Pharmaco of Endocrine Cancers Flashcards

1
Q

What class of drug is tamoxifen?

A

Selective Estrogen Receptor Modulator

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2
Q

What is tamoxifen used for

A

Breast cancer

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3
Q

Which isomers display what activity for tamoxifen?

A

Cis-isomer displays estrogenic activity
Trans-isomer displays anti-estrogenic activity

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4
Q

What is tamoxifen’s MOA

A

Competitively blocks endogenous estrogen binding to the estrogen receptor in the target tissue (e.g. breast)

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5
Q

What are the side effects of tamoxifen

A

hot flashes, increased risk of endometrial and uterus cancer (from cis-isomer accumulating in the uterus), DVT, menstrual irregularities, vaginal bleeding and discharge, nausea and vomiting

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6
Q

What toxicity is associated with tamoxifen?

A

High doses can lead to neurotoxicity

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7
Q

What class of drug is pembrollizumab?

A

Anti-PDL1 antibody

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8
Q

What is pembrolizumab’s MOA

A

Binds to PDL1 and blocks the masking effect, allowing T cells to kill the cancerous cells

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9
Q

How often should pembrolizumab be given?

A

every 3 weeks

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10
Q

What is pembrolizumab used for

A

Cervical cancer

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11
Q

What are the side effects associated with pembrolizumab?

A

Infusion related SE like rash and itch from hypersensitivity, fatigue, diarrhea, nausea, joint pain, possible life threatening immune-related inflammation on lungs, endocrine organs, liver, kidneys and sepsis

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12
Q

In which patient groups is pembrolizumab contraindicated in? (2)

A

Patients taking corticosteroids or immunosuppressants (stop for the course of medicine and can continue after)
Avoid in pregnant women

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13
Q

What class of drug is leuprorelin?

A

GnRH analogue

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14
Q

What is leuprorelin’s MOA?

A

Leuprorelin agonises pituitary GnRH receptors (negative feedback) and decreases testosterone production and decreases the stimulatory effect on androgen-sensitive prostate cancer cells, inducing apoptosis

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15
Q

What can be measured for patients on leuprorelin therapy?

A

PSA for first few weeks
LH, FSH and testosterone after 4 weeks (stabilise)

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16
Q

How often should leuprorelin be given?

A

Single dose LA depot at the 1 to 3/4 month interval

17
Q

What are the side effects of leuprorelin?

A

Local pain at site of injection (may act on nerves, especially depot), flushes, headaches and migraines, altered mood, hyperglycemia, hyperlipidemia, loss of libido, impotence

18
Q

What patient groups are contraindicated in leuprorelin use? (3)

A
  1. Hypersensitivity to GnRH agonists
  2. Preexisting HD
  3. Patients with osteoporosis risk
19
Q

What class of drug is bicalutamide?

A

Androgen receptor antagonist

20
Q

What is bicalutamide’s MOA?

A

Inhibits nuclear translocation of the androgen receptor and its interaction with the promoter, impairing cel proliferation and triggering apoptosis

21
Q

What are the side effects of bicalutamide

A

gynecomastia, sexual dysfunction, fatigue, GI disturbances, seizures (rare)