The Sound of Evolution
Norgestimate
Mechanism of action:
Norgestimate is a synthetic progestin and a derivative of 19-nortestosterone. Norgestimate suppresses the hypothalamic-pituitary-gonadal axis through negative feedback, reducing the luteinizing hormone (LH) surge and preventing normal follicular rupture, thereby inhibiting or delaying ovulation. Norgestimate also thickens cervical mucus, making it more difficult for sperm to pass through the cervix into the uterine cavity and reducing the likelihood of fertilization. In addition, norgestimate keeps the endometrium in a thin, non-proliferative state, which makes embryo implantation less favorable even if fertilization occurs.
Reference(s):
1. Saxena A et al. (2015). Quantification of 17-desacetyl norgestimate in human plasma by liquid chromatography-tandem mass spectrometry (LC-MS/MS) and its application to bioequivalence study. J Pharm Anal.
2. Ahire D et al. (2017). Metabolite Identification, Reaction Phenotyping, and Retrospective Drug-Drug Interaction Predictions of 17-Deacetylnorgestimate, the Active Component of the Oral Contraceptive Norgestimate. Drug Metab Dispos.
3. Hammond GL et al. (2003). Serum distribution of the major metabolites of norgestimate in relation to its pharmacological properties. Contraception.