Repro - Pharm - 1-6 Estrogens

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Estrogen and progesterone are derived from...

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cholesterol

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Ethinyl estradiol

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Synthetic estrogen

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Has some antiestrogenic character

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Tamoxifen or clomiphene

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A synthetic progestin

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Norethindrone or medroxyprogesterone

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An antiprogestin

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Mifepristone (RU486)

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Can stimulate ovulation

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FSH or hCG

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How is estrogen made from testosterone?

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aromatization of a ring.
Via P450 aromatase enzyme.

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Estriol

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Least potent but a lot is made during pregnancy so there is a large estrogenic stimulus still.

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Lipophilicity of estrogens

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very high

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Potency of estrogens

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Estradiol (Ovary) --> estrone (peripheral sites) --> estriol (placenta)

(highest to lowest)

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Precursor of all steroid hormones

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pregnenolone (derived from cholesterol)

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During luteal phase of the cycle, what happens to pregnenolone?

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Also converted to progesterone.

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Site of estrogen or progesterone synth

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Mainly in ovary (estradiol). Small amts in peripheral sites (adipose tissue - estrone)

During pregnancy - fetoplacental unit.

Placenta produces estriol and estrone

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Where are estrogens and progestins metab to less active (more water sol) compounds?

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Liver - excreted in urine.

(e.g. estradiol to estrone to estriol)

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How to estrogens/progesterone work?

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Bind to cytoplasmic receptors which translocate to nucleus and bind to elements in the DNA to activate estrogen receptor genes.

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Before ovulation (follicular/proliferative phase), what is secreted?

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Estrogen.

FSH develops the follicle and the cells surrounding follicle secrete estrogen. This stimulates prolif of endometrial cells lining the uterus and secretes a watery secretion too from cervical glands.

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Luteal phase (after ovulation), what is secreted?

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Estrogen and progesterone

FSH/LH surge at midcycle triggers ovulation and the cells that had formed the follicle now form the corpus luteum and secrete progesterone.

This converts uterus to a secretory state to counter estrogens effects. Also causes cervical gland secretions to be scant and viscous.

If there is no fert, the CL involutes and progesterone levels fall resulting in menstruation

If there is fert, proges levels maintain and pregnancy continues.

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What is implantation dependent on?

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Priming of the uterus (estrogen then progesterone).

Proper progesterone/estrogen ratio.

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Estrogens effect on progesterone receptors

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upregulates them.

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Slide 6 is good

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kljsdf

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Uterus during follicular phase

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proliferation

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Uterus during luteal phase

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conversion to secretory state

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Mech of action of some combo pills

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Normally, estrogen and progesterone inhibit FSH and LH secretion from ant. pituitary.

FSH and LH develops follicle and ovulation.

By giving estrogen and progesterone, you inhibit FSH and LH and don't develop follicles.

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Synthetic estrogen

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Estradiol with chem group on it (e.g. ethinyl - broken down less)

Used in combo OC pills.

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Conjugated estrogen

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A normal metabolite of estrogen excreted in the urine

(sulfated or glucorinidation)

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Premarin

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contains conjugates estrogens (a mixture of estrogen sulfates)

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Two groups of synthetic progestins

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Norethindrone (from nortestosterone) and medroxyprogesterone (from progesterone)

These have progesterone and androgen activities.

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Synthetic steroids and OCs

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They give improved oral absorption and extended half-life.

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Minipill

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progesterone only.

Doesn't stop ovulation all the time but has effects on uterus and cervical mucus.

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Mech of action of combo pills

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Contains synthetic estrogen (ethinyl estradiol) and synthetic progestin

Prevents secretion of FSH and LH and has effects on uterus and cervical mucus.

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Mech of action of progestin-only contraceptives

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Inhibit ovulation and produce viscous cervical mucus as a barrier to sperm and/or a uterine env hostile to implantation.

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Tamoxifen

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Blocks estrogen from binding receptor in breast. But is an agonist in bone and heart.

Can tx breast CA. (best with tumors expressing estrogen and progesterone receptors)

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Clomiphene

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An antiestrogen

Blocks the negative feedback by estrogen to increase FSH and LH secretion.

Good to get ovulation in anovulatory women.

Tx of infertility.

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SEs of clomiphene

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ovarian cysts or multiple births

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Anti-progestin

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has a bulky group on it.