Norgestrel is a synthetic progestin that has 2 stereoisomers, the active one is called levonorgestrel and the other one is dextronorgestrel. This drug is used in combination with ethinyl estradiol for oral contraception and prevention of pregnancy in women. Levonorgestrel (the active stereoisomer of norgestrel) binds the progesterone and estrogen receptors. Those receptors are found in the mammary glands, the hypothalamus, and in the pituitary gland. With this binding, levonorgestrel inhibits and downgrades the level of secretion of gonadotropin-releasing hormone (GnRH) from the hypothalamus. In consequence, this activity will lower the transcription rate of luteinizing hormone (LH) resulting in the inhibition of its normal surge needed for ovulation. This drug is administered as an oral tablet.
References
Norgestrel Pathway References
Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M: DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. doi: 10.1093/nar/gkx1037.
Hammond GL, Rabe T, Wagner JD: Preclinical profiles of progestins used in formulations of oral contraceptives and hormone replacement therapy. Am J Obstet Gynecol. 2001 Aug;185(2 Suppl):S24-31. doi: 10.1067/mob.2001.117415.
Kloosterboer HJ, Vonk-Noordegraaf CA, Turpijn EW: Selectivity in progesterone and androgen receptor binding of progestagens used in oral contraceptives. Contraception. 1988 Sep;38(3):325-32. doi: 10.1016/0010-7824(88)90104-7.
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