Prasterone enanthate
Prasterone enanthate, also known as dehydroepiandrosterone enanthate and sold in combination with estradiol valerate under the brand name Gynodian Depot among others, is a weak androgen, estrogen, and neurosteroid medication which is used as a component of menopausal hormone therapy to treat menopausal symptoms in women. It is available only as an injectable preparation in combination with estradiol valerate. The medication is given by injection into muscle typically once every 4 weeks.
Prasterone enanthate is a synthetic androgen, estrogen, and neurosteroid. It is a steroid ester and a long-lasting prodrug of prasterone in the body. Prasterone is a naturally occurring prohormone of androgens and estrogens and hence is an agonist of the androgen and estrogen receptors, the respective biological targets of androgens like testosterone and estrogens like estradiol. Prasterone also has a variety of activities of its own, including neurosteroid and other activities. An injection of prasterone enanthate has a duration of action in terms of elevated prasterone levels of about 18 days.
The combination of estradiol valerate and prasterone enanthate was developed as early as 1966 and was introduced for medical use in 1975. The formulation is marketed widely throughout Europe, and is also available in several Latin American countries and in Egypt. It is not available in any predominantly English-speaking countries.
Medical uses
The combination of estradiol valerate and prasterone enanthate is used in menopausal hormone therapy to treat menopausal symptoms in peri- and postmenopausal women. Estradiol valerate serves as an estrogen in the preparation, while prasterone enanthate is intended to serve as a weak androgen. It is thought that the inclusion of prasterone enanthate in the formulation may provide additional psychotropic benefits.Available forms
Prasterone enanthate is available only as a combination formulation of 4 mg estradiol valerate and 200 mg prasterone enanthate in oil for depot intramuscular injection.Side effects
Prasterone enanthate, in combination with estradiol valerate at the dosages used clinically, has no masculinizing side effects. This is in contrast to combinations of estrogens with other androgens, such as testosterone esters.The following is a list of possible side-effects that may occur in medicines that contain Estradiol Valerate / Prasterone Enanthate. This is not a comprehensive list. These side-effects are possible, but do not always occur. Some of the side-effects may be rare but serious. Consult your doctor if you observe any of the following side-effects, especially if they do not go away.
Dysmenorrhea
Vaginitis
Ovarian cancer
Endometrial hyperplasia
Endometrial cancer
Breast cancer
Stroke
Increase in blood pressure
Pulmonary embolism
Nausea
Vomiting
Abdominal cramps
Bloating
Cholestatic jaundice
Pruritus
Rash
Dizziness
Estradiol Valerate / Prasterone Enanthate may also cause side-effects not listed here.
Pharmacology
Pharmacokinetics
The pharmacokinetics of prasterone enanthate have been assessed in a number of studies.Prasterone enanthate is a prodrug of prasterone in the body. It is completely hydrolyzed into prasterone and heptanoic acid following absorption from the tissue depot after intramuscular injection.
Levels of DHEA peak at about 9 ng/mL within 1 to 4 days of an injection of prasterone enanthate. Subsequently, DHEA levels return to baseline by about 18 days following the injection. Prasterone enanthate has an elimination half-life of about 9 days. The plasma half-life of DHEA/prasterone enanthate following an intravenous injection is about 44 minutes. The half-lives of DHEA metabolites range up to 3.6 days.
Within 30 days, 91% of a dose of prasterone enanthate is eliminated. Approximately 94% is excreted in urine and 6% in feces. Prasterone enanthate is eliminated mainly in the form of metabolites and conjugates.