Possibility of Sublingual Mono Therapy

Transfem@lemmy.blahaj.zone – 26 points – 3 weeks ago

Is it possible for somebody to achieve testosterone suppression through sublingual Estradiol tablets? I know that in theory you should be able to just take several tablets a day but I was wondering if anybody else had chosen this route?

Sublingual results in some still being swallowed, so one concern is about putting really high doses on the liver. There is also just the logistical difficulty of dosing frequently enough to keep your levels high enough, there is less margin for error.

Why not injections for monotherapy?

What about patches? That should spread it out.

What I've heard about patches is that it can be difficult to get your estrogen high enough with them (for monotherapy at least). I've also heard other problems like rashes, the patches falling off too early (and being expensive to replace), and needing too many to make monotherapy reasonable.

Again, why not injections?

In my opinion, injections are the gold standard. I just wanted to know if sublingual monotherapy was a possibility and if anybody had accomplished it.

It looks like some people have tried it with doses like 6 - 8 mg / day: https://old.reddit.com/r/AskMtFHRT/comments/k6lkyi/can_you_effectively_do_estrogen_monotherapy_on/

Still, it seems inadvisable. Just because you can doesn't mean you should. 😄

Thank you for the link!

Just copy pasting my notes from that link:

Fri Dec 4 14:11:30 2020 UTC - Hello. I started HRT this past Monday. Spiro and estradiol. Now, I didn’t do anything to change my diet at all. I eat moderately well, and drink 2L of water a day, on top of any coffee or tea I might have. That being said, I scared the absolute shit out of myself last night. I’m pretty positive it was a combination of too little sodium and too much water, and of course the spiro. I’m only on 100mg a day and hadn’t even taken my evening dose, but I got very lightheaded, dizzy and disoriented if I was walking snd turned my head at all, when turning my head my eyes felt sluggish, as if my focus was lagging slightly behind. I felt nauseous, and my heart rate elevated. Still feeling a little shitty this morning but definitely improved. I haven’t had any other changes recently other than starting HRT so I’m sure it was the spiro. I’m gonna call my nurse practitioner soon here and explain what happened, but I definitely think I want to discontinue spiro. I went through PP so I’ll have to find a different doctor if I want a different AA, but I’d like probably to use up my prescription of estradiol pills and then go on monotherapy with injections. I hate needles, but fuck, I’ll take them over what I went through last night. So of course I’ll see what the nurse says, but can I increase my estradiol dosage in lieu of taking an AA?

chimaeraUndying 8 points - I did it for years and it worked fine.
Check this out. I don’t know if they are using the term “oral estradiol” the way we might in oral versus sublingual though. I think they might just mean oral versus injections, patches, etc and swallowed or dissolved sublingually I’m unsure. “Hormonal Treatment of Transgender Women With Oral Estradiol” https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5944393/Pulled from the footnotes in the “Medications” section here https://en.m.wikipedia.org/wiki/Transgender_hormone_therapy_(male-to-female)
pseudomugil 1 point Tbh that sounds like not enough water. On spiro (and even not in spiro tbh) your blood pressure can drop if you don't drink enough water. I tend to feel like that if I don't drink 6-8 liters of water a day currently. I say not enough because spiro is a potassium sparing diuretic and as an effect of that, will dehydrate you and deplete your body of sodium. Dehydration then leads to low blood pressure which leads to disorientation, lightheadedness, and can even lead fainting (it's happened to me before when I don't drink enough). It's possible taking some sodium pulled water into your bloodstream which would help, and sodium is a good idea generally on spiro. Still definitely talk to your NP about it, it's something they need to know about, but there's a decent to middling chance they'll say you need to drink more water. It is a ton of water a day, yeah. There's a reason you'll see memes about peeing all the time on spiro.

All at once, I don't want to stab myself, easier to put one on twice a week so I don't forget when lazy/tired. ESTRADIOL 0.1 MG PATCH (2/WK) is what I have.

One 0.1 mg patch isn't enough for monotherapy, but you could try multiple patches for monotherapy. What are you estradiol blood levels like with that dose?

I don't like stabbing myself either, but the benefits of injections outweigh those concerns (and I have done a lot to mitigate my needle phobia).

Well my hormones were off before I started and I'm post op now. My T before starting was 375 and my Estrogen total was 250. Now my T is 4 and my ESTRADIOL (E2) is 40

oh interesting, yeah - I am pre-op, so I am relying on monotherapy to suppress my T.

I just started HRT, Oral 2MG estradiol. I was just curious because I know that most of the sublingual meds are supposed to go directly into your blood stream and what heads to your liver should be minimal, as opposed to oral where the dose has to be high enough to pass through your liver.

I think I'm willing to pop them like tic tacs if needed.

Sublingual might have better absorption than oral, but that isn't saying much and you are still swallowing some of the dose. I still think the dose you would need to do monotherapy is more than is reasonable for oral or sublingual routes of administration.

Also, it's not just how many pills you would need to take to keep up your levels, but the exact timing. It also means all day you are constantly having sharp increases and decreases in your hormone levels. It's impractical for lots of reasons.

Injections are ideal for monotherapy, but if that's not an option I would stick to more typical doses of sublingual estrogen and an anti-androgen (though the anti-androgens can have side effects). Patches and gel are better for absorption than oral (most of the estrogen is absorbed by the liver, little of your dose gets into the bloodstream - it's really the worst route of administration), but they have their own logistical problems.

I highly recommend reading this: https://transfemscience.org/articles/transfem-intro/

https://www.liebertpub.com/doi/10.1089/trgh.2023.0022

this study that compares the differences between sublingual monotherapy, and oral estradiol in combination with cyproterone acetate. this is their conclusion.

Both treatments achieved similar clinical changes. At this stage, (sublingual estradiol), which repeatedly induces alarming excursions of serum estradiol throughout the day, appears to offer no advantage over the cyproterone acetate approach.

my conclusion from this is that you should only attempt sublingual monotherapy if it is cheaper and/or easier to obtain the larger amount of estradiol you need, than the lower dose of estradiol with some way to block t.

scientifically possible? yes

is it worth doing? probably not

injections are scary but you get used to them. I was doing 8mg sublingual for years and eventually did stop taking spiro (only after a few years), but injections are just so much more convenient.

I was able to do it. Since sublingual has a fast half life you'll need to spread the doses throughout the day as many times as you can. For me the bare minimum was 1mg every six hours for a total of 4mg each day though my body is pretty sensitive to estradiol overall. (The last pill I'd take directly before bed so I'd be sleeping more than 6 hours)

I do think it helps to start off slow and ramp things up over time so that your body adapts but that is anecdotal on my end and mostly theory on the research side. Also if you're able to get injections or tolerate an androgen suppressor it's much easier than doing sublingual 4 times a day

Did you get tablets formulated for sublingual or did you have to dissolve oral tablets under your tongue?

Most tablets can be used sublingually as long as they don't have a hard shell on the outside. You can dissolve them under your tongue, under your lip, or in your cheek. Personally I like to keep them behind my bottom lip.