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CHEMOTHERAPY DRUGS Flashcards

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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
cisplatin structural effect on DNA
binds to DNA and causes a critical 45 degree bend
26
cisplatin
- indicated for metastatic testicular tumours, metastatic ovarian tumours and advanced bladder cancer - small therapeutic window
27
dose-limiting toxicities
chemotherapy side effects severe enough to prevent giving more of the treatment. may result in treatment delay, dose reduction or discontinuation of treatment
28
carboplatin dose
IV 400mg/m2 over 15-60 minutes every 4 weeks
29
FOLFOX treatment
- indicated for colorectal cancer - combination of oxaliplatin and fluorouracil and folinic acid
30
anthracycline drugs
doxorubicin daunorubicin idarubicin
31
doxorubicin moa
- 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
doxorubicin dose
IV 60-75mg/m2 every 21 days
33
doxorubicin side effects
- nausea/vomiting - myelosuppression - infertility - dehydration - myocardial toxicity
34
actinomycin D
- indicated for paediatric cancer - no cardiotoxicity
35
vinca alkaloids
VINCRISTINE VINBLASTINE VINORELBINE - inhibits mitosis of affected cells causing apoptosis - bind to tubulin monomers keeping microtubules from forming
36
taxol
- indicated for ovarian/prostate/breast/head/neck cancer, non-small cell lung carcinoma, aids relayed Kaposi's sarcoma, gastric adenocarcinoma
37
taxol side effects
hair loss stomach issues neutropenia (DLT)
38
taxols
PACLITAXEL DOCETAXEL
39
paclitaxel moa
stabilises microtubules resulting in interference with normal breakdown of microtubules during cell division therefore cell cannot divide
40
antimetabolites moa
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
anti-folates
methotrexate hydroxyurea
42
anti-pyrimidines (pyrimidine analogues)
5-fluorouracil cytarabin
43
anti-purines (purine analogues)
6-mercaptopurine 6-thioguanidine
44
purines and pyrimidines
PURINES (double ring): adenine and guanine PYRIMIDINES (single ring): cytosine and thymine (uracil in RNA) needed for nucleic acid synthesis
45
de novo pathway
assembles nucleotides from amino acids and other small molecules
46
salvage pathway
recycle the free bases and nucleotides released from DNA breakdown
47
normal cells in nucleotide synthesis
- de novo pathway is inactive - salvage pathway is dominant
48
cancer cells in nucleotide synthesis
- de novo pathway is active - salvage pathway is inactive
49
mercaptopurine moa
prevents synthesis of guanosine monophosphate (dGMP)
50
mercaptopurine
- indicated for leukaemia - liver toxicity, enzyme elevation, jaundice, cirrhosis
51
mercaptopurine side effects
- nephrotoxicity - leucopenia - vomiting - myelosuppression
52
gemcitabine moa
- 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
indications for gemcitabine
indicated for bladder/pancreatic/breast cancer usual chemo toxic side effects
54
5-fluorouracil moa
antimetabolite inhibits thymidine synthase
55
methotrexate moa
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
methotrexate
oral/IV/IM or intrathecally injected folinic acid or folic acid given alongside to prevent side effects
57
methotrexate side effects
loss of appetite nausea GI discomfort diarrhoea hair loss
58
topoisomerase I inhibitors
irinotecan topotecan camptothecin
59
topoisomerase II inhibitors
etoposide doxorubicin epirubicin
60
topoisomerase inhibitors moa
- block the ligation step of cell cycle - this generates single-/double- strand breaks leading to apoptosis
61
topoisomerase
binds to DNA molecules that are supercoiled
62
topoisomerase I
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
topotecan
- indicated in ovarian cancer, small cell lung cancer - really potent radiosensitiser and chemosensitiser

MP421 (12 decks)

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