Contraceptives, HRT and SERMs

Question 1

What is climacteric

Answer 1

Period of transition to the menopause

Question 2

what is menopause

Answer 2

• Permanent cessation of menstruation

- Loss of ovarian follicular activity

Question 3

Average age of menopause

Answer 3

• Average age 51 (range 45-55)

Question 4

Symptoms of menopause? (6)

Answer 4

• Hot flushes (head, neck, upper chest)
• Urogenital atrophy and dyspareunia
• Sleep disturbance
• Depression
• Decreased libido
• Joint pain

Question 5

What happens to levels of oestradiol and inhibin during menopause and why

Answer 5

Low levels of oestradiol and inhibin B because of the follicular atresia

Question 6

What are the Gonadotrophin levels in menopause

Answer 6

there is less negative feedback due to oestrogen and inhibin levels falling bc of follicular atresia so gonadotrophin levels go up
So in a 55 year old woman you’d expect the LH and FSH to be HIGH

Question 7

2 main complications of menopause?

Answer 7

1. Osteoporosis

2. Cardiovascular disease

Question 8

pathogenesis of osteoporosis in menopause

Answer 8

Oestrogen deficiency leads to Loss of bone matrix

Question 9

pathogenesis of Cardiovascular disease in menopause

Answer 9

Oestrogen protects against CVD, this goes when oestrogen goes and by 70- men and women gave the same risk of CVD

Question 10

what does HRT aim to control

Answer 10

the vasomotor symptoms (hot flushes)

Question 11

what does HRT consist of

Answer 11

oestrogen and progestogen

Question 12

What does oestrogen do if prescribed by itself

Answer 12

• Causes endometrial proliferation Prevents endometrial hyperplasia
• Risk of endometrial cancer if you just give oestrogen

Question 13

what conditions do you only prescribe E in HRT and why

Answer 13

If they’ve had a hysterectomy, as then they have no uterus so no worry of endometrial hyperplasia

Question 14

what is a hysterectomy

Answer 14

uterus removal

Question 15

4 ways of administering E?

Answer 15

• Oral oestradiol (1mg)
• Oral conjugated equine oestrogen (0.625mg)
• Transdermal (patch) oestradiol (50microgram/day)
• Intravaginal For those with dyspareunia

Question 16

How to avoid the high first pass metabolism of E?

Answer 16

• Ethinyl oestradiol A semi-synthetic oestrogen Ethinyl protects from first pass metabolism

Question 17

Side effects of HRT? (5)

Answer 17

• Breast cancer
• Coronary heart disease
• Deep vein thrombosis (DVT)
• Stroke
• Gallstones

Question 18

What population has an increased risk of CHD if they take HRT?

Answer 18

women who entered menopause 10< years ago

Question 19

What population do not have an increased risk of CHD if they take HRT?

Answer 19

women who entered menopause <10 years ago

Question 20

why it can be bad for older women to take oestrogen

Answer 20

as it has prothrombotic effects and older women may have a level of atherosclerosis

Question 21

Why might adding progesterone to oestrogen be not good

Answer 21

it negates some of its cardioprotective effects

Question 22

What actions does tibolone have

Answer 22

• Oestrogenic, progestogenic and weak androgenic actions

Question 23

What does tibolone increase the risk of

Answer 23

stroke

breast cancer

Question 24

What does tibolone reduce the risk of

Answer 24

fracture risk

Question 25

What type of drug is raloxifene

Answer 25

SELECTIVE OESTROGEN RECEPTOR MODULATOR (SERM)

Question 26

what does raloxifene do

Answer 26

- Oestrogenic in BONE:  Reduces risk of vertebral fractures - ANTI-oestrogenic in BREAST and UTERUS  Reduces breast cancer risk

Question 27

bad thing about raloxifene (3)

Answer 27

- Does not reduce vasomotor symptoms | - Increases risk of fatal stroke and venous thromboembolism (VTE)

Question 28

what does TAMOXIFEN do and what is it used for

Answer 28

- Anti-oestrogenic on breast tissue | - Used to treat oestrogen-dependent breast tumours and metastatic breast cancers

Question 29

Reasons for menopause before 40 (4)

Answer 29

- Autoimmune - Surgery - Chemotherapy - Radiation

Question 30

What do combined oral contraceptives consist of

Answer 30

Oestrogen (ethinyl oestradiol) + progestogen (e.g. lovonorgestel or norethisterone)

Question 31

What does the combined oral contraceptive do

Answer 31

Suppresses ovulation

Question 32

What does oestrogen and progesterone do together in a combined oral contraceptive

Answer 32

E+P: Negative feedback actions at hypothalamus/pituitary axis

Question 33

What does progesterone do in a combined oral contraceptive

Answer 33

Thickens cervical mucus

Question 34

How does an oral combined contraceptive suppress ovulation

Answer 34

 E+P: Negative feedback actions at hypothalamus/pituitary axis  P thickens cervical mucus

Question 35

When do you prescribe progesterone only contraceptives

Answer 35

When oestrogens are contra-indicated Smoker, >35yrs old, migraine with aura

Question 36

What is key about taking the progesterone only contraceptive

Answer 36

Must be taken same time every day

Question 37

Half life and duration of action of the progesterone only contraceptive

Answer 37

 Short half-life |  Short duration of action

Question 38

How often do you taken the EP contraceptive pill

Answer 38

- Take for 21 days (or 12 weeks), stop for 7 days

Question 39

Emergency contraception? (3)

Answer 39

- Copper IUD (intrauterine contraceptive device) - Levonorgestrel (within 72 hours) - Ulipristal (up to 120hrs after intercourse)

Question 40

What activity does ulipristal have

Answer 40

Anti-progestin