Estradiol enantate
Estradiol enantate, sold under the brand names Perlutal and Topasel among others, is an estrogen medication which is used in hormonal birth control. It is formulated in combination with dihydroxyprogesterone acetophenide (DHPA; algestone acetophenide), a progestin, and is used as a combined injectable contraceptive. Estradiol enantate is not available alone. The medication is given by injection into muscle once a month.
Side effects of estradiol enantate include breast tenderness, breast enlargement, nausea, headache, and fluid retention. The drug is a synthetic estrogen and hence is an agonist of the estrogen receptor (ER), the biological target of estrogens like estradiol. Estradiol enantate is an estrogen ester and a long-lasting prodrug of estradiol in the body. Because of this, it is considered to be a natural and bioidentical form of estrogen.
Estradiol enantate was first described by 1954, and was first studied in combination with DHPA as a combined injectable contraceptive in 1964. The combination was introduced for clinical use by the mid-1970s. Estradiol enantate is not available as a standalone medication (i.e., by itself without DHPA). The combination is available in Latin America and Hong Kong, and was also previously marketed in Spain and Portugal.
Pharmacokinetics of estradiol
Estradiol can be taken sublingually instead of orally. Non-micronized estradiol is insoluble in water, but micronized estradiol is rapidly absorbed by the sublingual route. All oral estradiol tablets are micronized, as estradiol is not absorbed efficiently in the gastrointestinal tract otherwise. The absorption of sublingual estradiol can be attributed to the rich vascularization under the tongue. With administration of an oral estradiol tablet sublingually, complete dissolution of the tablet occurs within a few minutes and circulating levels of estradiol begin to rise within 5 minutes. Maximal levels of estradiol occur after 30 to 60 minutes of administration. After this, estradiol levels drop steeply within 4 hours, and this is followed by a more gradual decline in levels of estradiol and a return to baseline concentrations by 24 hours. The rapid rise and steep fall of estradiol levels with sublingual administration of estradiol is analogous to the case of intravenous injection and intranasal administration of the hormone.