Estradiol valerate/prasterone enanthate

Last updated
Estradiol valerate /
prasterone enanthate
Estradiol valerate.svg
Prasterone enanthate.svg
Estradiol valerate (top) and
prasterone enanthate (bottom)
Combination of
Estradiol valerate Estrogen
Prasterone enanthate Androgen; Estrogen; Neurosteroid
Clinical data
Trade names Gynodian Depot, Binodian Depot, Cidodian Depot, Klimax, Supligol NF
Other namesEV/DHEA-E; EV/PE; SH-70833-D
Routes of
administration 		Intramuscular injection
Identifiers
CAS Number
PubChem CID
UNII

Estradiol valerate/prasterone enanthate (EV/DHEA-E), sold under the brand name Gynodian Depot among others, is an injectable combination medication of estradiol valerate (EV), an estrogen, and prasterone enanthate (DHEA-E), an androgen, estrogen, and neurosteroid, which is used in menopausal hormone therapy for women. [1] [2] [3] [4] [5] [6] [7] [8] [9] It is provided in the form of 1 mL ampoules containing 4 mg estradiol valerate and 200 mg prasterone enanthate in an oil solution and is administered by intramuscular injection once every 4 to 6 weeks. [2] EV/DHEA-E reportedly has a duration of about 21 days. [10]

The medication is available in Europe, Latin America, and Egypt. [11] [12] [13] [14] EV/DHEA-E was developed and marketed by Schering, was first described in the literature in 1972, and was introduced for medical use in April 1975. [4] [15] [16] [17]

Androgen replacement therapy formulations and dosages used in women
RouteMedicationMajor brand namesFormDosage
Oral Testosterone undecanoate Andriol, JatenzoCapsule40–80 mg 1x/1–2 days
Methyltestosterone Metandren, EstratestTablet0.5–10 mg/day
Fluoxymesterone HalotestinTablet1–2.5 mg 1x/1–2 days
Normethandrone aGinecosideTablet5 mg/day
Tibolone LivialTablet1.25–2.5 mg/day
Prasterone (DHEA) b–Tablet10–100 mg/day
Sublingual Methyltestosterone MetandrenTablet0.25 mg/day
Transdermal Testosterone IntrinsaPatch150–300 μg/day
AndroGelGel, cream1–10 mg/day
Vaginal Prasterone (DHEA) IntrarosaInsert6.5 mg/day
Injection Testosterone propionate aTestovironOil solution25 mg 1x/1–2 weeks
Testosterone enanthate Delatestryl, Primodian DepotOil solution25–100 mg 1x/4–6 weeks
Testosterone cypionate Depo-Testosterone, Depo-TestadiolOil solution25–100 mg 1x/4–6 weeks
Testosterone isobutyrate aFemandren M, FolivirinAqueous suspension25–50 mg 1x/4–6 weeks
Mixed testosterone esters ClimacteronaOil solution150 mg 1x/4–8 weeks
Omnadren, SustanonOil solution50–100 mg 1x/4–6 weeks
Nandrolone decanoate Deca-DurabolinOil solution25–50 mg 1x/6–12 weeks
Prasterone enanthate aGynodian DepotOil solution200 mg 1x/4–6 weeks
Implant Testosterone TestopelPellet50–100 mg 1x/3–6 months
Notes: Premenopausal women produce about 230 ± 70 μg testosterone per day (6.4 ± 2.0 mg testosterone per 4 weeks), with a range of 130 to 330 μg per day (3.6–9.2 mg per 4 weeks). Footnotes:a = Mostly discontinued or unavailable. b = Over-the-counter. Sources: See template.
Estradiol and DHEA levels after a single intramuscular injection of Gynodian Depot (4 mg estradiol valerate, 200 mg prasterone enanthate in oil) in women. Estradiol and dehydroepiandrosterone levels after a single intramuscular injection of Gynodian Depot in women.png
Estradiol and DHEA levels after a single intramuscular injection of Gynodian Depot (4 mg estradiol valerate, 200 mg prasterone enanthate in oil) in women.

See also

Related Research Articles

<span class="mw-page-title-main">Estradiol valerate</span> Chemical compound

Estradiol valerate (EV), sold for use by mouth under the brand name Progynova and for use by injection under the brand names Delestrogen and Progynon Depot among others, is an estrogen medication. It is used in hormone therapy for menopausal symptoms and low estrogen levels, hormone therapy for transgender people, and in hormonal birth control. It is also used in the treatment of prostate cancer. The medication is taken by mouth or by injection into muscle or fat once every 1 to 4 weeks.

<span class="mw-page-title-main">Prasterone</span> Medical usage of the prasterone compound

Prasterone, also known as dehydroepiandrosterone (DHEA) and sold under the brand name Intrarosa among others, is a medication as well as over-the-counter dietary supplement which is used to correct DHEA deficiency due to adrenal insufficiency or old age, as a component of menopausal hormone therapy, to treat painful sexual intercourse due to vaginal atrophy, and to prepare the cervix for childbirth, among other uses. It is taken by mouth, by application to the skin, in through the vagina, or by injection into muscle.

<span class="mw-page-title-main">Polyestradiol phosphate</span> Chemical compound

Polyestradiol phosphate (PEP), sold under the brand name Estradurin, is an estrogen medication which is used primarily in the treatment of prostate cancer in men. It is also used in women to treat breast cancer, as a component of hormone therapy to treat low estrogen levels and menopausal symptoms, and as a component of feminizing hormone therapy for transgender women. It is given by injection into muscle once every four weeks.

<span class="mw-page-title-main">Estradiol benzoate</span> Chemical compound

Estradiol benzoate (EB), sold under the brand name Progynon-B among others, is an estrogen medication which is used in hormone therapy for menopausal symptoms and low estrogen levels in women, in hormone therapy for transgender women, and in the treatment of gynecological disorders. It is also used in the treatment of prostate cancer in men. Estradiol benzoate is used in veterinary medicine as well. When used clinically, the medication is given by injection into muscle usually two to three times per week.

<span class="mw-page-title-main">Estradiol cypionate</span> Chemical compound

Estradiol cypionate (EC), sold under the brand name Depo-Estradiol among others, is an estrogen medication which is used in hormone therapy for menopausal symptoms and low estrogen levels in women, in hormone therapy for trans women, and in hormonal birth control for women. It is given by injection into muscle once every 1 to 4 weeks.

<span class="mw-page-title-main">Estradiol enantate</span> Chemical compound

Estradiol enantate, also spelled estradiol enanthate and sold under the brand names Perlutal and Topasel among others, is an estrogen medication which is used in hormonal birth control for women. It is formulated in combination with dihydroxyprogesterone acetophenide, a progestin, and is used specifically as a combined injectable contraceptive. Estradiol enantate is not available for medical use alone. The medication, in combination with DHPA, is given by injection into muscle once a month.

<span class="mw-page-title-main">Estriol succinate</span> Chemical compound

Estriol succinate, sold under the brand name Synapause among others, is an estrogen medication which is used in the treatment of menopausal symptoms. It is taken by mouth, in through the vagina, and by injection.

<span class="mw-page-title-main">Estradiol undecylate</span> Chemical compound

Estradiol undecylate, also known as estradiol undecanoate and formerly sold under the brand names Delestrec and Progynon Depot 100 among others, is an estrogen medication which has been used in the treatment of prostate cancer in men. It has also been used as a part of hormone therapy for transgender women. Although estradiol undecylate has been used in the past, it was discontinued. The medication has been given by injection into muscle usually once a month.

An estrogen ester is an ester of an estrogen, most typically of estradiol but also of other estrogens such as estrone, estriol, and even nonsteroidal estrogens like diethylstilbestrol. Esterification renders estradiol into a prodrug of estradiol with increased resistance to first-pass metabolism, slightly improving its oral bioavailability. In addition, estrogen esters have increased lipophilicity, which results in a longer duration when given by intramuscular or subcutaneous injection due to the formation of a long-lasting local depot in muscle and fat. Conversely, this is not the case with intravenous injection or oral administration. Estrogen esters are rapidly hydrolyzed into their parent estrogen by esterases once they have been released from the depot. Because estradiol esters are prodrugs of estradiol, they are considered to be natural and bioidentical forms of estrogen.

<span class="mw-page-title-main">Estradiol hexahydrobenzoate</span> Chemical compound

Estradiol hexahydrobenzoate (EHHB), sold under a number of brand names including Benzo-Ginoestril A.P., BenzoGynoestryl Retard, Ginestryl-15-Depot, Menodin, and Tardoginestryl, is an estrogen medication which was previously used for indications such as menopausal hormone therapy and gynecological disorders. EHHB is given by injection into muscle at regular intervals, for instance once every few weeks.

<span class="mw-page-title-main">Estradiol dienantate</span> Chemical compound

Estradiol dienanthate (EDE), sold under the brand names Climacteron among others, is a long-acting estrogen medication which was previously used in menopausal hormone therapy for women and to suppress lactation in women. It was formulated in combination with estradiol benzoate (EB), a short-acting estrogen, and testosterone enanthate benzilic acid hydrazone (TEBH), a long-acting androgen/anabolic steroid. EDE has not been made available for medical use alone. The medication, in combination with EB and TEBH, was given by injection into muscle once or at regular intervals, for instance once every 6 weeks.

<span class="mw-page-title-main">Estradiol (medication)</span> Steroidal hormone medication

Estradiol (E2) is a medication and naturally occurring steroid hormone. It is an estrogen and is used mainly in menopausal hormone therapy and to treat low sex hormone levels in women. It is also used in hormonal birth control for women, in feminizing hormone therapy for transgender women, and in the treatment of hormone-sensitive cancers like prostate cancer in men and breast cancer in women, among other uses. Estradiol can be taken by mouth, held and dissolved under the tongue, as a gel or patch that is applied to the skin, in through the vagina, by injection into muscle or fat, or through the use of an implant that is placed into fat, among other routes.

<span class="mw-page-title-main">Prasterone enanthate</span> Chemical compound

Prasterone enanthate, also known as dehydroepiandrosterone enanthate (DHEA-E) 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.

The pharmacology of estradiol, an estrogen medication and naturally occurring steroid hormone, concerns its pharmacodynamics, pharmacokinetics, and various routes of administration.

<span class="mw-page-title-main">Estradiol benzoate/progesterone</span> Drug combination

Estradiol benzoate/progesterone (EB/P4), sold under the brand names Duogynon and Sistocyclin among others, is a combination medication of estradiol benzoate (EB), an estrogen, and progesterone (P4), a progestogen. It has been formulated both as short-acting oil solutions and long-acting microcrystalline aqueous suspensions and is given by injection into muscle either once or continuously at regular intervals.

<span class="mw-page-title-main">Polyestriol phosphate</span> Chemical compound

Polyestriol phosphate, sold under the brand names Gynäsan, Klimadurin, and Triodurin, is an estrogen medication which was previously used in menopausal hormone therapy and is no longer available.

<span class="mw-page-title-main">Estradiol valerate/cyproterone acetate</span> Combination drug

Estradiol valerate/cyproterone acetate (EV/CPA), sold under the brand names Climen and Femilar among others, is a combination product of estradiol valerate (EV), an estrogen, and cyproterone acetate (CPA), a progestogen, which is used in menopausal hormone therapy and as a birth control pill to prevent pregnancy. It is taken by mouth. Climen, which is used in menopausal hormone therapy, is a sequential preparation that contains 2 mg estradiol valerate and 1 mg CPA. It was the first product for use in menopausal hormone therapy containing CPA to be marketed and is available in more than 40 countries. Femilar, which is an estradiol-containing birth control pill, contains 1 to 2 mg estradiol valerate and 1 to 2 mg CPA, and has been approved for use in Finland since 1993.

<span class="mw-page-title-main">Estradiol benzoate/estradiol dienanthate/testosterone enanthate benzilic acid hydrazone</span> Combination drug

Estradiol benzoate/estradiol dienanthate/testosterone enanthate benzilic acid hydrazone (EB/EDE/TEBH), sold under the brand names Climacteron, Lactimex, Lactostat, and Amenose, is an injectable combination medication of estradiol benzoate (EB), an estrogen, estradiol dienanthate (EDE), an estrogen, and testosterone enanthate benzilic acid hydrazone (TEBH), an androgen/anabolic steroid, which is used in menopausal hormone therapy for peri- and postmenopausal women and to suppress lactation in postpartum women. Clinical studies have assessed this formulation.

<span class="mw-page-title-main">Estradiol valerate/testosterone enanthate</span> Combination drug

Estradiol valerate/testosterone enanthate (EV/TE), sold under the brand names Primodian Depot and Ditate among others, is an injectable combination medication of estradiol valerate (EV), an estrogen, and testosterone enanthate (TE), an androgen/anabolic steroid, which is used in menopausal hormone therapy for women. The medication is also used to suppress lactation in postpartum women.

Estradiol benzoate/estradiol valerate/norethisterone acetate/testosterone enanthate (EB/EV/NETA/TE), sold under the brand name Ablacton, is an injectable combination medication of estradiol benzoate (EB), an estrogen, estradiol valerate (EV), an estrogen, norethisterone acetate (NETA), a progestin, and testosterone enanthate (TE), an androgen/anabolic steroid, which has been used to suppress lactation in women. It contains 5 mg EB, 8 mg EV, 20 mg NETA, and 180 mg TE in oil solution and is provided in the form of ampoules. It is given as a single intramuscular injection following childbirth. The medication was manufactured by Schering and was previously marketed in Italy and Spain, but is no longer available.

References

  1. ↑ "Gynodian® Depot" (in German). Zürich: Bayer (Schweiz) AG. May 2017. Archived from the original on 29 May 2019. Retrieved 15 January 2022– via compendium.ch.
  2. 1 2 "Gynodian® Depot" (PDF). Bayer Middle East. Archived from the original (PDF) on 8 May 2019 – via HCP MEPPO (Modern Medicine).
  3. ↑ "Gynodian Depot" (PDF) (in Czech). Berlin: Bayer Pharma AG. 31 October 2011. Archived from the original (PDF) on 29 May 2019. Retrieved 15 January 2022– via www.sukl.cz.
  4. 1 2 Picha E, Weghaupt K (March 1972). "[Experience with a new hormone combination for menopausal disorders]" [Experience with a new hormone combination for menopausal disorders]. Medizinische Klinik (in German). 67 (11): 382–386. PMID   4259772. A new hormone combination for menopausal complaints. Since the treatment of menopausal complaints with estrogens as well as with the combination of estrogens and androgens causes undesired side effects such as bleeding, mammary changes and masculinisation, dehydroepiandrosteron (DHEA), a precursor of testosteron, has been synthesised, which has only a low conversion rate to free testosteron and no masculinising effect. The substance has been tested in combination with estrogen (200 mg DHEA-enanthate and 4 mg estradiolvalerianate per 1 ml) in 266 women with menopausal complaints. The duration of treatment has been up to 6 years with an injection interval of 3 to 8 weeks. The therapeutic results were as good as with estrogen-androgen-combinations, but there was no masculinising effect. Changes of voice, hair and libido caused by pretreatment partly disappeared. Side effects [such] as acne, mastodynia, and sensation of repletion were of transitory nature. This preparation seems to be a true alternative to the traditional estrogen-androgen-combinations.
  5. ↑ Lauritzen C (1980). "Erfahrungen in der Behandlung klimakterischer Beschwerden mit Depot-Injektionen von Östradiolvalerianat-Dehydroepiandrosteronönanthat" [Experience of treatment of climacteric symptoms with depot injections of estradiol valerianate-dehydroandrosterone enantate]. Die Therapiewoche. 30 (10): 1736–1742. ISSN   0040-5973. A trial of estradiol valerianate-dehydroandrosterone oenantate (Gynodian-Depot) was conducted in 68 post-menopausal women. The treatment exerted a very favorable influence on the typical subjective disorders of the climacteric and on the atrophic alterations of the target organs. Owing to its estrogenic and dehydroepiandrosterone components, the compound also exerts a favorable psychotropic effect. It was tolerated well and caused no side effects of any significance.
  6. ↑ Jurczok F (March 1976). "[Treatment of the climacteric symptom complex with a new combined hormone preparation]" [Treatment of the climacteric symptom complex with a new combined hormone preparation]. Fortschritte der Medizin (in German). 94 (9): 524–527. PMID   134967.
  7. ↑ Dinulović D, Radonjić G (1987). "[Gynodian-depot in the treatment of castration-induced postmenopause]" [Gynodian-depot in the treatment of castration-induced postmenopause]. Jugoslavenska Ginekologija I Perinatologija (in Croatian). 27 (1–2): 37–40. PMID   2960859.
  8. 1 2 Düsterberg B, Wendt H (1983). "Plasma levels of dehydroepiandrosterone and 17 beta-estradiol after intramuscular administration of Gynodian-Depot in 3 women". Hormone Research. 17 (2): 84–89. doi:10.1159/000179680. PMID   6220949.
  9. 1 2 Kuhl H, Taubert HD (1987). Das Klimakterium – Pathophysiologie, Klinik, Therapie[The Climacteric – Pathophysiology, Clinic, Therapy] (in German). Stuttgart, Germany: Thieme Verlag. p. 122. ISBN   978-3137008019.
  10. ↑ Ufer J (1 January 1978). Hormontherapie in der Frauenheilkunde: Grundlagen und Praxis[Hormone Therapy in Gynecology: Principles and Practice] (in German) (5th ed.). de Gruyter. p. 276. ISBN   978-3-11-006664-7. OCLC   924728827.
  11. ↑ "Prasterone (Dehydroepiandrosterone, DHEA) vaginal Uses, Side Effects & Warnings".
  12. ↑ Sweetman SC, ed. (2009). "Sex hormones and their modulators". Martindale: The Complete Drug Reference (36th ed.). London: Pharmaceutical Press. pp. 2100, 2124–2125. ISBN   978-0-85369-840-1.
  13. ↑ "Home". micromedexsolutions.com.
  14. ↑ Muller MF, Dessing RP (19 June 1998). European Drug Index: European Drug Registrations (Fourth ed.). CRC Press. pp. 566–567. ISBN   978-3-7692-2114-5.
  15. ↑ Sauer F (February 2008). Erfolgsfaktoren für das marktorientierte Management patentgeschützter Arzneimittel: eine Analyse der Produktwahrnehmung niedergelassener Vertragsärzte unter der Berücksichtigung unsicherer Therapieergebnisse. BoD – Books on Demand. pp. 37, 346. ISBN   978-3-936863-12-3.
  16. ↑ Kaufmann M, Costa SD, Scharl A (27 November 2013). Die Gynäkologie. Springer-Verlag. pp. 917–. ISBN   978-3-662-11496-4.
  17. ↑ Kleemann A, Engel J, Kutscher B, Reichert D (14 May 2014). Pharmaceutical Substances, 5th Edition, 2009: Syntheses, Patents and Applications of the most relevant APIs. Thieme. pp. 1172–1174, 2441–2442. ISBN   978-3-13-179525-0.
  18. ↑ Rauramo L, Punnonen R, Kaihola LH, Grönroos M (January 1980). "Serum oestrone, oestradiol and oestriol concentrations in castrated women during intramuscular oestradiol valerate and oestradiolbenzoate-oestradiolphenylpropionate therapy". Maturitas. 2 (1): 53–58. doi:10.1016/0378-5122(80)90060-2. PMID   7402086.


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