Contraceptives, HRT & SERMS Flashcards
Which of the following is a common symptom of menopause?
A. Sleep disturbance B. Headache C. Chest pain D. Breathlessness E. Leg swelling
A
Define menopause
Permanent cessation of menstruation
DUE TO
Loss of ovarian follicular activity
Average age when menopause occurs>
51 (45 - 55)
Define climacteric
Period of transition from predictable ovarian unction through the postmenopausal years
MAIN symptoms of menopause?
x Hot flushes (head, neck, upper chest)
x Urogenital atrophy
x Dyspareunia - painful sex
Other symptoms of menopause?
x sleep disturbance
x depression
x decreased libido
x joint pain
Normal hormone levels before menopause?
o Hypothalamus:
GnRH = HIGH
o Pituitary:
LH & FSH = HIGH
o Ovaries:
Oestradiol & inhibin B = HIGH
Hormone levels after/during menopause?
o Hypothalamus:
GnRH = HIGH
o Pituitary:
LH & FSH = HIGH
(as NO -ve feedback from oestradiol & inhibin B)
o Ovaries:
Oestradiol & inhibin B = LOW
2 major complications of menopause?
o Osteoporosis
- oestrogen deficiency
- loss of bone matrix
- 10x increase risk of fracture
o CVD
Main treatment for menopause?
HRT
Hormone replacement therapy
Which HRT will you normally prescribe?
A. Only Oestrogen
B. Only PG
C. Both E + PG
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)
Typical HRT forumlation?
Either:
o Cyclical:
- E (every day)
- PG (12-14 days in)
o Continuous combined
How can Oestrogen be prepared for HRT?
o Oral estradiol (1mg)
o Oral conjugated equine oestrogen (0.625mg)
o Transdermal (patch) oestradiol (50microgram)
o Intravaginal
Why is the ORAL dose of oestrogen larger than the others?
As undergoes FIRST-PASS METABOLISM
Different types of oestrogens that can be taken?
o Estradiol (oral)
o Estrone sulphate (conjugated oestrogen)
o Ethinyl estradiol (semi-synthetic oestrogen)
- the ethinyl group protects the molecule from first-pass metabolism
Risk of HRTs?
BCD
B - breast cancer
C - coronary HD
D - DVT
Stroke
Gallstones
BUT ABSOLUTE risk is VERY LOW
3 drugs used for HRT?
o Tibolone
o Raloxifene
o Tamoxifen
Tibolone?
Synthetic prohormone:
x oestrogenic, progestogenic & weak androgenic actions
- reduces fracture risks
BUT
o increased risk of stroke
o ? increased breast Ca risk
SERMs?
Selective
Oestrogen
Receptor
Modulator
Raloxifene?
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
Tamoxifen?
Anti-oestrogenic on breast tissue
Used to treat:
o oestrogen-dependent breast tumours
o metastatic breast cancers
Premature Ovarian insufficiency?
Menopause occurring BEFORE <40years
1% of women
COCs?
Combined Oral Contraceptives
o E (ethinyl oestradiol) \+ PG (e.g. levonorgestrel OR norethisterone)
How does COCs work?
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
