Antineoplastic Agents/Classification
Alkylating agents - Action Alter DNA structure by misreading DNA code, initiating breaks
in the DNA molecule, cross-linking DNA strands Cell cyle: nonspecific interferes with the
replication, transcription and translation of DNA S/S: Bone marrow suppression, N & V,
Cystitis, stomatitis, alopecia, gonadal suppression, renal toxicity.
Busulfan
carboplatin
chlorambucil
cisplatin- (V) aggressive prehydration 1-2liters of IV fluid is standard therapy before admin.
to prevent rental toxicity. (amifostine (Ethyol) – to reduce risk) Renal toxicity
cyclophosphamide - cystitis
dacarbazine
hexamethyl melamine,
ifosfamide – Bladder Toxicity - Mesna is admin with to reduce risk
melphalan
nitrogen mustard - (V)
oxaliplatin
thiotepa
Nitrosureas Action Similar to the alkylating agents; cross the blood –brain barrier. Cell
Cycle nonspecific S/S: Delayed and cumulative myelosuppression, especially
thrombocytopenia; N & V
Carmustine
lomustine
semustine,
streptozocin
Mitotic spindle poisons(V) Action Plant alkaloids. Arrest metaphase by inhibiting mitotic
tubular formation (spindle); inhibit DNA and prtein synthesis Cell cycle-specific (M phase)
Inhibits mitosis by interfering with the mitotic spindle.
S/S: bone marrow suppression (mild with VCR), neuropathies (VCR), stomatitis.
Bradycardia, hypersensitivity reactions, bone marrow suppression, alopecia, neuropathies
vinblastine,
VinCRistine – (V) does not have bone marrow suppression but exhibits a dose-limiting
neurotxicity.
Apply warm/moist compresses for extravasations from vinca alkaloids. (normally
cold/moist)
Misc: Action Unknown or too complex to categorize Cell cycle - varying
S/S:Varies: Anorexia, nausea, vomiting, bone marrow suppression, hepatotoxicity,
anaphylaxis, hypotension, altered glucose metabolism
Asparaginase
Neupogen –stimulates platelet production
Epogen - stimulate erythrocyte production
Hormonal agents Action Bind to hormone receptor sites that alter cellular growth; block
binding of estrogens to receptor sites (anti-estrogens); inhibit RNA synthesis; suppress
aromatase of P450 system, which decreases estrogen level. Cell cycle non-specific
Used in a number of cancers, but most often used in cancers with receptors for estrogens
or adrogens.
S/S: Hypercalcemia, jaundice, increased appetite, masculinization, feminization, sodium &
fluid retention, N&V, hot flashes, vaginal dryness
Androgens and anti-androgens, estrogens and anti-estrogens, progestins and antiprogestins, aromatase inhibitors
luteinizing hormone
steroids
Antimetbolites Action Interfere with the biosynthesis of metabolites or nucleic acids
necessary for RNA and DNA synthesis . Cell cyle-specific (S Phase)
S/S: N & V , diarrhea, bone marrow suppression, proctitus stomatitis, renal toxicity,
hepatotoxicity
5-Azacytadine
capecitabine
cytararbine
edatrexate fludarabine
5-fluorouracil,
hydroxyurea,
methotrexate, pentostatin
Topoisomerase I Inhibitors Action Induces breaks in the DNA strand by binding to
enzyme topoisomerase I, preventing cells from dividing . Cell cycle-specific S Phase
(McKenry says G2 Phase)
S/S: bone marrow suppression, diarrhea, nausea, vomiting hepatotoxicity.
Irinotecan, topotecan
Antitumor antibiotics (V) Action Interfere with DNA synthesis by binding DNA; prevent
RNA synthesis . Cell cycle – nonspecific
S/S: bone marrow suppression, N & V, alopecia, anorexia, cardiac toxicity
Bleomycin,
doxorubicin (V) Cardiac Toxicity Cumulative lifetime dose limit of 550 mg. (Dexrazoxane to
help prevent)
mitomycin - (V)
mitoxantrone
Dosage - based on
 pts total body surface area
 previous response to chemo or rad therapy
 function of major organ systems
are determined to maximize cell kill while minimizing impact on healthy tissues and
subsequent toxicities.
Labs: Hematologic, hepatic, renal, cardiovascular, pulmonary systems
Dose-limiting effects are adverse effects that prevent a drug from being administered in
higher doses tor that indicate caution in continuing to administer the drug at the current
dosage. Prednisone does not demonstrate bone marrow suppression or neurtotoixcity.
(V) - vesicant
if extravasation is suspected, the med admin is stopped immediately and dependent upon
drug – an attempt to aspirate any remaining through existing needle. application of heat /
cold dependent upon drug.
cytoprotectant - amifostine (Ethyol) – scavenger of free radicals that prevents damage to DNA.
Protects normal tissue from radiation damage