Antineoplastic Agents

Drug Class and Mechanism of Cell Cycle Common Side

Examples Action Specificity Effects
Alkylating Agents Alter DNA structure Cell cycle- Bone marrow
>Busulfan, by misreading DNA nonspecific suppression,
carboplatin, code, initiating vomiting, cystitis
chlorambucil, breaks in the DNA (cyclophosphamide,
cisplatin, molecule, cross- ifosfamide),
cyclophosphamide, linking DNA strands stomatitis, alopecia,
dacarbazine, gonadal
hexamethul, suppression, renal
melamine, toxicity (cisplatin)
ifosfamide,
melphalan, nitrogen
mustard, oxaliplatin,
thiotepa
Nitrosureas Similar to alkylating Cell cycle- Delayed and
>Carmustine agents; cross the nonspecific cumulative
(BCNU), lomustine blood-brain barrier myelosuppression,
(CCNU), semustine especially
(methylCCNU), thrombocytopenia;
streptozocin nausea, vomiting
Topoisomerase I Induce breaks in Cell cycle-specific Bone marrow
Inhibitors the DNA strand by (S Phase) suppression,
>Irinotecan, binding to diarrhea, nausea,
topotecan topoisomerase I, vomiting,
preventing cells hepatotoxicity
from dividing

Pharmacology lecture notes by najarrieta

Antimetabolites Interfere with the Cell cycle-specific Nausea, vomiting,
>5-Azacytadine, biosynthesis of (S phase) diarrhea, bone
capecitabine metabolites or marrow
(Xeloda), nucleic acids suppression,
cytarabine, necessary for RNA proctitis, stomatitis,
edatrexate and DNA synthesis renal toxicity
fludarabine, 5- (methotrexate),
flourouracil (5-FU), hepatotoxicity
FUDR, gemcitabine,
hydroxyurea,
leustatin, 6-
mercaptopurine,
methotrexate,
pentostatin, 6-
thioguanine
Antitumor Interfere with DNA Cell cycle- Bone marrow
Antibiotics synthesis by nonspecific suppression,
>Bleomycin, binding DNA; nausea, vomiting,
dactinomycin, prevent RNA alopecia, anorexia,
daunorubicin, synthesis cardiac toxicity
doxorubicin (daunorubicin,
(Adriamycin), doxorubicin)
idarubicin,
mitomycin,
mitoxantrone,
plicamycin
Mitotic Spindle
Poisons
>Plant alkaloids: Arrest metaphase Cell cycle-specific Bone marrow
etoposide, by inhibiting tubular (M Phase) suppression (mild
teniposide, formation; inhibit with VCR)
vinblastine, DNA and protein neuropathies
vincristine (VCR), synthesis (VCR), stomatitis
vindesine,
vinorelbine
>Taxanes: Arrest metaphase Cell cycle-specific Bradycardia,
paclitaxel, docetaxel by inhibiting tubulin (M Phase) hypersensitivity
depolymerization reactions, bone
marrow
suppression,
alopecia,
neuropathies

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Hormonal Agents Bind to hormone Cell cycle- Hypercalcemia,
>Androgens and receptor sites that nonspecific jaundice, increased
antiandrogens, alter cellular appetite,
estrogens and growth; block masculinization,
antiestrogens, binding of feminization,
progestins and estrogens to sodium and fluid
antiprogestins, receptor sites retention, nausea,
aromatase (antiestrogens); vomiting, hot
inhibitors, luteinizing inhibit RNA flashes, vaginal
hormone-releasing synthesis; suppress dryness
hormone analogues, aromatase of P450
steroids system, which
decrease estrogen
level
Miscellaneous Unknown or too Varies Anorexia, nausea,
Agents complex to vomiting, bone
>Asparaginase categorize marrow
suppression,
hepatotoxicity,
anaphylaxis,
hypotension,
altered glucose
metabolism

Pharmacology lecture notes by najarrieta