Reproductive + Post Reproductive Health Flashcards
What are the sex steroids derived from?
Cholesterol
What type of receptors do steroid hormones act on?
How do they exert their effects?
Nuclear receptors
Through gene transcription
What are the COCP and progesterone only pill metabolised by?
In liver by CYP 450 enzymes
What is oral contraceptive efficacy reduced by?
Examples
Why?
- CYP450 enzyme inducing drugs
e.g carbamazepine, phenytoin, rifampicin ,smoking - All increase production of hepatic CYP450
Difference in the role of high + low levels of progesterone
high: inhibits ovulation
low: thickens cervical mucus (does NOT inhibit ovulation)
What steroids are used in hormone replacement?
Natural oestrogen
Synthetic progesterone
Uses of bisphosphonates
Osteoporosis
Bone diseases e.g. Paget’s disease of bone + malignancy
Outline the absorption, metabolism + excretion of oestrogen in the body
- readily absorbed from skin + mucous membranes
- metabolised by hepatic CYP450
- excreted in urine as glucuronides + sulphates
Outline the absorption, metabolism + excretion of progesterone in the body
- injected progesterone is bound to albumin
- some stored in adipose tissue
- metabolised by hepatic CYP450
- excreted in urine conjugated to glucuronic acid
Pharmacokinetics of bisphosphonates
- long half life
- poor gut absorption which is affected by food > taken on empty stomach
What are the adverse drug effects of bisphosphonates?
What needs to be done about them?
- Oesophagitis (remain seated or standing for 30mins after taking)
- Hypocalcaemia (check Ca2+ + vit D levels before)
What is the mechanism of action of bisphosphonates
Reduce bone turnover by controlling osteoclast activity
What is the mechanism of action of mifepristone?
Progesterone receptor antagonist
- act as an anti-progesterone
- sensitising myometrium to prostaglandin induced contractions
What are the uses of mifepristone?
Termination of pregnancy
Medical management of miscarriage
What is the mechanism of action as ulipristal acetate (Ella one) as an emergency contraceptive?
- Selective progesterone receptor modulator
- Inhibition of ovulation via suppressing LH surge
What is the mechanism of action of clomiphene?
- selective oestrogen receptor modulator
- competes with oestrogen for ER binding
- causes ovulation induction through LH surge
What advice should be given when taking bisphosphonates?
Taken on empty stomach
Remain seated/standing for 30 mins after taking
Action of tamoxifen at the breast tissue
- used in treatment of breast cancer
- Oestrogen receptor antagonist
- causes antiestrogenic + antitumor effects
- slows cell cycling
Action of tamoxifen at bone
Oestrogen agonist > prevents osteoporosis in post menopausal women
Action of tamoxifen at hypothalamus
- Acts as oestrogen agonist in premenopausal women
- increases gonadotropin levels > induce ovulation
Action of tamoxifen at endometrium
Acts as oestrogen receptor agonist > endometrial hyperplasia (bad thing)
Actions of oestrogen
- endometrial proliferation
- Na+ H2O retention
- raises HDL + lowers LDL
- decreases bone resorption
- impaired glucose tolerance
- increased blood coagulability
What are side effects of oestrogen?
- breast tenderness
- N+V
- water retention
- thromboembolism
- increased blood coagulability
- impaired glucose tolerance
- increased risk of endometrial, ovarian + breast cancer
Actions of progesterone
- secretory endometrium
- maintains pregnancy
- mood changes
- increases bone mineral density
- fluid retention
Side effects of progesterone
Weight gain
Fluid rented on
Acne
N + V
Irritability
Lack of concentration
Actions of testosterone
Male secondary sex characteristics
Increased muscle mass
Side effects of testosterone
Aggression
Acne
Voice changes
Increase body hair/male pattern baldness
Increased risk of atherosclerotic disease
Uses of raloxifene
Prevention of osteoporosis in menopause and breast cancer
