Chemotherapy Drugs

Front 1

methotrexate

Back 1

inhibits formation of thymine. folate analog that inhibits dihydrofolate reductase. S-phase specific antimetabolite.

toxicity: myelosuppression (reversible with leucovorin a.k.a. folinic acid), macrovesicular fatty change in liver

Front 2

5-fluoruracil (5-FU)

Back 2

inhibits formation of thymine. pyrimidine analog bioactivated to 5F-dUMP which covalently complexes folic acid (CH2-THF). complex inhibits thymidilate synthase.

toxicity: myelosuppression (NOT reversible by leucovorin), photosensitivity. can rescue with thymidine

Front 3

6-mercaptopurine (6-MP)

Back 3

blocks de novo purine synthesis. activated by HGPRTase.

Toxicity:
BM toxicity, GI tox, liver tox. toxicity enhanced by allopurinol since both are metabolized by xanthine oxidase

Front 4

cytarabine (ara-C)

Back 4

inhibits DNA polymerase.

toxicity: leukopenia, thrombocytopenia, megaloblastic anemia

Front 5

cyclophosphamide

Back 5

alkylating agent. covalently x-link DNA strands at guanine N-7. bioactivated in liver

toxicity: myelosuppression, hemorrhagic cystitis (prevented partially by mesna which binds toxic metabolites through its sulfhydryl groups)

Front 6

carmustine

Back 6

nitrosoureas. alkylate DNA. require bioactivation. cross BBB -> CNS. CNS toxicity (dizziness, ataxia)

Front 7

lomustine

Back 7

nitrosoureas. alkylate DNA. require bioactivation. cross BBB -> CNS. CNS toxicity (dizziness, ataxia)

Front 8

semustine

Back 8

nitrosoureas. alkylate DNA. require bioactivation. cross BBB -> CNS

toxicity: CNS (dizziness, ataxia)

Front 9

streptozocin

Back 9

nitrosoureas. alkylate DNA. require bioactivation. cross BBB -> CNS. CNS toxicity (dizziness, ataxia)

Front 10

cisplatin, carabplatin

Back 10

alkylating agent.

toxicity: nephrotoxicity and acoustic nerve damage.

Front 11

busulfan

Back 11

alkylating agent

toxicity: pulmonary fibrosis, hyperpigmentation

Front 12

doxorubicin

Back 12

make free radicals and noncovalently intercalate in DNA. make breaks in strand to decrease replication.

toxicity: cardiotoxicity (dialated cardiomyopathy), myelosuppression, marked alopecia

Front 13

dactinomycin

Back 13

intercalates in DNA inhibiting txn. myelosuppression

toxicity: myelosuppression

Front 14

bleomycin

Back 14

induces free radicals which cause breaks in DNA strands.

toxicity: pulmonary fibrosis, skin changes, NOT much myelosuppression

Front 15

hydroxyurea

Back 15

inhibits ribonucleotide reductase -> decreased DNA synthesis (s-phase specific)

bone marrow suppression, GI upset

Front 16

etoposide (VP-16)

Back 16

inhibits topoisomerase II increasing DNA degredation

toxicity: myelosuppression, GI irritation, alopecia

Front 17

prednisone

Back 17

may trigger apoptosis. even on nondividing cells

toxicity:
cushings, hyperglycemia, immunosuppression, cataracts, acne, osteoporosis, peptic ulcers, hyperglycemia, psychosis

Front 18

tamoxifen, raloxifene

Back 18

receptor antagonists in breast, agonists in bone. block binding of estrogen to estrogen receptor-positive cells

Front 19

trastuzumab

Back 19

monoclonal Ab against HER2. Kills breast cancer cells that over express HER 2 through ADCC

toxicity: cardiotoxicity

Front 20

imantinib

Back 20

(gleevec). Abl tyrosine kinase inhibitor. inhibits Bcr-Abl tyrosine kinase in CML

Toxicity: fluid retention

Front 21

vincristine, vinblastin

Back 21

alkaloids that bind to tubulin and block polymerization of microtubules so that mitotic spindle cannot form

toxicity:
vincristine = neurotoxicity, paralytic ileus
vinblastin = bone marrow suppression

Front 22

paclitaxel

Back 22

bind tubulin and hyperstabilize polymerized microtubules so that mitotic spindle cannot break down (no anaphase)

toxicity: myelosuppression and hypersensitivity