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MP421 > CHEMOTHERAPY DRUGS > Flashcards

CHEMOTHERAPY DRUGS Flashcards

1
Q

types of cancer treatment

A

surgery
radiation
chemotherapy

treatment will depend on the type of cancer, progression of the disease, health of the pt and pt choice

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2
Q

chemotherapy

A

the treatment of cancer with one or more cytotoxic drugs

often used in conjunction with other treatments (radiation therapy, surgery etc.)

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3
Q

most common side effects of chemotherapy

A

myelosuppression (decreased production of blood cells, hence also immunosuppression)

mucositis (inflammation of the lining of the digestive tract)

alopecia (hair loss)

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4
Q

chemotherapy moa

A

act by killing cells that divide rapidly, one of the main properties of cancer cells, this means that chemotherapy also harms cells that divide rapidly under normal circumstances: cells in the bone marrow, digestive tract and hair follicles

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5
Q

problems with chemotherapy

A
  • treatments are non-specific, attack healthy cells as well as cancer cells
  • cancers are heterogenous - genes mutated so bits of some cancers or metastases may be resistant to some drugs
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6
Q

indicators that the cancer has developed resistance to therapy

A
  • decreased drug uptake/increased efflux
  • enhanced tolerance of DNA adducts
  • enhanced repair of DNA adducts
  • increasing drug deactivation by intracellular glutathione
  • toxicity to normal cells
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7
Q

types of anticancer drugs PATAAT

A

platinates
anthracyclines
taxanes
alkylators
antimetabolites
topoisomerase inhibitors

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8
Q

how do PATAAT drugs act

A

act by inducing cellular apoptosis (programmed cell death)

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9
Q

alkylation

A

transfer of an alkyl group from one molecule to another - alkylation of DNA is used in chemotherapy to damage the DNA of cancer cells

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10
Q

alkylating agents moa

A

attaches to an alkyl group (Cn H2n+1) to the guanine base of DNA, at the number 7 nitrogen atom of the purine ring

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11
Q

consequences of alkylating agents

A
  • DNA fragmented by repair enzymes in their attempts to replace the alkylated bases
  • addition of the alkyl group to the base causes the mispairing of the nucleotides leading to mutations
  • alkylating agents cause formation of cross-bridges, bonds between atoms in the DNA - 2 bases are linked together by an alkylating agent that has 2 DNA binding sites. cross-linking prevents DNA from being separated for synthesis or transcription. as this is necessary on DNA replication, the cells can no longer divide
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12
Q

6 groups of alkylating agents

A

nitrogen mustards
ethylamines
alkylsulfonates
triazenes
piperazines
nitrosureas

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13
Q

alkylating-like drugs: platinum-based drugs

A

CISPLATIN AND CARBOPLATIN
- platinum analogues act similarly to alkylating agents
- these agents do not have an alkyl group, but damage DNA
- they permanently coordinate to DNA to interfere with DNA repair

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14
Q

cisplatin effect on DNA

A
  • replication inhibition
  • transcription inhibition
  • cell-cycle arrest
  • DNA repair
  • cell death
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15
Q

cisplatin side effects

A
  • small therapeutic window
  • neurotoxic (nerve damage) - visual perceptions, hearing disorders
  • nephrotoxic - related to reactive oxygen species
  • nausea and vomiting - often given with anti-emetics
  • myelotoxicity - bone marrow suppression
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16
Q

carboplatin

A
  • delivers the same drug as cisplatin but with chloride ligands replaced with bidentate dicarboxylate
  • preferred first line with ovarian and small cell lung cancer
  • takes less time to administer than cisplatin
  • solution (10mg/ml)
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17
Q

satraplatin

A
  • first platinum anti-cancer drug that can be administered orally
  • most platinums are usually given in combination with other drugs
  • indicated for prostate cancer
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18
Q

anthracycline-based drugs - intercalating drugs

A
  • natural products derived from various strains of streptomyces bacteria
  • four-ring structure linked via glycoside bond to daunosamine
  • doxorubicin = for many solid tumours
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19
Q

anthracycline side effects

A
  • nausea and vomiting, extravasation can cause tissue necrosis, bone marrow depression/immunosuppression, myelosuppression, infertility, dehydration
  • myocardial toxicity from cumulative doses of around 450-500mg/m2 - patients need cardiac monitoring
  • 1 in 2 patients in every 100 develop acute myelogenous leukaemia or myelodysplastic syndrome. risk even higher for those concurrently treated with cyclophosphamides or radiotherapy.
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20
Q

actionmycin D

A
  • inhibits transcription
  • it does this by binding DNA at the transcription initiation complex and preventing elongation of RNA chain by RNA polymerase
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21
Q

microtubules function

A
  • cell shape
  • cell movement
  • movement of cargo within cell
  • mitosis
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22
Q

spindle poisons

A

alters structure and function of microtubules

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23
Q

example of spindle poisons: vincristine, used for…

A
  • acute leukaemia’s
  • Hodgkin’s lymphoma
  • non-Hodgkin’s lymphoma
  • small cell lung cancer
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24
Q

adverse effect of vincristine

A

peripheral neuropathy

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25
Q

cisplatin structural effect on DNA

A

binds to DNA and causes a critical 45 degree bend

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26
Q

cisplatin

A
  • indicated for metastatic testicular tumours, metastatic ovarian tumours and advanced bladder cancer
  • small therapeutic window
27
Q

dose-limiting toxicities

A

chemotherapy side effects severe enough to prevent giving more of the treatment. may result in treatment delay, dose reduction or discontinuation of treatment

28
Q

carboplatin dose

A

IV 400mg/m2 over 15-60 minutes every 4 weeks

29
Q

FOLFOX treatment

A
  • indicated for colorectal cancer
  • combination of oxaliplatin and fluorouracil and folinic acid
30
Q

anthracycline drugs

A

doxorubicin
daunorubicin
idarubicin

31
Q

doxorubicin moa

A
  • attaches to DNA, distorting its double helical structure
  • hydrophobic DNA base pairs interact with planar rings of doxorubicin
  • inhibits topoisomerase II inducing DNA breaks
32
Q

doxorubicin dose

A

IV 60-75mg/m2 every 21 days

33
Q

doxorubicin side effects

A
  • nausea/vomiting
  • myelosuppression
  • infertility
  • dehydration
  • myocardial toxicity
34
Q

actinomycin D

A
  • indicated for paediatric cancer
  • no cardiotoxicity
35
Q

vinca alkaloids

A

VINCRISTINE
VINBLASTINE
VINORELBINE
- inhibits mitosis of affected cells causing apoptosis
- bind to tubulin monomers keeping microtubules from forming

36
Q

taxol

A
  • indicated for ovarian/prostate/breast/head/neck cancer, non-small cell lung carcinoma, aids relayed Kaposi’s sarcoma, gastric adenocarcinoma
37
Q

taxol side effects

A

hair loss
stomach issues
neutropenia (DLT)

38
Q

taxols

A

PACLITAXEL
DOCETAXEL

39
Q

paclitaxel moa

A

stabilises microtubules resulting in interference with normal breakdown of microtubules during cell division therefore cell cannot divide

40
Q

antimetabolites moa

A

work via 2 methods:
- the antimetabolite gets incorporated instead of the normal metabolite (antimetabolites as competitive substrates)
- the antimetabolite inhibits the enzyme involved in the synthesis or reuptake of a metabolite (antimetabolites as enzyme inhibitors)

BOTH INDUCE CELLULAR APOPTOSIS
- many are nucleic acid analogues and can get incorporated into the DNA

41
Q

anti-folates

A

methotrexate
hydroxyurea

42
Q

anti-pyrimidines (pyrimidine analogues)

A

5-fluorouracil
cytarabin

43
Q

anti-purines (purine analogues)

A

6-mercaptopurine
6-thioguanidine

44
Q

purines and pyrimidines

A

PURINES (double ring): adenine and guanine

PYRIMIDINES (single ring): cytosine and thymine (uracil in RNA) needed for nucleic acid synthesis

45
Q

de novo pathway

A

assembles nucleotides from amino acids and other small molecules

46
Q

salvage pathway

A

recycle the free bases and nucleotides released from DNA breakdown

47
Q

normal cells in nucleotide synthesis

A
  • de novo pathway is inactive
  • salvage pathway is dominant
48
Q

cancer cells in nucleotide synthesis

A
  • de novo pathway is active
  • salvage pathway is inactive
49
Q

mercaptopurine moa

A

prevents synthesis of guanosine monophosphate (dGMP)

50
Q

mercaptopurine

A
  • indicated for leukaemia
  • liver toxicity, enzyme elevation, jaundice, cirrhosis
51
Q

mercaptopurine side effects

A
  • nephrotoxicity
  • leucopenia
  • vomiting
  • myelosuppression
52
Q

gemcitabine moa

A
  • structurally similar to deoxycytidine (dCTP) so competes for incorporation into DNA
  • nucleoside metabolic inhibitors kill cells undergoing DNA synthesis
  • once incorporated into DNA chain can no longer be elongated causing cell apoptosis
  • inhibits replication and repair
  • inhibits enzyme ribonucleotide reductase - decreases deoxynucleotide concentrations
53
Q

indications for gemcitabine

A

indicated for bladder/pancreatic/breast cancer

usual chemo toxic side effects

54
Q

5-fluorouracil moa

A

antimetabolite
inhibits thymidine synthase

55
Q

methotrexate moa

A

blocks the synthesis of folic acid by binding to dihydrofolate reductase and folic acid receptors on cancer cells which interferes with DNA synthesis/transcription

56
Q

methotrexate

A

oral/IV/IM or intrathecally injected

folinic acid or folic acid given alongside to prevent side effects

57
Q

methotrexate side effects

A

loss of appetite
nausea
GI discomfort
diarrhoea
hair loss

58
Q

topoisomerase I inhibitors

A

irinotecan
topotecan
camptothecin

59
Q

topoisomerase II inhibitors

A

etoposide
doxorubicin
epirubicin

60
Q

topoisomerase inhibitors moa

A
  • block the ligation step of cell cycle
  • this generates single-/double- strand breaks leading to apoptosis
61
Q

topoisomerase

A

binds to DNA molecules that are supercoiled

62
Q

topoisomerase I

A

relaxes supercoiled DNA to remove helical constraints by cutting the double strand to make a single strand to allow room for a new DNA strand

63
Q

topotecan

A
  • indicated in ovarian cancer, small cell lung cancer
  • really potent radiosensitiser and chemosensitiser

MP421 (12 decks)

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