Alkylating agents 2

Question 1

Severe myelosuppression (in
almost all cases), pulmonary
fibrosis, hyperpigmentation

Cross-links DNA

Answer 1

Busulfan

Question 2

Myelosuppression, SIADH,
Fanconi syndrome
(ifosfamide), hemorrhagic
cystitis and bladder cancer
(prevent with mesna)

Cross-link DNA
Require bioactivation by liver

Answer 2

Nitrogen mustards
Cyclophosphamide,
ifosfamide

Question 3

CNS toxicity (convulsions,
dizziness, ataxia)

Cross-link DNA
Require bioactivation by liver
Cross blood-brain barrier
Ž CNS entry

Answer 3

Nitrosoureas
Carmustine, lomustine

Question 4

Myelosuppression, pulmonary
toxicity, leukemia, disulfiramlike reaction

Mechanism unknown
Weak MAO inhibitor

Answer 4

Procarbazine

Question 5

Myelosuppression

DNA methylation

Answer 5

Temozolomide

Question 6

Nephrotoxicity (eg, Fanconi syndrome; prevent with amifostine), peripheral neuropathy, ototoxicity.

Cross-link DNA. Cell cycle nonspecific

Answer 6

Platinum compounds Cisplatin, carboplatin, oxaliplatin.

Question 7

Myelosuppression, neuropathy,
hypersensitivity

Hyperstabilize polymerized
microtubules Ž prevent
mitotic spindle breakdown.

Answer 7

Taxanes
Docetaxel, paclitaxel

Question 8

Vincristine (crisps the nerves):
neurotoxicity (axonal neuropathy), constipation
(including ileus) Vinblastine (blasts the

marrow): myelosuppression Bind β-tubulin and inhibit
its polymerization into microtubules Ž prevent mitotic spindle formation

Answer 8

Vinca alkaloids
Vincristine, vinblastine

Question 9

Severe myelosuppression,
diarrhea
Inhibit topoisomerase I

Answer 9

Irinotecan, topotecan

Question 10

Myelosuppression, alopecia

Inhibit topoisomerase II

Answer 10

Etoposide, teniposide

Question 11

Hot flashes,  risk of thromboembolic events (eg, DVT, PE) and endometrial cancer

Selective estrogen receptor modulator with complex mode of action: antagonist in breast tissue,
partial agonist in endometrium and bone. Blocks the binding of estrogen to ER in ER ⊕ cells.

Answer 11

Tamoxifen