Estradiol Valerate

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Estradiol Valerate
Skeletal formula for Estradiol valerate; a commonly prescribed estrogen.
Drug class: Estrogen
Dosage range:
Oral/Sublingual/Buccal
0.5 to 8 mg/day
IM Injection
2 to 20 mg (frequency varies)
Brand names: Progynova, Delestrogen, Progynon Depot
Elimination half-life:
Oral
12–20 hours (as E2)
IM injection
4–5 days

Estradiol Valerate is an estrogen medication that is primarily used in hormone therapy for transgender women, treating menopausal symptoms, and in hormonal birth control. It is one of the most widely used esters of estradiol alongside estradiol cypionate.

It is the most common form of estradiol prescribed for the purpose of MtF hormone replacement therapy and comes in the form of oral/sublingual tablets and intramuscular injections.

Method of Action

Estradiol valerate is a synthetic estrogen and acts as an agonist of the estrogen receptor, the biological target for estradiol.[1][2] The bioavailability of estradiol valerate varies widely between oral, sublingual, and intramuscular administration, with oral being the lowest.

Oral administration

The bioavailability of oral estradiol valerate is only 3 to 5%. When taken orally, nearly 80% of it is converted by the liver into estrone (E1) and estrone sulfate (E1S) during first-pass metabolism.[3] This is considered unfavorable for transgender women, as estrone is a significantly less potent estrogen compared to estradiol (E2), and will result in slower and less overall feminization. However, there is speculation that E1 and E1S may be beneficial for the first 6-12 months of a person's transition, as it may be beneficial for laying the groundwork for future breast growth, although this theory is unproven and a lot of research still needs to be done on this.

Sublingual/Buccal administration

Sublingual and buccal administration bypass the first-pass metabolism that is present with oral administration, and thus results in higher levels of estradiol. This method can be difficult to administer, however, as dissolving the pills sublingually takes a fair amount of time and may result in some of it being swallowed. If you are administering the drug sublingually (or buccally), it is important that you let it stay in place under your tongue (or in between your cheek and gums if taken buccally) as long as possible and avoid swallowing, as this will result in first-pass metabolism in the liver and thus a higher E1.

Intramuscular injection

Intramuscular injections are the most favorable option for transgender women as the bioavailability is 100%. This method completely bypasses the first-pass metabolism and results in the maximum amount of estradiol absorption when compared to oral, sublingual or buccal administration methods. The half-life is also substantially longer, meaning one only has to inject every 2 to 5 days rather than taking several pills every day of their life, especially when it's not guaranteed that the user will not swallow any that then goes through first-pass metabolism into E1.

A single 4 mg intramuscular injection is said to be approximately equivalent to 2 mg/day of an oral dose over the course of 3 weeks.[2]

Side Effects

The use of estradiol valerate may result in the following side effects...

  • Breast tenderness and enlargement
  • Nausea
  • Bloating
  • Edema (fluid retention)
  • Headache
  • Melasma (tan or dark skin discoloration)

High-dose estrogen therapy with injections may cause...

  • Increased risk of thromboembolism
  • Changes in blood lipid profile
  • Increased insulin resistance
  • Increased levels of prolactin

Dosage

The usual starting dose is 1 mg daily of estradiol valerate pills taken orally in one or two doses split evenly throughout the day, going up to a maximum of 8 mg daily taken sublingually split evenly throughout the day. 20 mg dosages taken intramuscular injection once every two weeks are prescribed by many doctors, however this is not recommended as the elimination half-life of estradiol valerate injections is only 5 days. In this case, transgender women opt to take about 7 mg via intramuscular injection once every 5 days. Estradiol valerate pills usually come with 2 mg per pill, so a pill cutter may be required if you choose to take only 1 mg or split a 2 mg dosage over the course of a day. Hormone levels should be monitored through blood tests to ensure you are receiving the appropriate dosages.
It's recommended you don't take too much, as there is speculation that increasing your dosage too quickly can hinder your future breast growth, and will elevate your SHBG levels which could result in slower or less feminization.

Brand Names

Estradiol Valerate is marketed under a large number of brand names throughout the world. The most common are Progynova (oral/sublingual), Progynon Depot (IM), Delestrogen (IM).

Sources

Online Pharmacies

Estradiol Valerate Pills (Progynova)

Product Price Bulk Website Shipping
Progynova 2mg x 21 12.00$ OTC-Online-Store Ships from Russia
Progynova 1mg x 28 9.10£ 8.46£ UnitedPharmacies-UK (UK-Centric)
Progynova 1mg x 28 11.07$ 9.96$ UnitedPharmacies (US-Centric)
Progynova 1mg x 28 8.03$ 6.30$ AllDayChemist Various fullfilment centers
Progynova 2mg x 28 10.50€ Aphrodite's Ships from Portugal
Progynova 2mg x 28 14.94£ 13.45£ UnitedPharmacies-UK (UK-Centric)
Progynova 2mg x 28 18.17$ 16.35$ UnitedPharmacies (US-Centric)
Progynova 2mg x 28 23.00€ 17.48€ ThailandPharmacy Ships from Thailand
Progynova 2mg x 28 11.74$ 9.45$ AllDayChemist Various Fullfilment Centers
Progynova 1mg x 84 19.73£ 18.35£ UnitedPharmacies-UK (UK-Centric)
Progynova 1mg x 84 24.00$ 22.32$ UnitedPharmacies (US-Centric)
Progynova 1mg x 84 40.00$ 36.00$ InHousePharmacy Ships from Vanuatu
Progynova 2mg x 84 39.99$ Amazon4Health Ships from Thailand
Progynova 2mg x 84 26.13£ 24.30£ UnitedPharmacies-UK (UK-Centric)
Progynova 2mg x 84 31.78$ 29.55$ UnitedPharmacies (US-Centric)
Progynova 2mg x 84 55.00€ 44.00€ ThailandPharmacies Ships from Thailand
Progynova 2mg x 84 34.00$ 27.20$ Favskinhouse Ships from Thailand
Progynova 2mg x 84 32.00$ 28.50$ GoodStuffStore Ships from Thailand
Progynova 2mg x 84 52.00$ 28.50$ InHousePharmacy Ships from Vanuatu
Progynova 2mg x 84 28.72$ 27.12$ WebOrderPharmacy Ships from India


Alibaba

Estradiol valerate can be purchased in tablet form through a variety of sources such as online pharmacies. However, it can also be purchased in bulk powdered form through vendors on websites such as Alibaba. From personal experience, Alibaba is substantially cheaper and some vendors will often go to great lengths to get your product to you by deliberately mislabelling packages in order to more easily get them through customs. We have personally had good luck with this particular vendor. It is also worth noting that in order to purchase products from these sites, you will need to personally contact the vendor and negotiate a price with them.

Lena Kiev

Lena Kiev is a transgender woman based in Ukraine that has been creating and selling her own estradiol valerate injections since 2006. Her vials of estradiol are incredibly inexpensive, coming in at around $7 USD/month. Each vial costs $60 and lasts 9 months on a dose of 7 mg (0.18 ml) every 5 days. You will need to buy at least 2 vials in order to make a purchase, which is a grand total of around ~$130 USD including shipping. This price point is vastly superior compared to the prices charged by pharmaceutical companies, however, and will save you a lot of money in the long run, especially if you are not on insurance. She also offers estradiol enanthate and a mixture of estradiol valerate with progesterone (or hydroxyprogesterone caproate), with custom EV/P ratios that you can specify. Check out her website for more information on what she has available. You will need to contact her via email for purchases, but she is very responsive and helpful throughout the process.

See also

External links

References

  1. H Kuhl (2005) Pharmacology of estrogens and progestogens: influence of different routes of administration, Climacteric, 8:sup1, 3-63, DOI: 10.1080/13697130500148875
  2. 2.0 2.1 B. Düsterberg (DECEMBER 01, 1982). "Pharmacokinetic and pharmacological features of oestradiol valerate" DOI: https://doi.org/10.1016/0378-5122(82)90064-0
  3. Michael Oettel; Ekkehard Schillinger (6 December 2012). Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen. Springer Science & Business Media. p. 261. ISBN 978-3-642-60107-1. Natural estrogens considered here include: [...] Esters of 17β-estradiol, such as estradiol valerate, estradiol benzoate and estradiol cypionate. Esterification aims at either better absorption after oral administration or a sustained release from the depot after intramuscular administration. During absorption, the esters are cleaved by endogenous esterases and the pharmacologically active 17β-estradiol is released; therefore, the esters are considered as natural estrogens.