Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Oncology > Anti Cancer Therapies > Flashcards

Anti Cancer Therapies Flashcards

1
Q

Cancer Drugs

A

-Tamoxifen
-Letrozole
-CDK4/6 inhibitors (eg palbociclib)
-Exemestane
-Goserelin
-Trastuzumab
-Imatinib
-Rituximab
-Capecitabine
-Zolendronic acid
-Pembrolizumab

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Mechanism of Tamoxifen

A

-SERM (Selective Oestrogen Receptor Modulator)
-Acts on oestrogen receptors
=Can act in an oestrogenic way or an anti-oestrogenic way, depending on the tissue

-Active in many tissues including breast, uterus, bone, liver, hypothalamus
=Breast: acts as an oestrogen receptor ANTAGONIST, i.e. anti-oestrogen activity
=Uterus: acts as an oestrogen-receptor agonist, which can cause endometrial hyperplasia - increased risk of uterine malignancy
=Bone: acts as an oestrogen-receptor agonist; inhibiting osteoclasts and therefore protecting against osteoporosis

-Requires metabolism in the liver by CYP450 enzymes to convert into the active form

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Indications of Tamoxifen

A

-Adjuvant treatment of ER positive breast cancer in pre-and post- menopausal women
=Early breast cancer
=Metastatic breast cancer
-Treatment of ER positive breast cancer in men
-(Primary prevention of breast cancer in women with a very strong family history)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Tamoxifen side effects

A

-Hot flushes in approx. 50%
-PV bleeding
-Fatigue
-Weight gain
-Less common
=Anaemia, cataracts, changes in LFTs, alopecia, elevated triglycerides

-SSRIs such as sertraline, paroxetine & fluoxetine decrease plasma level of tamoxifen (SSRIs inhibit CYP2D6 inhibitors so can prevent formation of active drug)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Main serious toxicities of Tamoxifen

A

-Increased risk of thrombotic disease
=Avoid if personal or family history of VTE; stop if clot
-Endometrial cancer (vaginal bleeding & polyps)
=Counsel patients
=Ix any new/changing PV symptoms early with gynae ref
-Avoid in pregnancy and breast feeding
-Radiation Recall dermatitis (rare!)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Mechanism of letrozole

A

-Aromatase Inhibitor
=Aromatase catalyses the last steps of oestrogen synthesis from androgens, transforming: Androstenedione to oestrone then Testosterone to oestradiol
=Competitively and reversibly binds to heme portion of cytochrome P450 unit of the aromatase enzyme= Inhibits the activity of aromatase= results in reduced levels of plasma oestrogen

Main source of oestrogen in pre-menopausal women is ovarian
-In post-menopausal women, most of the body’s oestrogen is produced via conversion of androgens into oestrogens by aromatase enzymes in peripheral tissues

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Indications of letrozole

A

-Neo-adjuvant treatment: in post menopausal women with ER positive cancer pre-operatively
-Adjuvant treatment
=Post-menopausal women with ER+ early breast Ca
=High risk pre-menopausal women with ER+ early breast Ca (+ LHRH analogue)
-Palliative treatment: in metastatic disease - post-menopausal women with ER+ breast Ca

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Common side effects of letrozole

A

-Myalgia & arthralgia (~70-80%)!!!
-Bone pains
-Hypercholesterolaemia
-Headaches
-Hot flushes, nausea
-Depression
-Alopecia
-Osteoporosis risk
-Avoid in renal impairment

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Mechanism of exemestane

A

-Steroidal aromatase inhibitor
-Suppresses synthesis of oestrogen; same MOA as letrozole
-BUT greater androgenic effect - so less hair thinning & assoc SEs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Indications of Exemestane

A

-Adjuvant treatment of ER positive early breast cancer in post menopausal women (or pre-menopausal with ovarian blockade)
-Alternative to letrozole if adverse effects
-Metastatic disease/palliative setting for disease control

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Drug interactions of Exemestane

A

CP450 inducers reduce the bioavailability of exemestane

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Common side effects of Exemestane

A

-Hot flushes and sweating (10%)
-Arthralgia
-Osteoporosis (note this is steroidal, so additional impact on bone mineral density)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Serious side effects of Exemestane

A

-Deranged LFTs
-Acute generalised exanthematous pustulosis (AGEP) (also called Toxic Pustuloderma in some books)
=Uncommon pustular drug eruption
=Classified as a severe cutaneous adverse reaction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Mechanism of Goserelin

A

-LHRH (luteinizing hormone-releasing hormone) agonist
-Also known as LNRH analogue or Gonadotropin-releasing hormone (GnRH)
-LHRH is produced in the hypothalamus

-Synthetic analogue of LHRH
-Initial phase of stimulation (FLARE) with initial release of FSH & LH
—>down regulation of gonadotrophin-releasing hormone receptors
—> desensitisation of pituitary to gonadotrophin-releasing hormone
—> decreased secretion of LH & FSH from pituitary

-SO:
=Reduction of gonadotrophin release
=Inhibition of androgen and oestrogen production

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Licensed indications for Zoladex

A

-Prostate Cancer
=Neo-adjuvant (prior to XRT)
=Adjuvant (post XRT or radical prostatectomy)
=Metastatic setting

-Breast Cancer
=Pre menopausal women as adjuvant treatment
=Advanced breast cancer

-Gynaecology
=Endometriosis
=Pre op in women with fibroids and anaemia
=Fertility treatments

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Drug interactions/ contraindications of Zoladex

A

-Undiagnosed vaginal bleeding
-Prostate cancer patients at risk of:
=MSCC
=Ureteric obstruction
-Caution in
=Diabetes/hypertension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Common toxicities of Zoladex

A

-Arthralgia and bone pain
-Gynaecomastia
-Heart failure
-Hot flushes
-Hyperhidrosis
-Sexual dysfunction: decreased libido, impotence
-Altered mood

18
Q

Serious side effects of Zoladex

A

-Tumour Flare
=MSCC
=Ureteric obstruction
-Psychotic disorder

19
Q

Mechanism of action of Herceptin/ Trastuzumab

A

-Monoclonal antibody that targets HER2 receptors expressed on the surface of some breast and gastric cancers
—> inhibits HER2 signalling pathways
—> induces apoptosis
-HER2 receptors are transmembrane receptors that have a key role in the signalling network that drives cell proliferation

-A monoclonal antibody targeting HER2.
-The HER2 pathway promotes cell growth and division when it is functioning normally; however, when it is over expressed, rapid cell growth and proliferation occur tumour formation and growth. Trastuzumab induces an immune-mediated response that down regulates HER2

20
Q

Licensed indications of Herceptin

A

-Early breast cancer that over expresses human epidermal growth factor 2 (HER2). This is approximately 20-30% of all early breast cancers
=Neo adjuvant
=Adjuvant
-Metastatic HER2 positive breast cancer
-Metastatic HER2 positive gastric cancer

21
Q

Common side effects of Herceptin

A

-Angioedema
-Infusion related reaction (50%)
-Flu like symptoms (very common!)
-Nausea

22
Q

Serious toxicities and drug interactions of Herceptin

A

-Severe infusion related reaction
-Thrombocytopaenia
-Cardiac toxicity:
=In 2-7% of patients, trastuzumab is associated with cardiac dysfunction, which includes congestive cardiac failure.
=Co-administration with anthracycline chemotherapy (-rubicin) increase this risk
=How do we monitor cardiac function? What specifically are we monitoring?
-Harmful to foetus

23
Q

Mechanism of action of Imatinib (Glivec)

A

-Targeted therapy, given orally
-Tyrosine kinase inhibitor
-Tyrosine kinases are important mediators of the cell signalling cascade. They phosphorylate tyrosine residues(phosphorylation – addition of a phosphate group)
-Tyrosine kinase inhibitors acts by inhibiting cell proliferation

24
Q

Licensed indications of Imatinib

A

-Treatment of Chronic Myeloid Leukaemia (CML)
-Treatment of Philadelphia positive
Acute Lymphoblastic Leukaemia (ALL)
-Adjuvant treatment of high risk GIST

25
Q

Drug Interactions of Imatinib

A

-Paracetamol
-Simvastatin
-Warfarin

26
Q

Common side effects of Imatinib

A

-Nausea and vomiting
-Facial oedema
-Muscle cramps and bone pain
-Diarrhoea
-Skin rash
-Mild fever

27
Q

Serious side effects of Imatinib

A

-Pancytopaenia
-Liver toxicity
-Thromboembolic events
-Reactivation of Hepatitis B infection
-Risk of severe CHF or left ventricular dysfunction
-Fetotoxic
-Risk of serious fluid retention

28
Q

Mechanism of action of Rituximab

A

-Monoclonal antibody that targets the CD20 antigen
-Binds to CD20 and mediates B-cell lysis (is an anti-CD20’)
-IV injection

-Many functions, not all of which are understood.
-What you need to remember is: It downregulates the B cell receptor
= It induces apoptosis of CD20+ cells

29
Q

Licensed indications of Rituximab

A

-Malignant disease
=Relapsed/refractory CLL
=Diffuse large B cell lymphoma
-Benign disease
=Rheumatoid arthritis

30
Q

Drug Indications of Rituximab

A

-Significant number of interactions
-As with trastuzumab (Herceptin), live vaccines are contra-indicated due to increased risk of generalised infection

31
Q

Common side effects of Rituximab

A

-Angioedema
-Bone marrow disorders

32
Q

Serious side effects of Rituximab

A

-Infusion related reaction
-Cytokine release syndrome
-Haemolytic anaemia
-Progressive multifocal leukoencephalopathy (JC virus)
-Hepatitis B reactivation

33
Q

Mechanism of action of Capecitabine

A

-Oral pro-drug of 5-fluorouracil (5-FU), meaning patients have quicker and more convenient dosing
-Anti metabolite that inhibits thymidylate synthase (TS)Thymidylate synthase (TS) is a DNA repair enzyme.
-Inhibition of TS leads to DNA damage that is fatal as cannot be repaired —> cell apoptosis

34
Q

Licensed indications of Capecitabine

A

-Colorectal cancer
=Adjuvant
=Metastatic

-Advanced Gastric cancer
=In combination with platinum chemotherapy

-Breast cancer
=Locally advanced and metastatic disease
=Role in adjuvant therapy in some subsets of early breast cancer (eg TNBC)

35
Q

Drug interactions of Capecitabine

A

-Avoid in patients with Dihydropyridine dehydrogenase deficiency (DPD deficiency) – they lack enough of the enzyme / enzyme activity to appropriately process capecitabine. This causes serious, potentially life-threatening toxicity.
-Allopurinol
- Folic acid
-Metronidazole

36
Q

Common side effects of Capecitabine

A

-Diarrhoea – very, very common
-Fatigue
-Pancytopenia
-Palmar-plantar syndrome

37
Q

Serious side effects of Capecitabine

A

-Severe diarrhoea: dehydration ++
-Acute coronary syndrome
-QT prolongation
-Severe cutaneous adverse reaction

38
Q

Mechanism of action of Zoledronic acid

A

-Inhibit osteoclastic bone resorption
-Given IV; dose dependent on renal function

39
Q

Licensed indications of Zoledronic acid

A

-Prevention of skeletal related events: in adjuvant treatment of high-risk breast cancer, or in metastatic breast cancer
-Malignant hypercalcaemia
-Used off licence for intractable bone pain secondary to bone metastases
-Osteoporosis: probably the commonest reason for bisphosphonates to be prescribed in the UK - alendronic acid

40
Q

Common side effects of zoledronic acid

A

-Oesophagitis / discomfort if given orally –advise to take with a full glass of water and sit up for 30 minutes after(alendronic acid)
-Flu like symptoms & arthralgia
-Bone pain
-Flushing

41
Q

Serious side effects of zolendronic acid

A

-Anaphylaxis/infusion reaction
-Osteonecrosis of the jaw rare but serious
-Atypical femoral fractures
-Thrombocytopaenia
-Renal impairment
- N.B. management of hypercalcaemia of malignancy

42
Q

Describe osteonecrosis of the jaw

A

-Rare side effect of bisphosphonates
-Mandible exposed e.g. post dental extraction
-Bone becomes deprived of oxygen
-Bone weakens and becomes necrotic
-Minimise by dental assessment prior to initiation of therapy and regularly on treatment

Oncology (9 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions