Alkylating agents Flashcards

1
Q

Name the 3 drugs in the nitrogen mustard class…

A

Mechlorethamine
Cyclophosphamide
Ifosfamide

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2
Q

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

A

Alkylating agents

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3
Q

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

A

Mechlorethamine

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4
Q

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

A

Cyclophosphamide and Ifosfamide

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5
Q

Name the 2 Nitrosoureas alkylating agents…

A

Carmustine

Lomustine

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6
Q

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

A

Mechlorethamine

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7
Q

What are the side effects of Mechlorethamine?

A

Severe N/V

Myelosuppression–leucopenia and thrombocytopenia

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8
Q

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

A

Cyclophosphamide

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9
Q

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

A

Ifosfamide–nitrogen mustard

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10
Q

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

A

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

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11
Q

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

A

Carmustine and Lomustine–Nitrosoureas

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12
Q

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

A

CNS toxicity
Profound myelosuppression
Severe N/V
Pulmonary fibrosis

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13
Q

What are the 3 triazene alkylating agents?

A

Dacrabazine
Procarbazine
Temozolomide

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14
Q

Which triazene alkylating agent produces free radicals?

A

Procarbazine

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15
Q

Which triazene alkylating agent is activated by liver cytochromes?

A

Dacarbazine

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16
Q

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

A

Temozolomide

17
Q

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

A

Dacarbazine

18
Q

Alkylating agent used for the treatment of Hodgkins lymphoma…

A

Procarbazine

19
Q

Alkylating agent used for the treatment of Malignant gliomas…

A

Temozolomide

20
Q

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

A

May cause leukemia

21
Q

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

A

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

22
Q

What is the route of administration for Dacarbazine?

A

IV

23
Q

What is the route of administration for Temozolomide?

A

PO

24
Q

Name the 3 platinum analog alkylating agents…

A

Cisplatin
Carboplatin
Oxaliplatin

25
Q

What class is cisplatin, an alkylating agent, in?

A

Platinum analogs

26
Q

What class is Carboplatin, an alkylating agent, in?

A

Platinum analogs

27
Q

What class is Oxaliplatin, and alkylating agent, in?

A

Platinum analogs

28
Q

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

A

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

29
Q

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

A

Platinum analongs

  • Cisplatin
  • Carboplatin
  • Oxaliplatin
30
Q

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

A

Cisplatin

31
Q

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

A

Carboplatin

32
Q

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

A

Oxaliplatin

33
Q

Cisplatin is used in the treatment of….

A

Testicular, ovarian, bladder and lung carcinomas

34
Q

Carboplatin is used in the treatment of…

A

Ovarian cancer

35
Q

Oxaliplatin is used in the treatment of…

A

Gastric and colorectal cancer

36
Q

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

A

Cisplatin

37
Q

What are some other side effects of Cisplatin?

A

Server N/V

Mild to moderate myelosuppression

38
Q

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

A

Myelosuppression– thrombocytopenia

39
Q

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

A

Peripheral sensory neuropathy and neutropenia