Susan's Place Transgender Resources

Hey guys,

So yesterday was my third appointment with my physician, and I decided to ask her the difference between taking estrogen sublingually or just taking it like a regular pill and she told me that she used to make people take it sublingually but then realized that the regular, chalky blue pill's properties don't allow it to dissolve under our tongues fully, and because of the pill's composition she was saying our tongues memebranes are too small to absorb it even if you dissolve it fully. Due to this, you end up swallowing most of it anyway. So she was saying there's really no difference between sublingual and oral.

This was her explanation and I wasn't really sure what to make of it. Taking it sublingually really is a bit of a pain and if it doesn't really affect anything, is there really a point of doing it this way?

Sublingually avoids the first pass through the liver lowering the estrone levels and raising the estradiol levels. I don't know if the pill you are taking would be absorbed or not but if it is, that could double your estradiol levels. With your doctors permission, a way to find out would be one week before your blood test you take your pill sublingually for a week and then compare it with a test where you didn't. If the estradiol levels are nearly the same, it makes little difference. If they are about double at test time, you are getting a far higher dosage because the half life of estradiol is only a few hours.

The principle of taking it sublingually is to take it easy on the liver by not involving the digestive system.  (Liver damage is one possible side effect of HRT.)  That assumes that the pill is designed to be absorbable sublingually.  So there is a point to it, if you have the right pill.

If you are getting a pill designed to be swallowed, it might not work sublingually.  That is what your doctor is saying.

Hi Sarah,

This is incorrect. The inside of your mouth and under your tongue is highly vascularized, and estradiol absorption occurs relatively efficiently.  From personal experience, I can tell you that estradiol pills disintegrate within a few minutes.  If you are careful not to swallow your saliva, gastroenteral absorption is minimal.

The idea that a molecule is too big to permeate the epithelial tissue of your buccal tissue or tongue is utter nonsense.  If that were the case, you would never taste anything.

"Sublingual administration resulted in rapid absorption with significantly E2 [estradiol] levels than did comparable oral doing"

Single-Dose Pharmacokinetics of Sublingual Versus Oral Administration of Micronized 17-beta-Estradiol
Obstretrics & Gynecology 89:340-345 (1997)

With kindness,

Terri

I will say this from a couple of months of cycling estradiol:

Swallowing has some effect, but the liver has to process it.

Sublingually, it works well when you keep it dry, but the problem is that we salivate heavily under the tongue, and any time you're tasting sweet, it's dissolving in your mouth and not through the buccal tissue.

Transbuccally, it seems to be the most effective because you are not allowing ANY saliva (except where it makes contact with the pill tucked between the gum and cheek) to touch and dissolve the pill away from buccal tissues (where it really needs to go).  When done right, when I'm not talking, it can take more than two hours for the pills to dissolve completely, and I rarely taste that sweetness (except at the very end, when I notice when the pill is gone, and I put my tongue up there to taste the powder remnants.  If I taste it, I back off immediately.  Let me clarify that in the upper jaw locations, it can take at least two hours to dissolve, but in the bottom jaw locations, it can take from 20 to 45 minutes to dissolve.  In comparison, if I tucked them under the tongue instead, it would be gone in 5 minutes (and it would be like I was sucking on a candy lozenge even though I'm leaving it alone).

The way I do the transbuccal method is to put one under the teeth on the lower jaw if I know I'm not going to be talking (evening), or above the teeth on the upper jaw if I'm going to be speaking or I'm taking near or at the maximum dosage.  The latter event means I have to put them in the upper and lower jaw locations at the same time.  That way, saliva is less likely to touch it.

I can tell that the transbuccal method is a lot more effective, and this means that I need to get my blood drawn when I'm near the primary peak (seeing the doctor next week a day before THE primary peak of the cycle).  Everything's just changed since I went to cycling estradiol (I was on a constant-dosage regimen for years); my thinking, my feelings, the way I look at things, good or bad, male or female, APPETITE even(!), breast development beyond what I had before, hair growing back again, etc.

The pill that I'm taking I believe is just the normal blue pill without the gel coating, but I can still dissolve it under my tongue. I think I'll keep doing it sublingually because she didn't say it was unsafe or anything.

Thanks guys!!

Hi Sarah,

If you Google estradiol oral vs sublingual you will find a graph by Price that actually did a study on blood levels every hour for 24 hours.  There was a significant difference.  I would post the link but it has dosage information.

Take care,
Paige :)

Sarah,

Published medical literature does not agree with your doctor.

She may be overly concerned about swallowing the saliva when taking estradiol sublingually. When I take my estradiol  I try hard to not swallow for at least 15 minutes. The tablet usually dissolves in about 2 to 3 minutes. I just let the dissolved tablet sit where it is under the tongue for another 10 minutes or so. It really does not taste bad at all.

Several studies have shown estradiol taken sublingually to yield far higher levels versus orally. Within minutes, levels peak but also drop quite quickly, within a couple of hours. Transbucally, could avoid swallowing some of it.

I did oral and sublingual. I found no difference whatsoever in feminization, well-being, breast development.

Mine dissolves sublingually, but it doesn't have a coating. It's the little oval ones.


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The doctor said it didn't make any different for synthetic estrogen, but my  medicine has a nice minty taste. I always figured I was supposed to put it under my tongue. The blue pill dissolves pretty quick if you get it wet on the counter or are talking or drinking alot when you put it in your mouth. I usually take my morning medication when I get in the car or start yoga so it dissolves slower. When I take it at night there is usually some left when I wake up in the morning. The big brown one tastes yuck so I swallow it.

My doctor never checks my hormone levels since I don't have any problems with the normal doses, so I don't know if how I take it makes any difference. But he checks my potassium level every time because it will kill you in minutes if it gets too high!

My apologies if this sounds like an awfully naive question, but given the dangers to the liver with oral/sublingual forms of HRT why aren't the other methods used more readily?  (i.e., patches, creams, injections, etc.)

I think there's cost and convenience factors. I've heard anecdotal claims that injections give more complete breast development but also have a heavier impact on libido. I'd be interested in others thoughts because I was contemplating switching.


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I have used oral and injected methods, singly or in conjunction, for over 5 years now...

At the moment, my insurance does not cover injectable E, so I have been on oral only, and yes, I use it sublingually. I have no data to back up my assertions, but I am quite sure that dissolving the pills under my tongue or between cheek and gums gives me a higher E level than merely swallowing them. I have had two different prescribers, and both agreed with my observations. I have no doubt that micronized formulations would be more effective, but I haven't ever been able to get them, except for my progesterone, which is also bio-identical, and is now administered via compounded vaginal suppository. I looove the additional benefits of being able to break the suppositories up into pieces that reflect the dosages I need day by day, and the positive effect the essential fatty-acid base has on my vaginal tissues.

I prefer injected estrogen over pills. I like being able inject and forgetta 'bout it, and I also like being able to carefully adjust my dosages to coincide with my cyclic needs. I have also used injections and oral in tandem, with even better results psychologically, and, in my opinion, developmentally. My last endo was a huge fan of this approach for me, but I am xx intersex, so I am uncertain if there would be any advantage for someone born male and in an MTF  transition.

My current endo/gyno say he has MTF patients that seem to also cycle to some degree, and he accommodates their needs accordingly. There is far more to cycling than just ovulation and menstration, and my body will attest to that fact, even though my uterus was mostly removed at a year and a half. I have leg and back and pelvic pain, and I retain water, and more. The day after my cycle ends, even if I am on a steady HRT regimen, I feel a great relief, and my pains subside. My emotional state also reflected my cycle even before HRT, and I can still be surprised by the bottom falling out of my emotional world 5-6 days before my cycle ends, or by a strong desire to copulate leading up to my 'ovulation' day. My cycle is synchronized to the lunar cycle, and though I can anticipate it, I pay it no mind, lol, but I always go through the same things, month after month, lol. I like it. It makes me feel more whole than I otherwise would..

Probably more info than you need, but hey, it's what happens to me...

Missy

Quote from: Mohini on October 08, 2016, 05:43:13 PM
Transbuccally, it seems to be the most effective because you are not allowing ANY saliva (except where it makes contact with the pill tucked between the gum and cheek) to touch and dissolve the pill away from buccal tissues (where it really needs to go).  When done right, when I'm not talking, it can take more than two hours for the pills to dissolve completely, and I rarely taste that sweetness (except at the very end, when I notice when the pill is gone, and I put my tongue up there to taste the powder remnants.  If I taste it, I back off immediately.  Let me clarify that in the upper jaw locations, it can take at least two hours to dissolve, but in the bottom jaw locations, it can take from 20 to 45 minutes to dissolve.  In comparison, if I tucked them under the tongue instead, it would be gone in 5 minutes (and it would be like I was sucking on a candy lozenge even though I'm leaving it alone).

Thanks for this!  I had been dropping it under my tongue, and often ended up tasting and feeling bits of the tablet as I proceeded through my morning rituals, evening as well.  I started yesterday, so please stand clear in case of a breast explosion.  :o

Erin

Quote from: MissGendered on January 21, 2017, 10:12:23 AM
I am quite sure that dissolving the pills under my tongue or between cheek and gums gives me a higher E level than merely swallowing them.

Several studies have confirmed that taking micronized E (which I believe is the standard form today for any bio-identical E) sublingually results in significantly higher levels (up to ten times, if I recall correctly) but the peak is short-lived and levels will drop quite rapidly.

Sublingual works great for me. My dose is lowish but I'm feeling the effects. I don't see a downside to sublingual vs. swallowing. While the peak may be higher and fall off quicker, the average is still higher than oral,

http://transascity.org/sublingual-versus-oral-estrogen/

My doc said to take it sublingually and ignore what the pharmacist recommends.

It seems to take between 5 and 20 minutes to fully dissolve under the tongue depending on how much saliva I have (and probably pH too as I drink lemon water on waking and after my spiro tablet).

Does the saliva destroy estradiol or no?

Quote from: Maybebaby56 on October 08, 2016, 03:17:16 PM
Hi Sarah,

This is incorrect. The inside of your mouth and under your tongue is highly vascularized, and estradiol absorption occurs relatively efficiently.  From personal experience, I can tell you that estradiol pills disintegrate within a few minutes.  If you are careful not to swallow your saliva, gastroenteral absorption is minimal.

The idea that a molecule is too big to permeate the epithelial tissue of your buccal tissue or tongue is utter nonsense.  If that were the case, you would never taste anything.

"Sublingual administration resulted in rapid absorption with significantly E2 [estradiol] levels than did comparable oral doing"

Single-Dose Pharmacokinetics of Sublingual Versus Oral Administration of Micronized 17-beta-Estradiol
Obstretrics & Gynecology 89:340-345 (1997)

With kindness,

Terri

Maybe before calling things nonsense, you find out if the OP is taking a micronized estradiol or not.. A non micronized form of estradiol is not suitable for sublingual administration.

Quote from: auroratrans on January 08, 2018, 12:03:48 PM
Does the saliva destroy estradiol or no?

Sublingual versus Oral Estrogen | Transas City (http://transascity.org/sublingual-versus-oral-estrogen/)

QuoteWhen you take estradiol sublingually, your oral mucosa are able to absorb quite a lot of the estradiol directly into the bloodstream, bypassing the liver at first and giving you a higher bioavailability. (Zhang) Ultimately your liver will break most of it down, but less than it has to from the oral route. Now it is true that your saliva will destroy some of the estradiol, but less than your stomach acid will. (Kuhl)