Contraceptives, HRT & SERMS Flashcards

1
Q

Which of the following is a common symptom of menopause?

A. Sleep disturbance
B. Headache
C. Chest pain
D. Breathlessness
E. Leg swelling
A

A

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Define menopause

A

Permanent cessation of menstruation

DUE TO

Loss of ovarian follicular activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Average age when menopause occurs>

A

51 (45 - 55)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Define climacteric

A

Period of transition from predictable ovarian unction through the postmenopausal years

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

MAIN symptoms of menopause?

A

x Hot flushes (head, neck, upper chest)

x Urogenital atrophy

x Dyspareunia - painful sex

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Other symptoms of menopause?

A

x sleep disturbance
x depression
x decreased libido
x joint pain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Normal hormone levels before menopause?

A

o Hypothalamus:
GnRH = HIGH

o Pituitary:
LH & FSH = HIGH

o Ovaries:
Oestradiol & inhibin B = HIGH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Hormone levels after/during menopause?

A

o Hypothalamus:
GnRH = HIGH

o Pituitary:
LH & FSH = HIGH

(as NO -ve feedback from oestradiol & inhibin B)

o Ovaries:
Oestradiol & inhibin B = LOW

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

2 major complications of menopause?

A

o Osteoporosis

  • oestrogen deficiency
  • loss of bone matrix
  • 10x increase risk of fracture

o CVD

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Main treatment for menopause?

A

HRT

Hormone replacement therapy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Which HRT will you normally prescribe?

A. Only Oestrogen
B. Only PG
C. Both E + PG

A

C! - prevents endometrial hyperplasia

x if only give E, increase risk of endometrial cancer due to ENDOMETRIAL PROLIFERATION so need to also give PG

x only if someone has had a hysterectomy can give E alone as no risk of cancer (due to NO endometrium)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Typical HRT forumlation?

A

Either:

o Cyclical:

  • E (every day)
  • PG (12-14 days in)

o Continuous combined

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

How can Oestrogen be prepared for HRT?

A

o Oral estradiol (1mg)

o Oral conjugated equine oestrogen (0.625mg)

o Transdermal (patch) oestradiol (50microgram)

o Intravaginal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Why is the ORAL dose of oestrogen larger than the others?

A

As undergoes FIRST-PASS METABOLISM

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Different types of oestrogens that can be taken?

A

o Estradiol (oral)

o Estrone sulphate (conjugated oestrogen)

o Ethinyl estradiol (semi-synthetic oestrogen)
- the ethinyl group protects the molecule from first-pass metabolism

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Risk of HRTs?

A

BCD

B - breast cancer
C - coronary HD
D - DVT

Stroke
Gallstones

BUT ABSOLUTE risk is VERY LOW

17
Q

3 drugs used for HRT?

A

o Tibolone

o Raloxifene

o Tamoxifen

18
Q

Tibolone?

A

Synthetic prohormone:
x oestrogenic, progestogenic & weak androgenic actions

  • reduces fracture risks
    BUT
    o increased risk of stroke
    o ? increased breast Ca risk
19
Q

SERMs?

A

Selective
Oestrogen
Receptor
Modulator

20
Q

Raloxifene?

A

SERM

o Tissue-selective

  • oestrogenic in bone (reduces fracture risk)
  • anti-oestrogenic in breast & uterus (reduces breast Ca risk)

o INCREASES risk of fatal stroke & VTE
o Does NOT affect vasomotor symptoms

21
Q

Tamoxifen?

A

Anti-oestrogenic on breast tissue

Used to treat:
o oestrogen-dependent breast tumours

o metastatic breast cancers

22
Q

Premature Ovarian insufficiency?

A

Menopause occurring BEFORE <40years

1% of women

23
Q

COCs?

A

Combined Oral Contraceptives

o E (ethinyl oestradiol)
\+ PG (e.g. levonorgestrel OR norethisterone)
24
Q

How does COCs work?

A

Suppresses ovulation:

o -ve feedback on E & PG on hypothalamus and P.G

o PG thickens cervical mucus

o O upregulates PG receptors

o O counteracts androgenic effects of synthetic PGs

Taken for 21 days (or 12 weeks) and stopped for 7 days

25
Q

Progesterone only contraceptive?

A

When E is not a good idea to take:
i.e. smoker, >35 years old, migraine w aura

Must be taken at SAME TIME each day as:
o short half-life
o short duration of action

Longer-acting preparation may be given via. intra-uterine system

26
Q

Emergency contraception?

A

Post-coital contraception!

3 examples:

o Copper IUD

  • exclude pregnancy first
  • affects sperm viability & function
  • effectiveness NOT reduced in obese women
  • 5 (up to 7) days after sex

o Levonorgestrel
- within 72hours of sex

o Ulipristal

  • anti-progestin activity
  • delays ovulation by 5 days
  • impairs implantation
  • up to 120hours after sex
27
Q

Issues with lack of oestrogen?

A

o osteoporosis

o fractures

28
Q

Issues with oestrogen in general?

A

o Increased weight

  • water retention
  • fat deposition

o CVS problems
- increased risk of fatal stroke & VTE

o Breast growth
- oestrogen-dependent cancers

o Endometrium
- proliferative effects

o Nausea
o Headache