Estradiol enantate/algestone acetophenide

Estradiol enantate/algestone acetophenide, also known as estradiol enantate/dihydroxyprogesterone acetophenide (E2-EN/DHPA) and sold under the brand names Perlutal and Topasel among others, is a form of combined injectable birth control which is used to prevent pregnancy. It contains estradiol enantate (E2-EN), an estrogen, and algestone acetophenide (dihydroxyprogesterone acetophenide; DHPA), a progestin. The medication is given once a month by injection into muscle.

E2-EN/DHPA is used widely throughout Latin America, is also marketed in Hong Kong, and was previously available in Portugal and Spain as well but was discontinued in these countries.

Medical uses

E2-EN/DHPA is used in combination as a once-monthly combined injectable contraceptive to prevent pregnancy in women in Latin America and Hong Kong. E2-EN/DHPA is used as a form of feminizing hormone therapy for travestis and trans women in South America.

Available forms

The following forms of E2-EN/DHPA are or have been available for use:

E2-EN 10 mg and DHPA 150 mg (brand names Perlutal, Topasel, many others)

E2-EN 5 mg and DHPA 75 mg (brand names Anafertin, Patector NF, Yectames)

E2-EN 10 mg and DHPA 120 mg (brand names Unalmes, Yectuna)

E2-EN 10 mg and DHPA 75 mg (brand name Ova Repos; discontinued)

A 6 mg E2-EN and 90 mg DHPA formulation was also studied, but was never marketed. The combination of E2-EN and DHPA has also been studied at other doses ranging from 5 to 50 mg E2-EN and 75 to 200 mg DHPA.

Pharmacology

Pharmacology

Clinical studies have found that, on the basis of endometrial changes, E2-EN/DHPA appears, at the doses used, to be an estrogen-dominant combination.

Pharmacokinetics

By intramuscular injection, the elimination half-life of E2-EN has been found to be 5.6 to 7.5 days, while the half-life of algestone acetophenide and its metabolites has been found to be 24 days. Following a single injection, E2-EN and DHPA are detectable in the circulation for up to 30 to 60 days.