Endo 10 - Contraceptives, HRT and SERMs Flashcards
What is the medical term for painful sex
Dyspareunia
Name a common symptom of menopause
Insomnia - sleep disturbance
What is menopause?
What is the transition period called just before menopause
Menopause = permanent cessation of menstruation - loss of ovarian follicular activity. Avg age = 51
Climacteric = transition period just before menopause, may have irregular periods
What are the symptoms of menopause
- Hot flushes (head, neck, upper chest)
- Urogenital atrophy and dyspareunia
- Sleep disturbance
- Depression
- Loss of libido
- Joint pain
Symptoms usually diminish with time
What hormonal changes occur during menopause
LH and FSH increase - as low estradiol and inhibin so less -ve feedback
Oestrogen is anabolic. Name 2 complications of menopause
- Osteoporosis - oestrogen deficiency causes loss of bone matrix - 10x increased risk of fracture
- CVD - oestrogen is cardioprotective - but women have the same risk of men by 70.
Oestrogen cardioprotective as it has beneficial effects on lipid profile and endothelial function
How is HRT given to prevent hot flushes?
Oestrogen and Progesterone given. This prevents endometrial hyperplasia.
- Giving oestrogen alone risks endometrial carcinoma (as oestrogen promotes endometrial proliferation)
BUT if hysterectomy patient (removed uterus), then can give just oestrogen
What are the 2 formulations by which the HRT (E+P) can be given?
- Cyclical: Oestrogen (E) daily and Progesterone (P) every 12-14 days
- Continuous combined
What are the different methods of administering oestrogen
- Oral
- Oral conjugated equine oestrogen
- Transdermal patch
- Intravaginal
Name 3 oestrogens that are prescribed
- Oestradiol - well absorbed but low bioavailability due to high first pass metabolism - so higher dose requied
- Oestrone sulphate
- Ethinyl estradiol - semisynthetic oestrogen - ethanol group protects molecule from first pass metabolism
Most oestrogen can be given transdermally
Which form of oestrogen is used in oral contraceptives?
Ethinyl oestradiol
What are the side effects of HRT (E+P)
- Breast cancer
- CHD
- DVT
- Stroke
(5. Gallstones)
Absolute risk of complications for healthy symptomatic postmenopausal women in their 50s is very low with HRT (5 years) - watch out though, women in their 60s have higher baseline risk (due to atherosclerosis etc, and they are older than menopausal age range)
Explain why HRT (E+P) will have different effects in younger and older people
Oestrogen has beneficial effects on lipid profile and endothelial function (in younger people). But synthetic progestins negate these effects
In older women (>60), atherosclerosis is higher. Also susceptible to prothrombotic and pro inflammatory effects of oestrogen, which contributes to increased CHD risk in older women
Describe Tibolone
Synthetic prohormone
- It has oestrogenic, progestogenic and weak androgenic actions.
- Reduces fracture risk
- Increases stroke risk (and breast cancer risk) so not commonly prescribed
What is a SERM, and give an example of one
Selective oEstrogen Receptor Modulator
Raloxifene = SERM
Oestrogenic in bone - reduces risk of fractures
Anti-oestrogenic in breast and uterus - reduces breast cancer risk
However, it doesn’t reduce vasomotor (hot flush) symptoms and increased risk of venous thromboembolism and fatal stroke
Describe tamoxifen
It has anti-oestrogenic effects on breast tissue
Treats oestrogen-dependent breast tumours and metastatic breast cancers
What are the HRT drugs that are prescribed
Tibolone, Raloxifene (SERM), Tamoxifen
These are not prescribed for osteoporotic reasons, only for Hot flushes, etc
Not prescribed for people with heart disease or over 60
What is premature ovarian insufficiency(/failure)
How would it present in patients
Menopause occurring before 40
Causes may be autoimmune or iatrogenic (i.e. chemotherapy, surgery, radiation)
With high FSH, high LH and low oestradiol
Describe combined oral contraceptives (COCP) that may be given
Oestrogen (ethinyl estradiol) and Progestogen (norethisterone or levonorgestrel)
The combined E+P suppresses ovulation - both E+P have negative feedback on Hyp/Pit so less FSH/LH = no ovulation
P also thickens cervical mucus
Must be taken for 21 days then stop for 7 days
When is the progesterone only contraceptive pill given
When oestrogens contraindicated - i.e. smoker, >35 years old, migraine with aura - because oestrogen has prothrombotic, proinflammatory effects
Describe the progesterone only pill
It is given when patient has cardio/vascular risks, as oestrogen may exacerbate these.
- Taken same time each day, because short half life
- Long acting preparations can be given via an intra-uterine system
Name emergency contraception options
- Copper IUD (intrauterine device) - must exclude pregnancy first.
- Affects sperm viability and function, and can be used in overweight/obese women
- 5 (upto 7) days after unprotected sex - Progesterone only contraceptive - Levonorgestrel - within 72 hours after sex
- Ulipristal - anti-progestin activity
- delays ovulation by 5 days
- impairs implantation
- upto 120 hours after intercourse
