Antineoplastics Flashcards
What is happening during the phases of the cell life cycle? (G1, S, G2, M)
G1: cell contents (besides chromosomes) are duplicated
S: Chromosomes duplicated
G2: Checking chromosomes and repairing if needed
M: Mitosis
What is the G0 phase?
‘fifth phase’
The arrest phase where the cell is not actively duplicating
(tumor cells continue to divide under conditions that would send normal cells to the G0 state)
Cell cycle non-specific antineoplastics do what? Examples.
Kill normal and malignant cells to the same extent
Ex-
Nitrosureas: carmustine, lomustine, semustine
Radiation
Cell cycle phase specific antineoplastics do what? Examples.
Target one of the cell cycles and do not affect cells in other phases
Ex-
M phase: vinca alkaloids, paclitaxel, docetaxel
S phase: topoisomerase inhibitors, purine, pyrimidine, folate antimetabolites
G1 phase: aspariginase, prednisone
G2 phase: bleomycin, etoposide
Proliferating cell antineoplastics do what? Examples.
Kill proliferating cells as opposed to resting cells. Can equally affect cell phase
Ex-
Alkylating agents: nitrogen mustards, cisplatin, carboplatin
Antibiotics: anthracyclines, dactinomycin
Why may proliferating cell antineoplastics help to target cancer cells?
Tumor cells may proliferate at a higher rate than the body’s normal cells, helping to target tumor cells
Common SE of treatment and why:
Hair loss, increased, susceptibility to infection, anemia, bleeding, N/V/D/C, stomatitis, anorexia, taste changes.
Cells in the GI tract, bone marrow, and hair are rapidly dividing making them a target of therapy.
Cytoprotective drugs include: (3)
Mesna (Uromitexan)
Dexrazoxane (Zinecard)
Amifostine (Ethyol)
What is Mesna (Uromitexan) and what does it do?
Cytoprotective agent used to treat antineoplastic toxicity
Prevents hemorrhagic cystitis. Reacts and detoxifies the toxic compound that can be released by ifosfamide or cyclophosphamide and cause hemorrhagic cystitis.
What is Dexrazoxane (Zinecard) and what does it do
Cytoprotective agent used to treat antineoplastic toxicity
Protects against cardiotoxicity of anthracyclines. It chelates iron that acts as an oxidizing agent in the heart
(anthracyclines can only be taken for a limited amount of time d/t this toxicity)
What is Amifostine (Ethyol) and what does it do?
Cytoprotective agent used to treat antineoplastic toxicity
Used with cisplatin and cyclophosphamide to reduce neutropenic fever and infection
Used with platinum agents to reduce cumulative renal toxicity
Free radical scavenger
Causes dec. in BP in 50% of patients
Which drugs are used in response to chemotherapy’s effect on bone marrow and their goal?
Biological Response Modifiers
Goal= enhance the body’s immune system and replenish the cells lost d/t chemo
Erythropoietin and darbepoetin stimulate:
RBCs
Filgrastim and peg-filgrastim (G-CSF) stimulate:
Neutrophils
Sargramostim (GM-CSF) stimulate:
Neutrophils
Thrombopoietin stimulates:
Platelets
Where is erythropoietin produced and what does it do?
Hormone produced by the kidneys to regulate RBC production. It induces erythropoiesis and therefore the release of reticulocytes from the BM into the bloodstream
Which two products available are used for the administration of exogenous erythropoietin and how often are they given?
Epoetin (Procrit, Epogen)- q wk
Darbepoetin (Aranesp)- q 1-2wks
IV/subQ
What are the exogenous forms of erythropoietin used for?
Anemia secondary to: Chemo CKD Surgery HIV therapy (ex. AZT) HCV therapy (ex-ribavirin)
What black box warning do exogenous forms of erythropoietin carry?
Increased mortality, serious CV and thromboembolic events (HF, MI, stroke, blood clots), and tumor progression
Related to higher than target Hgb
Erythropoietin treatments should target Hgb’s of:
10-12
Should not target normal Hgb d/t increased risk of significant events, always use lowest dose possible
What is the goal of treatment with erythropoietin?
Prevention of blood transfusion
How are Filgrastim (Neuopogen G-CSF), Pegfilgrastrim (Neulasta G-SCSF) and Sargramostim (Leukine, GM-CSF) different and what is the main SE associated with all three?
Filgrastim (Neupogen) and Pegfilgrastrim (Neulasta) are lineage specific, affected only neutrophils and Sargramostim (Leukine) is a multi-lineage growth factor, affecting neutrophils, macrophages, monocytes
SE: Bone pain
What is thrombopoietin (TPO) available as and what does it do?
Romiplostim (Nplate)
Increases platelet count by binding to and activating the human TPO receptor