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Pharmacology Test 3 > Cancer Chemotherapy Agents > Flashcards

Cancer Chemotherapy Agents Flashcards

1
Q

Akylating Agents

A

Non cell cycle specific

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2
Q

Where do alkylating agents originate from

A

sulfur and nitrogen mustard warfare agents

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3
Q

Later generation mustard agents

A

Akylating Agents
Non cell cycle specific

  • cyclophosphamide
  • ifosfamide generate
  • BCNU (carmustine
  • CCNU (lomustine)
  • thiotepa
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4
Q

Cyclophosphamide

A

Akylating Agents
Non cell cycle specific

  • Later generation mustard agent
  • generates acrolein, which is toxic to the bladder
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5
Q

Ifosfamide

A

Akylating Agents
Non cell cycle specific

  • later generation mustard agents
  • generate acrolein, which is toxic to the bladder
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6
Q

BCNU

carmustine

A

Akylating Agents
Non cell cycle specific
Later generation mustard agent

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7
Q

CCNU

lomustine

A

Akylating Agents
Non cell cycle specific
later generation mustard agent

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8
Q

All mustard agents

A
  • prodrugs
  • – need metabolic activation
  • orally active
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9
Q

Thiotepa

A

Akylating Agents
Non cell cycle specific

  • lipophilic
  • – penetrates well into brain and can kill metastases of non-neuronal neoplasms in the brain
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10
Q

Hydrazines

A 
alylating agent (non cell cycle specific)
- prodrugs
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11
Q

Procarbazine

A

hydrazine (alkylating agent, non cell cycle specific)

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12
Q

Dacarbazine

A

hydrazine (alkylating agent, non cell cycle specific)

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13
Q

Temozolomide

A

hydrazine (alkylating agent, non cell cycle specific)

  • orally active
  • penetrates brain blood barrier
  • useful for gliomas
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14
Q

Alkylating Agents Mechanism of Action

A
  • non cell cycle specific
  • highly reactive
  • – alkylate protein, RNA, DNA and cause strand breaks, crosslinks and mismatches, disrupting DNA synthesis/replication
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15
Q

Alkylating Agents Adverse Effects

A
  • classical - nausea, allopecia, myelosuppresion/immunosuppression
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16
Q

Akylating Agents

Resistance Mechanisms

A
  • increased glutathione conjugation
  • increased glutathione synthesis
  • increased DNA repair
  • decrease cellular update
  • increased cellular efflux
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17
Q

Antimetabolites

A

S phase specific

18
Q

Methotrexate

A

Antifolates

  • taken up and polygultamylated
  • inhibits dihydrofolate reductase (DHFR) and thymidiylate synthetase (TS)
19
Q

Methotrexate Active In

antifolate

A

Antimetabolites (s phase specific)

  • wide variety of cancers
  • – leukemia
  • – lymphoma
  • – solid tumors
20
Q

Methotrexate Adverse Effects

antifolate

A

antimetabolites (s phase specific)
- nephrotoxicity

Folate analogue LEUCOVORIN used as a rescue agent

21
Q

Leucovorin

A

rescue agent for nephrotoxicity seen with methotrexate

22
Q

Methotrexate Resistance

antifolate

A

antimetabolites (s phase specific)

  • cellular transport: less in, more out
  • decreased metabolic activiation
  • altered enzyme target
  • increased salvage of folate
23
Q

Purine/Pyrimidine Analogs

A

antimetabolites (s phase specific)

  • 6-mercaptopurine
  • 5-fluorouracil
  • cytosine arabinoside
24
Q

6-mercaptopurine

A 
Purine/Pyrimidine Analogs
antimetabolites (s phase specific)
- prodrug
- inhibits purine synthesis
- incorporated into RNA and DNA
25
Q

5-fluorouracil

A 
Purine/Pyrimidine Analogs
antimetabolites (s phase specific)
- prodrug that looks like thymine
- inhibits thymidylate synthetase
- incorporated into RNA and DNA
26
Q

Cytosine Arabinoside

A

Purine/Pyrimidine Analogs
antimetabolites (s phase specific)
- inhibits DNA polymerase
- incorporated into RNA and DNA

27
Q

Platinum Compounds

A

Cisplatin and other -platins

non cell cycle specific

28
Q

Platinum Compounds

Action

A

Cisplatin and other -platins
non cell cycle specific
- bind DNA and cause DNA double strand breaks
- BRCA 1/2 deficient tumors especially sensitive
— acquired resistance due to their reversion

29
Q

Platinum Compounds Adverse Events

A 
Cisplatin and other -platins 
non cell cycle specific
- NAUSEA & VOMITING 
- myelosuppression 
- renal and ototoxicity
30
Q

Poly (ADP-Ribose) Polymerase (PARP) Inhibitors

A

similar effects on DNA to the platins

31
Q

Anthracyclines

A

Doxorubicin (adriamycin)

non cell cycle specific

32
Q

Doxorubicin

A

Adriamycin
non cell cycle specific
Anthracyclines

33
Q

Cisplatin and other -platins

A
  • non cell cycle specific

- platinum compounds

34
Q

Anthracyclines Action

A

Doxorubicin (adriamycin)
non cell cycle specific
- DNA intercalator & topoisomerase inhibitor

35
Q

Anthracyclines Adverse Effects

A 
Doxorubicin (adriamycin)
non cell cycle specific
- nausea & vomiting
- vesicant
- cardiotoxicity
36
Q

Tubulin Disrupting Agents

A

M phase specific poisons

  • vinca alkaloids
  • taxanes: taxol (paclitaxel) and variants
37
Q

Vinca Alkaloids

A

Tubulin Disrupting Agents
(M phase specific poisons)
- Inhibit microtubule polymerization causing mitotic arrest

38
Q

Vincristine

A

Tubulin Disrupting Agents
(M phase specific poisons)
Vinca Alkaloids
- neurotoxic (microtubules are necessary for axonal transport)

39
Q

Vinblastine

A

Tubulin Disrupting Agents
(M phase specific poisons)
Vinca Alkaloids
- vesicant

40
Q

Taxol (paclitaxel) and variants

Action

A

Tubulin Disrupting Agents
(M phase specific poisons)
- promotes tubulin assembly and causes mitotic arrest

41
Q

Taxol (paclitaxel) and variants

Adverse Effects

A 
Tubulin Disrupting Agents
(M phase specific poisons) 
- peripheral neuropathy
- allergic reaction due to solvent used (cremaphore)
- myelosuppresion
- allopecia
42
Q

Cremaphore

A

solvent used for Taxols

- can illicit allergic reactions

Pharmacology Test 3 (9 decks)

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