Definition
Mifepristone is an anti-gestational, anti-progestogenic steroid, used to terminate early pregnancies, in females not more than 7 weeks pregnant. It is also effective in crushing’s syndrome. This French abortion pill is famously called RU-486. The medicine has 95% effectiveness. Some of the patients might need other medical interventions due to incomplete abortion. (1)(2)
Chemical and Physical Features
CAS Number: 84371-65-3 (3)
Molecular Structure: (4)
Molecular Formula: C29H35NO2 (5)
Weight: 429.6 g/mol. (5)
Appearance:
Mifepristone when in powder form is yellow.
Mifepristone in solid form is a white to light yellow color pill. It is cylindrical and biconvex in shape. (6)
Other Physical Features:
Mifepristone compound is a yellow powder, with a melting point of 191℃ - 196℃.
Mifepristone is highly soluble in methanol, chloroform, and acetone.
Mifepristone is poorly soluble in water, hexane, and isopropyl ethane. (5)
Mifepristone needs to be stored at 2℃ - 8℃. It can be kept in a frozen state. It needs to be protected from light and is carcinogenic in toxicity. Mifepristone has to be packaged under inert gas for transportation. (3)
Brand Names
Mifeprex, Korlym, RU-486, MifeGem, MifeGest, Mefipil, Mefiwis, Mefnil, Mifeprin, T-Pill. (7)
Mifepristone forms and specifications
Mifepristone API Powder 99%
Mifepristone is a yellow color powder and is poorly soluble in water, hexane, and isopropyl ether. It is very soluble in methanol, chloroform, and acetone. (5)
Mifepristone Tablets
Mifepristone tablets are white solid pills, taken orally. It does not let the fertilized egg attach to the uterine wall, by blocking the action of progesterone. Grapefruit products should not be consumed along with mifepristone tablets, as it increases serum levels. Mifepristone tablets contain active ingredients such as corn starch, colloidal silica anhydrous, magnesium stearate, and povidone microcrystalline cellulose. (2)(6)
Mifepristone capsules
Mifepristone comes in a tablet form only. Selling Mifepristone in capsules form is not legitimate.. (8)
Mifepristone and Misoprostol
Mifepristone is administered along with Misoprostol to increase the effectiveness of abortion. It can be taken in the interval of one to two days between the 2 tablets. While Mifepristone is orally consumed, Misoprostol is to be taken vaginally. It generally comes in a combination pack of 1 tablet of Mifepristone and 4 tablets of Misoprostol. (9)
Mechanism of action of Mifepristone
Mifepristone handicaps the actions of progesterone at the progesterone-receptors sites. This causes decidual breakdown, which leads to detachment of the blastocyte, decreasing HCG production. The blocked progesterone receptors in the uterus increase the levels of prostaglandin and sensitize the myometrium for contractions.
In Crushing’s syndrome, Mifepristone inhibits the binding of cortisol to its receptors. It reduces the effects of excess cortisol, such as high blood sugar levels. (5)
Mifepristone manufacturing process
The pharmaceutical preparation of mifepristone is done by mixing the following raw materials in the given mass ratios: 10-40% of microcrystalline cellulose, 5-30% of mifepristone particles, 2-10% of adhesives, 20-40% of dextrin, 20-40% of starch, 0.5-1% of glidant and 0.5-2% of lubricant. These raw materials are dissolved and prepared using simple preparation methods with minimum manufacturing costs. (11)
Mifepristone uses
Mifepristone is used to induce abortion early in pregnancy, by blocking the production of progesterone.
Mifepristone is used to treat Crushing’s syndrome.
Mifepristone is also used to treat symptomatic leiomyoma (uterine fibroids). (12)
Mifepristone dosage
For Abortion:
Day one- 200mg Mifepristone is to be taken as a single dose, orally.
Day two or three- 800mcg misoprostol, 24-48 hours after the first dose of mifepristone.
For Crushing’s Syndrome:
An initial dose of 300mg once a day, orally.
A maximum dose of 1200mg or 20mg/ kg, once a day can be taken. (13)
Mifepristone side effects
The side effects of Mifepristone include abdominal cramping, allergic reactions ( such as the closing of throat, swelling of lips, tongue, or face), anxiety, anemia, reduction in hemoglobin levels, back pain, dizziness, diarrhea, fatigue, fainting, indigestion, headache, nausea, insomnia, pelvic pain, leg pain, sinusitis, rigors, tired, stomach pain, vaginal discharge, uterine cramping and bleeding, vaginitis, viral infection, weakness, and vomiting. (1)
Mifepristone API Price
The API price of the Mifepristone tablet is somewhere around $904 per KG. (14)
Mifepristone API manufacturers in China
Below are some manufacturers who are professional in making api pharmaceutical ingredient.
Zhejiang Xianju Junye Pharmaceutical Co., Ltd.
Zhejiang Xianju Junye Pharmaceutical Co., Ltd. was founded in 1998. They specialize in research, development, production, and sales of intermediate products and steroid hormone drug APIs. They are one of the leading manufacturers of hormone raw material, and products such as progesterone, cortical hormones, androgen, estrogen, and their intermediates. (15)
Zhejiang Xianju Pharmaceutical Co., Ltd.
Zhejiang Xianju Pharmaceutical Co., Ltd. was established in 1972 and is dedicated to scientific research, development, manufacturing, and supply of over 100 active pharmaceutical products of steroids and hormones. They indulge in the production of APIs of steroids, male and female hormones, and their intermediates. They process tablets, capsules, granules, soft capsules, cream, gel, injection, powder inhalation, and powder injections. (16)
China Resources Zizhu Pharmaceutical Co., Ltd.
In the year 1969, China Resources Zizhu Pharmaceutical Co., Ltd came into existence. They deal in pharmaceutical development, manufacturing, and marketing their products in China and foreign markets. Their products mainly cover family planning drugs and reproductive health drugs. They manufacture and distribute several products under various categories like contraceptives, medical abortion, hormone replacement therapy, and endometriosis tablets. (17)
You can also find details around more suppliers for Mifepristone API in bulk at PharmaSources.com. PharmaSources.com is one of the leading and trustworthy vertical e-commerce online pharmaceutical marketplaces. It gives information on quality pharmaceutical products and suppliers for its esteemed customers and delivers services to 90,000+ active members. The services are provided to about 211 countries and regions. PharmaSources.com has been successfully selling over 1,600,000 products in 30 major pharmaceutical categories across the supply chain. (19)
FAQs:
What’s the market size of Mifepristone?
In 2014, an estimate of 272,400 cases was reported under medical abortions in the United States, which was on a 14% increase since 2011. In 2000, Europe reported more than 620,000 cases of medical abortions using mifepristone tablets. Denmark reported the use of 3000 to 4000 tablets of mifepristone for aborting over 15,000 cases, in 2005. In 2016, 623,471 cases were reported all over the world. The percentage use of mifepristone has thus been increasing every year considerably, in every country. (12)(18)
Is Mifepristone and Misoprostol same?
Mifepristone and misoprostol are two different medications but are generally taken together to induce efficient abortion in the early stages of pregnancy, for up to 70 days of gestation. Normally, Mifepristone is consumed orally, and then with a gap of a day or two, misoprostol is taken vaginally. (9)
Sources:
1) https://www.rxlist.com/mifepristone/definition.htm
2) https://www.dictionary.com/browse/mifepristone
3) https://www.merckmillipore.com/IN/en/product/Mifepristone-CAS-84371-65-3-Calbiochem,EMD_BIO-475838?ReferrerURL=https%3A%2F%2Fwww.google.com%2F
4) https://www.researchgate.net/figure/Chemical-structure-of-mifepristone_fig1_308762311
5) https://pubchem.ncbi.nlm.nih.gov/compound/Mifepristone
6) https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20687lbl.htm
7) http://www.medlineindia.com/genito-urinary/mifepristone.htm
8) https://www.ipas.org/our-work/abortion-self-care/abortion-with-pills/how-to-buy-abortion-pills-that-are-safe-and-effective/
9) https://academic.oup.com/humrep/article/26/10/2690/608278
10) https://www.medicines.org.uk/emc/product/3380/smpc#gref
11) https://patents.google.com/patent/CN101455671A/en
12) https://en.wikipedia.org/wiki/Mifepristone
13) https://www.drugs.com/dosage/mifepristone.html
14) https://www.pharmacompass.com/price/mifepristone
15) http://www.junyepharm.com/about_zh/id/1.html
16) http://en.xjpharma.com/
17) http://www.zizhu-pharm.com/a_overview.asp
18) https://www.pharmiweb.com/press-release/2021-01-15/abortion-drugs-market-technology-trends-growth-analysis-new-strategies-and-solution-key-companies
19) www.Pharmasources.com
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