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endo > CANCER > Flashcards

CANCER Flashcards

1
Q

tamoxifen - general

A
  • cis isomer: oestrogenic activity
  • trans isomer: anti-oestrogenic activity
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2
Q

tamoxifen indication

A

1) breast cancer
2) pre & post menopausal women
3) useful in chemoprevention of breast cancer at high risk
4) reduce severity of osteoporosis

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3
Q

tamoxifen - MOA

A
  • tumour cell respond to oestrogen -> proliferate & grow
  • competitively block endogenous oestrogen binding to oestrogen receptor in target tissue -> prevent binding & dissociate from AF-2 -> partially block translation & transcription
  • tamoxifen ER complex enter nucleus -> bind to DNA -> suppress cell division & proliferation protein & signals
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4
Q

tamoxifen - PK - absorption

A
  • oral
  • rapidly & extensively absorbed in intestine
  • peak time 5 hrs after ingestion
  • Css after 3-4 wks up to 16 wks
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5
Q

tamoxifen - PK - distribution

A
  • albumin bound
  • Vd 50-60 L/kg
  • concentrate in breast, uterus, ovary tissue
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6
Q

tamoxifen - PK - metabolism

A

1) CYP2D6

  • 4-OH-tamoxifen (anticancer) -> by CYP3A4 -> endoxifen

2) CYP3A4 -> N-desmethyl-tamoxifen -> by CYP2D6 -> endoxifen (most active metabolite)

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7
Q

tamoxifen - PK - elimination

A

shit

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8
Q

tamoxifen - interactions

A

1) food drug: grapefruit juice
2) DDI: diphenhydramine

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9
Q

tamoxifen SE

A

1) hot flash
2) increase risk of endometrial cancer
3) DVT
4) menstrual irregularities
5) vaginal bleeding & discharge
6) N/V

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10
Q

tamoxifen tox

A
  • high dose
  • neurotox: tremor, hyperreflexia, unsteady gait, dizziness
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11
Q

pembrolizumab - indication

A

cervical cancer

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12
Q

pembrolizumab - MOA

A

1) PD-1

  • expressed by T cell
  • recognise certain ligands (PD-L1, PD-L2)
  • PD-1 + PD-L1 -> inhibit T cell activation -> evade immune system

2) PD-1 blocker

  • bind to PD-1 -> prevent PD-L1 & PD-L2 from cancer cells from binding -> release PD-1 pathway mediated inhibition of T cell activities
  • block cancer metastasis
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13
Q

pembrolizumab - dose

A

IV 200mg over 30 mins every 3 wks

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14
Q

pembrolizumab - PK

A
  • distribution: small Vd, limited extravascular distribution
  • metabolism: nonspecific
  • t1/2 27 days, Css after 19 wks
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15
Q

pembrolizumab - SE

A

1) infusion related SE
2) Fatigue
3) N/D
4) joint pain
5) life-threatening

  • immune-related inflammation on lung, endocrine organs, liver, kidney, sepsis
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16
Q

pembrolizumab - CI

A

1) corticosteroids/immunosuppressant

  • stop -> start pembrolizumab -> continue

2) X pregnant (increase miscarriage risk)
3) hypersensitivity to other Ab therapy
45) infection, kidney/liver disease

17
Q

S&S of prostate cancer

A

1) difficulty urinating
2) low stream of urine
3) frequent nocturia
4) constant need to pee
5) dark reddish urine
6) weak/swollen lower limb
7) back pain

18
Q

lab values for prostate cancer

A

prostate specific antigen

  • 10 - 100 range
  • normal below 5
19
Q

how to achieve androgen deprivation

A

1) inhibit pituitary gonadotropin release

  • Leuprorelin

2) inhibit androgen synthesis

  • finasteride

3) inhibit androgen binding

  • androgen receptor blockers (flutamide)

4) surgical extirpation of glands

  • castration, adrenalectomy
20
Q

pharmaco strategies for prostate cancer - list

A

1) target upstream pathway/trigger: leuprorelin
2) direct blockage of hormone acting on its receptor: bicalutamide

21
Q

leuprorelin - general

A
  • GnRH analogue
  • GLP-1 agonist
22
Q

leuprorelin - MOA

A
  • decreased androgen (testosterone) production in testes -> minimise positive effect on androgen-sensitive prostate cancer cell -> cancer cell apoptosis
  • continuous administration -> decrease FSH & LH release -> suppress androgen synthesis
23
Q

leuprorelin - monitoring

A
  • prostate-specific antigen (PSA)
  • LH, FSH, serum testosterone after 4 wks of therapy
24
Q

leuprorelin - PK - absorption

A
  • SC/IM single dose long acting depot
  • interval between injection vary depending on dose (1/3/4 month interval)
  • Cmax 1-3 hrs
  • Css 4 wks
25
Q

leuprorelin - PK - distribution

A

Vd 27L after IV, 45% plasma protein binding

26
Q

leuprorelin - PK - metabolism

A
  • degraded proteolytically (potentially by peptidases) -> inactive peptides
  • t1/2 3 hrs
    ** D-leucyl residue help increase circulating t1/2 from 3-4 min to 3 hr
  • X metabolised in liver by CYP450
27
Q

leuprorelin - SE

A

1) local pain & redness @ injection site
2) hot flush during first few wks
3) headache/dizzy
4) GI disturbances
5) altered mood
6) hyperglycaemia
7) decreased libido

28
Q

leuprorelin - CI

A

1) hypersensitivity to leuprorelin or other GnRH agonist
2) pre-existing heart disease
3) pt w risk for osteoporosis

29
Q

bicalutamide - general

A
  • androgen receptor antagonist
  • stereoisomerism: possible racemic
30
Q

bicalutamide - indication

A

1) X monotherapy of prostate cancer

  • block androgen receptor = increase LH secretion = higher serum testosterone levels

2) conjunction w GnRH analogue -> alleviate effect of testosterone surge (tumour flare)

  • tumour flare in treatment of metastatic prostate cancer

3) androgen depriving therapy

  • initiation of LHRH agonist
  • reduce symptoms of tumour flare in pt w metastatic prostate cancer

4) locally advanced disease

    • radiation therapy/surgery
  • increase survival
31
Q

bicalutamide - PK

A

1) absorption

  • well absorbed orally
  • X affected by food
  • oral OD + GnRH analogue

2) distribution

  • highly plasma protein bound

3) metabolism

  • extensive in liver
  • stereoselective
    ** (S) -> inactive, rapidly cleared by glucuronidation
    ** (R) -> active, slow hydroxylation (CYP3A4) -> glucuronidation

4) elimination

  • parent + metabolite in bile, shit, urine
32
Q

bicalutamide - SE

A

hot flush, N/V, decreased sexual desire/ability, fatigue, C/D, mild swelling ankles/legs/feet

33
Q

bicalutamide - CI

A

women & children
known hypersensitivity

34
Q

bicalutamide - MOA

A
  • competitively antagonise androgen receptor
  • inhibit nuclear translocation of AR & interaction of AR w promoter at AR response element -> impair cell proliferation -> trigger apoptosis
  • androgen deprivation = reduced progression of prostate cancer

endo (8 decks)

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