What is Ulipristal acetate?
Ulipristal acetate is commonly used as an emergency contraceptive to prevent a pregnancy when a regular form of birth control has failed. It is not recommended to be used as a regular form of daily, weekly, or monthly birth control pill. (1) Ulipristal acetate is also used for the treatment of uterine fibroids, for intermittent treatment, and pre-operative treatment of moderate to severe symptoms of uterine fibroids including painful periods, heavy bleeding, and pelvic pain in adult women of reproductive age. (2)
Ulipristal acetate is marketed in the United States under the brand name Ella and in Canada under the brand name Fibristal. It is also marketed under the brand names EllaOne and Esmya in many countries including the United Kingdom and Ireland. (1,3)
Below are some key chemical features of ulipristal acetate that help in its identification:
Molecular formula: C30H37NO4
CAS number: 126784-99-4
Weight: 475.62
Identity: 1H-NMR
Appearance: White to light yellow crystalline powder
Melting Point: 185-188°C
Solvents: DMSO (30mg/ml), ethanol (30mg/ml), DMF (30mg/ml) (4,5,6)
Uses of ulipristal acetate
As we mentioned earlier, ulipristal acetate is used as an emergency contraceptive and also for the treatment of uterine fibroids and its associated symptoms in adult women of reproductive age. Fibroids are non-cancerous development around the uterus. Ulipristal acetate may benefit women with uterine fibroids as it reduces or stops the menstrual bleeding in the first 10 days of the treatment itself thus, providing relief from the symptoms associated with the fibroids. (2)
Emergency contraceptive: In a study, when ulipristal was given within 72 hours of unprotected sexual intercourse, it was found at least as effective as levonorgestrel, with pregnancy rates 0.9 to 1.8 percent. It was, however, found more effective than levonorgestrel in the 72 to 120-hour window. The latter was found applicable only to people with a BMI less than 25. Ulipristal was also found to be well-tolerated and with an adverse effect profile which is similar to that of levonorgestrel emergency contraception, also commonly known as Plan B. The cost for ulipristal acetate is also comparable with that of levonorgestrel. (7,8)
Uterine Fibroids: In a study, it was found that ulipristal acetate 5 mg was able to control uterine bleeding in 90% of uterine fibroid patients, while leuprolide acetate 5 mg was able to control for 89% of patients (difference of 1.2%). Ulipristal acetate 10 mg was also found to control uterine bleeding in 98% of patients, while leuprolide acetate 10 mg was able to control it for 89% of patients (difference of 8.8%), thus concluding ulipristal acetate had higher efficacy than leuprolide acetate for controlling bleeding in uterine fibroid patients. (9)
In another study, both the 5 mg and 10 mg daily doses of ulipristal acetate were found non-inferior to the once-a-month dose of leuprolide acetate in controlling uterine bleeding and were significantly less likely to cause hot flashes. (10)
Ulipristal acetate pill specifications
Ulipristal acetate is sold in the market in tablet formulation and is to be taken orally. The pill specifications differ based on its strength.
The 30 mg tablet is supplied in a PVC-PE-PVDC or PVC-PVDC-aluminium blister pack. It is a white to off-white, round, curved tablet marked with the brand name on both sides. (11)
Each 5 mg tablet of ulipristal acetate is colored white to off-white, is round biconvex, 7 mm thickness, and is engraved (with “ES5” for Esmya) on one face. (12)
Ulipristal acetate mechanism of action
Emergency contraceptives: Ulipristal acetate acts as a selective progesterone receptor modulator (SPRM), meaning that it attaches to progesterone receptors, preventing progesterone itself to show its’ effect. Therefore, it prevents pregnancies mainly by preventing ovulation or delaying it. (7,13)
-If taken before ovulation ulipristal acetate delays or inhibits ovulation
-When administered in the early luteal phase, it may decrease the thickness of the endometrium and affect the successful implantation of a fertilized egg to prevent pregnancy.
-If ovulation has already occurred then ulipristal acetate won’t be effective.
We can thus safely conclude that its mechanism of action varies based on the time of its administration during the ovulation cycle. (1,14) It is also important to understand that taking a single tablet of ulipristal acetate does not stop periods, but may delay or prepone them. (2)
Uterine fibroids: Even during the treatment of uterine fibroids, ulipristal acetate acts by showing its main feature of being an SPRM. It helps to reduce the size of the fibroids, stopping or controlling the bleeding, and increasing the red blood cell count by blocking the progesterone receptors. When the compound is given at a specific dose prescribed by the doctor, ulipristal acetate inhibits ovulation leading to the stopping of periods. Subsequently, benefitting women who experience heavy bleeding due to their fibroids. (2)
Safety
Common side effects and allergic reactions: Ulipristal acetate was approved by the EMA in May 2009 and by the USFDA in August 2010 for use as an emergency contraceptive. (8,13,15)
A generally safe medicine, it has some side effects just like all medicines. These include headache; dizziness, feeling tired; nausea, stomach pain; and menstrual pain also known as dysmenorrhea. If you want to purchase safe Ulipristal acetate, you can visit Pharmasource, which is one of the Medical Equipment wholesalers, providing pharmaceutical ingredients and pharmaceutical instruments for customers.
There are chances to experience some allergic reaction, which may include hives; difficulty in breathing; swelling of face, lips, tongue, or throat. (1)
Safety concerns with ulipristal acetate's use in the treatment of uterine fibroids: Ulipristal acetate was approved by the EMA for use in treating uterine fibroids and associated symptoms in 2012. (16)
EMA review committee:
The EMA's safety committee (PRAC) has recommended women stop taking the 5 mg ulipristal acetate (Esmya and generic medicines) for the treatment of uterine fibroids as a safety review is still ongoing. EMA started this review in March 2020 at the request of the European Commission (EC) following a case of liver injury that eventually led to a liver transplant in a patient taking the medicine.
EMA has recommended that no new patients should start treatment with the medicine which has been temporarily suspended throughout the EU during the review period. Many countries such as India have also banned the product following EMA recommendations. (17)
It is important to note that this review does not affect the use of single-dose ulipristal acetate pill as an emergency contraceptive (EllaOne and other trade names), emphasizing that there is no concern about liver injury with the medicine when used as a single-dose emergency contraceptive. (17,18)
Efficacy
The compound has been proven to be highly effective in preventing pregnancies when taken within 5 days of unprotected sexual intercourse after another method of contraception has failed. It is also found to be highly effective in controlling bleeding in adult women of reproductive age with uterine fibroids.
Doctors recommend waiting at least 5 days after taking ulipristal before a patient can start using hormonal birth control of the following forms: birth control pills, injections, implants, skin patches, vaginal rings. This is recommended because both ulipristal and hormonal birth control pills become less effective when they are used at the same time. A person is advised to use a barrier form of birth control until the hormonal birth control can take effect. (1)
Cost
One dose of ulipristal costs approximately $40 to $68 from a retail pharmacy. (7)
If you want to know the price to buy ulipristal acetate powder in large quantity, please contact us for more details.
Where to buy bulk ulipristal acetate?
In Europe, ulipristal acetate can be obtained without a prescription. (13) However, it requires a prescription in the US. (14) It can be purchased in bulk from online platforms such as PharmaSources.com which is one of the leading vertical e-commerce online pharmaceutical marketplaces. It provides information on quality pharmaceutical products and suppliers for its customers and delivers services to 90,000+ active members. The services are provided globally, across 211 countries and regions. PharmaSources.com sells over 1,600,000 products in 30 major pharmaceutical categories across the supply chain. (19)
Sources:
1.https://www.drugs.com/mtm/ulipristal.html
2.https://www.1mg.com/generics/ulipristal-acetate-213308
3.https://www.ncbi.nlm.nih.gov/books/NBK195459/
4.https://www.chemodex.com/products/ulipristal-acetate/
5.https://pubchem.ncbi.nlm.nih.gov/compound/Ulipristal-acetate
6.https://www.chemicalbook.com/ChemicalProductProperty_EN_CB31400406.htm
7.https://www.aafp.org/afp/2012/0815/p365.html
8.https://pubmed.ncbi.nlm.nih.gov/21175385/
9.https://www.nejm.org/doi/full/10.1056/nejmoa1103180
10.https://pubmed.ncbi.nlm.nih.gov/22296076/
11.https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=052bfe45-c485-49e5-8fc4-51990b2efba4#
12.https://www.medicines.org.uk/emc/medicine/26068#gref
13.https://www.ema.europa.eu/en/medicines/human/EPAR/ellaone
14.https://www.webmd.com/drugs/2/drug-154868/ulipristal-oral/details
15.https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022474s010lbl.pdf
16.https://www.ema.europa.eu/en/news/suspension-ulipristal-acetate-uterine-fibroids-during-ongoing-ema-review-liver-injury-risk
17.http://pharmabiz.com/ArticleDetails.aspx?aid=133514&sid=1
18.https://patient.info/medicine/ulipristal-acetate-for-uterine-fibroids-esmya
19.https://www.pharmasources.com/information/about
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