Estradiol valerate/prasterone enanthate

Last updated
Estradiol valerate /
prasterone enanthate
Estradiol valerate.svg
Prasterone enanthate.svg
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) bTablet10–100 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

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.