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Drugs and Disease > Cancer Chemotherapy > Flashcards

Cancer Chemotherapy Flashcards

1
Q

What are 4 characteristics of cancer cells?

A
  1. Anaplasia (loss of original function)
  2. Metastasis (malignant cells)
  3. Invasiveness
  4. Uncontrolled proliferation
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2
Q

What are the three avaliable treatments for cancer?

A
  1. Surgical removal
  2. Irradiation
  3. Chemotherapy
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3
Q

When could you use surgery to remove cancer?

A

Only if the tumours are solid and non-metastasised

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4
Q

When could you use irradiation to remove cancer?

A

Only if localised cancer

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5
Q

What are the two ways in which normal cells become cancer cells?

A
  1. inactivation of tumour supressor genes

2. activation of proto-oncogenes to oncogenes

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6
Q

What kind of drugs are most cancer drugs?

A

Cell cycle drugs to attack rapidly diving cells

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7
Q

What a the 6 main toxic effect of using anti-cancer drugs?

A
  1. Hair loss
  2. Damage to gastrointenstinal epithleium
  3. Depression of growth in children
  4. Sterility
  5. Teratogenicity (damage to embryo)
  6. Bone marrow suprresion - comprimised immune system
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8
Q

Why is it not enough if a drug kills 99.999% of cancer cells?

A

Because out of 10^9 cells that still leaves 10,000 cells that the host cant kill so must aim for total kill

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9
Q

What are the 6 main classes of anticancer drugs?

A
  1. Alkylating agents
  2. Antimetabolities
  3. Cytotoxic antibodies
  4. Microtubule inhibitors
  5. Sterioid hormones
  6. Hormone antagonists
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10
Q

How do alkylating agents kill cancer cells?

A

They form convalent bonds that cross link DNA either two strands together or cross-links within one strand which means transcription and replication cant take place

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11
Q

What are five examples of an alkylating agent?

A
  1. Nitrogen mustards
  2. Cisplatin
  3. Temozolomide
  4. Lomustine
  5. Bulsulphan
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12
Q

What are 4 types of nitrogen mustards?

A
  1. Mephalan
  2. Mechlorethamine
  3. Cyclophosphamide
  4. Isofamide
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13
Q

Which alkylating agent can penetrate the brain?

A

Lomustine

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14
Q

Which alkylating agent can be selective for the bone marrow?

A

Bulsuphan

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15
Q

What was the first of the nitrogen mustards to be used in the treatment of cancer?

A

Mechlorethamine

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16
Q

What was mechlorethamine first used against?

A

Hodkins lymphoma

17
Q

What is it about mechloroethamine that means it must be giving intravenously?

A

It is highly reactive

18
Q

Fusion of mechloroethamine and phenylalanine gives what nitrogen mustard?

A

Melphalan

19
Q

What are three advantages of melphalan over mechloroethamine?

A
  1. more stable
  2. able to absorb and distrubute
  3. can be given orally
20
Q

What kind of cancers in mephalan used to treat?

A

Mulitple melonomas, breast cancer and ovarian cancer

21
Q

What are the four advantages of the nitrogen mustard cyclophosphamide?

A
  1. Pro-drug, reduced in the liver
  2. Much less toxic
  3. Reduced side effects
22
Q

What is it about cyclophosphamide that means it has reduced side effects?

A

alcohol dehydrogenase protects against the drug and since ALDH is present in large quantities in the bone marrow, liver and intestine they selectively inactivate it which reduces its side effects

23
Q

What kind of tissues can cyclophosamide treat?

A

Those with low alcohol dehydrogenase content

24
Q

What does the alkylating agent cisplatin target in order to produce its effect?

A

the N7 of purine nucleotides

25
Q

What two ways have cancer cells become resistant to alkylating agents?

A
  1. Nucleotide excision repair mechanisms

2. Efflux transporters for copper

26
Q

How do antimetabolities work as anti cancer drugs?

A

They interfere with nucleotide synthesis or DNA synthesis

27
Q

What are the two classes of antimetabolities?

A
  1. Antifolates

2. Nucleotide analogues

28
Q

What is an example of a antifolate?

A

Methotrexate

29
Q

How does methotrexate act as an anticancer drug?

A

It is a competitve antagonist for dihydroflolate reductase whic hususally reduces folic acid to tetrahydrofolate so therefore inhibits the formation of tetrahydrofolate which leads to the inhibition of purine and primide syntehsis and therefore stops DNA and RNA synthesis

30
Q

What are three examples of nucleotide analogues?

A

Fluoro-uracil (a pyrimidine analogue)
Mercatopurines (a pure analogue)
Cyarabine (a nucleoside analogue)

31
Q

How does cyarabine work?

A

It is an S phase cell cycle specific drug that inhibits DNA poylmerase through cellular activation of ara-CTP which is added into the DNA by the polymerase and terminates the chain

32
Q

How do the anti cancer drugs cytotoxic antibodies work?

A

Intercalators of the DNA

33
Q

What are two examples of cytotoxic antibodies?

A

Dactinomycin and Doxorubicin (both isolated from streptomyces)

34
Q

How does the cytotix antibody dactinomycin work?

A

Inserts itself into the minor groove of the DNA helix so RNA polymerase function is disrupted

35
Q

How does the cytotoxic antibody doxorubicin work?

A

Inserts itself better base pairs and binds to the sugar phosphate backbone which leads to local uncoiling and impaired DNA and RNA synthesis

36
Q

What is an example of a microtubule inhibitor?

A

Vinca alkaloids

37
Q

How do vinca alakloids work?

A

Binds to microtubule protein and block tubulin polymerisation andtherefore blocking spindle formation and cell division

38
Q

What are two examples of steriod hormone anti-cancer drugs?

A
  1. Prednisone (synthetic adrenocortical hormone)

2. Predinsolone (supress lymphocyte growth)

39
Q

Apart from with testosterone repector antagonists what is another way to treat prostate cancer?

A

luitenizing hormone releasing hormone antagonists inhibit release of leutenizing hormone which is normally used to stimulate the testes to produce tesosterone so blocking this reduces testosterone

Drugs and Disease (15 decks)

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