Antineoplastics

Question 1

What is happening during the phases of the cell life cycle? (G1, S, G2, M)

Answer 1

G1: cell contents (besides chromosomes) are duplicated
S: Chromosomes duplicated
G2: Checking chromosomes and repairing if needed
M: Mitosis

Question 2

What is the G0 phase?

Answer 2

‘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)

Question 3

Cell cycle non-specific antineoplastics do what? Examples.

Answer 3

Kill normal and malignant cells to the same extent
Ex-
Nitrosureas: carmustine, lomustine, semustine
Radiation

Question 4

Cell cycle phase specific antineoplastics do what? Examples.

Answer 4

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

Question 5

Proliferating cell antineoplastics do what? Examples.

Answer 5

Kill proliferating cells as opposed to resting cells. Can equally affect cell phase
Ex-
Alkylating agents: nitrogen mustards, cisplatin, carboplatin
Antibiotics: anthracyclines, dactinomycin

Question 6

Why may proliferating cell antineoplastics help to target cancer cells?

Answer 6

Tumor cells may proliferate at a higher rate than the body’s normal cells, helping to target tumor cells

Question 7

Common SE of treatment and why:

Answer 7

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.

Question 8

Cytoprotective drugs include: (3)

Answer 8

Mesna (Uromitexan)
Dexrazoxane (Zinecard)
Amifostine (Ethyol)

Question 9

What is Mesna (Uromitexan) and what does it do?

Answer 9

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.

Question 10

What is Dexrazoxane (Zinecard) and what does it do

Answer 10

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)

Question 11

What is Amifostine (Ethyol) and what does it do?

Answer 11

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

Question 12

Which drugs are used in response to chemotherapy’s effect on bone marrow and their goal?

Answer 12

Biological Response Modifiers

Goal= enhance the body’s immune system and replenish the cells lost d/t chemo

Question 13

Erythropoietin and darbepoetin stimulate:

Answer 13

RBCs

Question 14

Filgrastim and peg-filgrastim (G-CSF) stimulate:

Answer 14

Neutrophils

Question 15

Sargramostim (GM-CSF) stimulate:

Answer 15

Neutrophils

Question 16

Thrombopoietin stimulates:

Answer 16

Platelets

Question 17

Where is erythropoietin produced and what does it do?

Answer 17

Hormone produced by the kidneys to regulate RBC production. It induces erythropoiesis and therefore the release of reticulocytes from the BM into the bloodstream

Question 18

Which two products available are used for the administration of exogenous erythropoietin and how often are they given?

Answer 18

Epoetin (Procrit, Epogen)- q wk
Darbepoetin (Aranesp)- q 1-2wks
IV/subQ

Question 19

What are the exogenous forms of erythropoietin used for?

Answer 19

Anemia secondary to:
Chemo
CKD
Surgery
HIV therapy (ex. AZT)
HCV therapy (ex-ribavirin)

Question 20

What black box warning do exogenous forms of erythropoietin carry?

Answer 20

Increased mortality, serious CV and thromboembolic events (HF, MI, stroke, blood clots), and tumor progression
Related to higher than target Hgb

Question 21

Erythropoietin treatments should target Hgb’s of:

Answer 21

10-12

Should not target normal Hgb d/t increased risk of significant events, always use lowest dose possible

Question 22

What is the goal of treatment with erythropoietin?

Answer 22

Prevention of blood transfusion

Question 23

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?

Answer 23

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

Question 24

What is thrombopoietin (TPO) available as and what does it do?

Answer 24

Romiplostim (Nplate)

Increases platelet count by binding to and activating the human TPO receptor

Question 25

What type of patients is TPO given to?

Answer 25

Used in patients with ITP when other therapies (corticosteroids, immune globulin, splenectomy) have been insufficient

Question 26

How is TPO administered and how often?

Answer 26

SubQ once weekly

half-life of a platelet is 8-11 days

Question 27

Why might patients have an inadequate response to thrombopoietin (TPO)?

Answer 27

Patients may have neutralizing antibodies to romiplostim or TPO or bone marrow fibrosis.