Estradiol benzoate/estradiol dienanthate/testosterone enanthate benzilic acid hydrazone explained

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.[1] [2] [3] [4] [5] [6] Clinical studies have assessed this formulation.[7] [8] [9] [10] [11] [12] [13] [14] [15] [16] [17] [18] [19]

Climacteron and Amenose contained 1.0 mg EB, 7.5 mg EDE, and 150 mg TEBH (69 mg free testosterone) and was used to treat menopausal symptoms.[20] [16] [21] They were administered by intramuscular injection typically once every 6 weeks but with a range of every 4 to 8 weeks or less frequently. Climacteron was marketed in Canada in 1961 but was withdrawn in this country in October 2005 due to risk of endometrial hyperplasia and cancer from unopposed estrogen exposure (i.e., no concomitant progestogen) as well as induction of supraphysiological testosterone levels.[22] [23]

Lactimex and Lactostat contained 6 mg EB, 15 mg EDE, and 300 mg TEBH in 2 mL of corn oil and were used to suppress lactation.[24] [25] They were administered as a single intramuscular injection after childbirth or during breastfeeding. They were previously available in Germany and Canada.

Estradiol and testosterone levels following a single intramuscular injection of EB/EDE/TEBH versus 10 mg estradiol valerate have been studied over 28 days.[15]

See also

Notes and References

  1. Book: Geburtshilfe und Frauenheilkunde: Ergebnisse der Forschung für die Praxis. 1969. Georg Thieme Verlag.. 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..
  2. Book: Zentralblatt für Gynäkologie. 1971. J. A. Barth. 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. [...].
  3. Book: Ginsburg ES . Seifer DB, Kennard EA . Menopause . 1999 . 18 . 209–219 . 10.1007/978-1-59259-246-3_13 . Androgen Replacement in Postmenopausal Women . Contemporary Endocrinology . Humana Press . 978-1-61737-129-5.
  4. Greenblatt RB, Barfield WE, Jungck EC . The treatment of the menopause . Canadian Medical Association Journal . 86 . 3 . 113–114 . January 1962 . 13901504 . 1848811 .
  5. Book: Menopause: Endocrinology and Management . Springer Science & Business Media . 27 July 1999 . Seifer DB . Seifer DB, Kennard EA . 183– . 978-1-59259-246-3 . 10.1007/978-1-59259-246-3.
  6. Book: Hager HH, Kern W, Heinz P, Roth HJ . Hagers Handbuch der Pharmazeutischen Praxis: Für Apotheker, Arzneimittelhersteller, Ärzte und Medizinalbeamte: Wirkstoffgruppen II Chemikalien und Drogen (A-AL). 29 July 2013. Springer-Verlag. 978-3-662-25655-8. 157–.
  7. Kelly MJ, Primrose T . Evaluation of a new preparation for the suppression of lactation . Canadian Medical Association Journal . 83 . 24 . 1240–1242 . December 1960 . 13752392 . 1938994 .
  8. Schneider J, Macarthur JL, Patrick JW, Burton GV . The Suppression of Lactation: An Objective Study . Obstetrics and Gynecology . 24 . 2 . 294–297 . August 1964 . 14199544 .
  9. Sherwin BB, Gelfand MM . 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 . March 1984 . 6367474 . 10.1016/0002-9378(84)90746-4 .
  10. Sherwin BB, Gelfand MM . Differential symptom response to parenteral estrogen and/or androgen administration in the surgical menopause . American Journal of Obstetrics and Gynecology . 151 . 2 . 153–160 . January 1985 . 3881960 . 10.1016/0002-9378(85)90001-8 .
  11. Sherwin BB . Changes in sexual behavior as a function of plasma sex steroid levels in post-menopausal women . Maturitas . 7 . 3 . 225–233 . September 1985 . 4079822 . 10.1016/0378-5122(85)90044-1 .
  12. Sherwin BB, Gelfand MM . Sex steroids and affect in the surgical menopause: a double-blind, cross-over study . Psychoneuroendocrinology . 10 . 3 . 325–335 . 1985 . 3903822 . 10.1016/0306-4530(85)90009-5 . 40861936 .
  13. Sherwin BB, Gelfand MM, Schucher R, Gabor J . Postmenopausal estrogen and androgen replacement and lipoprotein lipid concentrations . American Journal of Obstetrics and Gynecology . 156 . 2 . 414–419 . February 1987 . 3826177 . 10.1016/0002-9378(87)90295-X .
  14. Sherwin BB, Gelfand MM . Individual differences in mood with menopausal replacement therapy: possible role of sex hormone-binding globulin. Journal of Psychosomatic Obstetrics & Gynecology. 6. 2. 1987. 121–131. 0167-482X. 10.3109/01674828709016773.
  15. Sherwin BB . Affective changes with estrogen and androgen replacement therapy in surgically menopausal women . Journal of Affective Disorders . 14 . 2 . 177–187 . 1988 . 2966832 . 10.1016/0165-0327(88)90061-4 .
  16. Sherwin BB . Estrogen and/or androgen replacement therapy and cognitive functioning in surgically menopausal women . Psychoneuroendocrinology . 13 . 4 . 345–357 . 1988 . 3067252 . 10.1016/0306-4530(88)90060-1 . 24695692 .
  17. Book: Sherwin BB . Comprehensive Management of Menopause. The Effect of Sex Steroids on Brain Mechanisms Relating to Mood and Sexuality. 1994. 327–333. 0178-0328. 10.1007/978-1-4612-4330-4_31. Clinical Perspectives in Obstetrics and Gynecology. Springer . 978-1-4612-8737-7.
  18. Sherwin BB . Randomized clinical trials of combined estrogen-androgen preparations: effects on sexual functioning . Fertility and Sterility . 77 . S49–S54 . April 2002 . Suppl 4 . 12007902 . 10.1016/S0015-0282(02)03002-9 . free .
  19. Al-Imari L, Wolfman WL . The safety of testosterone therapy in women . Journal of Obstetrics and Gynaecology Canada . 34 . 9 . 859–865 . September 2012 . 22971455 . 10.1016/S1701-2163(16)35385-3 .
  20. Web site: Climacteron Drug Information, Professional. Drugs.com. 2 June 2019. 2 June 2019. https://web.archive.org/web/20190602054345/https://www.drugs.com/mmx/climacteron.html. dead.
  21. Book: Bundesverband der Pharmazeutischen Industrie (Germany). Rote Liste: Verzeichnis pharmazeutischer Spezialpräparate. 1974. Editio Cantor. 9783871930133. 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 . Drug safety and Health Canada . 2010 . International Journal of Risk & Safety in Medicine . 22 . 1 . 41–53 . 10.3233/JRS-2010-0490 .
  23. Web site: Discontinuation of CLIMACTERON® Injection (estradiol dienanthate ⁄ estradiol benzoate and testosterone enanthate benzilic acid hydrazone injection in corn oil) . 23 November 2005 . Sandoz Canada Inc . https://web.archive.org/web/20130111212103/http://www.hc-sc.gc.ca/dhp-mps/alt_formats/pdf/medeff/advisories-avis/prof/2005/climacteron_hpc-cps-eng.pdf. 2 June 2019. 2013-01-11.
  24. Book: Vorherr H . The Breast: Morphology, Physiology, and Lactation. 2 December 2012. Elsevier Science. 978-0-323-15726-1. 201–.
  25. Book: Compendium of Pharmaceuticals and Specialties. 1983. Canadian Pharmaceutical Association. 978-0-919115-04-0. 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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