Quick Details:
Drospirenone
Alias: 6b,7b:15b,16b-Dimethylen-3-oxo-17a-pregn-4-ene-21,17-carbolactone; Dihydrospirorenone
CAS NO: 67392-87-4
Molecular formula: C24H30O3
Molecular weight: 366.49
Assay:99%
Purity :99%
EINECS No.: 266-679-2
Density: 1.26g/cm3
Melting point: 196-200 ℃
Boiling point: 552.2 ° C at 760 mmHg
Flash point: 241.6 ° C
Steam pressure: 3.07E-12mmHg at 25 ° C
alpha: -180° (c=0.5, chloroform)
InChI: InChI=1/C24H30O3/c1-22-6-3-12(25)9-17(22)13-10-14(13)20-16(22)4-7-23(2)21(20)15-11-18(15)24(23)8-5-19(26)27-24/h9,13-16,18,20-21H,3-8,10-11H2,1-2H3/t13-,14+,15-,16+,18+,20-,21+,22-,23+,24+/m1/s1
Steam pressure: 3.07E-12mmHg at 25 ° C
Packing: Foil bag
Usage: Synthetic progestogen exhibiting antimineralocorticoid and antiandrogenic activity.Drospirenone (Drospirenone) and its analogues, is a kind of high efficient, low toxicity, no side effects of a new generation of steroidal contraceptives, first by France Schering company in 2000 developed the fourth generation of oral contraceptives, anti mineralocorticoid and anti androgenic effects, and wide market prospect
Description:
Drospirenone (INN, USAN), also known as 1,2-dihydrospirorenone, is a synthetic hormone used in birth control pills and postmenopausal hormone replacement therapy pills.
It is sold under the brand names Yasmin, Yasminelle, Yaz, Beyaz, Ocella, Zarah, Daylette and Angeliq, all of which arecombination products of drospirenone with an estrogen such as ethinylestradiol or estradiol.
Drospirenone differs from other synthetic progestins in that its pharmacological profile in preclinical studies shows it to be closer to the natural progesterone. As such it has potent antimineralocorticoid properties, counteracts the estrogen-stimulated activity of the renin-angiotensin-aldosterone system, and has also been shown to possess mild antiandrogen activity.
The antimineralocorticoid properties exhibited by drospirenone promote sodium excretion and prevent water retention.
Application:
Drospirenone is an ingredient in some birth control pills and hormone replacement therapy. In combination with ethinyl estradiolit is used as contraception, and for women who want contraception it is also approved by the U.S. Food and Drug Administration(FDA) to treat moderate acne and premenstrual dysphoric disorder.
Adverse effects:
Drospirenone is an aldosterone antagonist with potassium-sparing properties, though in most cases no increase of potassium levels is to be expected. In women with mild or moderate renal insufficiency, or in combination with chronic daily use of other potassium-sparing medications (ACE inhibitors, angiotensin II receptor antagonists, potassium-sparing diuretics, heparin, aldosterone antagonists, or NSAIDs), a potassium level should be checked after two weeks of use to test for hyperkalemia. In addition to contraindications common to all combined estrogen-progestin medications, drospirenone-containing medications are contraindicated in women with severe renal insufficiency according to European Medicines Agency (EMA)-approved labels, and contraindicated in women with renal insufficiency, adrenal insufficiency, or liver disease according to FDA-approved labels.
Women who take contraceptive pills containing drospirenone have a six- to sevenfold risk of developing thromboembolism (dangerous blood clots) compared to women who do not take any contraceptive pill, and have twice the risk (some epidemiological studies suggest thrice, according to the FDA) compared to women who take a contraceptive pill containing levonorgestrel, though the actual risk is small, in the neighborhood of 9 to 27 out of 10,000 women on an oral contraceptive for a year (up to 9 for levonorgestrel vs up to 27 for drospirenone, or about 0.09% vs 0.3% per year.)
Superiority
Estrogen is a female sex hormone, produced by the ovaries and placenta. Adrenal cortex also produced a few estrogen. Female children after puberty ovarian secretion of estrogen, start, in order to promote the vagina, uterus, fallopian tube and ovary itself development, at the same time caused menstrual endometrial hyperplasia. Estrogen can promote the subcutaneous fat accumulation, plump; hyperplasia of the breast, nipple, areola dark colors, and produce sexual desire; to promote the body sodium and water retention, bone calcium deposition
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