Antineoplastic agents

Question 1

Cyclophosphamide

Answer 1

Alkilating, Nitrogen mustard
Produg activated by P450, IV/oral, wide use esp solid tumors or immunosup
tox: SIADH, and HEMORRHAGIC CYSTITIS (toxic met: acrolein)-> tx w/ MESNA, hydration.

Question 2

Ifosfamide

Answer 2

alkylating agent, nitrogen mustard

similar to cyclophosphamide

Question 3

Chlorambucil

Answer 3

alkylating agent, nitrogen mustard

CLL

Question 4

Thiotepa

Answer 4

alkylating agent, mustard nitrogen

Bladder Ca

Question 5

Benadmustine

Answer 5

alkylating agent, nitrogen mustard

CLL, non-Hodgkin

Question 6

Busulfan

Answer 6

Alkylating agent
CML
Tox: hyperuricemia -> tx w/ allopurinol

Question 7

Carmustine

Answer 7

Nitrosurea, bifunctional alkylating agent (inhibits DNA/RNA synth)
Lipid soluble: brain tumors, lymphoma, mltp myeloma
Profound MYELOSUPPRESSION, pulm/renal tox

Question 8

Lomustine

Answer 8

Nitrosurea, bifunctional alkylating agent (inhibits DNA/RNA synth)
Lipid soluble: brain tumors, melanoma, GI
Profound MYELOSUPPRESSION, pulm/renal tox

Question 9

Streptozocin

Answer 9

Nitrosurea, bifunctional alkylating agent (inhibits DNA/RNA synth)
Pancreatic B-cell Ca
No myelosuppression

Question 10

Dacarbazine

Answer 10

Alkylating agent, acts via DNA crosslinking
Activated by P450, IV, not cell cycle specific
Hodgkin’s, malignant melanoma, sarcomas
Q x28d

Question 11

Temozolomide

Answer 11

Alkylating agent, DNA crosslinking

gliomas, astrocytomas

Question 12

Procarbazine

Answer 12

Alkylating agent, DNA crosslinking
Hodgkin’s/non-Hodgkin’s, brain tumors
metabolite is MAOI

Question 13

Cisplatin

Carboplatin
Oxaliplatin

Answer 13

Bifunctional alkylating agent, causes inter-intra strand DNA crosslinking
most effective in S phase, sensitizes cells to radiation
for TESTICULAR CANCER, solid tumors, varied
tox: nephrotoxicity (tx w/ amifostine), ACOUSTIC N. damage

Question 14

Methotrexate

Answer 14

Anti-metabolite, inhibits dihydrofolate reductase
High dose for cancer, low dose for immunosupp
Leucovorin reduces tox/rescue
Tox: nephro, hepato, pulm infiltrates, teratogenic

Question 15

Pemetrexed

Answer 15

Antimetabolite, Inhibits thymidylate synthase, similar to methotrexate
for mesothelioma, non-small cell lung Ca (+cisplatin)
Tox: BM supp, HAND-FOOT SYNDROME, teratogenic

Question 16

6-Mercaptopurine

Answer 16

Purine analog/anti-metabolite, inhib nt synth/metabolism, must be converted by HGPRT (dec in resistance), met by xanthine oxidase
breakdown blocked by allopurinol (reduce dose)
Use: leukemia
Tox: gradual BM depression, jaundice, hyperuricemia (tx w/ allopurinol)
Pro-drug: azathioprine- immunosupp

Question 17

Thioguanine
Pentostatin
Cladribine
Fludarabine

Answer 17

Similar to 6-Mercaptopurine: purine analog, antimetabolite, inhib nt synth/met
not affected by allopurinol
Use: AML, hairy cell leukemia
Tox: BM depression

Question 18

5-Fluorouracil

Answer 18

Antimetabolite, nt analog. binds thymidylate synthase. G1,S phase
requires folic acid (inc effect w/ Leucovorin)
Use: wide (solid tumors), topical- basal cell Ca, DOC: colorectal Ca (w/ leucovorin)
Tox: Ulceration, BM depression

Question 19

Capecitabine

Answer 19

Antimetabolite, generates 5-fluorouracil in tumor (more selective)
Use: metastatic breast, colorectal
Tox: no alopecia, less BM depression and ulceration.

Question 20

Cytarabine

Answer 20

Antimetabolite, inhibits DNA polymerase, S phase specific
Use: AML, ALL
Tox: BM depression, severe LEUKOPENIA, anemia, thrombocytopenia.

Question 21

Gemcitabine

Answer 21

Antimetabolite, inhibits DNA polymerase

Use: advanced PANCREATIC Ca

Question 22

Hydroxyurea

Answer 22

Antimetabolite, S phase, oral
inc senstivity to radiation
Use: CML
Tox: Radiation recall (hyperpigmentation)

Question 23

Mechlorethamine

Answer 23

Alkylating, Nitrogen mustard
Most effective G1-M phase
Part of MOPP regimen Hodgkin disease
Tox: VESICANT, hematologic, HYPERURICEMIA ->renal damage (tx w/ allopurinol), N/V, sterility, teratogenic