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Focus on
PHARMACOLOGY
ESSENTIALS FOR HEALTH PROFESSIONALS
CHAPTER
16
Antineoplastic
Agents
Cancer
• Second most common cause of death in
United States
– Most common types: breast, prostate,
lung, colorectal
– Characterized by uncontrolled cellular
division, hyperplasia, local tissue invasion,
and metastasis
– Two types of tumor: benign and malignant
Focus on Pharmacology: Essentials for Health Professionals, Second Edition
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Naming Benign and
Malignant Tumors
• Benign tumors: names are created by
adding –oma to name of cell type
– Adenoma: benign tumor of glandular origin
• Malignant: names often contain word
carcinoma
– Adenocarcinoma: malignant cancer of
glandular origin
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Benign Tumors
• Benign: cells resemble cells from which
they developed
– Slow growing
– Seldom metastasize; rarely recur once
removed
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Malignant Tumors
• Malignant: atypical appearance
– Proliferate rapidly; become more and more
atypical
– Invade and destroy surrounding tissues
– Induce formation of new blood vessels
(angiogenesis) to supply tumor with blood
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Malignant Cancer Terms
• Sarcoma: malignant growth of muscle
or connective tissue
• Carcinoma in situ: cancer limited to
epithelial cells where it begins
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7 Warning Signs of Cancer
Change in bowel or bladder habits
Sore that does not heal
Unusual bleeding or discharge
Thickening or lump in breast or
elsewhere
• Indigestion or difficulty swallowing
• Obvious change in wart or mole
• Nagging cough or hoarseness
•
•
•
•
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Topic of Cancer
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Neoplasms
• Arise from four tissue types
– Epithelial
– Connective
– Muscle
– Nerve
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Oncogenes
• Develop from normal genes: protooncogenes
– Protooncogenes are present in all cells and
regulate normal cell function, including cell
cycle.
– Genetic alteration of the protooncogene
may activate oncogenes.
– Alteration caused by carcinogenic agents.
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Tumor Suppressor Genes
• Normally function to regulate and
inhibit inappropriate cellular growth and
proliferation
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Cell Cycle
• G0: Resting, dormant stage
• G1: Cell makes proteins to prepare for
division (18–30 hours)
• S: DNA synthesis occurs (18–20 hours)
• G2: Occurs just before cell splits (2–10
hours)
• M: Mitosis (30–60 minutes)
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Figure 16-1
The four steps of the cell cycle.
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Chemotherapy
• Use of chemical agents to interact with
cancer cells to stop or control growth
– Primary: used alone to cure
– Palliative: used to ease disease’s effects
– Adjuvant: used before or after radiation or
surgery
– Neoadjuvant: given in preoperative setting
to reduce tissue damage, decrease tumor
size, or destroy micro metastases
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Chemotherapy Agents
• Characterized by mechanism of action
or origin
• Many agents target rapidly proliferating
cells at selective or multiple sites of cell
cycle.
– Agents with selective activity: cell cycle
phase-specific
• Agents may target cellular synthesis of
DNA, RNA, and proteins.
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Five Primary Cancer Therapies
• Surgery: treatment of choice for many
solid tumors; local treatment
• Radiation therapy: local treatment
• Chemotherapy: systemic treatment
• Immunotherapy: stimulates host’s
immune system
• Hormonal therapy: systemic treatment
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Response to Treatment
• Cure: free of disease
• Complete response: disappearance of
cancer with no evidence of new disease
for at least 1 month after treatment
• Partial response: 50% or greater
decrease in tumor size or other cancer
markers; no evidence of disease for at
least 1 month
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Response to Treatment
• Stable disease: no change in tumor size
• Progression of disease
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Chemotherapy
Routes of Administration
• Oral: becoming more popular because
of ease of use
• Intramuscular
• Subcutaneous
• Intravenous
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Alkylating Agents: Uses
• Greatest value in treating slow-growing
cancers
• Cell cycle phase–nonspecific: act
directly on DNA causing cross-linking of
DNA strands, abnormal base pairing, or
strand breaks
• Five types: nitrogen mustards,
ethyleneimines, alkyl sulfonates,
nitrosoureas, temozolomide
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Alkylating Agents:
Adverse Effects
• Dose-limiting toxicity to bone marrow
and intestinal mucosa
• Common: alopecia, toxicity to
reproductive system
• Serious: pulmonary fibrosis and
venoocclusive liver disease, renal
failure, central neurotoxicity
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Alkylating Agents:
Contraindications
• Do not use in pregnancy (teratogenic).
• May interact with antidepressants,
other anticancer medication, warfarin,
vaccines, aspirin, and vitamins
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Procarbazine Interactions
• Procarbazine can produce an acute
disulfiram-like reaction (flushing,
headache, acute vomiting, and chest or
abdominal pain) if combined with
alcohol.
• Taking procarbazine with tyraminecontaining foods (aged cheese,
chocolate, wine, etc.) can cause lifethreatening elevation of blood pressure.
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Alkylating Agents:
Patient Information
• Teach patients about symptoms and
signs of bone-marrow depression.
• Advise patients to avoid contact with
people who have colds or other
infections.
• Reassure patients that hair will regrow
after treatment.
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Antimetabolites: Uses
• Cell cycle phase–specific: replace
natural substances such as DNA
molecules that are required for cell
metabolism and protein synthesis
• Treat myelocytic leukemia, lymphocytic
leukemia, non-Hodgkin’s lymphoma,
metastatic breast and colorectal cancer,
keratoses, basal cell carcinomas,
meningeal leukemia, head and neck
cancers
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Antimetabolites:
Adverse Effects
• Common: anorexia, nausea and
vomiting, headache, hearing loss, sleep
disorders, depression, bone-marrow
depression, dyspnea, epistaxis, edema,
GI disturbances, alopecia,
myelosuppression, hyperuricemia
• Serious: hepatotoxicity, severe
leukopenia, bone marrow aplasia,
thrombocytopenia
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Antimetabolites:
Contraindications
• Avoid in first trimester of pregnancy; in
lactating women; and in patients with
acute infectious diseases, severe bonemarrow depression, and renal
dysfunction
• Interact with allopurinol, warfarin, and
drugs used to treat ulcerative colitis
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Antimetabolites:
Patient Information
• Advise patients that these drugs may
cause bone-marrow suppression and
damage to GI lining.
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Green Tea: Antioxidant
• Studies suggest green tea may reduce
the incidence of a variety of cancers,
including those of the colon, pancreas,
and stomach.
• Green tea contains high levels of
polyphenols, which have antioxidant
and chemopreventive properties.
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Table 16-1
Common Agents Used in the Treatment of Cancer
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Table 16-1 (continued) Common Agents Used in the Treatment of Cancer
Focus on Pharmacology: Essentials for Health Professionals, Second Edition
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Table 16-1 (continued) Common Agents Used in the Treatment of Cancer
Focus on Pharmacology: Essentials for Health Professionals, Second Edition
Jahangir Moini
Table 16-1 (continued) Common Agents Used in the Treatment of Cancer
Focus on Pharmacology: Essentials for Health Professionals, Second Edition
Jahangir Moini
Table 16-1 (continued) Common Agents Used in the Treatment of Cancer
Focus on Pharmacology: Essentials for Health Professionals, Second Edition
Jahangir Moini
Table 16-1 (continued) Common Agents Used in the Treatment of Cancer
Focus on Pharmacology: Essentials for Health Professionals, Second Edition
Jahangir Moini
Table 16-1 (continued) Common Agents Used in the Treatment of Cancer
Focus on Pharmacology: Essentials for Health Professionals, Second Edition
Jahangir Moini
Mitotic Inhibitors: Uses
• More effective in S- and M-phases of
cell cycle
• Inhibit DNA and RNA synthesis
• Used to treat breast, bladder, ovarian,
testicular, and lung cancers; leukemias;
and lymphomas
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Mitotic Inhibitors: Adverse Effects
• Common: nausea and vomiting,
diarrhea, alopecia, dizziness, weakness,
headache, depression, stomatitis,
anemia, hyperpigmentation of nails,
tongue, or oral mucosa
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Mitotic Inhibitors:
Contraindications
• Do not use in severe cardiac disease,
hypocalcemia, bleeding disorders,
myelosuppression, or pregnancy.
• Interact with phenytoin, erythromycin,
and itraconazole
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Mitotic Inhibitors:
Patient Information
• Tell patients that severe bone-marrow
depression and GI damage may occur.
• Tell them to avoid coffee, spicy foods,
fruits, and raw vegetables if diarrhea
occurs.
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Toxicity in Elderly Patients
• Older adults are at higher risk for
adverse effects of antineoplastic
agents.
• Lower dosages are administered.
• Creatinine clearance is used to monitor
renal function in elderly patients.
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Hormonal Therapy: Uses
• Act by blocking hormone production or
action
• Highly selective
• Treat acute lymphocytic leukemia and
reproductive tract cancers
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Hormonal Therapy:
Adverse Effects
• GI disturbances
• Impaired fertility
• Menstrual irregularities
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Hormonal Therapy:
Contraindications
• Most hormones are contraindicated
during pregnancy.
• Interactions occur with tamoxifen,
alcohol, St. John’s wort, zinc,
magnesium, vitamin B, and thyroid
supplements.
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Hormonal Therapy:
Patient Information
• Warn patients that these agents are
contraindicated in pregnancy and that
strict contraception should be used
during and for 3–4 months after
treatment.
• Some sources advise both men and
women to avoid conceiving for 2 years
after treatment.
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Infertility
• Instruct patients that infertility may
occur with antineoplastic agents and
may not be reversible.
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Antitumor Antibiotics: Uses
• Work by inhibiting DNA and RNA
synthesis
• Treat breast, ovary, testicular, cervical,
head, neck, penis, and bone cancers;
Wilms’ tumor, choriocarcinoma, solid
tumors, monocytic leukemia,
lymphoblastic and myeloblastic
leukemias, and lymphomas
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Antitumor Antibiotics:
Adverse Effects
• Common: bone-marrow suppression,
stomatitis, GI upset, alopecia,
pulmonary fibrosis
• Serious: renal impairment (mitomycin)
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Antitumor Antibiotics:
Contraindications
• Should not be used in patients with
heart, kidney, and liver disease
• Some agents interact with digoxin,
aspirin, heparin, warfarin, or NSAIDs.
• Some agents cause toxicity when used
together.
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Antitumor Antibiotics:
Patient Information
• Advise patients about signs and
symptoms of bone-marrow depression.
• Instruct patients to report cardiac
abnormalities.
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Interferon alfa-2b
(Intron A): Uses
• Work by targeting and purifying specific
proteins
• Treats kidney cancers, lymphoma, and
melanoma
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Interferon alfa-2b:
Adverse Effects
• Common: nausea and vomiting, weight
gain, fluid retention
• Serious: kidney, liver, lung, and nerve
damage
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Interferon alfa-2b:
Contraindications
• Safe use during pregnancy, lactation,
or in children younger than 18 is not
established.
• Use cautiously in severe, preexisting
cardiac, renal, or hepatic disease,
pulmonary disease, diabetes mellitus,
or those prone to ketoacidosis.
• Interacts with theophylline and
zidovudine
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Interferon alfa-2b:
Patient Information
• Teach patients how to reconstitute and
administer these agents.
• Warn patients not to change brands.
• Advise woman not to breast feed.
• Instruct patients to expect adverse
effects and to report severe adverse
effects.
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Interferon Administration
• All changes in interferon administration
must be directed by a physician.
• Instruct patients to not change
administration times or doses of these
drugs.
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