B / 30 : Drugs Used In Cancer Treatment II (Alkylating Agents)

Question 1

What is alkylation?

Answer 1

An alkyl group (C and H atoms) is transferred in exchange for an H atom

Question 2

How do alkylating agents exert their cytotoxic effects?

Answer 2

By binding to nucleophilic groups and causing cross links which damage the DNA

Question 3

What are the alkylating agents? (6)

Answer 3

• Cyclophosphamide
• Dacarbazine
• Temozolomide
• Cisplatin + oxiplatin
• Dactinomycin
• Bleomycin

Question 4

Cyclophosphamide
- Indication
- ROA

Answer 4

• For breast, ovarian, SCLC cancers, lymphomas, leukemias
• Oral, parenteral

Question 5

Indications of Dacarbazine

Answer 5

For malignant melanoma, hodgkin lymphoma

Question 6

Indications of Temozolomide

Answer 6

For CNS tumors (temoZOOlomide)

Question 7

What are the SE of alkylating agents?

Answer 7

• BM suppression
• Alopecia
• GI disturbances
• Pulmonary toxicity (Bleomycin)

Question 8

When do alkylating agents have the best action?

Answer 8

They are CCNS : cell cycle non specific - so they can act at all moments (except Bleomycin : G2)

Question 9

What are the platinum alkylators?

Answer 9

Cisplatin + oxaliplatin

Question 10

Cisplatin + Oxalipaltin
- MOA, effect
- Indications

Answer 10

• Platinum-based alkylating agent : acts on N7 guanine
• For ovarian, testicular, bladder and lung cancers + colorectal cancers

Question 11

What are the antibiotics that act as alkylating agents?

Answer 11

• Dactinomycin
• Bleomycin

Question 12

Dactinomycin
- MOA
- Effect
- Indication

Answer 12

• Antitumor antibiotic
• Inhibits DNA-dependent RNA polymerase
• Testicular cancer, Wilm’s tumor, rhabdomyosarcoma
  (Daredevil : daring act - d-act-inomycin)

Question 13

Bleomycin
- MOA
- Effect
- Indication
- SE

Answer 13

• Antitumor antibiotic
• Contains DNA and iron binding region : forms complexes and causes free radical formation : DNA breaks
• For Hodgkin and non Hodgkin lymphomas, testicular cancer
• Pulmonary toxicity (fibrosis)