W32/L6

Question 1

What does SERM stand for?

Answer 1

Selective oestrogen receptor modulators

Question 2

What drug is an ER-antagonist in the breast & CNS?

Answer 2

Tamoxifen

Question 3

Tamoxifen is an ER-agonist in which tissues?

Answer 3

Uterus
Bone
Cadriovascular

Question 4

Which SERM carries a heightened risk of endometrial hyperplasia and why?

Answer 4

Tamoxifen - it’s a uterine ER-agonist

Question 5

Which drug is an ER-antagonist in the breast, uterus and CNS?

Answer 5

Raloxifene

Question 6

Raloxifene is an agonist in which tissues?

Answer 6

Bone

Cardiovascular

Question 7

What are the A/E of tamoxifen?

Answer 7

Edometrial hyperplasia
Thromboemolus
Thrombocytopoenia
Ocular toxicity
Menopausal symptoms

Question 8

What do we use tamoxifen for and why?

Answer 8

Breast cancer, as many breast cancers have increased expression of the ERs

Question 9

Which enzyme is responsible for the production of oestrogens?

Answer 9

Aromatase

Question 10

Aromatase converts which two substrates into which two products?

Answer 10

Androstenedione -> oestrone

Testosterone -> oestradiol

Question 11

What’s an example of an aromatase inhibitor?

Answer 11

Exemestane

Question 12

When are aromatase inhibitors used?

Answer 12

Breast cancer for improved disease-free survival after tamoxifen

Question 13

5alpha-reductase converts which substrate into which product?

Answer 13

Testosterone to DHT

Question 14

Define priapism

Answer 14

A persistant and painful erection

Question 15

What are the coronary A/E of androgens?

Answer 15

Increased LDL
Decreased HDL
= increased risk of CHD

Question 16

What are the A/E of androgens in women?

Answer 16

Ance
Facial hair
Deepened voice
Male pattern baldness
Menstrual irregularities

Question 17

What are the A/E of androgens in men?

Answer 17

Priapism
Impotence
Decreased spermatogenesis
Gynaecomastia

Question 18

What are the A/E of androgens in children?

Answer 18

Premature close of epiphysial plates

Abnormal sexual d’ment

Question 19

What’s an example of a steroidal androgen antagonist?

Answer 19

Cyproterone

Question 20

What’s an example of a non-steroidal androgen antagonist?

Answer 20

Flutamide

Question 21

What’s an example of a 5alpha-reductase inhibitor?

Answer 21

Finasteride

Question 22

What are the A/E of 5alpha-reductase inhibitors

Answer 22

Impotence, decreased libido and ejaculation problems

Breast enlargement, tenderness and breast cancer

Question 23

What’s the mechanism for breast changes with Finasteride

Answer 23

Blocked conversion to DHT means a build up in testosterone, which means more substrate for the aromatases to convert to oestrogen.