What is Levonorgestrel?
Levonorgestrel is a medication used by women for the prevention of pregnancy in an event of birth control failure. Labeled as an emergency contraceptive, levonorgestrel is used after unprotected sex.
Definition
“A medication that is progestin hormone by nature which works by suppressing ovulation during menstrual cycle.”
Chemical & Physical Features
IUPAC name: (8R,9S,10R,13S,14S,17R)-13-ethyl-17-ethynyl-3-hydroxyimino-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-ol
Synonyms: Norelgestromin, D-Norgestrel 3-oxime, 17-Deacetylnorgestimate
CAS: 53016-31-2
Molecular formula: C21H29NO2
Molecular weight: 327.5
Form: Solid, crystals from methanol
Solubility: Soluble in ethanol, chloroform, diethyl ether
Trade names
Plan B, Plan B One-Step, My Way, Next Choice
Levonorgestrel Forms and Specifications
Levonorgestrel API powder 99%
This is the raw form from which levonorgestrel tablets are made. It is available in the form of white powder and combined with estrogen ethinylestradiol to manufacture the contraceptives sold in the market.
Levonorgestrel Capsules (0.75 mg, 1.5mg)
More often than not, a 0.75mg dose of levonorgestrel does the job efficiently. It is deemed safe for women. However, there might be some side effects that will be mentioned later in this brief. 1.5 mg dose of this drug is prescribed for only extremely critical cases, the decision still depends on various factors like age, weight, etc.
Levonorgestrel Tablet (levonorgestrel pill)
Levonorgestrel tablets (1.5mg) are effective within 72 hours. These work by interfering with ovulation, fertilization, and implantation. We will comment on the mechanism of action of this drug in detail in upcoming sections.
Levonorgestrel-Ethinyl Estradiol
This contraceptive is a combination hormone medication. It is used for preventing pregnancy. There are two hormones in this combination, these are progestin (which is again, levonorgestrel) and estrogen. Another name for estrogen is Ethinylestradiol. The medication works by suppressing ovulation i.e. release of an egg during the menstrual cycle.
Levonorgestrel vs. Norgestimate
Norgestimate is a second-generation progestin. Both active and inactive isomers are found in this medication. The inactive isomer is dextro-norgestrel while the active isomer is levonorgestrel. So, the difference between the two medicines lies in their composition as well as in some effects as well. Some of the effects produced by norgestimate include high androgenic activity and strong anti-estrogen effects.
Mechanism of Action of Levonorgestrel
As mentioned earlier, the primary mechanism of action of levonorgestrel is the inhibition of ovulation during the menstrual cycle. However, this is not the only way by which it prevents pregnancy. The hormone can make vaginal fluid thicker as well, this proves to help prevent sperm reaching from the egg and fertilizing it. Modifications in the lining of the uterus are also made to ensure that the fertilized egg doesn’t attach to the wall of the uterus.
Levonorgestrel Manufacturing Process
In this section of the discussion, we are going to briefly comment on the manufacturing process of levonorgestrel. The raw material used in this synthetic process is methoxydienone. In a reaction with an alkynyl lithium ammine complex, it is converted to an acetylide. The hydrolyzation of this acetylide produces levonorgestrel as the final product.
Levonorgestrel Uses
The primary purpose of this medication is used for is the prevention of pregnancy.
Levonorgestrel Birth Control
Using this medication within 72 hours is effective for the prevention of pregnancy. More often than not, the medicine is taken after a failure of a birth control device e.g. condom breakage. It is pertinent to mention here that levonorgestrel cannot terminate the pregnancy if the fertilized egg is already attached to the uterus. It is ideal to take one tablet within the first 12 hours for optimal results.
Levonorgestrel Dosage
These tablets are available in both 0.75 and 1.5 mg doses. The decision of taking either of these variants depends upon several factors including age, weight, etc. Levonorgestrel is not recommended for females at risk of ectopic pregnancy.
Levonorgestrel Side Effects
There are no major side effects reported with this drug. However, some of the minor side effects that might be experienced after taking this medication include vomiting, nausea, diarrhea, and headache. The frequency of these side effects may vary from patient to patient.
Levonorgestrel API Price
Although several import-export factors can influence the exact price of levonorgestrel API, the average price tag is around $4,971 per KG.
Levonorgestrel Sodium API manufacturers in China
Below are some professional active pharmaceutical ingredients manufacturers on Pharmasources in China.
Yangzhou Liberty Pharmaceutical Co. Ltd
This pharmaceutical producing company is mainly concerned with the production of traditional Chinese herbal medicines and raw materials used for manufacturing medicines like levonorgestrel.
Zhejiang Shenzhou Pharmaceutical co., ltd.
This is a company that specializes in the production of steroid API, intermediates and ships them to clients worldwide. LNG API is one of their specialties.
GreenPine Pharma Group Co. Ltd
GreenPine is involved in the production, research, and development of Chinese herbal medicines, synthetic chemicals, and raw materials for popular medications like levonorgestrel.
Huazhong Pharmaceutical Co., Ltd.
Been in this business since 1968, this pharmaceutical company is another reputable name in the world of levonorgestrel API production. World-class R& D facilities are also operational at this company.
Nanjing Baijingyu Pharmaceutical Co., Ltd
This pharmaceutical enterprise concerns itself with the production of pharmaceutical-grade raw materials that are used in the manufacturing of not just the levonorgestrel, but many other popular capsules and tablets as well.
China Resources Zizhu Pharmaceutical Co. Ltd.
This is another reputable name in the world of API producers, the company has been manufacturing premium-grade pharmaceuticals since 1969.
Pharmasources
Craving for knowing more? At pharmasources, you can search for hundreds of suppliers and manufacturers of levonorgestrel API in China, all of which are producing premium pharmaceutical grade levonorgestrel active pharmaceutical agents. Learn more about their modus operandi at pharmasources.
FAQs
In this section of the discussion, we are going to answer some commonly asked questions about levonorgestrel medication.
Who are the major suppliers of levonorgestrel?
Some major suppliers of levonorgestrel API all over the world include Shandong Octagon Chemicals Limited from China, Lupin from India, Industriale Chimica from Italy, and Flavine from Germany.
What’s the market size of levonorgestrel?
The line for levonorgestrel is likely to move upwards on the graph in between years 2020-2025. So, the future does seem to be bright for the producers of this API.
References
https://pubchem.ncbi.nlm.nih.gov/compound/Levonorgestrel-oxime
https://www.webmd.com/drugs/2/drug-17833-1347/levonorgestrel-oral/levonorgestrel-1-5-mg-oral/details
https://patents.google.com/patent/CN101982472B/en#:~:text=The%20synthesis%20process%20of%20the,is%20shown%20in%20the%20specification.
https://medlineplus.gov/druginfo/meds/a610021.html
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