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Pharmacology - Year 2 AC > Week 4 - Chemotherapy Drugs > Flashcards

Week 4 - Chemotherapy Drugs Flashcards

1
Q

Name the stages in the cell cycle

A 
M - mitosis 
G1 - gap one
(G0 - cells no longer dividing)
S phase - (DNA synthesis)
G2 - gap two
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2
Q

What enzyme catalyses mitosis?

A

DNA polymerase

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3
Q

Which cells are fitted with a safety mechanism that if they end up in the wrong tissue they lose their survival signals and die?

A

Muscle cells

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4
Q

What are the different options for cancer treatment?

A

Surgery
Irradiation (radiotherapy)
Drug therapy (chemo)
Combination of above

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5
Q

What type of cells are most susceptible to cytotoxic drugs?

A

Dividing cells

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6
Q

What is the aim of chemotherapy?

A

To kill all malignant cells in the body

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7
Q

Why can’t you rely on the immune system to kill malignant cells?

A

Unable to recognise tumour cells as foreign because essentially they are normal cells

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8
Q

What cancer has a cell doubling time of 24 hours?

A

Burkitt’s lymphoma

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9
Q

Why are the effects of chemotherapy so toxic?

A

all rapidly dividing normal tissues are affected

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10
Q

What are the toxic effects of chemotherapy?

A 
Bone marrow suppression
Impaired wound healing
Loss of hair 
Damage to GI epithelium (inc. mouth)
Growth stunted (children)
Reproductive system - sterility 
Teratogenicity - cause harm to foetus 
Bleeding/bruising due to lack of platelets/clotting factors 
N+V 
Kidney damage
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11
Q

What are the possible targets for anti-cancer drugs?

A
  • hormonal regulation of tumour growth

- defective cell cycle controls

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12
Q

What are the classes of anti-cancer drugs?

A
  • Cytotoxic (block DNA synthesis/ prevent cell division)
  • Hormones -and their antagonists (suppress hormone secretion or inhibit their actions)
  • Monoclonal antibodies (target specific cancer cells)
  • Protein kinase inhibitors (block cell signalling pathways in rapidly dividing cells)
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13
Q

What causes cancer?

A

DNA mutation

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14
Q

What are the classes of alkylating agents?

A

Nitrogen mustards, nitrosoureas, busulphan, platinum compounds

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15
Q

How do alkylating agents work?

A
  • target cells in S phase (DNA synth phase)

- form covalent bonds with DNA (cross linking) - prevent uncoiling –> inhibits replication

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16
Q

What are the side effects for prolonged use of alkylating agents?

A
  • sterility (esp. men)

- higher risk of non-lymphocytic leukaemia (AML)

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17
Q

Name some nitrogen mustards

A

Cyclophosphamide, melphalan, chlorambucil, bendamustine, estramustine

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18
Q

What is estramustine and what is it often used in the treatment of?

A

A nitrogen mustard
-analogue of oestrogen so stops cell division and has a hormonal effect

-prostate cancer

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19
Q

How are nitrogen mustards administered?

A

IV only

-very reactive, often infused with large volumes of fluid

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20
Q

What is cyclophosphamide and how does it work?

A
  • nitrogen mustard

- prodrug (can be administered orally -activated in liver to phosphoramide mustard and acrolein)

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21
Q

What is a well known side effect that can occur from cyclophosphamide?

A

Acrolein –> haemorrhagic cystitis (sudden onset of haematuria combined with bladder pain and irritative bladder symptoms)

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22
Q

What is a prodrug?

A

A biologically inactive compound which can be metabolised in the body to produce a drug

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23
Q

What are nitrosoureas? Name some examples

A

Alkylating agents

-lomustine (CCNU), carmustine (BCNU)

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24
Q

How do nitrosoureas work?

A

-highly lipophillic - cross b.b.b. -> CNS tumours

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25
Q

What is carmustine (BCNU), how is it administered and what does it treat?

A
  • nitrosourea - alkylating agent
  • given IV
  • multiple myeloma, non-Hodgkin’s lymphomas, brain tumours e.g. glioblastomas
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26
Q

What is lomustine (CCNU), how is it administered and what does it treat?

A
  • nitrosoureas - alkylating agent
  • given orally
  • Hodgkin’s disease resistant to conventional therapy, malignant melanoma and certain solid tumours
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27
Q

What is busulphan and what does it treat?

A
  • alkylating agent

- selective for bone barrow - leukaemia treatment

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28
Q

What does procarbazine treat and what are its side effects?

A

-alkylating agent

  • used to treat Hodgkin’s disease
  • can cause hypersensitivity rash and inhibits MOA (monoamine oxidase)
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29
Q

What does trabectedin treat and what is a side effect?

A

-alkylating agent

  • soft tissue (skin, adipose tissue, muscle) sarcoma and advanced ovarian cancer
  • hepatotoxic
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30
Q

What class of drugs are platinum compounds? Name some examples

A
  • alkylating agents

- cisplatin, carboplatin, oxaliplatin

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31
Q

What is cisplatin, how does it work, how is it administered and what is it used to treat?

A

-potent alkylator, platinum compound

  • binds to RNA>DNA>protein
  • binds to purine bases (e.g. G, A, U)
  • resistance may develop -> DNA repair by DNA polymerase
  • testicular/ovarian cancer - low levels of repair enzymes so more sensitive to drug, lung, cervical, bladder, head and neck
  • given by slow IV injection/infusion
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32
Q

What are the side effects of cisplatin?

A
  • very nephrotoxic - requires hydration/infusion
  • causes severe N+V
  • risk of tinnitus, peripheral neuropathy, hyperuricaemia (gout) and anaphylaxis
  • numbness/tingling in hands and feet
  • changes in taste
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33
Q

What is carboplatin, what does it treat and what are its side effects?

A
  • platinum compound - alkylating agent
  • derivative of cisplatin
  • less side effects (can be given as out patient) but more myelotoxic (bone marrow suppression)
  • advanced ovarian cancer and lung cancer
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34
Q

What is oxaliplatin and what is it used to treat?

A
  • platinum compound -alkylating agent

- colorectal cancer (with fluorouracil and folinic acid)

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35
Q

What are the classes of antimetabolites?

A

Folate antagonists, pyrimidine analogues, purine analogues

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36
Q

What is folate essential for in the body?

A

DNA synthesis/cell division

37
Q

Name a folate antagonist

A

Methotrexate

38
Q

What is methotrexate and what is its mechanism of action?

A
  • folate antagonist - antimetabolite

- inhibits dihydrofolate reductase

39
Q

How can methotrexate be given?

A

Orally
IM
IV
Intrathecally - between bones of vertebrae

40
Q

What is methotrexate used to treat?

A

Childhood acute lymphoblastic leukaemia
Choriocarcinoma
Non-Hodgkin’s lymphoma
A number of solid tumours

41
Q

Explain about the complications of methotrexate

A
  • low lipid solubility - doesn’t readily cross b.b.b.
  • mostly excreted unchanged in urine - lower doses in patients with renal impairment
  • NSAIDS can reduce excretion - increases toxicity
  • tumour cells may develop resistance
42
Q

What is methotrexate administered with in high doses and what effect does it have?

A
  • given with folinic acid (folate derivative) at high doses

- given to rescue normal cells

43
Q

What other disease apart from cancer is methotrexate used in?

A

Rheumatoid arthritis

-used to suppress immune system

44
Q

Name some pyrimidine analogues and what group of drugs they come from

A

Antimetabolite

Fluorouracil

Capecitabine, cytarabine, gemcitabine

45
Q

How do pyrimidine analogues work?

A

Compete with C and T bases which make up RNA and DNA - inhibits DNA synthesis

46
Q

How are pyrimidine analogues given?

A

Parenterally - IV

-less well absorbed (orally) than methotrexate

47
Q

When is fluorouracil commonly used?

A
  • pyrimidine analogue -antimetabolite
  • commonly used with folinic acid in advanced colorectal cancer
  • may also be used topically for certain malignant and pre malignant skin lesions
48
Q

Name some purine analogues and the group of drugs they are in

A

Antimetabolites

  • fludarabine
  • mercaptopurine, tioguanine, pentostatin
49
Q

How do purine analogues work?

A

-compete with A and G - inhibit purine metabolism

50
Q

What is tioguanine mainly used in the treatment of?

A

Leukaemia

51
Q

Name some cytotoxic antibiotics

A

Doxorubicin, bleomycin

Dactinomycin, mitomycin

52
Q

What is doxorubicin and what is its mechanism of action?

A

-cytotoxic antibiotic

  • binds to DNA and inhibits DNA/RNA synthesis
  • inhibits topoisomerase II (helps to swivel DNA when separating - so when inhibited DNA can’t replicate properly)
53
Q

How are cytotoxic antibiotics administered and what precautions should be taken?

A
  • IV infusion

- must be careful to avoid extravasation at injection site - causes local necrosis (make sure it goes in vein)

54
Q

What are the side effects of doxorubicin?

A

-cardiac dysrhythmias, heart failure in high doses

55
Q

What is bleomycin and what is its mechanism of action?

A

Cytotoxic antibiotic

  • degrades pre-formed DNA
  • active against non-dividing cells (G0 - useful feature)
56
Q

What are the side effects of bleomycin?

A
  • causes little myelosuppression but causes pulmonary fibrosis in 10% pts
  • 50% pts develop mucocutaneous reactions (mouth sores, hair loss, fungal infections etc)
  • hyperpyrexia
57
Q

Name some plant derivatives

A

Vinca alkaloids: vincristine, vinblastine, vindesine

Taxanes: paclitaxel, docetaxel

Etoposide

58
Q

What are vinca alkaloids and what is their mechanism of action and side effects?

A

Plant derivatives

  • derived from Madagascar periwinkle
  • prevent polymerisation of tubulin –> microtubules –> prevents spindle formation
  • effects only occur during mitosis

-relatively non-toxic
(Except vincristine - neuromuscular effects)

59
Q

What are taxanes and what is their mechanism of action and side effects?

A

Plant derivatives

  • derived from bark of yew tree
  • similar mechanism to vinca alkaloids (prevent polymerisation of tubulin–>microtubules–>prevents spindle formation
  • treats adv. breast cancer
  • paclitaxel/carboplatin - ovarian cancer
60
Q

What is Etoposide, what is its mechanism of action and side effects?

A

Plant derivative

  • derived from mandrake root
  • treats testicular cancer/lymphomas
  • must avoid skin contact
  • can cause rapid fall in BP during IV infusion
61
Q

When are hormones used in the treatment of cancer?

A
  • used in treatment of cancers in hormone-sensitive tissues (e.g. breast, prostate, ovaries)
  • tumour growth inhibited by R antagonists, hormones with opposing actions, or drugs which block synthesis of endogenous hormones
  • rarely cure disease but reduce symptoms
62
Q

Name some types of hormones used in cancer treatment

A 
Glucocorticoids
Oestrogens
Progestogens
Gonadotropin-releasing hormone analogues
Antioestrogens
Antiandrogens
63
Q

Name some glucocorticoids

A

Prednisolone

Dexamethasone

64
Q

What else are glucocorticoids used for?

A

Asthma, arthritis

65
Q

How do prednisolone and dexamethasone work in treating cancer

A
  • glucocorticoids
  • inhibit lymphocyte proliferation - treatment of lymphomas/leukaemias

Counter some side effects of other anti-cancer drugs (e.g. N&V)

-used as supportive therapy/in palliative care

66
Q

Name some oestrogens

A

Diethylstilbestrol

Ethinyloestradiol

67
Q

How does Diethylstilbestrol and Ethinyloestradiol work?

A

Oestrogens

  • antagonists of androgen dependant prostate cancer (used in palliative treatment)
  • Diethylstilbestrol sometimes used to treat prostate cancer (not usually 1st line therapy due to side effects)
68
Q

What are the side effects of oestrogens (Diethylstilbestrol and Ethinyloestradiol)?

A
  • nausea
  • fluid retention
  • thrombosis
  • impotence and gynaecomastia
  • stimulate resting mammary cancer cells to proliferate - proliferating cells are more susceptible to drugs (easier to destroy)
69
Q

Name some progestogens and what they are used to treat

A

Megestrol, medroxyprogesterone, norethisterone

-used to treat endometrial cancer

70
Q

Name some gonadotropin-releasing hormone analogues and what they do

A

Goserelin, buserelin, leuprorelin, triptorelin

  • inhibit GnRH release - so lowers LH/FSH - so decreases testosterone
  • used to treat prostate cancer/advanced breast cancer (in pre menopausal women)
71
Q

Name some antioestrogens and what they do

A

Tamoxifen (+ fulvestrant)

-competitive antagonist at oestrogen Rs - inhibits transcription of oestrogen-responsive genes - breast cancer treatment

Tamoxifen - treats oestrogen R-positive breast cancer, also approved for prevention of of cancer in women at high risk of breast cancer in the US

72
Q

What are the side effects of antioestrogens?

A
  • similar to menopausal effects
  • may cause endometrial cancer
  • high risk of blood clots
73
Q

Name some aromatase inhibitors, their mechanism of action and potential side effects

A

Letrozole, exemastine

  • block conversion of androgens to oestrogens in peripheral tissues
  • aromatase = enzyme involved in key stage of oestrogen synthesis
  • don’t inhibit ovarian oestrogen synthesis

-shouldn’t be used in premenopausal women

74
Q

Name some Antiandrogens and what they are used in the treatment of

A

Flutamide, cyproterone, bicalutamide

-androgen antagonists - prostate cancer treatment

75
Q

Name some somatostatin analogues and what they do

A

Octreotide, lanreotide (also treats thyroid tumours)

-inhibit cell proliferation/hormone (CCK/gastrin) secretion - used to treat hormone secreting tumours of GI tract

  • somatostatin secreted by hypothalamus and stomach/intestines - inhibits release of GH/TSH and gut hormones such as gastrin/CCK - red gut motility and gastric emptying and also pancreatitis secretions
  • works because tumours reliant on hormone secretion in order to grow
76
Q

How are monoclonal antibodies produced?

A

By cultured hybridoma cells (hybridoma cells formed by fusing antibody producing B lymphocytes with B cell cancer (myeloma))

77
Q

How are monoclonal antibodies used to treat cancer and what are the +ves and -ves?

A
  • react with specific target proteins expressed on cancer cells - activates immune system - lysis of cancer cells
  • some mAbs activate GF-Rs on cancer cells - inhibit survival/promote apoptosis

+ves - targeted therapy - fewer side effects
-ves - expensive, must be given in combo with other drugs

78
Q

Name some monoclonal antibodies

A

Rituximab, trastuzumab (herceptin), ofatumumab, bevacizumab

79
Q

How does rituximab work, what does it treat and what are its side effects?

A
  • binds to CD20 protein, expressed on certain lymphoma cells - lysis of B lymphocytes
  • effective in 40-50% cases (when combined with trad. chemo)
  • used to treat non-Hodgkin’s lymphoma (only useful if tumour cells express CD20 protein - requires biopsy and staining)
  • hypotension, chills and fever
  • long term - hypersensitivity - can be fatal
80
Q

How does trastuzumab (herceptin) work, what does it treat and what are its side effects?

A
  • binds to HER2 (a GF-R)
  • induces immune response and cell cycle inhibitors
  • HER2 over expressed in 25% of breast cancer patients - rapid proliferation (I.e. aggressive form)
  • given with standard drugs - inc. survival rate

-tremor, flu-like symp, itchy eyes, BP changes, palpitations

81
Q

What is ofatumumab used to treat?

A

Resistant chronic lymphocytic leukaemia

82
Q

What does bevacizumab do and what does it treat?

A
  • colorectal cancer
  • neutralises VEGF, prevents angiogenesis
  • given IV - usually with other drugs
83
Q

Name some protein kinase inhibitors

A

Imatinib, dasatinib, nilotinib

84
Q

How does imatinib work, what does it treat and what side effects does it cause?

A
  • blocks tyrosine kinases involved in GF signalling pathways
  • used to treat chronic myeloid leukaemia (CML) - prev. poor prognosis - 90% sufferers have a chromosome defect (Philadelphia chromosome) which encodes an active tyrosine kinase protein - leads to uncontrolled cell proliferation

-problems with drug resistance (may be primary - poor initial response or acquired - following s period of successful treatment) - if resistant - high dose of imatinib or dasatinib or nilotinib

85
Q

What is the treatment regime of cytotoxic drugs?

A

Often given in combination

  • inc. cytotoxicity without inc. general toxicity (drugs have diff. side effects)
  • decreases chance of developing resistance to individual drugs
  • often given in large doses ever 2-3 weeks (usually over 6 months)
  • allows bone marrow to regenerate - which decreases chance of resistance
  • more effective than several small doses
86
Q

How is the side effect nausea and vomiting controlled?

A
  • needs to be controlled because patient compliance decreases
  • ondansetron, granisetron - 5HT3R antagonists -effective vs. cytotoxic drug induced vomiting
  • metoclopramide - dopamine D2R antagonist
87
Q

How is the side effect anxiety controlled?

A

Lorazepam - anti-anxiety drug (benzodiazepine)

88
Q

How is the side effect myelosuppression controlled?

A

-stem cell transplant
(Autologous - stem cells harvested from patient and if used back after chemo)

(Allogenic - stem cells from matched donor - collected by blood dialysis or bone marrow)

-lenograstim (recombinant GM-CSF) - used to boost stem cell production - speeds recovery of immune system

Pharmacology - Year 2 AC (14 decks)

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