Norgestrel / Levonorgestrel CAS 6533-00-2 / CAS 797-63-7
Product Name: Norgestrel
Quality Standard : USP / BP / CP
Appearance: white crystalline powder
CAS No. : 6533-00-2
EINECS No. : 229-433-5
Molecular Formula: C21H28O2
Molecular Weight: 312.4458
Usage: Norgestrel is used in hormonal contraceptives.
Storage: Norgestrel should be stored in a well-closed container at low temperature, keep away from moisture, heat and light.
Note: Norgestrel for R&D use only.
Introduction of Norgestrel:
Norgestrel, sold under the brand name Ovral among others, is a progestin medication which is used in birth control pills and in menopausal hormone therapy. It is available both in combination with an estrogen and alone. It is taken by mouth.
Side effects of norgestrel include menstrual irregularities, headaches, nausea, breast tenderness, mood changes, acne, increased hair growth, and others. Norgestrel is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It has weak androgenic activity and no other important hormonal activity.
Norgestrel was introduced for medical use, specifically in birth control pills, in 1966. It was subsequently introduced for use in menopausal hormone therapy as well. Norgestrel is sometimes referred to as a "second-generation" progestin. It is marketed widely throughout the world. Norgestrel is available as a generic medication.
Norgestrel is used in combination with ethinylestradiol or quinestrol in combined birth control pills, alone in progestogen-only birth control pills, and in combination with estradiol or conjugated estrogens in menopausal hormone therapy. It has also been used as an emergency contraceptive in the Yuzpe regimen.
Pharmacodynamics / See also: Levonorgestrel § Pharmacodynamics
Norgestrel is a progestogen, or an agonist of the progesterone receptor. The biological activity of norgestrel lies in the levo enantiomer, levonorgestrel, whereas the dextro isomer is inactive. As such, norgestrel is identical in its hormonal activity to levonorgestrel except that it is half as potent by weight. Levonorgestrel, and by extension norgestrel, have some androgenic activity, but no estrogenic, antimineralocorticoid, or glucocorticoid activity.
What is Levonorgestrel?
Levonorgestrel is a second-generation progestin and is the most widely prescribed contraceptive progestin worldwide. It has high progestational and androgenic effects. Levonorgestrel negatively affects serum lipoproteins.
Levonorgestrel is used both as an emergency contraceptive as well as for long-term prevention of pregnancy. For the former it can be administered as an oral tablet after unprotected sexual intercourse. One 0.75 mg tablet should be taken as soon as possible within 72 hours of intercourse and a second 0.75 mg tablet should be taken 12 hours after the first dose.
For long-term pregnancy prevention and Intra-uterine system is inserted into the uterine cavity which releases 20 mcg Levonorgestrel/day over 5 years. It may be removed and replaced with a new unit at anytime during menstrual cycle.
Specification of Levonorgestrel:
BETWEEN 232°C AND 239°C
BETWEEN -30° AND -35°
LOSS ON DRYING
NOT MORE THAN 0.5%
RESIDUE ON IGNITION
NOT MORE THAN 0.3%
BETWEEN 7.81% AND 8.18%
BETWEEN 98.0% AND 102.0%
NOT MORE THAN 3000PPM
NOT MORE THAN 3000PPM
CONFORMS WITH USP30
More details about Norgestrel:
Norgestrel, also known as rac-13-ethyl-17α-ethynyl-19-nortestosterone or as rac-13-ethyl-17α-ethynylestr-4-en-17β-ol-3-one, is a synthetic estrane steroid and a derivative of testosterone. It is a racemic mixture of stereoisomers dextronorgestrel (the C13α isomer; l-norgestrel, L-norgestrel, or (+)-norgestrel) and levonorgestrel (the C13β isomer; d-norgestrel, D-norgestrel, or (–)-norgestrel), the former of which is inactive (making norgestrel exactly half as potent as levonorgestrel). Norgestrel is more specifically a derivative of norethisterone (17α-ethynyl-19-nortestosterone) and is a member of the gonane (18-methylestrane) subgroup of the 19-nortestosterone family of progestins.
History about Norgestrel:
Norgestrel was first introduced, as a birth control pill in combination with ethinylestradiol, under the brand name Eugynon in Germany in 1966. It was subsequently marketed as a combined birth control pill with ethinylestradiol in the United States under the brand name Ovral in 1968, and was marketed in many other countries as well.