Ethynyl Estradiol Powder CAS 57-63-6

Ethynyl estradiol powder is 3- hydroxy -19- nor17α-pregnane -1,3,5⑽- triene -20- alkyne-17-ol. Calculated by dry product, the content of C20H24O2 should be 97.0% ~ 103.0%.

It is white or white-like crystalline powder; Odorless.

The product is soluble in ethanol, propanol, or ether, soluble in chloroform, and insoluble in water.

Melting point The melting point of this product is 180 ~ 186℃.

Specific rotation takes the product, weighs it precisely, adds pyridine to dissolve it, and dilutes it quantitatively to make a solution containing about 10mg per 1ml.

According to the law, the specific rotation is-26 to-31.

[Content determination] Determination by high-performance liquid chromatography. Chromatographic conditions and system applicability test use octadecyl silane bonded silica gel as filler; Methanol-water (70:30) is the mobile phase, and the detection wavelength is 281nm. The theoretical plate number should be no less than 1,000 according to the Ethynyl estradiol peak, and the separation degree between the Ethynyl estradiol peak and internal standard substance peak should meet the requirements.

Preparation of internal standard solution Take about 20mg megestrol acetate, accurately weigh it, put it in a 10ml volumetric flask, dissolve it in absolute ethyl alcohol, dilute it to scale, and shake it well.

What is Ethynyl estradiol?

Ethynyl estradiol powder is an estrogen drug, which is widely used in contraceptives in combination with progesterone. In the past, it was widely used in various indications, such as treating climacteric symptoms, gynecological diseases, and some hormone-sensitive cancers. It is usually taken orally, but it is also used as a patch and vaginal ring.

Its general side effects include breast pain, headache, fluid retention, and nausea. In men, it can also lead to breast development, general feminization, hypogonadism, and sexual dysfunction. But rare and serious side effects include thrombosis, liver injury, and uterine cancer.

It is an estrogen, or estrogen receptor agonist, and the biological target of estrogen such as estradiol. It is a synthetic derivative of estradiol (a natural estrogen), which is different from it in many ways. Compared with estradiol, it greatly improves the bioavailability when taken orally, is more resistant to metabolism, and shows a relatively enhanced effect in some parts of the body such as the liver and uterus. These differences make it more suitable for contraceptives than estradiol, but it also leads to an increased risk of thrombosis and some other rare side effects.

It was developed in the 1930s and introduced into medical use in 1943. It began to be used for contraceptives in the 1960s. Today, it exists in almost all combinations of contraceptives, and it is almost the only estrogen used for this purpose, even if it is not the most widely used estrogen, it is one of them.

How does Ethynyl estradiol work?

Ethynyl estradiol powder has positive and negative feedback effects on the hypothalamus and pituitary, and a small dose can stimulate gonadotropin secretion. A large dose can inhibit its secretion, thus inhibiting ovulation of the ovary and achieving the antifertility effect. It can stimulate the pituitary gland to synthesize and release gonadotropin, while gonadotropin stimulates the gonad to release sex hormones. The secretion of the gonadotropin-releasing hormone in the hypothalamus is regulated by many factors, including circulating sex hormones. Single-agent can increase sex hormones in circulation; Continuous use can down-regulate gonadotropin-releasing hormone receptors in the adenohypophysis, thus reducing the secretion of sex hormones.

Where does Ethynyl estradiol fit in?

1. Ethynyl estradiol supplements estrogen deficiency to treat female gonadal dysfunction, amenorrhea, climacteric syndrome, etc. For the treatment of advanced breast cancer (postmenopausal women) and advanced prostate cancer; Combined with progestogen drugs, it can inhibit ovulation and can be used as a contraceptive. Mainly used as an ovulation inhibitor in clinics; It is also used for cryptorchidism, androgen excess, and pituitary tumor in children. The diagnosis of hypothalamic-adenohypophysis-gonadal dysfunction can be based on the changes in gonadotropin and sex hormone levels.

2. It can be used to treat amenorrhea and infertility caused by hypogonadism due to insufficient gonadotropin secretion, and infertility caused by the follicular ovary. The amenorrhea related to weight loss should be corrected by diet first. It is also used for prostate cancer (often combined with cyproterone or Fluoroformylamine), delayed or advanced puberty, and endometriosis. Mainly used to inhibit ovarian ovulation and achieve the purpose of contraception.

What are the adverse reactions of Ethynyl estradiol?

Except for treatment, women with breast cancer should avoid using Ethynyl estradiol because the prognosis may worsen.

Because of the increased risk of venous thromboembolism, breastfeeding women less than 21 days after delivery should also avoid using it. It should be discussed with the provider to use EE in breastfeeding women at least 21 days after delivery, and include information about the advantages, disadvantages, and alternatives of using it.

Because of the risk of cholestatic hepatotoxicity, it is generally believed that women with a history of cholestasis of pregnancy, liver tumors, active hepatitis, and family defects in bile excretion should avoid using the compound oral contraceptives containing Ethynyl estradiol.

The severity may vary with its dosage and route of administration. Its general side effects are the same as other estrogens, including breast pain, headache, fluid retention (abdominal distension), nausea, dizziness, and weight gain. The estrogen component of oral contraceptives, almost always, can cause breast pain and fullness.

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Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure or prevent any disease.

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