke Angina MI DVT DOES NOT CROSS PLACENTA. |
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Heparin Toxicity
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Bleeding
Thrombocytopenia (HIT) Osteoporosis Drug-drug interactions |
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Drug used to immediately reverse Heparin...
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Protamine sulfate (positively charged molecule that acts by binding negatively charged heparin)
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LMWH's act on what more than regular heparin???
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Factor Xa
They have better bioavailability and 2-4 times longer half life. Can be administered subcutaneously and without laboratory monitoring. |
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Heparin Induced Thrombocytopenia Mechanism....
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Heparin binds platelets causing autoantibody production that destroys platelets and overactivates the remaining ones resulting in a....
THROMBOCYTOPENIC, HYPERCOAGULABLE STATE |
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Direct Thrombin Inhibitors...
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Hirudin Derivatives; Lepirudin and bivalirudin
*used in patients who have HIT |
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Warfarin (Coumadin) MOA...
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Interferes with normal synthesis and gamma-carboxylation of vitamin K-dependent clotting factors 2, 7, 9, 10 and protein C and S.
*Metabolized by the cytochrome P-450 pathway. Long 1/2 life. |
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Warfarin Toxicity....
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Bleeding
Teratogenic Skin/tissue necrosis Drug drug interactions |
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Names of 4 thrombolytics...
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Streptokinase
Urokinase tPA (alteplase) APSAC (anistreplase) |
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Drug that causes increase in PT and PTT but no change in platelet count....
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Thrombolytics
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Clinical use of thrombolytics...
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Early MI
Early Ischemic Stroke |
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Thrombolytic toxicity...
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Bleeding
Contraindicated in the following... Active Bleeding History of Intracranial bleeding recent surgery known bleeding diatheses severe hypertension |
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What do you treat Thrombolytic toxicity with???
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Aminocaproic acid (it is an inhibitor of fibrinolysis)
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Clopidogrel and ticlopidine MOA...
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Irreversible blocker of ADP receptors.
Inhibits fibrinogen binding by preventing glycoprotein IIb/IIIa expression |
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Clinical use for Clopidogrel/ticlopidine
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Acute coronary syndrome
Coronary stenting Decreased incidence or recurrence of thrombotic stroke |
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Abciximab MOA...
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Monoclonal antibody that binds to the glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation.
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Abciximab clinical use...
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Acute coronary syndromes
percutaneous transluminal coronary angioplasty |
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Cell cycle specific Cancer drugs...
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Antimetabolites (MTX, 5-FU, 6-MP)
Etoposide Bleomycin Vinca Alkaloids Paclitaxel |
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Cell cycle non-specific Cancer drugs....
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Alkylating agents
Antibiotics (dactinomycin, doxorubicin) |
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Methotrexate (MTX) MOA....
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S-phase specific antimetabolite.
Folic acid analog that inhibits DHF reductase, results in DECREASED dTMP and therefore DECREASED DNA and PROTEIN SYNTHESIS. |
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Toxicity of Methotrexate....
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Myelosuppression---> reversible with leucovorin (folinic acid) "rescue"
Macrovesicular fatty change in liver. Mucositis. |
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Toxicity of....
5-FU |
Myelosuppression, which is NOT reversible with leucovorin.
Photosensitivity--> can rescue with thymidine. |
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MOA of...
5-FU |
S-phase specific antimetabolite.
Pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes folic acid. This inhibits thymidylate synthase, resulting in decrease dTMP |
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Toxicity of....
6-MP |
Bone marrow
GI Liver Metabolized by xanthine oxidase....thus increased toxicity with allopurinol. |
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MOA of...
6-MP |
Blocks de novo purine synthesis.
Activated by HGPRTase. |
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Toxicity of....
Cytarabine (ara-C) |
Leukopenia
Thrombocytopenia Megaloblastic anemia |
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MOA of...
Cytarabine (ara-C) |
Inhibits DNA polymerase
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Toxicity of....
Cyclophosphamide/ifosfamide |
Myelosuppression
Hemorrhagic cystitis-which can be partially prevented with mensa. |
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MOA of...
Cyclophosphamide/ifosfamide |
Alkylating agents;
Covalently x-link (interstrand) DNA at guanine N-7. Requires bioactivation by liver. |
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MOA....
Nitrosoureas |
Carmustine, lomustine, semustine, streptozocin.
Alkylate DNA. Require bioactivation. Cross BBB- CNS |
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Toxicity of...
Nitrosoureas |
CNS toxicity (dizziness, ataxia)
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MOA of Cisplatin and carboplatin...
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Act like alkylating agents.
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Toxicity of Cisplatin and carboplatin...
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Nephrotoxicity and acoustic nerve damage.
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MOA of Busulfan...
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Alkylates DNA
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Toxicity of Busulfan...
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Pulmonary fibrosis
Hyperpigmentation |
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MOA of Doxorubicin (Adriamycin), and daunorubicin ...
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Generate free radicals and noncovalently intercalate in DNA (creating breaks in DNA strand to decrease replication)
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Toxicity of Doxorubicin (Adriamycin) and daunorubicin....
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Cardiotoxicity (dilated cardiomyopathy)
Myelosuppression Marked alopecia Toxic extravasation. |
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MOA 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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Bleomycin MOA
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Induces the formation of free radicals, which cause breaks in DNA strands.
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Bleomycin Toxicity...
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Pulmonary fibrosis
Skin Changes Minimal myelosuppression |
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MOA hydroxyurea....
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Inhibits Ribonucleotide Reductase--> decreases DNA synthesis
S-phase specific |
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Toxicity of hydroxyurea...
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Bone marrow suppression
GI upset |
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Etoposide MOA...
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G2-phase specific agents that inhibits TOPOISOMERASE II and increases DNA degradation.
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Etoposide Toxicity...
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Myelosuppression
GI irritation Alopecia |
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Prednisone MOA...
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May trigger apoptosis
May work on nondividing cells??? |
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Prednisone Toxicity.
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Cushing like symptoms
immunosuppression cataracts acne osteoporosis hypertension peptic ulcers hyperglycemia psychosis |
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Tamoxifen/ raloxifene MOA
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Receptor antagonists in breast
Agonists in bone Block binding of estrogen to estrogen receptor-positive cells |
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Tamoxifen/ raloxifene Toxicity.
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Increase the risk of endometrial carcinoma (tamoxifen) via partial agonist effects.
*hot flashes* Raloxifene- does not cause endometrial carcinoma b/c it is an endometrial antagonist. |
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Trastuzumab (Herceptin) MOA...
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Monoclonal antibody against HER-2 (erb-B2).
Helps to kill breast cancer cells that overexpress HER 2- antibody dependent cytotoxicity??? |
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Trastuzumab (Herceptin) toxicity...
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Cardiotoxicity
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Imatinib (Gleevec) MOA...
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Philadelphia chromosome bcr-abl tyrosine kinase inhibitor.
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Imatinib (Gleevec) toxicity...
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Fluid retention
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Vincristine/Vinblastine MOA
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M-phase specific alkaloids that bind to tubulin and block polymerization of microtubules so that mitotic spindle can't form.
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Vincristine/Vinblastine Toxicity...
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Vincristine: Neurotoxicity (areflexia, peripheral neuritis), paralytic ileus
VinBLASTine BLASTS BONE MARROW (suppression) |
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Paclitaxel and other taxols MOA...
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M phase specific agents that bind to tubulin and hyperstabilize polymerized microtubules so that mitotic spindle cannot break down (anaphase cannot occur)
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Paclitaxel and other taxols Toxicity...
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Myelosuppression and hypersensitivity.
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