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Estradiol benzoate/estradiol dienanthate/testosterone enanthate benzilic acid hydrazone

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(Redirected fromClimacteron)
Not to be confused withClimactericorLactinex.
EB/EDE/TEBH
Combination of
Estradiol benzoateEstrogen
Estradiol dienanthateEstrogen
Testosterone enanthate benzilic acid hydrazoneAndrogen;Anabolic steroid
Clinical data
Trade namesClimacteron, Lactimex, Lactostat, Amenose
Other namesEB/EDE/TEBH
Routes of
administration		Intramuscular injection
Identifiers
CAS Number
PubChemCID

Estradiol benzoate/estradiol dienanthate/testosterone enanthate benzilic acid hydrazone(EB/EDE/TEBH), sold under the brand namesClimacteron,Lactimex,Lactostat,andAmenose,is aninjectablecombination medicationofestradiol benzoate(EB), anestrogen,estradiol dienanthate(EDE), an estrogen, andtestosterone enanthate benzilic acid hydrazone(TEBH), anandrogen/anabolic steroid,which is used inmenopausal hormone therapyforperi-andpostmenopausalwomen and to suppresslactationinpostpartumwomen.[1][2][3][4][5][6][7]Clinical studies have assessed this formulation.[8][9][10][11][12][13][14][15][16][17][18][19][1]

Climacteron and Amenose contained 1.0 mg EB, 7.5 mg EDE, and 150 mg TEBH (69 mg freetestosterone) and was used to treatmenopausal symptoms.[20][17][21]They were administered byintramuscular injectiontypically once every 6 weeks but with a range of every 4 to 8 weeks or less frequently.[20]Climacteron was marketed inCanadain 1961 but waswithdrawnin this country in October 2005 due to risk ofendometrial hyperplasiaandcancerfrom unopposed estrogen exposure (i.e., no concomitantprogestogen) as well as induction of supraphysiologicaltestosteronelevels.[1][22][23]

Lactimex and Lactostat contained 6 mg EB, 15 mg EDE, and 300 mg TEBH in 2 mL ofcorn oiland were used to suppress lactation.[2][3][24][25]They were administered as a single intramuscular injection afterchildbirthor duringbreastfeeding.[2]They were previously available inGermanyand Canada.[2][25]

Estradiolandtestosteronelevels following a single intramuscular injection of EB/EDE/TEBH versus 10 mgestradiol valeratehave been studied over 28 days.[14][16]

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:Premenopausalwomen produce about 230 ± 70 μgtestosteroneper 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.
Potencies and durations of natural estrogens by intramuscular injection
Estrogen Form Dose (mg) Duration by dose (mg)
EPD CICD
Estradiol Aq. soln. ? – <1 d
Oil soln. 40–60 – 1–2 ≈ 1–2 d
Aq. susp. ? 3.5 0.5–2 ≈ 2–7 d; 3.5 ≈ >5 d
Microsph. ? – 1 ≈ 30 d
Estradiol benzoate Oil soln. 25–35 – 1.66 ≈ 2–3 d; 5 ≈ 3–6 d
Aq. susp. 20 – 10 ≈ 16–21 d
Emulsion ? – 10 ≈ 14–21 d
Estradiol dipropionate Oil soln. 25–30 – 5 ≈ 5–8 d
Estradiol valerate Oil soln. 20–30 5 5 ≈ 7–8 d; 10 ≈ 10–14 d;
40 ≈ 14–21 d; 100 ≈ 21–28 d
Estradiol benz. butyrate Oil soln. ? 10 10 ≈ 21 d
Estradiol cypionate Oil soln. 20–30 – 5 ≈ 11–14 d
Aq. susp. ? 5 5 ≈ 14–24 d
Estradiol enanthate Oil soln. ? 5–10 10 ≈ 20–30 d
Estradiol dienanthate Oil soln. ? – 7.5 ≈ >40 d
Estradiol undecylate Oil soln. ? – 10–20 ≈ 40–60 d;
25–50 ≈ 60–120 d
Polyestradiol phosphate Aq. soln. 40–60 – 40 ≈ 30 d; 80 ≈ 60 d;
160 ≈ 120 d
Estrone Oil soln. ? – 1–2 ≈ 2–3 d
Aq. susp. ? – 0.1–2 ≈ 2–7 d
Estriol Oil soln. ? – 1–2 ≈ 1–4 d
Polyestriol phosphate Aq. soln. ? – 50 ≈ 30 d; 80 ≈ 60 d
Notes and sources
Notes:Allaqueous suspensionsare ofmicrocrystallineparticle size.Estradiolproduction during themenstrual cycleis 30–640 µg/d (6.4–8.6 mg total per month or cycle). Thevaginalepitheliummaturation dosage ofestradiol benzoateorestradiol valeratehas been reported as 5 to 7 mg/week. An effectiveovulation-inhibiting doseofestradiol undecylateis 20–30 mg/month.Sources:See template.
Hormone levels with estradiol benzoate/estradiol dienanthate/testosterone enanthate benzilic acid hydrazone by intramuscular injection

See also

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References

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  1. ^abcAl-Imari L, Wolfman WL (September 2012). "The safety of testosterone therapy in women".Journal of Obstetrics and Gynaecology Canada.34(9): 859–865.doi:10.1016/S1701-2163(16)35385-3.PMID22971455.
  2. ^abcdGeburtshilfe und Frauenheilkunde: Ergebnisse der Forschung für die Praxis.Georg Thieme Verlag. 1969. p. 387,390.[Kelly and Primose and Dodek found the following androgen-estrogen combination to be particularly effective and well-tolerated: 300 mg 3-benzilic acid hydrazone-testosterone-17-enanthate, 15 mg estradiol di-enanthate, 6 mg estradiol benzoate in 2 ml corn oil. This product is sold in Germany under the name Lactimex and has been clinically examined by us.] [...] Of 1200 postpartum patients one quarter stopped breast feeding for a variety of reasons and received an injection of Lactimex (Protina: Benzil acid hydrazon-testosteron-oenanthat 300 mg, Oestradiol-di-oenanthat 15 mg and Oestradiol-benzoate 6 mg in 1.0 ml of oil). In 76% of cases one injection was sufficient and the remaining 24% required a second injection. A second injection was required rarer if the first injection had been longer after delivery. A higher dosage of Lactimex was not necessary in cases with a preceding medical induction with intraveinous Oxytocin (Orasthin). Mothers who had been treated postpartum with methylergobasin did not as often require a second injection. No localized or generalized adverse reaction to the drug was noticed.
  3. ^abZentralblatt für Gynäkologie.J. A. Barth. 1971.The preparation Lactimex (300 mg 3-benzyl hydrazone-testosterone-17-enanthate + 15 mg estradiol-dienanthate + 6 mg estradiol benzoate in 2 ml corn oil) was injected. [...]
  4. ^Ginsburg ES (1999). "Androgen Replacement in Postmenopausal Women". In Seifer DB, Kennard EA (eds.).Menopause.Contemporary Endocrinology. Vol. 18. Humana Press. pp. 209–219.doi:10.1007/978-1-59259-246-3_13.ISBN978-1-61737-129-5.
  5. ^Greenblatt RB, Barfield WE, Jungck EC (January 1962)."The treatment of the menopause".Canadian Medical Association Journal.86(3): 113–114.PMC1848811.PMID13901504.
  6. ^Seifer DB (27 July 1999). Seifer DB, Kennard EA (eds.).Menopause: Endocrinology and Management.Springer Science & Business Media. pp. 183–.doi:10.1007/978-1-59259-246-3.ISBN978-1-59259-246-3.
  7. ^Hager HH, Kern W, Heinz P, Roth HJ (29 July 2013).Hagers Handbuch der Pharmazeutischen Praxis: Für Apotheker, Arzneimittelhersteller, Ärzte und Medizinalbeamte: Wirkstoffgruppen II Chemikalien und Drogen (A-AL).Springer-Verlag. pp. 157–.ISBN978-3-662-25655-8.
  8. ^Kelly MJ, Primrose T (December 1960)."Evaluation of a new preparation for the suppression of lactation".Canadian Medical Association Journal.83(24): 1240–1242.PMC1938994.PMID13752392.
  9. ^Schneider J, Macarthur JL, Patrick JW, Burton GV (August 1964)."The Suppression of Lactation: An Objective Study".Obstetrics and Gynecology.24(2): 294–297.PMID14199544.
  10. ^Sherwin BB, Gelfand MM (March 1984). "Effects of parenteral administration of estrogen and androgen on plasma hormone levels and hot flushes in the surgical menopause".American Journal of Obstetrics and Gynecology.148(5): 552–557.doi:10.1016/0002-9378(84)90746-4.PMID6367474.
  11. ^Sherwin BB, Gelfand MM (January 1985). "Differential symptom response to parenteral estrogen and/or androgen administration in the surgical menopause".American Journal of Obstetrics and Gynecology.151(2): 153–160.doi:10.1016/0002-9378(85)90001-8.PMID3881960.
  12. ^Sherwin BB (September 1985). "Changes in sexual behavior as a function of plasma sex steroid levels in post-menopausal women".Maturitas.7(3): 225–233.doi:10.1016/0378-5122(85)90044-1.PMID4079822.
  13. ^Sherwin BB, Gelfand MM (1985). "Sex steroids and affect in the surgical menopause: a double-blind, cross-over study".Psychoneuroendocrinology.10(3): 325–335.doi:10.1016/0306-4530(85)90009-5.PMID3903822.S2CID40861936.
  14. ^abcdeSherwin BB, Gelfand MM, Schucher R, Gabor J (February 1987). "Postmenopausal estrogen and androgen replacement and lipoprotein lipid concentrations".American Journal of Obstetrics and Gynecology.156(2): 414–419.doi:10.1016/0002-9378(87)90295-X.PMID3826177.
  15. ^abcdSherwin BB, Gelfand MM (1987). "Individual differences in mood with menopausal replacement therapy: possible role of sex hormone-binding globulin".Journal of Psychosomatic Obstetrics & Gynecology.6(2): 121–131.doi:10.3109/01674828709016773.ISSN0167-482X.
  16. ^abSherwin BB (1988). "Affective changes with estrogen and androgen replacement therapy in surgically menopausal women".Journal of Affective Disorders.14(2): 177–187.doi:10.1016/0165-0327(88)90061-4.PMID2966832.
  17. ^abSherwin BB (1988). "Estrogen and/or androgen replacement therapy and cognitive functioning in surgically menopausal women".Psychoneuroendocrinology.13(4): 345–357.doi:10.1016/0306-4530(88)90060-1.PMID3067252.S2CID24695692.
  18. ^Sherwin BB (1994). "The Effect of Sex Steroids on Brain Mechanisms Relating to Mood and Sexuality".Comprehensive Management of Menopause.Clinical Perspectives in Obstetrics and Gynecology. Springer. pp. 327–333.doi:10.1007/978-1-4612-4330-4_31.ISBN978-1-4612-8737-7.ISSN0178-0328.
  19. ^Sherwin BB (April 2002)."Randomized clinical trials of combined estrogen-androgen preparations: effects on sexual functioning".Fertility and Sterility.77(Suppl 4): S49–S54.doi:10.1016/S0015-0282(02)03002-9.PMID12007902.
  20. ^ab"Climacteron Drug Information, Professional".Drugs.com.Archived fromthe originalon 2 June 2019.Retrieved2 June2019.
  21. ^Bundesverband der Pharmazeutischen Industrie (Germany) (1974).Rote Liste: Verzeichnis pharmazeutischer Spezialpräparate.Editio Cantor.ISBN9783871930133.49035 В Amenose® Rp Ampullen Zus.: 1 Amp. 1 ml enth.: Benzilsäurehydrazid-N-testosteron-hydrazon-17-oenanthat 150 mg, Oestradiol-di-oenanthat 7.5 mg. Oestradiolbenzoat 1 mg in öl-Lösg. Ind.: Androgen-Oestrogen-Gemisch. Gegen Ausfallserscheinungen im Klimakterium und nach Ovarektomie. Osteoporose. Kontraind.: A 90, О 5 Dos.: Durchschnittl. alle 6 Wochen 1 Amp. im. 1 Amp. I ml 6.75 3 Amp 17.40 AP.: 10 Amp.
  22. ^Lexchin J (2010)."Drug safety and Health Canada".International Journal of Risk & Safety in Medicine.22(1): 41–53.doi:10.3233/JRS-2010-0490.
  23. ^"Discontinuation of CLIMACTERON® Injection (estradiol dienanthate ⁄ estradiol benzoate and testosterone enanthate benzilic acid hydrazone injection in corn oil)"(PDF).Sandoz Canada Inc.23 November 2005. Archived fromthe original(PDF)on 2013-01-11.Retrieved2 June2019.
  24. ^Vorherr H (2 December 2012).The Breast: Morphology, Physiology, and Lactation.Elsevier Science. pp. 201–.ISBN978-0-323-15726-1.
  25. ^abCompendium of Pharmaceuticals and Specialties.Canadian Pharmaceutical Association. 1983.ISBN978-0-919115-04-0.LACTOSTAT [...] Each 2 mL of injectable solution contains testosteorne enanthate benzilic acid hydrazone 300 mg, estradiol dienanthate 15 mg, estradiol benzoate 6 mg, benzyl alcohol 7.5% as preservative, benzyl benzoate 0.75 mg, corn oil q.s. Available in 2 mL ampuls, boxes of 25.
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