Estradiol valerate/testosterone enanthate

Last updated
Estradiol valerate /
testosterone enanthate
Estradiol valerate.svg
Testosterone enanthate.svg
Combination of
Estradiol valerate Estrogen
Testosterone enanthate Androgen; Anabolic steroid
Clinical data
Trade names Deladumone, Despamen, Ditate, Ditate-DS, Gravignost, Primodian Depot, Valertest, others
Other namesEV/TE; TEEV
Routes of
administration
Intramuscular injection
Identifiers
CAS Number
PubChem CID
UNII

Estradiol valerate/testosterone enanthate (EV/TE), sold under the brand names Primodian Depot and Ditate among others, is an injectable combination medication of estradiol valerate (EV), an estrogen, and testosterone enanthate (TE), an androgen/anabolic steroid, which is used in menopausal hormone therapy for women. [1] [2] The medication is also used to suppress lactation in postpartum women (brand name Deladumone). [3] [4] [5] [6]

Ditate was provided in the form of multi-use 10 mL vials containing 4 mg/mL EV and 90 mg/mL TE in an oil solution and was administered by intramuscular injection at regular intervals. [7] Conversely, another preparation, Ditate-DS, was provided in the form of single-use 2 mL vials containing 8 mg/mL EV and 180 mg/mL TE in an oil solution, and was administered as a single intramuscular injection. [7] Another product, Primodian Depot, was provided in the form of 1 mL ampoules containing 4 mg/mL EV (3.0 mg/mL free estradiol) and 90.3 mg/mL TE (65 mg/mL free testosterone) in an oil solution, and was administered by intramuscular injection once every 4 to 6 weeks. [8] [9] [10] [11] The elimination half-life of EV in oil by intramuscular injection is approximately 4 or 5 days. [12] Similarly, the elimination half-life of TE in oil by intramuscular injection is approximately 4 or 5 days. [13] EV/TE reportedly has a duration of about 21 days. [14]

Deladumone OB was a double-dosage formulation of Deladumone, which was intended to provide the same dosage with a smaller injection volume. [15]

Primodian Depot was introduced for medical use by 1955. [16] An oral tablet product with the similar brand name of Primodian, containing ethinylestradiol and methyltestosterone, was marketed around the same time, and should not be confused with the injectable Primodian Depot. [8] EV/TE was discontinued in the United States by 2011. [17] EV/TE has been discontinued in most other countries as well, but formulations of EV/TE continue to be marketed in a few countries, including Japan, Mexico, Peru, and Taiwan. [18] [19] [20]

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.

See also

Related Research Articles

<span class="mw-page-title-main">Estradiol valerate</span> Chemical compound

Estradiol valerate (EV), sold for use by mouth under the brand name Progynova and for use by injection under the brand names Delestrogen and Progynon Depot among others, is an estrogen medication. It is used in hormone therapy for menopausal symptoms and low estrogen levels, hormone therapy for transgender people, and in hormonal birth control. It is also used in the treatment of prostate cancer. The medication is taken by mouth or by injection into muscle or fat once every 1 to 4 weeks.

<span class="mw-page-title-main">Estradiol butyrylacetate</span> Chemical compound

Estradiol butyrylacetate (EBA), sold under the brand names Follikosid and Klimanosid-R Depot, is an estrogen medication which is no longer marketed. It is an estrogen ester, specifically, an ester of estradiol. It is administered by intramuscular injection and a single 10 mg dose has been said to have a duration of action of 2 to 3 weeks. The excretion of EBA in women has been studied.

<span class="mw-page-title-main">Estradiol phenylpropionate</span> Chemical compound

Estradiol phenylpropionate (EPP), also known as estradiol 17β-phenylpropionate and sold under the brand name Menformon Prolongatum, is an estrogen which is no longer marketed. It is an estrogen ester, specifically the C17β phenylpropionate ester of estradiol.

<span class="mw-page-title-main">Estradiol dienantate</span> Chemical compound

Estradiol dienanthate (EDE), sold under the brand names Climacteron among others, is a long-acting estrogen medication which was previously used in menopausal hormone therapy for women and to suppress lactation in women. It was formulated in combination with estradiol benzoate (EB), a short-acting estrogen, and testosterone enanthate benzilic acid hydrazone (TEBH), a long-acting androgen/anabolic steroid. EDE has not been made available for medical use alone. The medication, in combination with EB and TEBH, was given by injection into muscle once or at regular intervals, for instance once every 6 weeks.

<span class="mw-page-title-main">Testosterone isobutyrate</span> Chemical compound

ñ

<span class="mw-page-title-main">Prasterone enanthate</span> Chemical compound

Prasterone enanthate, also known as dehydroepiandrosterone enanthate (DHEA-E) and sold in combination with estradiol valerate under the brand name Gynodian Depot among others, is a weak androgen, estrogen, and neurosteroid medication which is used as a component of menopausal hormone therapy to treat menopausal symptoms in women. It is available only as an injectable preparation in combination with estradiol valerate. The medication is given by injection into muscle typically once every 4 weeks.

<span class="mw-page-title-main">Estradiol valerate/prasterone enanthate</span> Combination drug

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. 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. EV/DHEA-E reportedly has a duration of about 21 days.

<span class="mw-page-title-main">Estradiol benzoate/testosterone isobutyrate</span> Combination drug

Estradiol benzoate/testosterone isobutyrate (EB/TiB), sold under the brand names Femandren M and Folivirin, is an injectable combination medication of estradiol benzoate (EB), an estrogen, and testosterone isobutyrate (TiB), an androgen/anabolic steroid, which is used in menopausal hormone therapy for women. It is provided in the form of 1 mL ampoules containing 2.5 mg estradiol benzoate and 25 mg testosterone isobutyrate in a microcrystalline aqueous suspension and is administered by intramuscular injection once every 4 to 6 weeks. EB/TiB reportedly has a duration of about 14 to 21 days.

<span class="mw-page-title-main">Estradiol benzoate/estradiol dienanthate/testosterone enanthate benzilic acid hydrazone</span> Combination drug

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. Clinical studies have assessed this formulation.

<span class="mw-page-title-main">Estradiol benzoate/estradiol phenylpropionate</span> Combination drug

Estradiol benzoate/estradiol phenylpropionate (EB/EPP), sold under the brand name Dimenformon Prolongatum, is an injectable combination formulation of estradiol benzoate (EB), a shorter-acting estrogen, and estradiol phenylpropionate (EPP), a longer-acting estrogen, which has been used in menopausal hormone therapy for women in Europe but appears to no longer be available. It has also been used to suppress lactation in women and has been used in feminizing hormone therapy for transgender women. It has been provided in the form of 1 mL ampoules containing 2.5 mg EB and 10 mg EPP in oil solution and is administered by intramuscular injection at regular intervals.

<span class="mw-page-title-main">Estradiol cypionate/testosterone cypionate</span> Combination drug

Estradiol cypionate/testosterone cypionate (EC/TC), sold under the brand names Depo-Testadiol and Femovirin among others, is an injectable combination medication of estradiol cypionate (EC), an estrogen, and testosterone cypionate (TC), an androgen/anabolic steroid, which is used in menopausal hormone therapy for women. It is specifically indicated for the treatment of moderate-to-severe vasomotor symptoms, but can also be used for other estrogen indications in women. The medication has also been used to suppress lactation in postpartum women.

Estradiol benzoate/estradiol phenylpropionate/testosterone propionate/testosterone phenylpropionate/testosterone isocaproate (EB/EPP/TP/TPP/TiC), sold under the brand names Estandron Prolongatum, Lynandron Prolongatum, and Mixogen, was an injectable combination medication of the estrogens estradiol benzoate (EB) and estradiol phenylpropionate (EPP) and the androgens/anabolic steroids testosterone propionate (TP), testosterone phenylpropionate (TPP), and testosterone isocaproate (TiC) which was used in menopausal hormone therapy for women. It was also used to suppress lactation in postpartum women.

<span class="mw-page-title-main">Estradiol butyrylacetate/testosterone ketolaurate/reserpine</span> Combination drug

Estradiol butyrylacetate/testosterone ketolaurate/reserpine (EBA/TKL/R), sold under the brand name Klimanosid R-Depot, is an injectable combination medication of estradiol butyrylacetate (EBA), an estrogen, testosterone ketolaurate, an androgen/anabolic steroid, and reserpine, an antipsychotic, which was previously used in menopausal hormone therapy for women, particularly in those with pronounced neurovegetative symptoms. It contains 2 mg EBA, 50 mg TKL, and 0.4 mg reserpine in oil solution in each 1 mL ampoule and is administered by intramuscular injection at regular intervals. The medication was marketed in 1957.

Estradiol benzoate/estradiol valerate/norethisterone acetate/testosterone enanthate (EB/EV/NETA/TE), sold under the brand name Ablacton, is an injectable combination medication of estradiol benzoate (EB), an estrogen, estradiol valerate (EV), an estrogen, norethisterone acetate (NETA), a progestin, and testosterone enanthate (TE), an androgen/anabolic steroid, which has been used to suppress lactation in women. It contains 5 mg EB, 8 mg EV, 20 mg NETA, and 180 mg TE in oil solution and is provided in the form of ampoules. It is given as a single intramuscular injection following childbirth. The medication was manufactured by Schering and was previously marketed in Italy and Spain, but is no longer available.

Testosterone propionate/testosterone valerate/testosterone undecylenate (TP/TV/TUe), sold under the brand name Triolandren, is an injectable combination medication of testosterone propionate (TP), testosterone valerate (TV), and testosterone undecylenate (TUe), which are all androgens/anabolic steroids. It contains 20 mg/mL TP, 80 mg/mL TV, and 150 mg/mL TUe in oil solution and is administered by intramuscular injection at regular intervals. The medication has been reported to have a duration of action of about 10 to 20 days.

<span class="mw-page-title-main">Testosterone propionate/testosterone ketolaurate</span> Combination drug

Testosterone propionate/testosterone ketolaurate (TP/TKL), sold under the brand name Testosid-Depot, is an injectable combination medication of testosterone propionate (TP), an androgen/anabolic steroid, and testosterone ketolaurate, an androgen/anabolic steroid. It contains 25 mg TP and 150 to 300 mg TKL in oil solution and is administered by intramuscular injection at regular intervals. The medication has been reported to have a duration of action of about 14 to 20 days.

Testosterone propionate/testosterone enanthate/testosterone undecylenate (TP/TE/TUe), sold under the brand name Durasteron, is an injectable combination medication of testosterone propionate (TP), testosterone valerate (TV), and testosterone undecylenate (TUe), all of which are androgens/anabolic steroids. It contains 20 mg TP, 80 mg TE, and 150 mg TUe in oil solution and is administered by intramuscular injection at regular intervals, for instance once every 3 or 4 weeks. Use of Durasteron by bodybuilders has been reported.

Estradiol benzoate/progesterone/testosterone propionate (EB/P4/TP), sold under the brand names Lukestra, Steratrin, Trihormonal, and Trinestryl, is an injectable combination medication of estradiol benzoate (EB), an estrogen, progesterone (P4), a progestogen, and testosterone propionate (TP), an androgen/anabolic steroid. It contained 1 to 3 mg EB, 20 to 25 mg P4, and 25 mg TP, was provided in the form of ampoules, and was administered by intramuscular injection. The medication was introduced by 1949 and was marketed in the United States, the United Kingdom, and Germany among other places. It is no longer available.

References

  1. Shellenberger TE (6 December 2012). "Pharmacology of estrogens". In Notelovitz M, van Keep PA (eds.). The Climacteric in Perspective: Proceedings of the Fourth International Congress on the Menopause, held at Lake Buena Vista, Florida, October 28–November 2, 1984. Springer Science & Business Media. pp. 397–. doi:10.1007/978-94-009-4145-8_36. ISBN   978-94-009-4145-8.
  2. Kahr H, Müller HA (1956). "Das Klimakterium". Konservative Therapie der Frauenkrankheiten. Springer. pp. 85–102. doi:10.1007/978-3-7091-5694-0_2. ISBN   978-3-7091-5696-4.
  3. McNeilly AS (2011). "Physiology of lactation". Journal of Biosocial Science. 9 (S4): 5–21. doi:10.1017/S0021932000023804. ISSN   0021-9320. S2CID   24614184.
  4. Vorherr H (July 1972). "Suppression of postpartum lactation". Postgraduate Medicine. 52 (1): 145–152. doi:10.1080/00325481.1972.11713186. PMID   5037562.
  5. Vorherr H (2 December 2012). "Suppression of Lactation". The Breast: Morphology, Physiology, and Lactation. Elsevier Science. pp. 200–203. ISBN   978-0-323-15726-1.
  6. Copeland Jr WE (1986). "Lactation Suppressants.". Drug Therapy in Obstetrics and Gynecology. p. 241.
  7. 1 2 de Haen P (1972). "Drugs Released for Clinical Use". The Journal of Clinical Pharmacology and New Drugs. 12 (1): 58–60. doi:10.1002/j.1552-4604.1972.tb00038.x. ISSN   0021-9754.
  8. 1 2 Hager HH, Kern W, List PH, Roth HJ (29 July 2013). "Gestagene, Progestagene". Hagers Handbuch der Pharmazeutischen Praxis: Für Apotheker, Arzneimittelhersteller, Ärzte und Medizinalbeamte: Wirkstoffgruppen II Chemikalien und Drogen (A-AL). Springer-Verlag. pp. 142, 156, 185. ISBN   978-3-662-25655-8.
  9. Saure A (11 November 2013). "Hormonpräparate, die zur Behandlung der Wechseljahre eingesetzt werden". Die Wechseljahre der Frau: Hormone — Präparate — Therapien. Springer-Verlag. pp. 157–. ISBN   978-3-0348-6676-7.
  10. Arends G, Zörnig H, Hager H, Frerichs G, Kern W (14 December 2013). "Hormone". Hagers Handbuch der pharmazeutischen Praxis: Für Apotheker, Arzneimittelhersteller, Drogisten, Ärzte u. Medizinalbeamte. Springer-Verlag. pp. 1164–. ISBN   978-3-662-36329-4.
  11. Kaiser R (2 July 2013). "Ovar". In Buchborn E, Jahrmärker H, Karl HJ, Martini GA, Müller W, Riecker G, Schwiegk H, Siegenthaler W, Stich W (eds.). Therapie innerer Krankheiten. Springer-Verlag. pp. 405–. ISBN   978-3-662-10489-7.
  12. Düsterberg B, Nishino Y (December 1982). "Pharmacokinetic and pharmacological features of oestradiol valerate". Maturitas. 4 (4): 315–324. doi:10.1016/0378-5122(82)90064-0. PMID   7169965.
  13. Luetjens CM, Wistuba J, Weinbauer G, Nieschlag E (2007). "The Leydig Cell as a Target for Male Contraception". In Payne AH, Hardy MP (eds.). The Leydig Cell in Health and Disease. Contemporary Endocrinology. Humana Press. pp. 415–442. doi:10.1007/978-1-59745-453-7_29. ISBN   978-1-58829-754-9.
  14. 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   978-3110066647. OCLC   924728827.
  15. Physicians Desk Reference to Pharmaceutical Specialties and Biologicals. Medical Economics. 1971. p. 1262. Deladumone OB contains the same hormonal agents as Deladumone (Testosterone Enanthate and Estradiol Valerate Injection) but at twice the potency, in order to provide a high dosage concentration in a low volume.
  16. Geburtshilfe und Frauenheilkunde: Ergebnisse der Forschung für die Praxis. Georg Thieme Verlag. 1955. pp. 1061–1062.
  17. Food and Drug Administration (2011). Approved Drug Products with Therapeutic Equivalence Evaluations - FDA Orange Book 31st Edition (2011): FDA Orange Book 31st Edition (2011). DrugPatentWatch.com. pp. 586–. ISBN   978-1-934899-81-6.
  18. "Estradiol". Drugs.com.
  19. 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.
  20. "IBM Watson Health Products: Please Login". www.micromedexsolutions.com.