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21 Cards in this Set
- Front
- Back
What is the Mechanism of Action and General Toxic Side Effects of Alkylating Agents?
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MOA: all act by alkylating macromolecules, notably DNA; and or by forming covalently-bound cross-links in DNA.
General Side Effects: acute and chronic; nausea and vomiting; bone-marrow suppression; alopecia, teratogenicity and carcinogenicity. Cross resistance occurs between many of these agents |
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What are the Anthracyclines and what is their mechanism of action?
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doxorubicin and daunorubicin
MOA: single and double strand breaks occur. mediated by drung binding to DNA and topoisomerase II. Also generates free radicals. Cell exposure leads to apoptosis. |
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What are the therapeutics and toxicities of Daunorubicin?
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Therapeutics: useful in treatment of acute lymphocytic and acute myelogenous leukemias. severe local vesicant action can occur. may impart a red color to the urine.
Tox: bone marrow depression, stomatitis, alopecia, GI disturbances, dermatological manifestations, cardiac tox |
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what are the therapeutic uses and clinical toxicities of doxorubicin?
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therapeutic uses: effective in acute leukemias and malignant lymphomas. in contrast to daunorubicin is active in a number of solid tumors (breast cancer). severe local vesicant action can occur. may impart a red color to the urine.
clinical tox: similar to those of daunorubicin. erythematous streaking near the site of infusion, cardiomyopathy |
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What is the MOA, therapeutics, and toxicites of actinomycin D?
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MOA: intercalates into DNA; blocks transcription of DNA by RNA polymerase
Therapeutic Uses: childhood neoplasms, soft tissue sarcomas, to inhibit immune responses (transplants) Tox: nausea and vomiting, allopecia, reduction in bone marrow function, loss of appetite, dysphagia, rashes/acne, mouth, sores, fever, diarrhea, temporarily altered liver function |
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What is the MOA, clinical uses and toxicities of Bleomycin?
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MOA: DNA cleaving antibiotic; can cause oxidative damage to DNA leading to single and double stranded breaks in DNA
Therapeutic uses: highly effective against germ cell tumors of the testis and ovary. Can be used in combination therapy in esophagus as well as in Hodgkin's and non Hodgkin's lymphoma clinical toxicites: little myelosuppression, significant cutaneous and pulmonary toxicity. toxicities do not overlap with other drugs |
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What are the therapeutic uses of Cisplatin (metal compounds)?
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used for treatment of ovarian cancer; results in renal, hearing and neurological toxicity; hydration recommended; combination therapy with bleomycin, etoposide and vinblastine for advanced testicular cancer
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what are the therapeutic uses of carboplatin (a metal)?
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-similar mechanism to cisplatin
-less nausea, neurotic, ototoxicity, and nephrotoxicity -dose limiting tox is myelosuppression, primarily evident as thrombocytopenia -effective alternative for patients with reponsive tumors who are unable to tolerate cisplatin because of impaired renal function -approved for use in combination with paclitaxel or cyclophosphamide in patients with advanced ovarian cancer |
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what are the therapeutic uses of arsenic trioxide (metal)?
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-used for the treatment of acute promyelocytic leukemia
-mechanist: induces differentiation and apoptosis -side effects: lightheadedness during infusion, fatigue, muscoloskeletal pain, hyperglycemia and peripheral neuropathy |
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What is the MOA, therapeutic use and tox for Tamoxifen (steroid, antiestrogen)?
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MOA: competitve inhibitor of estradiol binding to the estrogen receptor; when bound to the ER, induces a change in 3D shape of the receptor, inhibiting binding of the estrogen responsive element on DNA.
Therapeutic use: endocrine treatment of choice for postmenopausal women with estrogen receptor positive breast cancer clinical tox: hot flashes, nausea and vomiting, weight gain, endometriosis, blood clotting abnormalities, depression, tiredness and dizziness |
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What is the therapeutic use and mechanism of Dexamethasone (steroid, anti estrogen)?
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-used in conjunction with X-ray therapy to reduce edema related to tumors in the brain and spinal cord
-antitumor effects are mediated by binding to a specific cytoplasmic receptor, which, when activated, induces a program of gene expression that leads to apoptosis |
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What are the actions and side effects of asparaginase (enzyme)?
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action: deprives certain leukemic cells of the essential metabolite, asparagine
side effects: acute: can cause fever chronic: can include mental depression (coma in extreme cases) and h |
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what does aromatase do?
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an enzyme which produces estrogen from androgens
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what are the two aromatase inhibitors? what is their MAO? therapeutics? and tox?
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-anastrozole, letrozole
-inhibit aromatase -starting to replace tamoxifen in breast cancer treatment in many postmenopausal women independent of ER status -tox not as great as tamoxifen and is as effective |
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what is the MAO, therapeutic and tox of Trastuzumab (herceptin)?
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-monoclonal antibody against the Her2 protein which is over expressed in 25-30% of breast cancer
-expression of this protein is associated with decreased survival due to more aggressive disease -MOA: cell cycle arrest via antibody mediated cytotox -used in her2 breast cancer patients in combo with paclltaxel tox: diarrhea and hematologic effects are most common |
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what is MAO, effect, uses of alpha methyl tyrosine?
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-inhibits TH
-decreased synthesis of catecholamines -used rarely: hypertension, adrenal gland tumor |
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reserpine?
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-irreversible inhibitor of VMAT
-low dose: increase MAO metabolism -high dose: enhanced leakage through NET -used for hypotension, depression, appetite suppression -adverse: dependence, hypertension, CNS |
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tyramine?
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-used in conjunction with MAO inhibitor
-displaces NT from vesicle- cheese effect -hypotension, depression, appetite suppression -adverse: dependence, hypertension, CNS |
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amphetamine (ephedrine)
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displaces catecholamines from vesicles
-inhibits mao weakly -hypotension, depression, appetite suppression -adverse: hypertension, dependence, CNS |
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atomoxetine
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-inhibition of NET; inhibits reuptake
-adverse- drug abuse, non selective inhibition of transmitter uptake |
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phenelzine
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MAO inhibitor, nonselective
-accumulation of catecholamines -more available in vesicles for release -used for depression -adverse: cheese effect with tyramine, seratonin syndrome in combo with SSRI |