Chapter 8 anticancer - hormonal anticancer agents + hematopoetic agents Flashcards
estrogen
hormonal
- counteracts endogenous testosterone (since it enhances tumor growth) in patients w/ prostate cancer
progestin
hormonal
- progesteron receptor agonist
indication:
* endometrial carcinoma
* metasatic renal carinoma
* breast cancer
mechanism unclear..
tamoxifen
hormonal
estrogen receptor antagonist
* prevent endogenous estrogens from stimulating tumor growth
* used to tx estrogen receptor positive bresat cancer in postmenopausal women
effect
* increased risk of uterine cancer observed in women tx’d w/ tamoxifen
aromatase inhibitor
hormonal
- non steroidal aromatae inhibitor selectively reduecs circulation estradiol levles for tx of advanced breast cancer
- anastrazole and letrozole are the drug names
androgen
hormonal
testerone receptor agonist
* active against some breast and renal cancers
flutamide
hormonal
- testosterone receptor antagonist
- augments late effects of leuprolide
- stiulates LH and FSH via leuprolide
treat men with prostate cancer
abiraterone (zytiga)
hormonal
- prodrug => abirterone, which inhibits androgen biosynthesis
- drug itself blocks CYP17, which is expressed in testicular, adrenal and prostatic tumors and is required in androgen biosynthesis
- abiraterone is used with prednisone for tx of castration-resistant metastatic prostate cancer (androgen antagonists no longer work!)
adrenocorticosteroid
hormonal
lnhibit DNA and protein synthesis + mitosis
indication
* acute lymphocytic lekemia
* chronic lymphocytic leukemia
* acute myelogenous (bone marrow) leukemia
* multiple myeloma (plasma cells in bone marrow)
* breast cancer
* lymphoma (starts in lymph node)
leuprolide, goserelin
hormonal
- analog of gonadotropin releasing hormone (GNRH)
- densensitizes GNR receptors in pituitary causing dec release of gonadotropin
- results in decreased sex hormone release
indication
* advanced prostate cancer
effect
* initally stimulates transient release of sex hormones (LH anad FSH) — initial leuprolide effect
estramustine (EmCyt)
estrogen agonist linked to alkylating agent
* drug uptake is enhanced in estrogen receptor + cells => l/t selective accumulation of alkylating agent in tumor cells
indication
* prostate carcinoma
epoetin alpha (epogen)
hematopoetic agent
- recombinant human erthropoetin
- erythropoetin is synthesized in kidney in repsone to hypoxia or anemia, stimulates erythropoiesis
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indication
* drug is indicated for anema in pts w/ chronic renal failure (unable to synthesize erthropoetin
* for correcting zidovudine (AZT)-induced anemia in HIV infected + chemotherapy induced anema in cancer pts
pharmco
* takes several weeks of therapy before hematocrit rise; this drug cannot replace transfusions for acute tx of severe anemia
contra
* not used in pts w/ uncontrolled HTN d/t elevated hematocrit exacerbating HTN
filgrastim (G-CSF) (neupogen)
hematopoetic agent
- human recombinant granulocyte colonyl stimulating factor (G-CSF)
- helps induces synthesis of neutrophils from progenitor cells
- prevent neutropenia espcially with chemotherapy that includes highers doses of myelosuppressive drugs — l/t potential development of toxicities that were previously rarely seen
indication:
* tx of severe cyclic neutropenia and severe chronic neutropenia
effect
* medullary bone pain d/t rapid cell proliferation wtihin marrow
contra
* should not be used within 24 hrs of administration of cancer drugs d/t effect of cytotoxic agent w/ rapidly dividing myleloid cells not clear
sargramostim (GM-CSF)
hematopoetic agent
- human recombinant granulocyte-macrophage colony timualting factor (GM-CSF)
- stimulates proliferation of all lines of blood cells
- induces maturation of granulocytes and macrophages BUT NOT erthrocytes or megakaryoctes
- this drug also activates the former two as well!
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indication
* accerlerate bone marrow replenishment following autologus (obtained from same individual) bone marrow transplantation
risk of it acting as a growth factor for other cancer types unknown…
oprelvekin (interleukin II, neumega)
hematopoetic agent
- recombinant growth factor that stimulates platelet production
indication
* maintaining platelet counts following chemotherapy
* shows limited efficacy
toxicity includes
* fluid retention
* tachycardia
* other CV rxn
