Antineoplastic Agents

Antineoplastic agents comprise one aspect of chemotherapy. These drugs act

on and kill altered human cells. While their action is intended to target abnormal
cells, normal cells are also affected. These drugs can work by affecting cell
survival or by boosting the immune system in its efforts to combat the abnormal
cells.

• Antineoplastic Agents: Generic and Brand Names

• Disease Spotlight: Cancer
• Alkylating Agents
o Therapeutic Action
o Indications
o Pharmacokinetics
o Contraindications and Cautions
o Adverse Effects
• Antimetabolites
o Therapeutic Action
o Indications
o Pharmacokinetics
o Contraindications and Cautions
o Adverse Effects
• Antineoplastic Antibiotics
o Therapeutic Action
o Indications
o Pharmacokinetics
o Contraindications and Cautions
o Adverse Effects
• Mitotic Inhibitors
o Therapeutic Action
o Indications
o Pharmacokinetics
o Contraindications and Cautions
o Adverse Effects
• Hormones and Hormone Modulators
o Therapeutic Action
o Indications
o Pharmacokinetics
o Contraindications and Cautions
o Adverse Effects
• Cancer Cell-Specific Agents
o Therapeutic Action
 o Indications
o Pharmacokinetics
o Contraindications and Cautions
o Adverse Effects
o Interactions
• Nursing Considerations
o Nursing Assessment
o Nursing Diagnoses
o Implementation with Rationale
o Evaluation

Antineoplastic Agents: Generic and Brand Names

Here is a table of commonly encountered antineoplastics, their generic names,

and brand names:

Classification Generic Name Brand Name

altretamine Hexalen

bendamustine Treanda

busulfan Busulfan, Myleran

carboplatin Paraplatin

Alkylating Agents carmustine BiCNU, Gliadel

chlorambucil Leukeran

cisplatin Platinol-AQ

cyclophosphamide Cytoxan, Neostar

dacarbazine DTIC-Dome
 ifosfamide Ifex

lomustine CeeNu

mechlorethamine Mustargen

melphalan Alkeran

oxaliplatin Eloxatin

procarbazine Matulane

streptozocin Zanosar

temozolomide Temodar

thiotepa Thioplex

capecitabine Xeloda

cladribine Leustatin

clofarabine Clolar

cytarabine DepoCyt, Tarabine PFS

floxuridine FUDR
Antimetabolites

fludarabine Fludara

Adrucil, Carac, Efudex,

fluorouracil
Fluoroplex

gemcitabine Gemzar

mercaptopurine Purinethol
 methotrexate Rheumatrex, Trexall

pemetrexed Alimta

pentostatin Nipent

pralatrexate Folotyn

thioguanine Tabloid

bleomycin Blenoxane

dactinomycin Cosmegen

daunorubicin DaunoXome

doxorubicin Adriamycin, Doxil

Antineoplastic Antibiotics epirubicin Ellence

idarubicin Idamycin

mitomycin Mutamycin

mitoxantrone Novantrone

valrubicin Valstar

cabazitaxel Jevtana

docetaxel Taxotere
Mitotic Inhibitors
etoposide Toposar, VePesid

ixabepilone Ixempra
 paclitaxel Abraxane, Onxol Taxol

teniposide Vumon

vincristine Oncovin, Vincasar

vinorelbine Navelbine

anastrozole Arimidex

bicalutamide Casodex

degarelix Degarelix for Injection

estramustine Emcyt

exemestane Aromasin

flutamide (generic)

fulvestrant Faslodex
Hormones and Hormone
Modulators
goserelin Zoladex

histrelin Vantas

letrozole Femara

leuprolide Lupron, Eligard

megestrol Megace

mitotane Lysodren

nilutamide Nilandron
 tamoxifen Soltamox

toremifene Fareston

triptorelin pamoate Trelstar Depot

Cancer Cell-Specific Agents

everolimus Afinitor
gefitinib Iressa
imatinib Gleevec
lapatinib Tykerb
• Protein Tyrosine Kinase
nilotinib Tasigna
Inhibitors
pazopanib Votrient
sorafenib Nexavar
sunitinib Sutent
temsirolimus Torisel
• Epidermal Growth
erlotinib Tarceva
Factor Inhibitor
• Proteasome Inhibitor bortezomib Velcade
arsenic trioxide Trisenox
asparaginase Elspar
azacitidine Vidaza
bexarotene Targretin
decitabine Dacogen
hydroxyurea Hydrea
irinotecan Camptosar
Other antineoplastics nelarabine Arranon
pegaspargase Oncaspar
porfimer Photofrin
sipuleucel-T Provenge
talc powder Sclerosol
topotecan Hycamtin
tretinoin Vesanoid
vorinostat Zolinza
Disease Spotlight: Cancer

• Cancer is the second leading cause of death in the United States.

Treatment is usually multidisciplinary, prolonged, and often debilitating.
It can develop at any age.
• Proliferation of abnormally-dividing cells starts the pathologic process.
Genetic abnormalities are passed along daughter cells, eventually
producing a tumor or neoplasm that has characteristics quite different
from those of the original tissue.
• Consequently, original cell characteristics are lost. Anaplasia is the loss
of cellular differentiation and organization. Autonomy is the ability to
grow without usual homeostatic restrictions that regulate cell growth
and control.
• Uncontrolled growth of neoplastic cells will lead to invasion of healthy
tissues in the area and metastasis, or traveling from the place of origin
to develop new tumors in other areas of the body.
• Cancers can be divided into two groups: 1) solid tumors; and 2)
hematological malignancies. Solid tumors can further be differentiated
into carcinomas, or tumors that originate in epithelial cells,
and sarcomas, or tumors that originate in the mesenchyme and are
made up of embryonic connective tissue cells.
• The goal of cancer chemotherapy is to decrease the size of neoplasm
so that the human immune system can deal with it.
Alkylating Agents

• Alkylating agents are non-cell cycle specific antineoplastics drugs. They

can affect cells even in the resting phase.
• These are the agents of choice for slow-growing cancers.

Therapeutic Action

The desired and beneficial action of agents for alkylating agents is:

• Reacting chemically with portions of RNA, DNA, or other cellular

proteins to produce their cytotoxic effects.
• Alkylating agents are most potent when binding with cellular DNA.
• The oldest drugs in this class are nitrogen mustards.

Indications

Alkylating agents are indicated for the following medical conditions:

• Treatment of slow-growing cancers, like lymphomas, leukemias,

myelomas, some ovarian, testicular, and breast cancers, and
pancreatic cancers.
Here are some important aspects to remember for indication of antineoplastics
in different age groups:

Children

• Treatment of pediatric cancers follow developed antineoplastic

protocols and combination therapy is stressed to eliminate as many of
the mutant cells as possible. Checking the dosage for children is crucial
because of possible drug toxicity. In addition, the nutritional needs and
hydration status of children should be included in the considerations for
formulating a care plan.
• Even under therapy, children must be allowed to explore and learn like
any other children. They would need extra support and comfort as
body image problems, lack of energy, and risk for infection can isolate
them. Lastly, bone marrow activity should be monitored carefully and
dose should be adjusted carefully.
Adults

• Adults are also challenged with changes in body image and activities
that come with chemotherapy. It is usual for this age group to fear the
diagnosis too. Therefore, establishing a good support system is
important.
Antineoplastic agents are contraindicated to pregnant and nursing
•
women. Education, support, and referrals to appropriate specialists are
important. Women of childbearing age should use barrier
contraceptives when these drugs are being taken.
Older adults

• Older patients are more susceptible to GI and CNS adverse effects of

antineoplastic therapy, particularly those with hepatic and renal
dysfunctions. Precautions are used accordingly. Protection from
infection and injury should be the focus of nurses.

Pharmacokinetics

Here are the characteristic interactions of alkylating agents and the body in
terms of absorption, distribution, metabolism, and excretion:

Route Onset Peak Duration

Oral Varies 1h 15-20 h

Metabolism: liver
Excretion: kidney (urine)

Contraindications and Cautions

The following are contraindications and cautions for the use of alkylating agents:

• Pregnancy and lactation. Severe effects to fetus and neonate.

• Known allergy to drugs. Caution is exercised to prevent hypersensitivity
reactions.
 • Bone marrow suppression. The index for redosing and dosing levels
• Suppressed renal or hepatic function. Interfere with drug metabolism
and excretion.

Adverse Effects

Use of alkylating agents may result to these adverse effects:

• GI: nausea, vomiting, anorexia, diarrhea, and mucous membrane

deterioration, hepatic toxicity
• GU: renal toxicity,
• Hematological: bone marrow suppression
• Alopecia or hair loss

Antimetabolites

• Antimetabolites are drugs that have chemical structures similar to those

of various natural metabolites that are necessary for growth and
division of rapidly growing neoplastic cells and normal cells.

Therapeutic Action

The desired and beneficial action of antimetabolites is:

• Inhibiting DNA production in cells that depend on certain natural

metabolites to produce their DNA. They replace these needed
metabolites and thereby prevent normal cellular function.
• Inhibit thymidylate synthase, DNA polymerase, or folic acid reductase,
all of which are needed for DNA synthesis.
• They are most effective in rapidly dividing cells, preventing cell
replication, and leading to cell death.
Indications

Antimetabolites are indicated for the following medical conditions:

• Treatment of various leukemias and some GI and basal cell cancers

• Use has been somewhat limited because neoplastic cells rapidly
develop resistance to these agents. Therefore, they are commonly
administered as part of combination therapy.

Pharmacokinetics

Here are the characteristic interactions of antimetabolites and the body in terms
of absorption, distribution, metabolism, and excretion:

Route Onset Peak

Oral Varies 1-4 h

IV Rapid 0.5-2 h

Metabolism: none
Excretion: kidney (urine); unchanged

Contraindications and Cautions

The following are contraindications and cautions for the use of antimetabolites:

• Known allergy to drug. Prevent hypersensitivity reactions

• Pregnancy and lactation. Severe effects on the fetus and neonate
• Bone marrow suppression. Index of redosing and dosing levels
• Renal and hepatic dysfunction. Interfere with drug metabolism and
excretion
• Known GI ulceration or ulcerative diseases. Can be exacerbated by
the effects of the drug
Adverse Effects

Use of antimetabolites may result to these adverse effects:

• CNS: headache, drowsiness, aphasia, fatigue, malaise, dizziness

• Respiratory: pulmonary toxicity, interstitial pneumonitis
• Hematological: bone marrow suppression
• GI: nausea, vomiting, anorexia, diarrhea, mucous membrane
deterioration, hepatic toxicity
• GU: renal toxicity

Antineoplastic Antibiotics

• This group of drugs is selective for bacterial cells. However, they are also
toxic to human cells.
• They are aimed towards rapidly-multiplying cells.

Therapeutic Action

The desired and beneficial action of antineoplastics antibiotic is:

• Either breaking up DNA links or preventing DNA synthesis

• They interfere with cellular DNA synthesis by inserting themselves
between base pairs in the DNA chain. This causes a mutant DNA
molecule, leading to cell death.
Indications

Antineoplastic antibiotics are indicated for the following medical conditions:

• Treatment of various types of cancer, particularly those with rapidly-

dividing nature.
• These drugs have potentially adverse effects which limit their usefulness
in patients with pre-existing disease and those who are debilitated.

Pharmacokinetics

Here are the characteristic interactions of antineoplastic antibiotics and the

body in terms of absorption, distribution, metabolism, and excretion:

Route Onset Peak Duration

IV Rapid 2h 24-36 h

Metabolism: liver
Excretion: kidney (urine), liver (bile), colon (feces)

Contraindications and Cautions

The following are contraindications and cautions for the use of antineoplastic
antibiotics:

• Known allergy to drug. Prevent hypersensitivity reactions

• Pregnancy and lactation. Severe effects on the fetus and neonate
• Bone marrow suppression. Index of redosing and dosing levels
• Renal and hepatic dysfunction. Interfere with drug metabolism and
excretion
• Known GI ulceration or ulcerative diseases. Can be exacerbated by
the effects of the drug
• Pulmonary problems. Exacerbated by bleomycin or mitomycin
 • Cardiac problems. Exacerbated by idarubicin or mitoxantrone

Adverse Effects

Use of antineoplastic antibiotics may result to these adverse effects:

• CNS: headache, drowsiness, aphasia, fatigue, malaise, dizziness

• Respiratory: pulmonary toxicity, interstitial pneumonitis
• Hematological: bone marrow suppression
• GI: nausea, vomiting, anorexia, diarrhea, mucous membrane
deterioration, hepatic toxicity
• GU: renal toxicity
• Alopecia

Mitotic Inhibitors

• Drugs that kill cells as the process of mitosis begins.

• Mitotic inhibitors are cell cycle-specific agents that inhibit DNA
synthesis.

Therapeutic Action

The desired and beneficial action of mitotic inhibitors is:

• Interfering with the ability of the cell to divide by blocking or altering

the M phase of the cell cycle.

Indications

Mitotic inhibitors are indicated for the following medical conditions:

• Treatment of a variety of tumors and leukemias

Pharmacokinetics

Here are the characteristic interactions of mitotic inhibitors and the body in
terms of absorption, distribution, metabolism, and excretion:

Route Onset Peak

IV Varies 15-30 min

Metabolism: liver
Excretion: kidney (urine), colon (feces)

Contraindications and Cautions

The following are contraindications and cautions for the use of mitotic inhibitors:

• Known allergy to drug. Prevent hypersensitivity reactions

• Pregnancy and lactation. Severe effects on the fetus and neonate
• Bone marrow suppression. Index of redosing and dosing levels
• Renal and hepatic dysfunction. Interfere with drug metabolism and
excretion
• Known GI ulceration or ulcerative diseases. Can be exacerbated by
the effects of the drug

Adverse Effects

Use of mitotic inhibitors may result to these adverse effects:

• CNS: headache, drowsiness, aphasia, fatigue, malaise, dizziness

• Respiratory: pulmonary toxicity and interstitial pneumonitis
• Hematological: bone marrow suppression
• GI: nausea, vomiting, anorexia, diarrhea, mucous membrane
deterioration, hepatic toxicity
• GU: renal toxicity
 • Can cause necrosis and cellulitis if extravasation occurs

Hormones and Hormone Modulators

• Some cancers are sensitive to estrogen stimulation. Estrogen-receptor

sites on the tumor react with circulating estrogen, and this reaction
stimulates the tumor cells to grow and divide.
• Hormones and hormone modulators block or interfere with these
receptor sites to prevent growth of the cancer and cause cell death.
• Some hormones are used to block the release of gonadotropic
hormones in breast or prostate cancer if the tumors are responsive to
gonadotropic hormones. Others may block androgen-receptor sites
directly.

Therapeutic Action

The desired and beneficial action of hormones and hormone modulators is:

• Blocking the stimulation of growing cancer cells that are sensitive to the
presence of that hormone.

Indications

Hormones and hormone modulators are indicated for the following medical
conditions:

• Treatment of breast cancer in postmenopausal women or in other

women without ovarian function.
• Treatment of prostatic cancers that are sensitive to hormone
manipulation.
Pharmacokinetics

Here are the characteristic interactions of hormones and hormone modulators

and the body in terms of absorption, distribution, metabolism, and excretion:

Route Onset Peak

Oral Varies 4-7 h

Metabolism: liver
Excretion: colon (feces)

Contraindications and Cautions

The following are contraindications and cautions for the use of hormones and
hormone modulators:

• Known allergy to drug. Prevent hypersensitivity reactions

• Hypercalcemia.

• Pregnancy and lactation. Severe effects on the fetus and neonate

• Bone marrow suppression. Index of redosing and dosing levels
• Renal and hepatic dysfunction. Interfere with drug metabolism and
excretion
• Known GI ulceration or ulcerative diseases. Can be exacerbated by
the effects of the drug

Adverse Effects

Use of hormones and hormone modulators may result to these adverse effects:

• Menopause-associated effects: hot flashes, vaginal spotting, vaginal

dryness, moodiness, and depression
• Hematological: bone marrow suppression
 • GI: hepatic toxicity
• GU: renal toxicity

Cancer Cell-Specific Agents

• These agents are only specific to cancer cells and spare the healthy
cells its devastating effects. Patients do not experience the numerous
adverse effects associated with antineoplastic chemotherapy.
• Three groups of drugs are cancer cell-specific: protein tyrosine kinase
inhibitors, epidermal growth factor inhibitor, and proteasome inhibitor.

Therapeutic Action

The desired and beneficial action of cancer cell-specific agents is:

• Protein tyrosine kinase inhibitors act on specific enzymes that are

needed for protein building by specific tumor cells. Blocking of these
enzymes inhibits tumor cell growth and division.
• Epidermal growth factor inhibitors are drugs that act on epidermal
growth factor receptors which are found in both normal and
cancerous cells but are more abundant on the latter.
• Proteasome inhibitors are drugs indicated for inhibition of proteasome
in human cells, a large protein complex that works to maintain
cell homeostasis and protein production.

Indications

Cancer cell-specific agents are indicated for the following medical conditions:

• Imatinib, the first drug approved protein tyrosine kinase inhibitor, is

given orally and is approved to treat chronic
myelocytic leukemia (CML). It selectively inhibits the Bcr-Abl tyrosine
kinase created by the Philadelphia chromosome abnormality in CML.
• Bortezomib is used for the treatment of multiple myeloma in patients
whose disease had progressed after two standard therapies.
Pharmacokinetics

Here are the characteristic interactions of cancer cell-specific agents and the
body in terms of absorption, distribution, metabolism, and excretion:

Route Onset Peak

Oral Slow 2-4 h

Metabolism: liver
Excretion: colon (feces)

Contraindications and Cautions

The following are contraindications and cautions for the use of cancer cell-
specific agents:

• Pregnancy. All drugs in this class is pregnancy category D.

• Women of childbearing age. Must be advised to use barrier
contraceptives while taking these drugs.
• Lactation.

• Hepatic dysfunction. Increased risk of toxicity with imatinib and

pazopanib.
• Risk for prolonged QT intervals (hypokalemia, hypomagnesia, taking
drugs that can prolong QT intervals). Contraindicated with nilotinib.
• Known allergy to the drug. Prevent hypersensitivity reactions.

Adverse Effects

Use of cancer cell-specific agents may result to these adverse effects:

• Imatinib: GI upset, muscle cramps, heart failure, fluid retention, skin

rash.
 • Gefitinib: potentially severe interstitial lung disease and
various eye symptoms
• Pazopanib: some bone marrow depression, diarrhea, hypertension,
and liver impairment, change in hair color
• Lapatinib: diarrhea, liver impairment and altered heart function
• Erlotinib and bortezomib: cardiovascular events, pulmonary toxicity
• Bortezomib: peripheral neuropathy, liver and kidney impairment

Interactions

The following are drug-drug interactions involved in the use of antineoplastic

agents:

• Any drug that has potential for hepatic or renal toxicity

• Adversely affect drugs metabolized in the liver (e.g.
oral anticoagulants)
• Antineoplastic antibiotics can increase toxicity of drugs that are toxic to
the heart and lungs.
• Echinacea: increased risk of hepatotoxicity with antineoplastics
• Ginkgo: inhibits blood clotting, which can cause problems
after surgery or with bleeding neoplasms
• Saw palmetto: increase the effects of various estrogen hormones and
hormone modulators; advise patients taking such drugs to avoid this
herb
• St. John’s wort: can greatly increase photosensitivity, which can cause
problems in patient who have received radiation therapy or are taking
drugs that cause other dermatological effects. In addition, it can
decrease the effectiveness of some antineoplastic agents.
Nursing Considerations

Here are important nursing considerations when administering antineoplastic

agents:

Nursing Assessment

These are the important things the nurse should include in conducting
assessment, history taking, and examination:

• Assess for the mentioned cautions and contraindications (e.g. drug

allergies, hepatorenal impairment, bone marrow suppression,
pregnancy and lactation, etc.) to prevent any untoward
complications.
• Perform a thorough physical assessment (other medications taken,
orientation and reflexes, vital signs, bowel sounds, etc.) to establish
baseline data before drug therapy begins, to determine effectiveness
of therapy, and to evaluate for occurrence of any adverse effects
associated with drug therapy.
• Monitor result of laboratory tests such as CBC with differential to identify
possible bone marrow suppression and toxic drug effects and establish
appropriate dosing for the drug; and liver and renal function tests to
determine need for possible dose adjustment and identify toxic drug
effects.

Nursing Diagnoses

Here are some of the nursing diagnoses that can be formulated in the use of
these drugs for therapy:

• Acute pain related to GI, CNS, and skin effects of the drug
• Disturbed body image related to alopecia, skin effects, and impaired
fertility
• Anxiety related to diagnosis
• Risk for infection related to bone marrow suppression
Implementation with Rationale

These are vital nursing interventions done in patients who are taking alkylating
agents:

• Arrange for blood tests before, periodically during, and for at least 3
weeks after therapy to monitor bone marrow function to aid in
determining the need for a change in dose or discontinuation of the
drug.
• Administer medication according to scheduled protocol and in
combination with other drugs as indicated to improve effectiveness.
• Ensure that patient is well hydrated to decrease risk of renal toxicity.
• Protect the patient from infection; limit invasive procedures when bone
marrow suppression limits the patient’s immune/inflammatory
responses.
• Provide small, frequent meals, frequent mouth care, and dietary
consultation as appropriate to maintain nutrition when GI effects are
severe.
• Arrange for proper head covering at extremes of temperature if
alopecia occurs; a wig, scarf, or hat is important for maintaining body
temperature.
• Plan for rest periods because fatigue and weakness are common
effects of the drug.

Evaluation

Here are aspects of care that should be evaluated to determine effectiveness

of drug therapy:

• Monitor patient response to therapy (alleviation of cancer being

treated, palliation of signs and symptoms of cancer).
• Monitor for adverse effects (bone marrow suppression, GI toxicity,
neurotoxicity, and alopecia, renal or hepatic dysfunction).
• Evaluate patient understanding on drug therapy by asking patient to
name the drug, its indication, and adverse effects to watch for.
• Monitor patient compliance to drug therapy.