Chemotherapy drugs Flashcards

1
Q

What are the 6 classes of cytotoxic drugs?

A
  1. Alkylating drugs
  2. Platinating drugs
  3. Anti-metabolites
  4. Cytotoxic antibodies
  5. Mitotic inhibitors
  6. Topoisomerase inhibitors
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2
Q

What is the mechanism of action of alkylating agents?

A

The reactive alkyl group forms covalent bonds with DNA, crosslinking DNA & disrupting its replication & transcription

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3
Q

What are the 2 alkylating drugs?

A

Cyclophosphamide, chlorambucil

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4
Q

What are the 3 methods of resistance to alkylating agents?

A
  1. Decreased entry into or increased exit of agent from cell
  2. Inactivation of agent in cell
  3. Enhanced repair of DNA lesions produced by alkylation - upregulation of DNA repair genes
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5
Q

What are the 4 general side effects of chemotherapy?

A
  1. Myelosuppression
  2. Nausea, vomiting, GI effects
  3. Mucous membrane ulceration
  4. Alopecia
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6
Q

What is the mechanism of action of platinum-based chemotherapy drugs?

A

Platinum-based drugs act as alkylating agents, causing intra-strand crosslinks hence disrupting DNA replication & transcription

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7
Q

What are the 3 platinum-based chemotherapy drugs?

A

cisplatin, carboplatin, oxaliplatin

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8
Q

What are the adverse effects of platinum-based chemotherapy drugs?

A

Nephrotoxicity as excreted renally; contraindicated in patients with renal dysfunction

Cisplatin & oxaliplatin may cause peripheral sensory neuropathy

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9
Q

What is the mechanism of action of anti-metabolites?

A

Anti-metabolites interfere with the synthesis of nucleotides purine & pyramidine, inhibiting DNA replication

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10
Q

What are the 2 cell-cycle specific chemotherapy drugs?

A

Anti-metabolies & mitotic inhibitors

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11
Q

What are the 4 cell-cycle non-specific chemo drugs?

A

Alkylating, platinum-based, cytotoxic antibiotics & topoisomerase inhibitors

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12
Q

What are the 2 anti-metabolites?

A

Methotrexate & 5-fluorouracil

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13
Q

What is the mechanism of action of methotrexate?

A

Methotrexate is an anti-metabolite that inhibits dihydrofolate reductase, preventing thymidine monophosphate synthesis

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14
Q

What is the mechanism of action of 5-fluorouracil?

A

5-fluorouracil is an anti-metabolite which inhibits thymidylate synthase (TS) and is used in place of uracil, hence causing DNA damage

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15
Q

What are the clinical indications for methotrexate?

A

Lymphoma & breast cancer

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16
Q

What are the clinical indications of 5-fluorouracil?

A

Colorectal cancer

17
Q

What are the 4 mechanisms of action of cytotoxic antibiotics?

A
  1. Inhibit DNA & RNA synthesis by intercalating base pairs along DNA strands
  2. Create free O2 radicals that damage DNA & cell membranes
  3. Inhibit topoisomerase II
  4. Alter membrane fluidity & ion transport
18
Q

What are the 2 cytotoxic antibiotics?

A

Doxurubicin, daunorubicin

19
Q

What is the mechanism of action of Vinca alkaloids?

A

Vinca alkaloids disrupt the function of microtubules by binding to polymerising end of the beta subunit of tubulin, preventing elongation of the microtubule

20
Q

What is the mechanism of action of taxanes?

A

Taxanes disrupt the function of microtubules by binding to the beta subunit of tubulin, stabilising the microtubule and preventing shortening or depolymerisation

21
Q

What are the 2 classes of mitosis inhibitors?

A

Vinca alkaloids & taxanes

22
Q

What is the mechanism of action of topoisomerase inhibitors?

A

Topoisomerase inhibitors interfere with the transcription and replication of DNA by disrupting appropriate DNA supercoiling due to inhibition of Topoisomerase I/II

23
Q

What is an example of a Vinca alkaloid?

A

Vinblastine

24
Q

What is an example of a taxane?

A

Paclitaxel

25
Q

What is an example of a type 1 topoisomerase inhibitor?

A

Irinotecan

26
Q

What is an example of a type 2 topoisomerase inhibitor?

A

Etoposide