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regub 21: reproductive pharmacology (i) (Progestogens (uses (contraception…
regub 21: reproductive pharmacology (i)
oestrogens effects
inhibits FSH
mineral corticoid effect
increases HDL, decreases LDL
increases coagulability
maintains bone density + elasticity of skin + blood vessels
oestrogens MOA
Rs = ERalpha + ERbeta
intracellular
differ in location + expression density
1) classical
binds to intracellular Rs + induces/represses transcription
2) non-classical
binds to membrane Rs + causes non-genomic signalling
e.g. acute vasodilation
only applies to high doses
synthetic therapeutic oestrogens
less rapidly degraded by liver than natural forms
e.g. mestranol, stilbestrol, ethinylestradiol
many admin methods
topical used for vaginal atrophy (post-menopause)
almost always given with a progestogen
given as monotherapy after historectomy
uses
contraception
HRT
in primary ovarian failure (e.g. Turner's syndrome - only 1 X chromosome)
in secondary ovarian failure (i.e. menopause)
SEs: nausea, vomiting, thromboembolism, oestrogen positive cancer, feminisation, hypertension
can't be given in: liver disease, undiagnosed genital bleeding, thromboembolic history, smokers, cancer, breastfeeding
anti-oestrogens
compete with hormone @ R
Tamoxifen
SERM
antagonist @ breast
partial agonist in endometrium, plasma lipids, bone
uses: oestrogen +ve breast cancer, osteoporosis
Clomifene
SERM
antagonist @ ant pit
stops -ve feedback
increase FSH+LH
1st line therapy for infertility
Progestogens
increases insulin + responsiveness to it
increases body temp
naturally hormone orally inactive (1st pass metabolism)
synthetic derivatives given IM
e.g. hydroxypregesterone
newer ones = testosterone derivatives (e.g. norgestel, desogestrel)
uses
contraception
HRT
endometriosis
endometrial cancer (minor)
SEs: androgenic effects (e.g. acne), oedema, weight changers, libido changes, depression, PMS, irregular menses, thromboembolism