Template:Potencies and durations of natural estrogens by intramuscular injection

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v · d · e Potencies and durations of natural estrogens by intramuscular injection
Estrogen Form Major brand names EPD CIC-D Duration Refs
Estradiol Oil solution – 40–60 mg – 1–2 mg ≈ 1–2 days [1]
Aqueous suspension Aquadiol, Diogyn, Progynon, Mego-E ? 3.5 mg 0.5–2 mg ≈ 2–7 days; 3.5 mg ≈ >5 days [2][3][4]
Microspheres Juvenum-E, Juvenum ? – 1 mg ≈ 30 days [5]
Estradiol benzoate Oil solution Progynon-B 25–35 mg – 1.66 mg ≈ 2–3 days; 5 mg ≈ 3–6 days [6][7]
Aqueous suspension Agofollin-Depot, Ovocyclin M 20 mg – 10 mg ≈ 16–21 days [8][9][10][11]
Emulsion Menformon-Emulsion, Di-Pro-Emulsion ? – 10 mg ≈ 14–21 days [11][12]
Estradiol dipropionate Oil solution Agofollin, Di-Ovocylin, Progynon DP 25–30 mg – 5 mg ≈ 5–8 days [6]
Estradiol valerate Oil solution Delestrogen, Progynon Depot, Mesigyna 20–30 mg 5 mg 5 mg ≈ 7–8 days; 10 mg ≈ 10–14 days;
40 mg ≈ 14–21 days; 100 mg ≈ 21–28 days		 [7]
Estradiol benzoate butyrate Oil solution Redimen, Soluna, Unijab ? 10 mg 10 mg ≈ 21 days [13][14]
Estradiol cypionate Oil solution Depo-Estradiol, Depofemin 20–30 mg – 5 mg ≈ 11–14 days [7]
Aqueous suspension Cyclofem, Lunelle ? 5 mg 5 mg ≈ 14–24 days [15][16][17]
Estradiol enanthate Oil solution Perlutal, Topasel, Yectames ? 5–10 mg 10 mg ≈ 20–30 days [18][19][20]
Estradiol dienanthate Oil solution Climacteron, Lactimex, Lactostat ? – 7.5 mg ≈ >40 days [21][22]
Estradiol undecylate Oil solution Delestrec, Progynon Depot 100 ? – 10–20 mg ≈ 40–60 days;
25–50 mg ≈ 60–120 days		 [23][24]
Polyestradiol phosphate Aqueous solution Estradurin 40–60 mg – 40 mg ≈ 30 days; 80 mg ≈ 60 days;
160 mg ≈ 120 days		 [25][26]
Estrone Oil solution Estrone, Kestrin, Theelin ? – 1–2 mg ≈ 2–3 days [1]
Aqueous suspension Estrone Aq. Susp., Kestrone, Theelin Aq. ? – 0.1–2 mg ≈ 2–7 days [27]
Estriol Oil solution – ? – 1–2 mg ≈ 1–4 days [1][28]
Polyestriol phosphate Aqueous solution Gynäsan, Klimadurin, Triodurin ? – 50 mg ≈ 30 days; 80 mg ≈ 60 days
Notes: All aqueous suspensions are of microcrystalline particle size. Estradiol production during the menstrual cycle is 30–640 µg/day (6.4–8.6 mg total per month or cycle). The vaginal epithelium maturation dosage of estradiol benzoate or estradiol valerate has been reported as 5 to 7 mg/week. An effective ovulation-inhibiting dose of estradiol undecylate is 20–30 mg/month. Sources: Main/General: [29][30][31][32][33][34][35][36][37] Miscellaneous: [38][39][40]
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See also

References

  1. ↑ 1.0 1.1 1.2 Brown, J. B. (1957). "The relationship between urinary oestrogens and oestrogens produced in the body". Journal of Endocrinology 16 (2): 202–212. doi:10.1677/joe.0.0160202. ISSN 0022-0795. 
  2. ↑ Arthur Osol; Robertson Pratt (1973). The United States dispensatory. Lippincott. p. 498. ISBN 978-0-397-55901-5. https://books.google.com/books?id=jQy0AAAAIAAJ. "The following dosages for estradiol in the form of aqueous suspension injected intramuscularly, or pellets implanted subcutaneously, are recommended by a leading maunfacturer: Menopausal syndrome.—In average cases, 1 mg. intramuscularly 2 or 3 times weekly for 2 or 3 weeks; in more severe cases, 1 to 1.5 mg. Thereafter dosage is reduced to the minimum requirement, usually within the range of 0.5 to 1 mg. of estradiol twice weekly." 
  3. ↑ "Estrogen therapy by implantation of estradiol crystals". Am. J. Obstet. Gynecol. 60 (3): 661–4. September 1950. doi:10.1016/0002-9378(50)90438-8. PMID 14771156. 
  4. ↑ "The effect of monthly injectable contraceptive megestrol acetate compound on pituitary-ovarian function". Journal of Shanghai Second Medical University (02): 7–12. 1987. ISSN 1001-6686. http://new.oversea.cnki.net/KCMS/detail/detail.aspx?dbcode=CJFD&filename=SHEI198702001. 
  5. ↑ "Juvenum E (estradiol) – Medicamentos PLM". http://www.serviciosplm.com/micrositios/fsimilares/Home/DrugDetail?divisionId=%2035&categoryId=%20101&productId=%2054291&pharmaFormId=%20194. 
  6. ↑ 6.0 6.1 Reifenstein, Edward C. (1944). "Endocrinology: A Synopsis of Normal and Pathologic Physiology, Diagnostic Procedures, and Therapy". Medical Clinics of North America 28 (5): 1232–1276. doi:10.1016/S0025-7125(16)36180-6. ISSN 00257125. 
  7. ↑ 7.0 7.1 7.2 "A comparison of the pharmacokinetic properties of three estradiol esters". Contraception 21 (4): 415–24. April 1980. doi:10.1016/S0010-7824(80)80018-7. PMID 7389356. 
  8. ↑ "Die Östrogenausscheidung im Zyklus und nach Injektion von Östradiolestern. Ein Beitrag zur Therapie mit Depotöstrogenen" (in German). Geburtshilfe Frauenheilkd 21: 868–78. September 1961. ISSN 0016-5751. PMID 13750804. 
  9. ↑ Kaiser, R (1962). "Über die Oestrogenausscheidung nach Injektion von Oestradiolestern" (in German). Gewebs-und Neurohormone: Physiologie des Melanophorenhormons. Springer, Berlin, Heidelberg. pp. 227–232. doi:10.1007/978-3-642-86860-3_24. ISBN 978-3-540-02909-0. 
  10. ↑ Toppozada, Hussein K. (1950). "Oestrogenic Therapy with Prolonged Action". Obstetrical & Gynecological Survey 5 (4): 531. doi:10.1097/00006254-195008000-00021. ISSN 0029-7828. 
  11. ↑ 11.0 11.1 Heinrich Kahr (8 March 2013). Konservative Therapie der Frauenkrankheiten: Anzeigen, Grenzen und Methoden Einschliesslich der Rezeptur. Springer-Verlag. pp. 20–. ISBN 978-3-7091-5694-0. https://books.google.com/books?id=Hte1BgAAQBAJ&pg=PA20. 
  12. ↑ "Relative duration of action of natural and synthetic estrogens administered parenterally in women with estrogen deficiency". J. Clin. Endocrinol. Metab. 12 (1): 28–35. January 1952. doi:10.1210/jcem-12-1-28. PMID 14907837. 
  13. ↑ "The clinical use of monthly injectable contraceptive preparations". Obstet Gynecol Surv 32 (6): 335–47. June 1977. doi:10.1097/00006254-197706000-00001. PMID 865726. 
  14. ↑ Mokhtar K. Toppozada (1983). "Monthly Injectable Contraceptives". Long-Acting Contraception. pp. 93–103. OCLC 35018604. https://scholar.google.com/scholar?cluster=14664537528797672080. 
  15. ↑ "Medroxyprogesterone acetate and estradiol cypionate injectable suspension (Cyclofem) monthly contraceptive injection: steady-state pharmacokinetics". Contraception 87 (6): 738–43. June 2013. doi:10.1016/j.contraception.2012.11.010. PMID 23265980. 
  16. ↑ Rahimy, Mohamad H; Ryan, Kristi K; Hopkins, Nancy K (1999). "Lunelle™ monthly contraceptive injection (medroxyprogesterone acetate and estradiol cypionate injectable suspension): steady-state pharmacokinetics of MPA and E2 in surgically sterile women". Contraception 60 (4): 209–214. doi:10.1016/S0010-7824(99)00086-4. ISSN 0010-7824. 
  17. ↑ "Quantification of estradiol cypionate in plasma by liquid chromatography coupled with tandem mass spectrometry: Application in a pharmacokinetic study in healthy female volunteers". J Pharm Biomed Anal 170: 273–278. June 2019. doi:10.1016/j.jpba.2019.03.053. PMID 30947128. 
  18. ↑ "Pharmacokinetic studies of estradiol enantate in menopausic women". Arzneimittelforschung 36 (11): 1674–7. 1986. PMID 3814225. 
  19. ↑ "Pharmacodynamic assessment of dihydroxyprogesterone acetophenide plus estradiol enanthate as a monthly injectable contraceptive". Contraception 33 (6): 579–89. June 1986. doi:10.1016/0010-7824(86)90046-6. PMID 3769482. 
  20. ↑ Gual, C.; Pérez-Palacios, G.; Pérez, A.E.; Ruiz, M.R.; Solis, J.; Cervantes, A.; Iramain, C.; Schreiber, E.C. (1973). "Metabolic fate of a long-acting injectable estrogen-progestogen contraceptive 1,2". Contraception 7 (4): 271–287. doi:10.1016/0010-7824(73)90145-5. ISSN 00107824. 
  21. ↑ Sherwin, Barbara B.; Gelfand, Morrie M. (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. ISSN 0167-482X. 
  22. ↑ "Postmenopausal estrogen and androgen replacement and lipoprotein lipid concentrations". Am. J. Obstet. Gynecol. 156 (2): 414–9. February 1987. doi:10.1016/0002-9378(87)90295-X. PMID 3826177. 
  23. ↑ Wied GL (January 1954). "Östradiol-valerianat und Östradiol-undecylat; zwei neue protrahiert wirkende Östrogene. Wirkungsvergleich mit Östradiol-benzoat" (in German). Geburtshilfe Und Frauenheilkunde 14 (1): 45–52. ISSN 0016-5751. PMID 13142295. 
  24. ↑ "Un oestrogène-retard liposoluble: l'undecylate d'oestradiol" (in French). Thérapie 11 (5): 909–17. 1956. ISSN 0040-5957. PMID 13391788. 
  25. ↑ "Experiences with the Use of Polyestradiol Phosphate, a Long-acting Estrogen". Obstetrics & Gynecology 17 (1): 115–118. 1961. doi:10.1097/00006250-196101000-00024. https://journals.lww.com/greenjournal/Citation/1961/01000/Experiences_with_the_Use_of_Polyestradiol.24.aspx. 
  26. ↑ "Pharmacokinetics and testosterone suppression of a single dose of polyestradiol phosphate (Estradurin) in prostatic cancer patients". Prostate 28 (5): 307–10. May 1996. doi:10.1002/(SICI)1097-0045(199605)28:5<307::AID-PROS6>3.0.CO;2-8. PMID 8610057. 
  27. ↑ Micromedex (1 January 2003). USP DI 2003: Drug Information for Healthcare Professionals. Thomson Micromedex. p. 1246. ISBN 978-1-56363-429-1. https://books.google.com/books?id=zEzWtsVl-KgC. "ESTRONE Parenteral Dosage Forms ESTRONE INJECTABLE SUSPENSION USP Usual adult dose Atrophic vaginitis or Menopausal (vasomotor) symptoms or Vulvar atrophy—Intramuscular, 100 to 500 mcg (0.1 to 0.5 mg) two or three times a week, cyclically or continuously as appropriate. Estrogen deficiency, due to ovariectomy or Female hypogonadism or Primary ovarian failure—Intramuscular, 100 mcg (0.1 mg) to 1 mg a week, administered as a single dose or in divided doses, cyclically or continuously. A few patients may need doses of up to 2 mg a week." 
  28. ↑ Heithecker, R.; Aedo, A.-R.; Landgren, B.-M.; Cekan, S.Z. (1991). "Plasma Estriol Levels after Intramuscular Injection of Estriol and Two of Its Esters1". Hormone Research 35 (6): 234–238. doi:10.1159/000181911. ISSN 1423-0046. 
  29. ↑ "Natürliche und Synthetische Sexualhormone – Biologische Grundlagen und Behandlungsprinzipien" (in German). Grundlagen und Klinik der Menschlichen Fortpflanzung. Walter de Gruyter. 1988. pp. 229–306. ISBN 978-3110109689. OCLC 35483492. https://books.google.com/books?id=v4HvAQAACAAJ. 
  30. ↑ Karl Knörr; Henriette Knörr-Gärtner; Fritz K. Beller; Christian Lauritzen (1982). Lehrbuch der Geburtshilfe und Gynäkologie: Physiologie und Pathologie der Reproduktion. Springer-Verlag. pp. 508–. ISBN 978-3-662-00526-2. https://books.google.com/books?id=OjvMBgAAQBAJ&pg=PA508. 
  31. ↑ Karl Knörr; Fritz K. Beller; Christian Lauritzen (1972). Lehrbuch der Gynäkologie. Springer-Verlag. pp. 212–213. ISBN 978-3-662-00942-0. https://books.google.com/books?id=ACybBwAAQBAJ&pg=PA212. 
  32. ↑ A. Labhart (1974). Clinical Endocrinology: Theory and Practice. Springer Science & Business Media. pp. 551–553. ISBN 978-3-642-96158-8. https://books.google.com/books?id=DAgJCAAAQBAJ&pg=PA551. 
  33. ↑ Horský, Jan; Presl, Jiří (1981). "Hormonal Treatment of Disorders of the Menstrual Cycle". Ovarian Function and its Disorders: Diagnosis and Therapy. Springer Science & Business Media. pp. 309–332. doi:10.1007/978-94-009-8195-9_11. ISBN 978-94-009-8195-9. https://books.google.com/books?id=7IrpCAAAQBAJ&pg=PA145. 
  34. ↑ Ufer, Joachim (1 January 1978) (in German). Hormontherapie in der Frauenheilkunde: Grundlagen und Praxis (5 ed.). Walter de Gruyter. p. 100. ISBN 978-3110066647. OCLC 924728827. https://www.amazon.com/Hormontherapie-Frauenheilkunde-Grundlagen-Praxis-German/dp/3110066645. 
  35. ↑ Joachim Ufer (1969). The Principles and Practice of Hormone Therapy in Gynaecology and Obstetrics. de Gruyter. pp. 44,138. https://books.google.com/books?id=G8VsAAAAMAAJ. "Table: Composition: Oestradiol valerate. Preparation: Primogyn Depot. Form of application: i.m. Proliferation dose in mg: 20–30. Estimated duration of action following a single application in days: 12–14." 
  36. ↑ Willibald Pschyrembel (1968). Praktische Gynäkologie: für Studierende und Ärzte. Walter de Gruyter. pp. 598–599,601. ISBN 978-3-11-150424-7. https://books.google.com/books?id=vVaTnHDFzZ0C&pg=PA598. 
  37. ↑ "Pharmacokinetics of once-a-month injectable contraceptives". Contraception 49 (4): 347–59. April 1994. doi:10.1016/0010-7824(94)90032-9. PMID 8013219. 
  38. ↑ "17 beta-estradiol for postmenopausal estrogen replacement therapy". Obstet Gynecol Surv 39 (4): 230–45. 1984. doi:10.1097/00006254-198404000-00022. PMID 6717863. 
  39. ↑ Kaiser, R. (2008). "Gestagen-Östrogen-Kombinationen in der Gynäkologie. Zur Geschichte, Dosierung und Anwendung eines Hormonprinzips". Geburtshilfe und Frauenheilkunde 53 (07): 503–513. doi:10.1055/s-2007-1022924. ISSN 0016-5751. 
  40. ↑ "Depot estrogen as a monthly contraceptive in nulliparous women with mild uterine hypoplasia". Am. J. Obstet. Gynecol. 112 (4): 575–6. February 1972. doi:10.1016/0002-9378(72)90319-5. PMID 5008627. 
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