Sublingual estradiol

[Katie Ellen]

I'm about to start HRT. I'm 68 years young. In pretty good shape.

I always thought that if I started HRT I would most certainly be on the patch because of age. I don't now, and never have smoked. My doctor deals with many trans people. Last week she did a complete family history and blood work up. Most everything came back at perfect levels (except potassium - due to BP meds).

She's starting me on low dose Estradiol pill (sublingual) and Finasteride (due to potassium concerns). We talked about the safety and that I need to take it this way to avoid potential liver issues. She comes highly recommended and I have no reason to not trust her.

Anyone else, especially in my age range, following a similar regimen?

[Dani]

Here I am!   

Same age and a late transitioner as well.  I take my Estradiol sublingual.

While patches offer a more steady blood level than sublingual, both routes bypass the liver and go straight to your blood system for distribution throughout your entire body. Injectable Estradiol offer similar steady blood levels to patches. Only oral Estradiol that you swallow and dissolves and absorbed in the stomach goes straight to the liver for the first pass at metabolizing Estradiol.

Proponents of patches and injectable Estradiol like to point out the rapid peak and fall of sublingual administration.
Advocates of sublingual route say that the peak and fall is not really a problem and point out the low overall cost of the sublingual method. Both methods are safe and effective, assuming you are in good health.

Sublingual works for me, but there are a few others on this forum who have different experiences. Some girls just do not like the rapid peak and fall of sublingual and they say that they feel better on patches or injectable Estradiol with a more steady blood level..

[Anne Blake]

I have been doing my estradiol sublingually for almost two years now with no problems. My dosage dropped post surgery and my doctor sees no need to step away from the pills. I did not want to go to the patches do to chronically sensitive skin. I turned 70 last February.

[Laurie]

Hi Katie Ellen,

  Dani has summed up the pluses and minuses well enough. If you need more clarification as to why your doctor has decided this delivery method please do ask them to explain further.
  I an 65 and have been taking my estradiol in pill form almost since I started. I do mine between my upper gum and cheek (buccal) instead of sublingual. By putting the pill in the buccal area I am still able to drink and talk. My potassium is a bit on the high side but I do still take Spironlactone. I do watch my potassium intake somewhat because of the Spiro. I am also taking a beta blocker and an ace inhibitor.

Hugs,
  Laurie

[steph2.0]

Here I am!   

Same age and a late transitioner as well.  I take my Estradiol sublingual.

While patches offer a more steady blood level than sublingual, both routes bypass the liver and go straight to your blood system for distribution throughout your entire body. Injectable Estradiol offer similar steady blood levels to patches. Only oral Estradiol that you swallow and dissolves and absorbed in the stomach goes straight to the liver for the first pass at metabolizing Estradiol.

Proponents of patches and injectable Estradiol like to point out the rapid peak and fall of sublingual administration.
Advocates of sublingual route say that the peak and fall is not really a problem and point out the low overall cost of the sublingual method. Both methods are safe and effective, assuming you are in good health.

Sublingual works for me, but there are a few others on this forum who have different experiences. Some girls just do not like the rapid peak and fall of sublingual and they say that they feel better on patches or injectable Estradiol with a more steady blood level..

I tried taking half of my prescribed estradiol pills sublingually, and it seemed like my emotions went wild and my mood crashed. It's hard to know for sure, though, since there were other outside forces affecting me at the time, too. I've gone back to swallowing them and I feel fine now, but of course most of the other things that were bothering me have stabilized as well.

I have been prescribed estradiol pills to be swallowed. I vaguely remember discussing this with you when we met, but I can't remember the answer. Are these the same pills that you can take sublingually or buccaly?

Also, would switching from swallowing to sublingual or buccal have a large effect on moods?

Stephanie

[josie76]

The kind of pill that can be swallowed or taken sublingual and buccally, is bioidentical estradiol (17beta estradiol) brand name "Estrace". Usually an oval blue or greenish pill depending on dosage. These have a sweet like flavor. I take mine buccally as it disolves slower and there is less that I swallow compared to sublingual.

The point of taking them sublingual or buccal is to get the most absorbed into the bloodstream in the form of estradiol. When it is absorbed in the intestine, the largest part is converted to estrone and sulfates of estrone by the liver. Estrone has a much lower activation of estrogen receptors but is a stable storable form of estrogen. estrone and estriol forms of estrogen also have the effect of increasing the blood clotting factor where estradiol does not.



Finasteride only blocks the production of type2 and type3 alpha5-reductase enzyme. By blocking this it lowers the blood concentration of DHT (dihydrotestosterone) by around 60-70%. It is effective at stopping most skin and prostate production of the enzyme.
This will not lower the body's testosterone production or block androgen receptors from being affected by T.

Spiro does block androgen receptors and via other enzyme blockages tends to lower T more than Estrogen and Progesterone alone do. In time estrogen will drop the body's T production down into the female range. Spiro does however flush sodium out of the body but does not do so to potasium. Sodium levels in the blood control the potasium blood levels. When sodium drops, more potasium is free to circulate.
Last year when I was still working outdoors alot I started carrying packets of salt with me. When I started to feel weak or nausious, I would pour a couple of packets on my tongue and wash it down with water. From my own blood tests I saw how raising my sodium brought my potasium back into range.

I'm very happy I don't need any T blockers anymore though. Seems like so fewer pills to take now.

[Dani]

I have been prescribed estradiol pills to be swallowed. I vaguely remember discussing this with you when we met, but I can't remember the answer. Are these the same pills that you can take sublingually or buccaly?

In most products, yes they are the same tablets as long as the tablet is not coated with a sugar candy like coating. If the tablets dissolve in 5 to 10 minutes under a wet tongue, then it is OK to take sublingual or buccal.

Also, would switching from swallowing to sublingual or buccal have a large effect on moods?

Stephanie

This really depends on the individual taking the medication. I have no problems with mood swings but other ladies do and they attribute their mood swings to the rapid rise and fall of Estradiol blood levels with each administration of Estradiol sublingual or buccal. A few ladies here on Susan's Place have said that their mood swings have gone away with injectable or topical Estradiol.

If you have mood swings that seem to match your sublingual administration schedule, then I would say that it is a very strong contributing factor.

[Chloe]

Anyone else, especially in my age range, following a similar regimen?

Am 62, started ft HRT 'bout 52 otherwise been on/off/on again since early 20's. Having tried 'every-which-way' simply swallow 'lil blue in dial pack but, having recently started progesterone cream (on very dry fore-legs), do notice almost immediate breast 'peaking' so perhaps there's something to 'rush theory'?

Took light dose Casodex in past but don't take any anti-antigens at all anymore. Am slowly becoming firm believer in the "less unnatural drug interactions the better"! lol Being 'older' perhaps 'T' receptors (not to mention 'factory parts') are completely dead from long-time abuse?

[fefi]

Hi girls:
            I think there is a big deal with taking estradiol orally or sublingually. In my case, I have tried both methods, and I have not seen major differences. I take estradiol valerate pills, not micronized estradiol pills, because the last ones are not available in my country.
The pills are not coated, plain pills and they dissolve easily under the tongue, so I suspect I am doing the things right. Most doctors I have asked, they advise me to take the pills with a glass of water but if I want to make the estrogen enter more quicky into the bloodstream, take it sublingually. Any of you take estradiol pills but in the form of estradiol valerate and sublingually? Experiences are welcome.
                                                               Hugs!!!

[Dani]

fefi,

Estradiol valerate tablets are not available in the USA, so we cannot help you with personal experiences.

It is an inactive pro-drug and needs to have the valerate portion cleaved off in order to activate the Estradiol. This is done in the liver, blood and other tissues. Because of this, the half-life is much longer than sublingual micronized bio-identical Estradiol. The down side is that Estradiol valerate is only 3 to 5% bio-available, so dosages are different from other forms of Estradiol.

Once the valerate portion is cleaved off, the remaining Estradiol is the same as micronized Estradiol. Estradiol valerate works just as well as other forms of Estradiol, but it does need activation, mainly in the liver, and because of this, it makes little difference, in terms of half-life of absorption and elimination, if you take Estradiol valerate orally or sublingually.

Intramuscular injection is a different story. 100% bio-available and a much longer half-life.

[fefi]

Hi Dani, I sent you a PM message!!!

[KayXo]

Estradiol valerate works just as well as other forms of Estradiol, but it does need activation, mainly in the liver

Studies dating back to the 1970's have shown that estradiol valerate is quickly broken down in blood and also intestinal mucosa so that essentially, it is practically identical to estradiol, pharmacokinetics are the same and it can thus be taken sublingually, if your doctor so approves. Cleavage takes place before entering the liver. If the liver was absolutely needed for cleavage, then taking EV orally or IM would be the same and make no difference which we know is not the case as bio-availability is much higher when taken by IM.

[AnneK]

I started on Estradiol (Estrace) 4 weeks ago.  I have little white pills, which I take sublingually, twice a day.  I find they only take a couple of minutes to dissolve, though I refrain from swallowing for a few minutes.

[Ricki Wright]

Hiya!

52 and just passed my 6 month mark taking estradiol sublingual without any adverse results. I will say that taking the low dose to start the journey to my daily dosage I noticed an insane rush sensation from ankles to head like invisible goose bumps everywhere! I have no idea if it was psychosomatic or an actual physical reaction and I don't care because it was awesome.

Some things I have found that help me is once I got up to twice a day, I have been aiming at 12 hours apart as consistently as possible. I have noticed if I get to 15 hours I become, as my wife puts it, bitchy as hell.

Welcome Sister!!!!

Ricki

[pamelatransuk]

Hello again Katie Ellen

I assume you actually started HRT shortly after your post - presumably around May 1st - and if so, I offer you my congratulations. I'm sure you 'll remember taking your first tablets forever. Welcome to the rollercoaster ride!

I am 64 and have been on HRT 15 months but (as you anticipated for yourself) I started and remain on E Patches and Finasteride.

Hugs

Pamela  xx

[Allie Jayne]

Hi Katie, I'm 65 and like Pamela, on patches. My pre HRT T was low enough I didn't need blockers. At my 2 month checkup, my endo said I was exactly where I should be with both T and E.


Allie

[Katie Ellen]

I haven't been around much in the last few months, so I was surprised to see this post again today when I logged in.

I did start my HRT a year ago last week. Sublingual Estradiol and Finasteride (swallowed). Both at extremely low doses until November 2018. I would call it "transition" dosage since then. I've had my levels tested every 3 months and will have them tested again in 2 weeks. I think my E will be fine, but my T still a little too high.

Physically though, I'm disappointed. I wouldn't go shirtless, but I have no problem keeping things hidden. The biggest change I've seen is a lot less body hair and my slightly thinning top has filled in.

I go back and forth on whether or not to continue on HRT. As of now, I've decided to just keep going. Whatever happens, happens. That could change at any time though! The best way to describe it so far is SLOW.