So I've read frequently that taking your HRT sublingually is better than orally, either for bigger effect or for more safety. I don't know how accurate these statements are but my question is, to take it sublingually do you need a specific medication or pill? For example, I take estradiol valerate orally, I swallow the pill, if I wanted to go sublingual should I just put in under my tongue and let it dissolve everyday or do I need to tell my doctor to prescribe a different drug that is specifically taken sublingually?

Valerate needs to be swallowed.  Plain old micronized estradiol (estrace or the generic versions) is the one that you can typically just pop under your tongue.

I asked my endocrinologist this exact question last week. He said the pills are specifically designed to be taken a certain way, and using the wrong method makes them less, not more, effective.

I did try putting pills under my tongue or in the buccal fold, but with no way to measure effectiveness, and considering the inconvenience, I just went back to swallowing them.


- Stephanie

If you're in the US you most likely have the generic Estrace which is just fine to use sublingualy.  If oral valerate is available here,  I've never seen it in my 30 years as a pharmacist

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Quote from: Charlie Nicki on February 22, 2018, 07:26:03 AM
So I've read frequently that taking your HRT sublingually is better than orally, either for bigger effect or for more safety.

Just based on my personal experience and what I've come across in terms of findings on oral estradiol, taking estradiol orally vs. sublingually made no difference as far as breast growth/overall feminization AND oral estradiol seems quite safe so that sublingual wouldn't really make much a difference, also one tends to inevitably swallow.

Quoteto take it sublingually do you need a specific medication or pill?

All pills containing estradiol and estradiol valerate are micronized which means the particles are made so small as to be able to cross the sublingual/buccal barrier. Several women take them this way, if their doctor agrees to it and it works just fine but levels will rapidly spike and then fall so this could result in wide fluctuations which may, in some, lead to PMS. I personally didn't enjoy that.

Studies have also shown that micronized estradiol taken sublingually works just fine and results in significantly higher levels of estradiol, up to 10 fold higher.

Quotedo I need to tell my doctor to prescribe a different drug that is specifically taken sublingually?

No but you need to discuss this with them and let them know.

Quote from: Colleen_definitely on February 22, 2018, 07:28:49 AM
Valerate needs to be swallowed.  Plain old micronized estradiol (estrace or the generic versions) is the one that you can typically just pop under your tongue.

Estradiol valerate is also micronized (according to the manufacturer) so can pass through the sublingual/buccal barrier. In the blood, estradiol valerate has been shown, according to studies, to rapidly be cleaved and broken down into estradiol.

Quote from: Steph2.0 on February 22, 2018, 08:11:52 AM
I asked my endocrinologist this exact question last week. He said the pills are specifically designed to be taken a certain way, and using the wrong method makes them less, not more, effective.

There is a study in transwomen where those pills even if designed to be swallowed were taken sublingually by all participants. The findings showed no complications or adverse effects from this, just a reduction in blood pressure. Even the protocol for transwomen at the University of California, San Francisco suggests it can be taken sublingually or orally.

Well yeah, that's how estradiol valerate works.  The problem is that the tablets I've seen were coated so they wouldn't dissolve readily under the tongue.  I imagine this is to allow absorption later in the GI tract but I'm not a pharmacist or doctor.

Thanks everyone. The brand I take is Progynova, just in case that clarifies things a bit more.

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Quote from: KayXo on February 22, 2018, 08:42:08 AM
Studies have also shown that micronized estradiol taken sublingually works just fine and results in significantly higher levels of estradiol, up to 10 fold higher.

No but you need to discuss this with them and let them know.

Estradiol valerate is also micronized (according to the manufacturer) so can pass through the sublingual/buccal barrier. In the blood, estradiol valerate has been shown, according to studies, to rapidly be cleaved and broken down into estradiol.

There is a study in transwomen where those pills even if designed to be swallowed were taken sublingually by all participants. The findings showed no complications or adverse effects from this, just a reduction in blood pressure. Even the protocol for transwomen at the University of California, San Francisco suggests it can be taken sublingually or orally.

Quote from: Charlie Nicki on February 22, 2018, 05:45:24 PM
Thanks everyone. The brand I take is Progynova, just in case that clarifies things a bit more.

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So I haven't been doing this for very long, but I did so much research on this subject, and there is a LOT of disinformation. Basically what it boils down to is what KayXo said about micronized EV. I suck off the sugar coating and take my Progy under the tongue, and it must be working BC I've only been on E for a month and I'm seeing slow steady changes. Now, to me--and I could be way off--if the instructions say you can administer vaginally, it would make sense for one to effectively administer sublingual. I've seen several trans women's blood results (in fact I'm sure one those threads is on this forum) showing their levels over time, which qickly progressed each time--and these results were without a morning dose. Not to mention the studies which have been conducted on sub admin of estradiol and estradiol valerate. Also, even though these studies show there's more reason to administer sublingual after the age of 50, reducing the strain on ones liver is, which can be minimal (dependant on medical history, substance abuse, etc.) they've also shown it to be a more efficient way to administer the drug, since it can be slightly easier on the liver and reduces risk of clots. Hopefully that all came out correctly. Bottom line, you CAN take EV pills either way, orally or sublingual, and lad studies with bloodwork HAVE shown that sublingual administration is more efficient and has a higher medium, even over the same period of time when taken orally.

And yes, your levels will spike initially, but if you spread your dose evenly over twenty four hours, it makes things smoother, for example, three times a day between 8 hours..but YMMV. I'm no medical expert, that's just where a ton of research lead me. Though you'll find it is still a heavily debated subject. I believe at one point Progynova was not micronized, or least not labeled as. Anyways, it seems to work well for me, and so I've heard from others as well.

--Had to edit this on my desktop lol, sorry for anyone who read the original, kind of typo'd.

Quote from: AutumnGurl81 on February 22, 2018, 06:23:09 PM
So I haven't been doing this for very long, but I did so much research on this, and there is a LOT of disinformation. Basically what it boils down to is what KayXo said about micronized EV. I suck off the sugar coating and take my Progy under the tongue, and it must be working BC I've only been on E for a month and I'm seeing slow steady changes. Now, to me--and I could be way off--if the instructions say you can administer vaginally, it would make sense for one to effectively administer sublingually. I've seen several trans women's blood results showing their levels over time, and these were without a morning dose. Not to mention the studies which have been done the sub admin estradiol and estradiol Valerate. Also, even though these studies show there's more reason to administer sublingually after the age of 50, reducing the strain on ones liver is, which can be minimal (dependant on medical history, substance abuse, etc.) But, it has been shown that while it is also a more efficient way to administer the drug, it is can be slightly easier on the liver and reduces risk of clots. Hopefully that all came out correctly. Bottom line, you can take EV pills either way, but studies and bloodwork have shown that sublingual administration is more efficient.

And yes, your levels will spike initially, but if you spread your dose evenly over twenty four hours it makes things smoother, for example, three rimes a day..but YMMV. I'm no medical expert, that's just where alot of reading lead me.

Very informative. So you take Progynova as well?

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Quote from: Charlie Nicki on February 22, 2018, 06:31:31 PM
Very informative. So you take Progynova as well?

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Yep But hopefully moving to valerate injections end of next month. Pills are such a pain to manage, IMO.