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For spironolactone, twice a day dosing in 12 hour intervals is recommended (e.g. 50mg twice a day for a total of 100mg per day, or 100mg twice a day for 200mg per day, etc).
Transfeminine Guide: Forms
What forms of estradiol are there?
Section titled “What forms of estradiol are there?”There are many forms of estradiol, each with their drawbacks, pros, and levels of ease in terms of obtaining them.
This section does not cover dosing (see the Dosing section for more information). Given prices are rough estimates for DIY sourced HRT.
$20-40/m, $280-480/yrPills are by far the most popular and well known option, and they’re easy to obtain if you are DIYing. The downside is that they can be relatively expensive. It’s best to choose bioidentical estrogens, meaning the pills contain the same form of estrogen naturally produced by the human body.
Bioidentical estradiol pills usually come in three forms:
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Estradiol hemihydrate (for example, Estrofem or Estrace). This is chemically equivalent to estradiol itself, which is what homebrewers may use.
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Estradiol valerate (for example, Progynova). This is another form of estradiol, but it is about 75% as potent as estradiol or estradiol hemihydrate.
Oral intake is simply swallowing your pills. Usually twice per day in ~12 hour intervals. Results in more stable levels versus sublingual/buccal administration.
Sublingual intake refers to placing a tablet under the tongue and letting it dissolve, and buccal intake refers to placing a tablet between your gum and the inside of your cheek to dissolve. These two administration methods are interchangeable and have essentially the same results.
Sublingual/Buccal administration causes higher peak levels of estradiol in the blood that quickly dissipate. Because of this, it is recommended that sublingual administration be three times a day, in 8 hour intervals.
Transdermal (patches/gels/etc)
Section titled “Transdermal (patches/gels/etc)”Transdermal (estradiol applied to the skin) comes in forms like gels, patches, sprays/solutions, etc.
Patches are typically switched out once to twice a week and are designed to give out a set dose of estradiol every day. Usually applied to the lower stomach or upper buttocks. Note that there has been a global patch shortage for a few years, so it may be very difficult and expensive to acquire patches from any DIY sources.
Prescribed gels typically come in packets or in a pump that dispenses a set amount each time. Estradiol gels are compounded in an alcohol base to increase absorption. Usually applied to the skin once per day.
Squeeze tube style gels that aren’t properly dosed are not recommended due to difficulty of accurate dosing. Unfortunately many gels available from DIY sources are in this category.
Solutions/Sprays are usually sold from homebrewers, containing estradiol in an alcohol-based solution that is applied to the skin, usually in an spray style bottle.
Estrogen Creams are not very relevant to transfeminine people because of the low absorption rate into the bloodstream and the difficulty of accurate dosing.
Injections
Section titled “Injections”Estradiol is usually made in an esterified form so it stays in the body longer. Injecting plain (un-esterified) estradiol would cause it to break down very quickly, which is why all injectable estradiol is esterified. After injection, the body slowly converts the ester back into regular estradiol over time, allowing the estradiol to stay in the body for longer.
The most common estradiol esters are valerate, cypionate, enanthate, and undecylate, each with a different half life, meaning how long it lasts inside your body.
If you inject the same dose, esters with shorter half lives produce higher peaks but for a shorter time. Esters with longer half lives produce lower peaks and it lasts longer, and they let you inject less often.
Basically, the term “half life” describes how long the medication lasts inside your body.
| Estradiol Formulation | Recommended Injection Frequency |
|---|---|
| Estradiol Valerate (EV) | Every 5 days |
| Estradiol Cypionate (EC) | Every 7 days |
| Estradiol Enanthate (EEn) | Every 7-10 days |
| Estradiol Undecylate (EUn) | Every 20-30 days |
Notes:
- EEn should be treated similarly to EC, with potentially slightly longer duration
- These are general guidelines for injection frequencies
Detailed information on estradiol injection dosing will be found later in this guide in the Estradiol injection dosing section.
Valerate is sometimes prescribed by doctors, with cypionate being occasionally prescribed. Cypionate, enanthate and undecylate are most commonly sold by homebrew estrogen sellers.
Pellets
Section titled “Pellets”Estradiol pellets are implanted into the body (usually the butt) and slowly release estrogen into your body over the course of many months.
This cannot be found from DIY sources. They can only be produced with highly specialized equipment.
These are more experimental in terms of dosages compared to the other more common methods. You can get them implanted if your insurance covers it (or if you’re very wealthy). Because they slowly dissolve and release estrogen over time, you don’t have to worry about missing a dose.
They last about 3-6 months. Most doctors that offer pellets compound them to give a patient quite a high dosage of estradiol.
What are the different types of antiandrogens?
Section titled “What are the different types of antiandrogens?”All of these should be swallowed unless stated otherwise.
Spironolactone (Spiro)
Section titled “Spironolactone (Spiro)”Spironolactone is a weak antiandrogen, albeit quite safe.
Common side effects include increased thirst, salt cravings and frequent urination.
Can be taken alongside a regular HRT regimen as an experimental erection-prevention drug if getting erections is bothersome due to its blood pressure lowering effects (recommend 100-400mg/day¹ for this (start low)).
Cyproterone acetate (Cyproterone, Cypro)
Section titled “Cyproterone acetate (Cyproterone, Cypro)”Cyproterone is a very effective antiandrogen when combined with estrogen.
High doses should be avoided due to a harsher risk profile.
Keeping under a certain dosage is important, especially considering that cyproterone is usually sold in dosages 4-8 times that of recommended dosages for transfeminine individuals (get a pill cutter!).
Bicalutamide (Bica)
Section titled “Bicalutamide (Bica)”Bicalutamide is a very effective antiandrogen, moreso when paired with estrogen. It works in a unique way by preventing testosterone from having an effect on your body, but it does not actually prevent your body from producing testosterone. Ironically, this will increase your blood testosterone levels (your body thinks that you have zero testosterone inside you and tells your testes to produce even more), but don’t worry, all that extra testosterone can’t do anything.
People tend to report bica being better at preserving penile function, libido and semen volume better versus other antiandrogens².
In cis male prostate cancer patients, bicalutamide has about a 1/4000 chance of causing either severe liver or severe lung toxicity. All published case reports of either severe liver or lung toxicity have been in cis men over 59 years of age. It is likely that trans women will face a much lower but still present risk.
GNRH Agonists/Antagonists
Section titled “GNRH Agonists/Antagonists”Extremely safe and effective antiandrogens that prevent your testes from producing testosterone. Commonly referred to as puberty blockers, they work just as well at blocking T for people who have gone through a full natal testosterone puberty.
Some of the longest lasting forms are not feasible to buy from DIY sources due to being prohibitively expensive or difficult to administer.
Some DIY sources now sell a type of pill form oral GNRH antagonist called Relugolix. It can be moderately expensive though.
An GNRH agonist called buserelin can also be found DIY, but its administration method can be quite annoying (sprayed into the nostrils 3 times a day).
Estradiol Monotherapy
Section titled “Estradiol Monotherapy”Monotherapy means to only use one type of medication.
Estradiol monotherapy uses only high doses of estradiol to suppress your body’s testosterone production, as estradiol itself functions as an antiandrogen.
High enough levels of estradiol in the body is enough to cause your body’s testosterone production to lower significantly. This is usually only easily achievable with estradiol injections, which allow a person to more easily achieve high estradiol levels versus other methods of administration.
Some people are able to maintain an estradiol monotherapy regimen using transdermal estrogens. It may be more difficult to achieve this though versus injections.
The vast majority of people on a decent estradiol injection monotherapy regimen (only taking estrogen, no antiandrogen) are able to suppress testosterone levels adequately without needing to take antiandrogens.
Footnotes:
Section titled “Footnotes:”2
Supported by evidence in men who take bicalutamide for the treatment of prostate cancer. Bica tends to preserve sex drive better in this population versus other antiandrogens, which can probably be extrapolated to trans populations.