B/33. Cancer Chemotherapy II (alkylating Agents)

Question 1

Drugs need to know in this topic

Answer 1

Cyclophosphamide (nitrogen mustard)

Platinum based
Cisplatin
Oxaliplatin

Dacarbazine
Temozolomide

Antitumor antibiotics
Bleomycin
Dactinomycin

Question 2

Alkylating agents

Answer 2

Akylation of DNA

Cytotoxic reaction that is lethal to the tumor cells

Question 3

Alkylating agents

Common SEs

Answer 3

Depress bone marrow function; Aplatic anemia
Leukemia
Hair loss
GI disturbances
Infertility
Teratogenic

Question 4

Cyclophosphamide

Answer 4

CCNS
Requires hepatic P450 activation (Prodrug)
Alkylating agent->attacts guanin N7, resulting in dysfuctional DNA
Classified chemically as nitrogen mustard

Oral/parenteral

1. Solid tumor: Breast, Ovarian cancer
2. Non-Hodgkin lymphoma
3. Leukemia
4. Multiple sclerosis
5. Immunoablative
   Small vessel vasulitis; granulomatosis w/ polyangitis, microscopic angitis
   Medium vessel vasculitis; polyangitis nodosa

Nausea, vomiting, Myelosuppression
Hemorrhagic cystitis (due to acrolein); cured byt fluid intake, sulfhydryl donor (Mensa, sodium 2-mercaptoethane sulfonade)
SIADH; water retention, euvolemic hyponatremia

Question 5

Cisplatin

Answer 5

CCNS
Platinum based anticancer agent (platins)
Cross links DNA strands

IV administration
Kidney elimination

Testicular, Bladder, Ovarian, Lung, cervical cancer, osteosarcoma

Nausea, vomiting (severe; prevented by antiemetic, Ondansetron)
Nephrotoxicity (can be prevented by Amifostine which is free radical scavenger and saline infusions or mannitol)
Neurotoxicity (Ototoxicity;tinnitus, hearing loss and peripheral)
Mild myelosuppression

Question 6

Oxalipatin

Answer 6

CCNS
Paltinum-based anticancer agent
Cross-links DNA strands

Colon cancer (Advanced stage)
Heptobiliary, pancreatic, ovarian carcinoma
Lymphoma 

Similar SEs but less toxic than cisplatin
Nausea, vomiting (severe; prevented by antiemetic, Ondansetron)
Nephrotoxicity (can be prevented by Amifostine which is free radical scavenger and saline infusions or mannitol)
Neurotoxicity (Ototoxicity;tinnitus, hearing loss and peripheral)
Mild myelosuppression

Question 7

Dacarbazine

Answer 7

CCNS
Required hepatic P450 activation

Hodgkin lymphoma
Melanoma

Nausea, Vomiting
Alopecia, skin rash, photosensitivity
Myelosuppression

Question 8

Temozolomide

Answer 8

CCNS
Prodrug; Activation in physiologic pH

CNS tumor

Nausea, Vomiting
Myelosuppression

Question 9

bleomycin

Answer 9

Antitumor, antibiotics
CCS(G2 phase)
Complexes with fe and O2->free radicals->oxidize DNA bases-> stop DNA replication
Inactivated by hydrolase
Low hydrolase enzyme in lung and tissue (related to SEs)

Hodgkin lymphoma
Testicular cancer
Squamous cell carcinoma

Pulmonary fibrosis, pneumonitis (Lung symptoms)
Skin rash, exfoliation, hyperpigmentation (Skin symptoms)
Minimal myelosuppression
Mucocutaneous reactions (alopecia, mucocitis)

Question 10

Dactinomycin

Answer 10

(Actinomycin-D)

Antitumor, antibiotics
CCNS
Inhibits DNA depedent RNA polymerase via intercalation btw DNA base pairs
generate free radical

Pediatric tumor (Wilm’s tumor, Ewing’s sarcoma, Rhabdomyosarcoma)

Nausea, Vomiting
Myelosuppression
Alopecia