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Ethynyl estradiol
Basic information
Drug name: ethinylestradiol.
Drug alias: ethinyl estradiol.
Chemical formula: C20H24O2.
Category: sex hormone drugs.
Pharmacological effects
Ethinylestradiol has positive and negative feedback effect to the hypothalamus and
pituitary, small dose can stimulate gonadal hormone;To suppress the secretion at
higher doses, thus inhibiting ovarian oviposit, achieve anti fertility action.Synthesis and
release of the goods can stimulate the pituitary gonadotropic hormone (FSH and LH),
gonadotrophin, stimulate gonadal sex hormone release.The hypothalamus
gonadotropin releasing hormone secretion regulation by various factors, including
circulating hormones.Single agent can increase the sex hormones in loop when
using;Continuous use can cause the adenohypophysis gonadotropin releasing
hormone receptor, thus reducing the secretion of hormones.
dynamics
Oral is absorbed by the gastrointestinal tract and can be combined with plasma
protein medium, within the liver metabolism, most of the prototype to discharge,
about 60% by urinary excretion.The goods static note after the peak blood levels of 3
minutes, quickly via renal metabolism after discharge.Its effect on the increase of
serum LH faster, stronger, and the effect on FSH increased slower and weaker.Few
oral absorption, plasma t1/2 only a few minutes after intravenous administration,
hydrolyzed into inactive metabolites in plasma and urine excreted.
indications
supplement estrogen deficiency, treatment of female gonadal dysfunction,
amenorrhea, menopausal syndrome, etc.;For advanced breast cancer (after
menopause women), the treatment of advanced prostate cancer.In combination with
pregnant hormonal drugs inhibit ovulation, by birth control pills.Mainly used for clinical
inhibit ovulation medicine;Also used in children with cryptorchidism and androgen
excess, pituitary tumor, etc.Used to diagnose the hypothalamus - adenohypophysis -
gonadal dysfunction, according to the gonadotropin and sex hormone level changes.
This treatment gonadotropin secretion due to insufficiency of low sex gland function of
amenorrhea, infertility, ovarian follicles of infertility.Amenorrhea, related to the weight
loss should be correct weight with diet.Also used for prostate cancer (often with
cyproterone or fluorine formyl imine share), late or early puberty and
endometrial.Mainly used in the inhibition of ovarian oviposit, achieve the purpose of

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contraception.
Interact with each other
(1) with anticoagulants, estrogen can decrease the anticoagulant effect, must be the
same, anti-clotting drug dosage should be adjusted.
Diction and carbamazepine, phenobarbital and phenytoin sodium, ketone, rifampicin
equality used at the same time, can reduce the effect of estrogen, this is due to the
induced liver microsomal enzymes, the faster the metabolism of estrogen.
(3) used in conjunction with tricyclic antidepressants, a lot of estrogen can strengthen
the antidepressant drug adverse reactions, and reduce its effects.
(4) and at the same time with anti-hypertensive drugs, can reduce the effect of
antihypertensive.
(5) reduce the therapeutic effect of tamoxifen.
(6) to increase the absorption of calcium.