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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?
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
What are the Anthracyclines and what is their mechanism of action?
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.
What are the therapeutics and toxicities of Daunorubicin?
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
what are the therapeutic uses and clinical toxicities of doxorubicin?
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
What is the MOA, therapeutics, and toxicites of actinomycin D?
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
What is the MOA, clinical uses and toxicities of Bleomycin?
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
What are the therapeutic uses of Cisplatin (metal compounds)?
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
what are the therapeutic uses of carboplatin (a metal)?
-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
what are the therapeutic uses of arsenic trioxide (metal)?
-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
What is the MOA, therapeutic use and tox for Tamoxifen (steroid, antiestrogen)?
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
What is the therapeutic use and mechanism of Dexamethasone (steroid, anti estrogen)?
-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
What are the actions and side effects of asparaginase (enzyme)?
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
what does aromatase do?
an enzyme which produces estrogen from androgens
what are the two aromatase inhibitors? what is their MAO? therapeutics? and tox?
-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
what is the MAO, therapeutic and tox of Trastuzumab (herceptin)?
-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
what is MAO, effect, uses of alpha methyl tyrosine?
-inhibits TH
-decreased synthesis of catecholamines
-used rarely: hypertension, adrenal gland tumor
reserpine?
-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
tyramine?
-used in conjunction with MAO inhibitor
-displaces NT from vesicle- cheese effect
-hypotension, depression, appetite suppression
-adverse: dependence, hypertension, CNS
amphetamine (ephedrine)
displaces catecholamines from vesicles
-inhibits mao weakly
-hypotension, depression, appetite suppression
-adverse: hypertension, dependence, CNS
atomoxetine
-inhibition of NET; inhibits reuptake
-adverse- drug abuse, non selective inhibition of transmitter uptake
phenelzine
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