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Cology 2 Exam 4 > Antineoplastic therapy- Alkylating agents 1-18 > Flashcards

Antineoplastic therapy- Alkylating agents 1-18 Flashcards

1
Q

Are alkylatic agents synthetic or natural?

A

They’re synthetic, so are antimetabolites

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2
Q

In general, what do alkylatic agents do?

A

Alkylate purine/pyrimidine bases, block DNA synthesis

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3
Q

Name the nitrogen mustards

A 
Mechlorethamine
Cyclophosphamide
Ifosfamide
Chlorambucil
Melphalan
Bendamustine
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4
Q

Name the nitrosureas

A

Carmustine
Lomustine
Streptozocin

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5
Q

What are the “other” alkylatic agents

A 
Dacarbazine
Procarbazine
Temozolamide
Altretamine
Busulfan
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6
Q

Name the platinum coordination complexes

A

Cistplatin
Carboplatin
Oxaliplatin

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7
Q

Where do alkylating agents work in the cell cycle?

A

Non-specific! G1 and S

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8
Q

What 3 general properties are there of alkylatic agents?

A

Mutagenic, carcinogenic, teratogenic

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9
Q

What is the MOA of alkylatic agents?

A

Form carbonium ion or transition intermediates. They alkylate the nitrogen on: 7 of guanine, 1 and 3 of adenosine, 3 of cytosine, and 6 O of guanine

  • They form cross-links with adjacent bases to prevent strand from coming apart to block transcription
  • Cross-linking also increases p53 activity to cause apoptosis

Can cause abnormal pairing of G with T, removal of purines, and increased ring cleavage due to binding

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10
Q

Which agents were used during WW1 as chemical warfare agents? Why were they dangerous?

A

Nitrogen mustards; they had significant vesicant actions and caused tissue damage

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11
Q

How is Mechlorethamine administered?

A

IV

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12
Q

What is Mechlorethamine used for?

A

Hodgkin’s disease (part of MOPP’s regimen) - LIMITED use

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13
Q

Adverse effects of mechlorethamine?

A

Nausea, vomiting, leukopenia, thrombocytopenia, reduced reproductive function

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14
Q

Does mechlorethamine have a rescue?

A

You can treat extravasation with sodium thiosulfate

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15
Q

How is cyclophosphamide administered?

A

Oral, IV

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16
Q

Does mechlorethamine require activation?

A

Quick activation, quick inactivation

17
Q

Does cyclophosphamide require activation?

A

Yes by p-450 system

18
Q

What is cyclophosphamide used for?

A

Chronic and acute lymphytic leukemia
Lymphoma
Used in combination for breast, lung, testicular, ovarian, sarcoma, non-hodgkins and hodgkins

19
Q

What toxicities are associated with cyclophosphamide?

A

Nausea, vomiting, cystitis, GI ulceration, alopecia, pulmonary fibrosis, immunosuppression

20
Q

Does cyclophosphamide have a rescue?

A

Give mercaptoethane sulfonate (MESNA) to reduce cystitis in the bladder, MUST hydrate patient

21
Q

Does Ifosfamide require activation?

A

Yes CYP3A4 activation

22
Q

What is Ifosfamide usually compared to?

A

Cyclophosphamide

It is less potent, but has CNS side effects and more nephrotoxicity, platelet suppression

23
Q

Does Ifosfamide have a rescue?

A

Mercaptoethane sulfonate (MESNA) to prevent cystitis, MUST hydrate patient

24
Q

What is Ifosfamide used for?

A

Sarcoma, testicular cancer, bone marrow ablation

Used to deplete bone marrow before transplants

25
Q

What drug is used for bone marrow ablation?

A

Ifosfamide, Melphalan

26
Q

What is Melphalan used for?

A

Multiple myeloma, bone marrow ablation

27
Q

How is Melphalan administered?

A

Oral, IV

28
Q

Toxicities of Melphalan?

A

Bone marrow suppression, less nausea and vomiting and no alopecia!
Leukemias
Teratogenic

29
Q

What is Chlorambucil used for?

A

Chronic lymphocytic leukemia (CLL)

30
Q

How is Chlorambucil administered?

A

Given orally only

31
Q

Toxicities with Chlorambucil?

A

GI discomfort, pulmonary fibrosis, seizures, dermatitis, bone marrow suppression, teratogenic, infertility

32
Q

What is Bendamustine used for?

A

CLL and Non-hodgkin’s lymphoma

33
Q

How is Bendamustine administered?

A

IV infusion on day 1 and 2 of a 28 day cycle

34
Q

Toxicities with bendamustine?

A

Myelosuppression, mucositis, nausea, vomiting

35
Q

How does Bendamustine compare to other agents?

A

Lacks resistance to other alkylating agents

Cology 2 Exam 4 (16 decks)

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