L12 Female Reproduction Flashcards
What is the principal source of circulating oestrogen in premenopausal women?
Ovaries
What is the main secretory product from the ovaries?
Oestradiol
Examples of ways oestrogens can be produced
- by the ovaries
- from androgens by the actions of aromatase
- from oestrogen conjugates by hydrolysis
What are oestrogens largely responsible for?
pubertal changes in girls and secondary sexual characteristics
How is oestrogen production tightly controlled?
Oestrogen production is under tight neuroendocrine control via the HPO hormone feedback regulation axis
How do oestrogens exert their effects?
By interaction with nuclear receptors: ERα (encoded by ESR1) and ERβ (encoded by ESR2). Oestrogen receptors act as transcription factors - transcriptional regulatory effects.
How do oestrogens have positive effects on bone mass?
Osteoclasts and osteoblasts express both ERα (plays a greater role) and ERβ. They regulate bone remodelling.
Where is progesterone secreted from and when?
Progesterone is secreted by the ovary, mainly from the corpus luteum, during the second half of the menstrual cycle (secretory/luteal phase)
__, acting via its __, stimulates progesterone secretion during the normal cycle.
LH, acting via its GPCR
2 most frequent uses of progestins
- For contraception, either alone or with an oestrogen
- In combination with oestrogen for hormone therapy of postmenopausal women
Effects of progestins on the reproductive system
Progesterone decreases oestrogen-driven endometrial proliferation. This leads to the development of a secretory endometrium. The abrupt decline in progesterone at the end of the cycle is the main determinant of the onset of menstruation.
Effect of progesterone on mammary glands
Mammary gland development requires both oestrogen and progesterone. During pregnancy, progesterone acts with oestrogen to bring about proliferation of the acini of mammary glands. Towards the end of pregnancy, the acini fill with secretions and the vasculature of the gland notably increases.
Effect of progesterone on the CNS
Increase in basal body temp of ~0.6℃ mid-cycle (correlating with ovulation)
Metabolic effects of progesterone
- increases basal insulin levels and the rise in insulin after carb ingestion, but it does not normally alter glucose tolerance
- stimulates lipoprotein lipase activity and seems to enhance fat deposition
Example of a more potent progestin that may decrease glucose tolerance
Norgestrel
Naturally occurring progestin
the endogenous steroid hormone progesterone
To which series do 17α-acetoxyprogesterone derivatives belong?
the pregnane series
To which series do 19-nortestosterone derivatives belong?
the estrane series
To which series do Norgestrel and related compounds belong?
the gonane series
What is the most widely used method for contraception?
oral contraceptive pill
2 types of oral contraception
- combination pills
- progestin-only pills
What is the pharmacologic activity of progestins based on?
the progestational activity and bioavailability of each progestin, as well as the dose
Place the following progestins in order of decreasing relative potency:
norgestrel, norethindrone, levonorgestrel
levonorgestrel > norgestrel > norethindrone
What is the active oestrogen component of oral contraceptives?
ethinyl oestradiol