Term
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Definition
MOA: mab CD20, which is found on most B-Cell neoplasms
Use: Non-Hodkins Lymphoma, Rheumatoid arthritis (with methotrexate. |
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Term
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Definition
MOA: Inhibits Philadelphia chromosome (bcr-abl) tyrosine kinase
USE: CML, GI stromal tumos
Toxicity: Fluid retention |
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Term
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Definition
MOA: mab against breast cancers that express HER2 (erb-B2). (possible through antibody depenendent cytotoxicity)
Use: Metastatic Breast cancer (does not cross BBB)
Toxicity: Cardiotoxicity |
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Term
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Definition
MOA: SERMs- receptor antagonists in breast and agonists in bone. (blocks estrogen from binding to its recepter)
Use: 1) breast cancer 2) prevent osteoporosis
Toxicity: Tamoxifen- inc risk of endometrial carcinoma via partial agonist effect "hot flashes". (raloxifene is an endometrial antagonist and therefore does not have this effect) |
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Term
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Definition
| MOA: May trigger apoptosis. May even work on dividing cells Use: Most commonly used glucocorticoid in cancer chemotherapy. CLL, Hodgkins lymphoma (part of MOPP regimen) Tox: Cushing like symptoms, immunosuppression, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis. |
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Term
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Definition
MOA: inhibits Ribonucleotide Reductase-->dec DNA Synthesis (s-phase)
Use: Melanoma, CML, sickle cell (inc HbF)
Tox: bone marrow suppression, GI upst |
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Term
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Definition
MOA: Cross link DNA
Use: Testicular, bladder, ovary, and lung carcinomas
Toxicity: nephrotoxicity, acoustic nerve damage
**admin with AMIFOSTINE(a free radical scavenger), and aggressive hydration to prevent negative SE** |
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Term
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Definition
Class: Microtubule inhibitors
MOA: bind tubulin in M-phase to block polymerization
Use: Hodgkins, Wilms tumor, Chorio carcinoma
Tox: Vincristine-NEUROTOXICITY (areflexia, peripheral neuritis), paralytic ileus
VinBLASTine-BLASTS Bone Marrow (suppression) |
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Term
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Definition
Class: Microtubule inhibitors
MOA: prevents breakdown of mitotic spindle
Use: Ovarian and breast carcinoma
Tox: myelosuppression and hypersensitivity |
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Term
4 Primary anti tumor antibiotics
*BEDD* |
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Definition
Bleomycin
Etoposide (VP-16)
Dactinomycin
Doxorubicin |
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Term
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Definition
Class: Antitumor antibiotic
MOA: Intercalates DNA
Use: Wilms, Ewing Sarcoma, Rhadbdomyosarcoma (used for childhood tumors)
Tox: Myelosuppression |
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Term
| Doxorubicin (adriamycin), daunorubicin |
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Definition
Class: Antitumor Antibiotics
MOA: Generates free radicals. (noncovalently intercalates in DNA->breaks DNA->dec replication)
USE: Hodgkins, myeloma's,, sarcomas, and solid tumors (breast, ovary, lung)
Tox: CARDIOTOXICITY, myelosuppression, alopecia |
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Term
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Definition
Class: Antitumor antibiotics
MOA: induces free radicals that break DNA strands
use: TESTICULAR CANCER, Hodgkins.
Toxicity: PULMONARY FIBROSIS, skin changes, minimal myelosuppression |
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Term
| Etoposide (VP-16), teniposide |
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Definition
Class: Antitumor antibodies
MOA: Inhibits TOPOisomerase II-->inc DNA degradation
Use: SMALL CELL CARCINOMA (lung & prostate), testicular carcinoma.
Tox: Myelosuppression, GI irritation, alopecia |
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Term
| Cyclophosphamide, ifosfamide |
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Definition
Class: Alkylating Agents
MOA: Covalently cross links DNA at GUANINE N-7. (these drugs req bioactivation in liver)
Use: Non-Hodgkins lymp, breas and ovarian carcinomas, IMMUNOSUPPRESANT
Toxicity: Myelosuppression, HEMORRHAGIC CYSTITIS (acrolein is toxic metabolite-treat with MESNA) |
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Term
| Nitrosoureas (carmustine, lomustine, semustine, streptozocin) mustard gas derivitives? |
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Definition
Class: Aklylating agents
MOA: requires bioactivation. Crosses the Blood BRAIN BARRIER!!
Use: BRAIN-tumors (inc. glioblastoma multiforme)
Tox; BRAIN:CNS toxicity-dizziness, ataxia |
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Term
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Definition
Class: Alkylating Agents
MOA: Alklyates DNA
USE: CML. (also used to destroy pt's bone marrow before transplant)
Tox: pulmonary fibrosis, hyperpigmentation |
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Term
| 5 antimetabolites? what cell cycle phase do they target? |
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Definition
MTX, 5-FU, 6-MP, 6-TG, ara-C
all are S-Phase specific |
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Term
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Definition
C: Antimetabolites
MOA: Folic acid analog that inhibits DIHYDROFOLATE reductase-> dec dTMP-->dec DNA & protein synthesis
Use: Leukemia, lymphomas, Choriocarcionoma, sarcomas. (also Abortion, ectopic pregnancy, RA, psoriasis)
Tox 1) myelosuppression (folic rescue w/ LEUCOVORIN) 2) macrovesicular fatty liver 3) mucositis. 4) TERATOGENIC |
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Term
| Drug used to reverse Methotrexate toxicity |
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Definition
| LEUCOVORIN (Folinic acid) rescue |
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Term
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Definition
Class: Antimetabolite
MOA: PYRIMIDINE ANALOG. (5F-dUMP) that inhibits Thymidilate Synthase (dec dTMP which leads to dec DNA & Protein synthesis)
Use: Colon cancer, basal cell carcinoma (topical) solid tumors. (synergy with MTX)
1) myelosuppression which require THYMIDINE (not leucovorin) 2) Photosensitivity |
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Term
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Definition
Purine (thiol) analog--> dec de novo purine synthesis
*activated by HGORTase*
USE: Leukemia, lymphomas (not CLL or hodgkins)
Tox: Bone marrow, GI, liver. METABOLIZED by xanthine oxidase thus inc toxicity with allopurinol administration*** |
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Term
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Definition
C: antimetabolite
MOA: same as 6MP
Use: ALL
Tox Mone marrow depression. CAN BE GIVEN WITH ALLOPURINOL |
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Term
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Definition
MOA: Pyrimdine antagonist--> inhibits DNA polymerase.
USE: AML, ALL, High Grad HODGKINS*
Tox: leukopenia, thrombocytopenia, megaloblastic anemia. |
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Term
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Definition
MOA: binds glycoprotein receptor IIb/IIIa on activated platelets, prevents aggregation
Use: acute coronary syndromes, percutaneous transluminal coronary angioplasty
Tox: bleeding, thrombocytopenia |
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Term
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Definition
MOA: inhbit platelet aggregation by irreversibly blocking ADP recepters. Inhibit fibrinogen bind by preventing glycoprotein IIb/IIIa expression
Use: Acute coronary syndrome, coronary stenting, dec recurrence of thrombotic stroke
Tox: Neutropenia (ticlopidine) |
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Term
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Definition
MOA: acetylates and irreversibly inhibits COX 1&2, to prevent TXA2 formation. INCREASE BLEEDING Time, but no effect on PT, PTT
Use: Antipyretic, analgesic, anti-inflammatory antiplatelet drug
Tox: gastric ulceration, hyperventilation, Reye's syndrome, tinnitus (CN VIII) |
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Term
Thrombolytics:
Streptokinase, tPA (alteplase) APSAC (anistreplase) |
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Definition
MOA: converts plasminogen to plasmin, whiche cleaves thrombing and fibrinn clots. increases PT, PTT, with no change in platelete count.
use: Early MI, early ischemic stroke
Tox: Bleeding.
contraindicated in pt's with active bleeding, history of intracranial bleeding, recent surgery, known bleeding diathesis, or sever hypertension.
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Term
| Drug used to treat toxicity of thrombolytics? |
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Definition
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Term
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Definition
MOA: interferes with the gamma carobylation of Vitamin K dependent clotting factos II, VII, IX, X, protein C and S. Metabolized by cyp-450. Inc PT.
Long half life.
Use: chronic anticoagulatant. Not used in pregant women. Follow PT/INR values
Tox: Bleeding, tetratogenic, skin/tissue necrosis, drug drug interaction. |
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Term
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Definition
| Hirudin derivatives directly inhibit thrombin. Used as an alaternative to heparin for anticoagulating pt's with HIT. |
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Term
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Definition
MOA: cofactor for the inactivation of antithrombin (dec thrombin and Xa) has a short half life
Use: immediate anticoagulation in PE, stroke, MI, DVT. *used during pregnancy* follow PTT
Tox: bleeding, HIT, osteoporosis, d
For reversal of heparin tox use Protamine sulfate
Dosing: low molecular weight heparings (enoxaparin) act more on Xa, have better bioavailability and don't require monitoring. |
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Term
| Heparin Induced Thrombocytopenia (HIT) |
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Definition
Mech: heparing binds to platelet factor IV, causing antibody production that binds to and activates platelets leading to their clearance and thus resulting in thrombocytopenic hypercoagulable state
Treat: Protamine sulfate (positively charged molecule that binds to negatively charged heparin) |
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