What is "norgestimate"

n. A form of progestin, used in hormonal contraceptives.

Norgestimate ( INN, USAN, BAN) is an acetylated progestin used as an oral contraceptive. It acts as a prodrug to norelgestromin (17-deacetylnorgestimate or levonorgestrel 3-oxime), the primary active metabolite, and levonorgestrel (~22% of an administered dose; deacetylation of norgestimate occurs in the intestines and the liver), as well as levonorgestrel-17-acetate. Unlike levonorgestrel, norgestimate shows high selectivity for the progesterone receptor and low androgenic action due to a large drug-induced elevation in the level of sex hormone-binding globulin (SHBG) (which preferentially binds androgens and thus inhibits their action). Moreover, unlike other 19-nortestosterone progestins, norgestimate does not bind to or occupy SHBG itself. In accordance, clinical trials of norgestimate have observed minimal androgenic side effects. The drug is used in combination with ethinyl estradiol as an oral contraceptive. It was introduced in 1986.