Gonadotropin-Releasing Hormone Analogues , Angiogenesis Inhibitors, Tyrosine Kinase Inhibitors

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  1. Gonadotropin-releasing hormone analogues:
    agonist drugs:
    • Goserelin
    • Buserelin·        
    • Leuprolide
    • Triptorelin 
    • Gonadorelin
    • Nafarelin
    • Histrelin       
    • Deslorelin
  2. GRHA
    Antagonist drugs:
    • Abarelix
    • Cetrorelix
    • Ganirelix
    • Degarelix
    • GnRH is synthesized in the hypothalamus and controls the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary
    • Continuous administration of GnRH results in suppression of gonadotropin release via down-regulation of GnRH receptors, a process called desensitization (receptor desensitization)
    • GnRH antagonists simply block the GnRH receptor, resulting in reduced release of FSH and LH.
    •      Can use for fertility treatments- pulses, and increase estrogen
  4. kinetics for Goserelin:
    • Depot injection  IM or subq (releases med overtime)
    •       Provides continuous release of drug over a 29-day period
  5. kinetics for Leuprolide:
    • Depot injection (IM or subq)
    •       Available in formulations that can be administered every month, 3 months, 4 months, or 6 months
  6. kinetics for Buserelin:
    Available as both a nasal spray and an injection formulation
  7. GRHA indications:
    • Conditions that benefit from hypoestrogen states 
    •    Cancers:  Breast, ovarian, and endometrialo   
    •    Endometriosis, dysfunctional uterine bleeding, uterine fibroids
    •    Precocious puberty
  8. Hormonal therapy in breast CA:
    (surgery [mass or lump ectomy], RT, then testfor ER, PR, & HER2- then need to decrease amount of estrogen with Tamoxifen(pre or post menopause) or aromatase inhibitors for postmenopausal oroophorectomy in premenopausal
  9. Hormona therapy in Breast CA fro premenopausal pts:
    • Surgical removal of the ovaries·         Radiation of the ovaries (rarely used in the United States)·        
    • Inhibition of the pituitary-hypothalamic-gonadal axis with gonadotropin-releasing hormone analogues (goserelin, leuprolide acetate)·        
    • Tamoxifen
  10. GRHA SE:
    related to androgen deprivation:
    related to estrogen deprivation:
    rare, serious: antagonists only:
    • Related to androgen deprivation:       Decreased libido
    • Flushing·        
    • Gynecomastia·        
    • Weight gain·        
    • Loss of bone and muscle mass
    • Related to Estrogen Deprivation:
    • Hot flashes·        
    • Vaginitis·        
    • Sweating·        
    • Change in breast size
    • Rare, serious:
    • Ovarian hyperstimulation syndrome (OHSS)
    • Leaky capillaries resulting in edema and ascites
    • Antagonists only (Abarelix):
    • Allergic rxnx
  11. GRHA CI:
    • Pregnancy
    • Undiagnosed vaginal bleeding
  12. Angiogenesis inhibitor drugs:
    • Bevacizumab (Avastin)- colon and brain CA
    • Ranibizumab (Lucetis)
  13. Angiogenesis inhib MOA:
    • Bevacizumab and ranibizumab bind to VEGF-A, preventing it from binding to its receptor
    • Its “tumorstatic”
  14. kinetics for Bevacizumab & Ranibizumab:
    • Bevacizumab: Administered by intravenous infusion
    • Metabolism via proteolysis: Occurs throughout the body, including within endothelial cells
    • Ranibizumab: Administered by intravitreal injection Into the vitreus of the eye
  15. CI for Angiogenesis inhibs:
    • Ranibizumab
    •     Suspected ocular infections
    •         Increased risk of endophthalmitis
  16. indication for angiogenesis inhibs:
    • Bevacizumab
    •    Colorectal cancer (1st line FUL FOX)
    •    Breast (HER2-negative) cancer·        
    •    Lung (non-small cell) cancer·
    •    Glioblastoma·        
    •    Renal Cell
    • Ranibizumab 
    •    Age-related macular degeneration
  17. SE for angiogenesis inhibs:
    • Bevacizumab:  - on exam ·        
    • GI perforation
    • Hemorrhage
    • Hypertension
    • Thrombosis·        
    • Decreased wound healing·        
    • Proteinuria
  18. Colon CA tx regime: 2nd line
    FOLFIRI: Fluorouracil Continuous Infusion/ Leucovorin/Irinotecan) + Bevacizumab
  19. Non-small Cell Lung CA tx regime:
  20. Glioblastoma tx regime: 1st line
    • Temozolomide + Bevacizumab
  21. imp to know about Bevacizumab and surgery:
    • Significant side effect
    •    Increased bleeding risk·        
    •      Should be discontinued at least 6 weeks before surgery ·        
    •      Cannot be initiated within 4 weeks after surgery
  22. Tyrosine kinase inhibs categories of drugs:
    • monoclonal antibodies
    • EGFR- for NSCLC
    • BCR-ABL/src- for leukemia
    • Multikinase inhibs - renal cell carcinoma
    • dual kinase inhibitors - EGFR/HER2
    • Anaplastic lymphoma kinase
  23. TKI
    monoclonal antibodies drugs:
    • Human Epidermal Growth Factor Receptor (HER2) 
    •    Trastuzumab (Herceptin)- breast CA, when + for HER2·        
    • Epidermal Growth Factor Receptor (EGFR)
    •    Cetuximab (Erbitux)- colon CA
    •    Panitumumab (Vectibix)- colon CA·     
    • HER2 and Microtubule Inhibitor
    •    Ado-trastuzumab emtansine (Kadcyla)
    • HER2 and EGFR
    •    Pertuzumab (Perjeta)
  24. TKI
    EGFR drugs:
    • for nonsmall cell lung CA ·        
    • Erlotinib (Tarceva) ·        
    • Gefitinib (Iressa)
  25. TKI
    • leukemia:
    • Imatinib  (Gleevec)
    • Dasatinib (Sprycel)
    • Nilotinib (Tasigna)
  26. TKI
    multikinase inhibs:
    • Sorafenib  (Nexavar)
    • Sunitinib  (Sutent)
    • Axitinib (Inlyta)
    • Pazopanib (Votrient)
    • Regorafenib (Stivarga)
  27. TKI
    dual kinase inhibitors: EGFR/HER2
    Lapatinib (Tykerb)
  28. TKI
    Anaplastic lymphoma kinase drugs:
    Crizotinib (Xalkori) (1st line for ALK + in non small cell lung CA)
  29. TKI MOA:
    • Binding and neutralizing ligands
    • Occupying receptor-binding sites
    • Blocking receptor signaling within the cancer cells
    • Interfering with downstream intracellular molecules
    • Monoclonal antibodies (water soluble and large) target extracellular components of these pathways, such as ligands and receptor domains
    • Small molecule inhibitors can enter cells, thereby blocking receptor signaling and interfering with downstream intracellular molecules.
  30. if you test + for ALK gene, give:
  31. if you test + for EGFR, give:
  32. if you test + for HER2 mutant, give:
    Trastuzumab, Iapatinib, Pertuzumab
  33. kinetics of the small molecule TKI:
    all PO- nibs
  34. kinetics of the monoclonal antibodies:
    IV infusion- mabs
  35. kinetics of Sunitinib,sorafenib, imatinib, dasatinib, and erlotinib?
    • Primarily eliminated by hepatic metabolism
    • All metabolized by CYP3A4 (Many DI’s)
  36. 1st line for renal cell carcinoma:
    Sorafenib or Sunitinib
  37. CI of TKI?
  38. SE of TKI?
    • Diarrhea
    • Acneiform Rash   (NOT a CI to continued EGFR inhibitor therapy) those who get the rash usually have better outcomes on the med. Usually a good sign.       Taking EGFR inhibitor ·        
    •     Common when taking  EGFR inhibitors or multikinase inhibitors. Likely because of inhibition of epidermal turnover
  39. SE of-
    Sorafenib, Sunitinib, and Dasatinib;
    Gefitinib and Erlotinib:
    • SSD: QT prolongation
    • GE: interstitial lung disease
    • E: hepatotox
  40. serious SE of Trastuzmab:
    • Cardiotoxicity (also c/ doxoruzimab)
    •    synergism c/ anthracycline chemo
  41. Serious SE of Cetuximab and Panitumumab:
    • cardiopulmonary arrest
    • Hypomagnesemia (common)
Card Set:
Gonadotropin-Releasing Hormone Analogues , Angiogenesis Inhibitors, Tyrosine Kinase Inhibitors
2013-07-30 01:41:05
Gonadotropin Releasing Hormone Analogues Angiogenesis Inhibitors Tyrosine Kinase

Gonadotropin-Releasing Hormone Analogues , Angiogenesis Inhibitors, Tyrosine Kinase Inhibitors pharm
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