Gonadotrophins

Question 1

What are the main Gonadotropin-affecting drugs? (6)

Answer 1

1. Danazol
2. Cetrorelix
3. Ganirelix
4. Tamoxifen
5. Leuprorelin
6. Triptorelin

Question 2

What are the indications of Danazol? (3)

Answer 2

1. Endometriosis
2. Relief of severe pain and tenderness in benign fibrocystic breast disease
3. Long-term management of angioedema (unlicensed)

Question 3

What is the mode of action of Cetrorelix and Ganirelix?

Answer 3

LH releasing antagonists which inhibit the release of LH and FSH

Used in the treatment of infertility by assisted reproductive techniques

Question 4

What is the mode of action of Danazol?

Answer 4

Anterior pituitary suppressant, inhibiting the pituitary output of gonadotrophins, LH and FSH

Question 5

What are the main gonadorelin analogues? (2)

Answer 5

1. Leuprorelin

2. Triptorelin

Question 6

What are the indications of gonadorelin analogues? (8)

Answer 6

1. Endometriosis
2. Precocious puberty
3. Infertility
4. Male hypersexuality and severe sexual deviation
5. Anemia due to uterine fibroids (together with iron supplementation)
6. Breast cancer
7. Prostate cancer
8. Before intra-uterine surgery to reduce uterine volume, fibroid size and associated bleeding (initiated 3-4 months before surgery)

Question 7

What is the management of breast pain? (3)

Answer 7

1. Rule out any serious underlying pathology
2. Most women will respond to reassurance and reduction in dietary fat
3. Withdrawal of oral contraceptives or HRT

Question 8

What is the management of mild, mid-cyclical breast pain?

Answer 8

Simple analgesics

Question 9

Does Tamoxifen have a role in the treatment of mastalgia?

Answer 9

Yes, may be a useful adjunct in the treatment of mastalgia [unlicensed indication] especially when symptoms can definitely be related to cyclic oestrogen production; it may be given on the days of the cycle when symptoms are predicted

Question 10

What is the mechanism of action of Tamoxifen?

Answer 10

Anti-estrogen which induces gonadotrophins release by occupying estrogen receptors in the hypothalamus, thereby interfering with feedback mechanisms

Question 11

Treatment of breast pain should be reviewed after ________ months and continued if necessary

Answer 11

6

Symptoms recur in about 50% of women within 2 years of withdrawal of therapy but may be less severe

Question 12

What are the indications of tamoxifen? (4)

Answer 12

1. Pre and perimenopausal women with estrogen-receptor-positive breast cancer not previously treated with tamoxifen
2. Anovulatory infertility
3. Gynecomastia (prevention in men undergoing long-term bicalutamide therapy)
4. Breast cancer (chemo-prevention in women at moderate to high risk

Question 13

What is the main contraindication to tamoxifen therapy?

Answer 13

Treatment of infertility contra-indicated if personal or family history of idiopathic venous thromboembolism or genetic predisposition to thromboembolism

Question 14

What are the adverse effets of tamoxifen? (5)

Answer 14

Tamoxifen is a SERM (estrogen receptor antagonist AND partial agonist)

1. Menstrual disturbance (vaginal bleeding, amenorrhea)
2. Hot flushes (3% of patients stop taking it due to climacteric effects)
3. VTE
4. Endometrial cancer

*Raloxifene is a pure estrogen receptor antagonist and carries a lower risk of endometrial cancer

Question 15

What is the indication for cetrorelix?

Answer 15

Adjunct in the treatment of female infertility (initiated under specialist supervision)

Question 16

What are the side effects of cetrorelix?

Answer 16

1: ovarian hyperstimulation syndrome (fertility treatment)

Less common: headache, hypersensitivity, nausea