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pharmacology 2 > chemotherapy drugs > Flashcards

chemotherapy drugs Flashcards

1
Q

name the 4 classes of chemotherapy drugs

A

cytotoxic drugs

  • alkylating agents
  • antimetabolites
  • cyctotoxic antibiotics
  • plant derivatives

hormones

monoclonal antibodies

protein kinase inhibitors

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2
Q

name the 4 types of drug within the cytotoxic drugs class

A
  • alkylating agents
  • antimetabolities
  • cytotoxic antibodies
  • plant derivative
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3
Q

name the 4 types of alkylating agent

A
  • nitrogen mustards
  • nitrosoureas
  • platinium compounds
  • other
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4
Q

what is the mechanism of action of all alkylating agents?

A

targets cell in phase S (DNA synthesis)

forms covalent bonds with DNA (cross linking) to prevent uncoiling thus inhibiting replication

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5
Q

name a common nitrogen mustard

A

cyclophosphamide

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6
Q

cyclophosphamide is a prodrug, where is it activated and to what?

A

liver ⇒phosphoramide mustard & acrolein

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7
Q

name some other nitrogen mustards

A
  1. methlorethamine
  2. melphalon
  3. chlorambucil
  4. bendamustine
  5. estramustine⇒prostate cancer
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8
Q

name 2 nitrosoureas

A
  1. carmustine (BUNU)→IV
  2. lomustine (CCNU)→oral
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9
Q

which alkylating agent is highly lipophilic and can cross the blood brain barrier?

A

nitrosoureas

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10
Q

with cancers do nitrosoureas treat?

A

CNS tumours

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11
Q

name three platinium compounds used as chemotherapy drugs

A
  1. cisplatin
  2. carboplatin
  3. oxaliplatin
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12
Q

what is the specific mechanism of action of cisplantin?

A

binds to RNA►DNA►protein

binds to purine bases (ie. G, A, U)

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13
Q

resistance may develop with cisplatin, why?

A

DNA repair by DNA polymerase

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14
Q

which cancer is cisplatin used to treat?

A

testicular/ovarian - low levels of repair enzymes (ie. more sensitive to drug)

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15
Q

how is cisplantin administered?

A

slow IV injection/infusion

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16
Q

what are the side effects of cisplantin?

A
  • v.nephrotoxic (hydration required)
  • N&V
  • tinnitus
  • peripheral neuropathy
  • hyperuricaemia
  • anaphlaxis
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17
Q

what is carboplatin derived from?

A

cisplantin

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18
Q

what are the pros and cons of carboplantin over cistoplatin?

A

pros - less side effects /outpatient admin

cons- more myelotoxic (more effects on bone marrow)

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19
Q

which cancer is oxaliplatin used to treat

A

colorectal cancer

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20
Q

name 3 other alkylating agents

A
  1. busulfan
  2. procarbazine
  3. trabectedin
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21
Q

which cancer is busulfan used to treat?

A

selective for bone marrow→leukaemia treatment

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22
Q

which cancer is procarbazine used to treat?

A

Hodgkin’s disease (can cause hypersensitivity and inhibit MAO)

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23
Q

which cancer is trabectedin used to treat?

A

soft tissue sarcoma / advanced ovarian (hepatotoxic)

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24
Q

name the 3 types of antimetabolites

A
  1. folate antagonists
  2. pyrimide analogue
  3. purine analogue
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25
Q

what is the mechanism of action fo folate antagonists?

A

inhibits dihydrofolate reductase (rate limiting step in folate synthesis)

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26
Q

why is folate a useful target for chemotherapy drugs?

A

folate is essential for DNA synthesis/ cell devision

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27
Q

does metotrexate cross the blood brain barrier?

A

no

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28
Q

if metotrexate is given in high does what should also be given?

A

folinic acid (folate derivative) to resue normal cells

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29
Q

name 4 pyrimidine analogues

A
  1. flurouracil
  2. capecitabine
  3. cytarabine
  4. gemcitabine
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30
Q

what is the mechanism of action of pyrimidine analogues?

A

completes with cytosine and thymine bases which make up RNA & DNA→inhibits DNA synthesis

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31
Q

name 4 purine analogues

A
  1. mercaptopurine
  2. tioguanine
  3. pentostatin
  4. fludarabine
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32
Q

what is the mechanism of action of purine analogues?

A

compete with adenine and guanine - inhibit purine metabolism

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33
Q

which 2 purine analogues aremainly used to treat leukaemia?

A
  1. mercaptopurine
  2. tioguanine
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34
Q

name 4 cytotoxic antibiotics

A
  1. doxourubicin
  2. bleomycin
  3. dactinomycin
  4. mitomycin
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35
Q

what is the mechanism of action of doxorubicin?

A

binds to DNA→inhibits DNA & RNA synthesis

inhibits topoisomerase II (helps swivel DNA when seperating)

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36
Q

doxorubincin can cause local necrosis, how?

A

given IV, extravasation (tissuing) at injection site can cause necrosis

37
Q

what are the side effects of doxorubicin?

A

cardiac arrythmias

heart failure (high dose)

38
Q

what is the mechanism of action of bleomycin?

A

degrades pre-formed DNA

active against non-dividing cells (G0 )

39
Q

what are the side effects of bleomycin?

A

little myelosupression

pulmonary fibrosis

mucocutaneous reactions

hyperpyrexia

40
Q

name 3 vinca alkaloids

A
  1. vincristine
  2. vinblastine
  3. vindesine
41
Q

name 3 types of plant derived cytotoxic chemotherapy agents

A
  1. vinca alkaloid
  2. taxanes
  3. etoposide
42
Q

what is the mechanism of action of vinca alkaloids?

A

prevent polymerisation of tublin→microtubles→prevents spindle formation in chromosomes

43
Q

which phase of mitosis do vinca alkaloids target?

A

M phase (cell division)

44
Q

name 2 taxanes

A
  1. paclitaxel
  2. docetaxel
45
Q

what is the mechanism of action of taxanes?

A

similar to vinca alkaloids - affects spindle formation

46
Q

which cancers do taxanes treat?

A

advanced breast

paxlitaxal (& carboplatin) - ovarian

47
Q

which cancers does etoposide treat

A

testicular cancer/ lymphomas

48
Q

what must be monitored when giving etoposide?

A

BP - drops rapidly during infusion

49
Q

name the 6 types of hormone used in chemotherapy treatment

A
  1. oestrogens
  2. progesterones
  3. GnRH analogues
  4. somatostain analogues
  5. Hormone antagonists
  6. glucocorticoids
50
Q

when are hormones used to treat cancer?

A

in hormone sensitive tissue (eg. breast, prostate, ovaries)

51
Q

name 2 oestrogens used in chemotherapy

A
  1. ethinloesteadiol
  2. diethylstilbestrol
52
Q

what is the mechanism of action of oestrogens?

A

anatagonists androgen -dependant prostate cancer (palliative)

53
Q

what are the side effects of oestrogens?

A

nausea

fluid retention

thrombosis

impotence & gynaecomastia (men)

54
Q

what are oestrogens also used for?

A

stimulating resting mammary cells to proliferate (need dividing cells to target with drugs)

55
Q

name 3 progestogens

A
  1. megestrol
  2. medroxyprogesterone
  3. norethisterone
56
Q

what are progesterones use to treat?

A

endometrial cancer

57
Q

name 4 GnRH analogues

A
  1. goserelin
  2. buserelin
  3. leuprorelin
  4. triptorelin
58
Q

what is the mechansim of action of GnRH analogues?

A

inhibits GnRH release→ reduces LH/FSH→testosterone

59
Q

what are GnRh analogues used to treat?

A

prostate

advanced breast cancer (premenopausal)

60
Q

name 2 somatostatin analogues

A
  1. octreotide
  2. lanrectide
61
Q

what is the mechanism of action of somatostatins?

A

inhibits cell proliferation / hormone (CCK/gastrin) secretion

62
Q

what are somatostatin analogues used to treat?

A

hormone secreting GI tract tumours

63
Q

name 7 hormone antagonists

A
  1. tamoxifen
  2. fluvestrant
  3. letrozole
  4. exemastine
  5. flutamide
  6. cyproterone
  7. bicalutamide
64
Q

what are the mechanisms of action of tamoxifen and fluvestrant

A

competative antangonist at oestrogen receptors→inhibit transcription of oestrogen responsive genes

65
Q

what are tamoxifen and fluvestrant used to treat?

A

breast cancer

66
Q

what are the side effect of tamoxifen and fluevestrant?

A

menopausal effects

risk of endometrial cancer

increased risk blood clots

67
Q

what is the mechanism of action of letrozole and exemastine?

A

aromatase inhibitor→blocks conversion of androgens to oestrogens

68
Q

what is the mechanism of action of flutamide, cyproterone and bicalutamide?

A

androgen antagonists

69
Q

what do flutamide, cyproterone and bicalutamide treat?

A

prostate cancer

70
Q

name 2 glucocorticoids used in chemotherapy

A
  1. prednisolone
  2. dexamethasone
71
Q

what are the mechanisms of action of glucocorticiods in relation to chemotherapy?

A

inhibits lymphcyte proliferation

72
Q

which cancers are glucocorticoids used to treat?

A

lymphomas/ leukaemias - supportive/palliative therapy

73
Q

name 4 monoclonal antibodies used in chemotherapy

A
  1. rituximab
  2. trastuzamab
  3. ofatumumab
  4. bevaizumab
74
Q

how do monoclonal anitbodies help to treat cancer?

A

acts with specific target protein expresssed on cancer cells→activates immune system→lysis of cancer cells

75
Q

what is the mechanism of action of rituximab?

A

binds to CD20 protein expressed on certain lymphoma cells→lysis of B-lymphocytes

76
Q

what are the side effects of rituximab?

A

hypotension

chills

fever

hypersensitivity

77
Q

what is the mechanism of action of trastuzamab (herciptin)?

A

binds to HER2 (a GF receptor)→induces immune response & cell cycle inhibitors

HER2 is over expressed on 25% of breast cancers (aggressive form)

78
Q

what are the side effects of trastuzamab?

A

tremor

flu symptoms

itchy eyes

BP changes

palpitations

79
Q

what is the mechanism of action of bevaizumab?

A

neutralises VEGF→prevents angiogensis

80
Q

what does bevaizumab treat?

A

colorectal cancer

81
Q

what does ofatumumab treat?

A

resistant chronic lymphocytic leukaemia

82
Q

name 3 protein kinase inhibitors

A
  1. imatinib
  2. dasatinib
  3. nilotinib
83
Q

what is the mechanism of action of protein kinase inhibitors?

A

blocks tyrosine kinase involved in GF signalling pathways

84
Q

what do protien kinase inhibitors treat?

A

chronic myeloid leukaemia (CML)

85
Q

cytotoxic drugs are often given in combination, why?

A
  • inrease cytotoxicity with increasing general toxicity
  • reduce chance of resistance to drugs
86
Q

what is the typical treatment regime in chemotherapy?

A

large doses every 2-3 weeks - allows bine marrow regen.

87
Q

how can myelosuppression be treated?

A

stem cell transplant

  • autologous - from patient
  • allogenic - from donor
88
Q

which drug is used to boost stem cell production?

A

lenograstim (recombinant GM-CSF)

89
Q
A

pharmacology 2 (11 decks)

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