Contraceptives, HRT and SERMs Flashcards
What is climacteric
Period of transition to the menopause
what is menopause
- Permanent cessation of menstruation
- Loss of ovarian follicular activity
Average age of menopause
- Average age 51 (range 45-55)
Symptoms of menopause? (6)
- Hot flushes (head, neck, upper chest)
- Urogenital atrophy and dyspareunia
- Sleep disturbance
- Depression
- Decreased libido
- Joint pain
What happens to levels of oestradiol and inhibin during menopause and why
Low levels of oestradiol and inhibin B because of the follicular atresia
What are the Gonadotrophin levels in menopause
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
2 main complications of menopause?
- Osteoporosis
2. Cardiovascular disease
pathogenesis of osteoporosis in menopause
Oestrogen deficiency leads to Loss of bone matrix
pathogenesis of Cardiovascular disease in menopause
Oestrogen protects against CVD, this goes when oestrogen goes and by 70- men and women gave the same risk of CVD
what does HRT aim to control
the vasomotor symptoms (hot flushes)
what does HRT consist of
oestrogen and progestogen
What does oestrogen do if prescribed by itself
- Causes endometrial proliferation Prevents endometrial hyperplasia
- Risk of endometrial cancer if you just give oestrogen
what conditions do you only prescribe E in HRT and why
If they’ve had a hysterectomy, as then they have no uterus so no worry of endometrial hyperplasia
what is a hysterectomy
uterus removal
4 ways of administering E?
- Oral oestradiol (1mg)
- Oral conjugated equine oestrogen (0.625mg)
- Transdermal (patch) oestradiol (50microgram/day)
- Intravaginal For those with dyspareunia
How to avoid the high first pass metabolism of E?
- Ethinyl oestradiol A semi-synthetic oestrogen Ethinyl protects from first pass metabolism
Side effects of HRT? (5)
- Breast cancer
- Coronary heart disease
- Deep vein thrombosis (DVT)
- Stroke
- Gallstones
What population has an increased risk of CHD if they take HRT?
women who entered menopause 10< years ago
What population do not have an increased risk of CHD if they take HRT?
women who entered menopause <10 years ago
why it can be bad for older women to take oestrogen
as it has prothrombotic effects and older women may have a level of atherosclerosis
Why might adding progesterone to oestrogen be not good
it negates some of its cardioprotective effects
What actions does tibolone have
- Oestrogenic, progestogenic and weak androgenic actions
What does tibolone increase the risk of
stroke
breast cancer
What does tibolone reduce the risk of
fracture risk
What type of drug is raloxifene
SELECTIVE OESTROGEN RECEPTOR MODULATOR (SERM)
what does raloxifene do
- Oestrogenic in BONE:
Reduces risk of vertebral fractures - ANTI-oestrogenic in BREAST and UTERUS
Reduces breast cancer risk
bad thing about raloxifene (3)
- Does not reduce vasomotor symptoms
- Increases risk of fatal stroke and venous thromboembolism (VTE)
what does TAMOXIFEN do and what is it used for
- Anti-oestrogenic on breast tissue
- Used to treat oestrogen-dependent breast tumours and metastatic breast cancers
Reasons for menopause before 40 (4)
- Autoimmune
- Surgery
- Chemotherapy
- Radiation
What do combined oral contraceptives consist of
Oestrogen (ethinyl oestradiol) + progestogen (e.g. lovonorgestel or norethisterone)
What does the combined oral contraceptive do
Suppresses ovulation
What does oestrogen and progesterone do together in a combined oral contraceptive
E+P: Negative feedback actions at hypothalamus/pituitary axis
What does progesterone do in a combined oral contraceptive
Thickens cervical mucus
How does an oral combined contraceptive suppress ovulation
E+P: Negative feedback actions at hypothalamus/pituitary axis
P thickens cervical mucus
When do you prescribe progesterone only contraceptives
When oestrogens are contra-indicated Smoker, >35yrs old, migraine with aura
What is key about taking the progesterone only contraceptive
Must be taken same time every day
Half life and duration of action of the progesterone only contraceptive
Short half-life
Short duration of action
How often do you taken the EP contraceptive pill
- Take for 21 days (or 12 weeks), stop for 7 days
Emergency contraception? (3)
- Copper IUD (intrauterine contraceptive device)
- Levonorgestrel (within 72 hours)
- Ulipristal (up to 120hrs after intercourse)
What activity does ulipristal have
Anti-progestin
