Contraceptives, HRT and SERMs Flashcards
What is menopause?
Permanent cessation of menstruation with a loss of ovarian follicular activity
What is the average age and the age range for menopause?
Age 51
Range 45-55
What is the climacteric period?
The period of transition period
What are symptoms of menopause?
Hot flushes (head, neck, upper chest)
Urogenital atrophy and dyspareunia (painful sex)
Sleep disturbance
Depression
Decreased libido
Joint pain
Symptoms usually diminish or disappear with time
What happens to the reproductive axis in menopause?
No oestradiol and no inhibin,
no neg feedback so LH and FSH goes up
What are complications of menopause
Osteoporosis - 10 fold increased risk of fracture
Cardiovascular disease - protected against CVD before menopause but after that they have same risk as men
Why is osteoporosis a complication of menopause
Due to the oestrogen deficiency, there is a loss of bone matrix. Thin bones
Why is HRT given during menopause?
To control vasomotor symptoms (hot flushes)
What do you prescribe as HRT for menopause?
A mix of oestrogen and progesterone. Progesterone is given to protect against risk of endometrial carcinoma from endometrial proliferation
What hormones would you prescribe for HRT for menopause if the patient has had a hysterectomy?
Oestrogen only as no risk of endometrial cancer
What are the different HRT formulations can you give for menopause?
Cyclical - E every day and P (12-14 days)
Continuous combined hormones
What are the different ways you can administer HRT for menopause?
Oral oestradiol (1mg)
Oral conjugated equine oestrogen (0.625mg)
Transdermal (patch) oestradiol (50microgram/day)
Intravaginal
What is the bioavailability of oestradiol like?
Well absorbed but low bioavailability - first pass metabolism
What is an example of conjugated oestrogen?
Estrone sulphate
What is ethinyl estradiol? What does the ethinyl group do?
A semi-synthetic oestrogen - the ethinl group protects the molecule from first pass metabolism
How can most oestrogens be administered?
Via transdermal skin patches
What are side effects of HRT for menopause?
Breast cancer Coronary heart disease Deep vein thrombosis Stroke Gallstones
What is the absolute risk of complications in HRT for healthy symptomatic post menopausal women in their 50s taking HRT for five years
VERY LOW
What kind of beneficial effects do oestrogen have on women when given in HRT
Beneficial effects on lipid profile and endothelial function but in older women >60 it has prothrombotic and proinflammatory effects with an increased risk of atherosclerosis as well!
What is tibolone?
It is a synthetic prohormone
What are the effects of tibolone?
Oestrogenic, progestogenic and weak androgenic actions. Reduces fracture risk but increased risk of stroke and breast cancer
What is raloxifene?
A selective oestrogen receptor modulator - binds to oestrogen receptors but have different effects
What is the effect of raloxifene in bone?
Reduces risk of vertebral fractures
What is the effect of raloxifene in breast and uterus?
Reduces breast cancer risk
