Alkylating agents

Question 1

Name the 3 drugs in the nitrogen mustard class…

Answer 1

Mechlorethamine
Cyclophosphamide
Ifosfamide

Question 2

Produce strong electrophiles through carbonic or ethyleneimonium ion intermediates–> covalently bond via alkylation of nucleophilic moieties in DNA

Answer 2

Alkylating agents

Question 3

Name the alkylating agent that spontaneously converts to active metabolites in body fluids or enzymatically converts in the liver…

Answer 3

Mechlorethamine

Question 4

Which 2 alkylating agent converts by hepatic cytochrome P450 to active metabolite phosphoramide mustard?

Answer 4

Cyclophosphamide and Ifosfamide

Question 5

Name the 2 Nitrosoureas alkylating agents…

Answer 5

Carmustine

Lomustine

Question 6

Alkylating agent used for the treatment of Hodgkin’s disease, T-cell lymphoma…

Answer 6

Mechlorethamine

Question 7

What are the side effects of Mechlorethamine?

Answer 7

Severe N/V

Myelosuppression–leucopenia and thrombocytopenia

Question 8

Which of the alkylating agents is the most widely used for ALL, CLL, non-hodgkins lymphoma, breast, lung and ovarian cancers?

Answer 8

Cyclophosphamide

Question 9

Which alkylating agent is used for Sarcoma and testicular cancer and what class is this drug in?

Answer 9

Ifosfamide–nitrogen mustard

Question 10

Name the side effects that can occur with the Nitrogen mustard alkylating agents Cyclophosphamide and Ifosfamide…

Answer 10

Hemorrhagic cystitis–treat with hydration and MESNA
N/V
Myelosuppression

Question 11

What are the two alkylating agents used in the treatment of brain cancer and what class are these in?

Answer 11

Carmustine and Lomustine–Nitrosoureas

Question 12

What are the side effect of the nitrosoureas alkylating agents Carmustine and Lomustine?

Answer 12

CNS toxicity
Profound myelosuppression
Severe N/V
Pulmonary fibrosis

Question 13

What are the 3 triazene alkylating agents?

Answer 13

Dacrabazine
Procarbazine
Temozolomide

Question 14

Which triazene alkylating agent produces free radicals?

Answer 14

Procarbazine

Question 15

Which triazene alkylating agent is activated by liver cytochromes?

Answer 15

Dacarbazine

Question 16

Which triazene alkylating agent is nonenzymatically converted to methyl hydrazine at physiologic pH?

Answer 16

Temozolomide

Question 17

Alkylating agent used for the treatment of Hodgkins disease and malignant melanoma

Answer 17

Dacarbazine

Question 18

Alkylating agent used for the treatment of Hodgkins lymphoma…

Answer 18

Procarbazine

Question 19

Alkylating agent used for the treatment of Malignant gliomas…

Answer 19

Temozolomide

Question 20

Procarbazine has a very specific side effect that must be taken into consideration when prescribing this drug. What is it?

Answer 20

May cause leukemia

Question 21

Dacarbazine and Temozolomide are Triazene alkylating agents that have the same side effects. What are these side effects?

Answer 21

N/V
Myelosuppression–neutropenia and thrombocytopenia
Flu-like symptoms– fever and fatigue

Question 22

What is the route of administration for Dacarbazine?

Answer 22

IV

Question 23

What is the route of administration for Temozolomide?

Answer 23

PO

Question 24

Name the 3 platinum analog alkylating agents…

Answer 24

Cisplatin
Carboplatin
Oxaliplatin

Question 25

What class is cisplatin, an alkylating agent, in?

Answer 25

Platinum analogs

Question 26

What class is Carboplatin, an alkylating agent, in?

Answer 26

Platinum analogs

Question 27

What class is Oxaliplatin, and alkylating agent, in?

Answer 27

Platinum analogs

Question 28

Cisplatin, Carboplatin and Oxaliplatin are all platinum analog alkylating agents that work through the same mechanism, what is this mechanism?

Answer 28

Covalently bind nucleophilic sites on DNA---converted to active form by reacting with water---forming a + charge---the hydrated intermediate reacts with DNA guanine--forms inter and intrastand cross links

Question 29

What class of alkylating agent drugs are activated by reacting with water and form a cross link with DNA guanine?

Answer 29

Platinum analongs - Cisplatin - Carboplatin - Oxaliplatin

Question 30

Which platinum analog alkylating agent is used in the treatment of testicular, ovarian, bladder, and lung carcinomas?

Answer 30

Cisplatin

Question 31

Which platinum analog alkylating agent is used in the treatment of ovarian cancer?

Answer 31

Carboplatin

Question 32

Which platinum analog alkylating agent is used in the treatment of gastric and colorectal cancer?

Answer 32

Oxaliplatin

Question 33

Cisplatin is used in the treatment of....

Answer 33

Testicular, ovarian, bladder and lung carcinomas

Question 34

Carboplatin is used in the treatment of...

Answer 34

Ovarian cancer

Question 35

Oxaliplatin is used in the treatment of...

Answer 35

Gastric and colorectal cancer

Question 36

Nephrotoxicity, ototoxicity, peripheral motor and sensory neuropathy are all important side effects of which platinum analog alkylating agent?

Answer 36

Cisplatin

Question 37

What are some other side effects of Cisplatin?

Answer 37

Server N/V | Mild to moderate myelosuppression

Question 38

There is one side effect for Carboplatin, a platinum analog alkylating agent, what is it?

Answer 38

Myelosuppression-- thrombocytopenia

Question 39

What are the side effects seen with oxaliplatin, a platinum analog alkylating agent?

Answer 39

Peripheral sensory neuropathy and neutropenia