Estradiol valerate/prasterone enanthate

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Estradiol valerate /
prasterone enanthate
Estradiol valerate (top) and
prasterone enanthate (bottom)
Combination of
Estradiol valerateEstrogen
Prasterone enanthateAndrogen; Estrogen; Neurosteroid
Clinical data
Trade namesGynodian 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

Estradiol valerate/prasterone enanthate (EV/DHEA-E), sold under the brand name Gynodian Depot among others, is a 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
Route Medication Major brand names Form Dosage
Oral Testosterone undecanoate Andriol, Jatenzo Capsule 40–80 mg 1x/1–2 days
Methyltestosterone Metandren, Estratest Tablet 0.5–10 mg/day
Fluoxymesterone Halotestin Tablet 1–2.5 mg 1x/1–2 days
Normethandronea Ginecoside Tablet 5 mg/day
Tibolone Livial Tablet 1.25–2.5 mg/day
Prasterone (DHEA)b – Tablet 10–100 mg/day
Sublingual Methyltestosterone Metandren Tablet 0.25 mg/day
Transdermal Testosterone Intrinsa Patch 150–300 μg/day
AndroGel Gel, cream 1–10 mg/day
Vaginal Prasterone (DHEA) Intrarosa Insert 6.5 mg/day
Injection Testosterone propionatea Testoviron Oil solution 25 mg 1x/1–2 weeks
Testosterone enanthate Delatestryl, Primodian Depot Oil solution 25–100 mg 1x/4–6 weeks
Testosterone cypionate Depo-Testosterone, Depo-Testadiol Oil solution 25–100 mg 1x/4–6 weeks
Testosterone isobutyratea Femandren M, Folivirin Aqueous suspension 25–50 mg 1x/4–6 weeks
Mixed testosterone esters Climacterona Oil solution 150 mg 1x/4–8 weeks
Omnadren, Sustanon Oil solution 50–100 mg 1x/4–6 weeks
Nandrolone decanoate Deca-Durabolin Oil solution 25–50 mg 1x/6–12 weeks
Prasterone enanthatea Gynodian Depot Oil solution 200 mg 1x/4–6 weeks
Implant Testosterone Testopel Pellet 50–100 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.[9][8][18]

See also

References

  1. ^ https://web.archive.org/web/20190529041314/https://compendium.ch/FrmMainMonographie.aspx?Id=4a7e55ac-b11f-4d80-96d0-b468ab0eb4e3&lang=de&MonType=fi&start=1
  2. ^ a b http://www.meppo.com/pdf/drugs/859-GYNODIAN-DEPOT-1440663828.pdf
  3. ^ https://web.archive.org/web/20190529041214/http://www.sukl.cz/download/pil/PI23959.pdf
  4. ^ a b Picha E, Weghaupt K (March 1972). "Erfahrungen mit einer neuen Hormonkombination bei klimakterischen Beschwerden" [Experience with a new hormone combination for menopausal disorders]. Med Klin (in German). 67 (11): 382–6. ISSN 0025-8458. 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). "Behandlung des klimakterischen Symptomenkomplexes mit einem neuen Hormon-Kombinationspräparat" [Treatment of the climacteric symptom complex with a new combined hormone preparation]. Fortschr. Med. (in German). 94 (9): 524–7. ISSN 0015-8178. PMID 134967.
  7. ^ Dinulović D, Radonjić G (1987). "Gynodian-depot u lecenju kastracione postmenopauze" [Gynodian-depot in the treatment of castration-induced postmenopause]. Jugosl Ginekol Perinatol (in Croatian). 27 (1–2): 37–40. ISSN 0352-5562. PMID 2960859.
  8. ^ a b Düsterberg B, Wendt H (1983). "Plasma levels of dehydroepiandrosterone and 17 beta-estradiol after intramuscular administration of Gynodian-Depot in 3 women". Horm. Res. 17 (2): 84–9. doi:10.1159/000179680. PMID 6220949.
  9. ^ a b Kuhl, Herbert; Taubert, Hans-Dieter (1987). Das Klimakterium – Pathophysiologie, Klinik, Therapie [The Climacteric – Pathophysiology, Clinic, Therapy] (in German). Stuttgart, Germany: Thieme Verlag. p. 122. ISBN 978-3137008019.
  10. ^ Ufer, Joachim (1 January 1978). Hormontherapie in der Frauenheilkunde: Grundlagen und Praxis [Hormone Therapy in Gynecology: Principles and Practice] (in German) (5 ed.). de Gruyter. p. 276. ISBN 978-3110066647. OCLC 924728827.
  11. ^ https://www.drugs.com/international/prasterone.html
  12. ^ Sweetman, Sean C., 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. ^ https://www.micromedexsolutions.com/
  14. ^ Muller (19 June 1998). European Drug Index: European Drug Registrations, Fourth Edition. CRC Press. pp. 566–567. ISBN 978-3-7692-2114-5.
  15. ^ Florian Sauer (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. ^ Manfred Kaufmann; Serban-Dan Costa; Anton Scharl (27 November 2013). Die Gynäkologie. Springer-Verlag. pp. 917–. ISBN 978-3-662-11496-4.
  17. ^ A. Kleemann; J. Engel; B. Kutscher; D. Reichert (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): 53–8. doi:10.1016/0378-5122(80)90060-2. PMID 7402086.


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