Hi everybody, I want to share your experiences for those mtf who are on pills, I´d like to know if you feel better feminization in terms of breast growth, fat redistribution, skin, hair, while taking estrogen pills orally or sublingually? I have tried both forms, and sublingual I feel better, in my case my pills are formulated as estradiol valerate pills and the majority of doctors I have consulted they have told me to take my pills orally better, but I do not feel that way the right one for my body feminization at least. My pills are similar to estrofem pills in size, but not estradiol hemihydrate, they are estradiol valerate. Anyone here in the forum that take estradiol valerate pills sublingual and how do you feel? Thanks!!!

I have a friend who takes her e sublingual and has been doing fine.

Sublingual should have almost all the advantages of IM injected ev (avoids first pass metabolism by the liver) however the indicated dose should be much lower than if you swallow. My endo won't play ball with that; it seems to not be available locally, if at all in the US so I can't say from firsthand experience.

You need to take the med as its designed to be taken and as instructed by your doc.   A higher number, or different absorption or availability curve, for whatever reason is not better.   If the doc is worried about your liver, he'll change the meds and method as appropriate.

If you trust the doc enough to let him radically alter your world, trust him enough to follow directions.

Sublingual just cuts the half life even shorter but you experience a higher peak (higher levels) because of its direct absorption. I havent been on pills in years but swallowing vs sublingual didn't really matter from what I remember, I still had a great deal of positive effects.

Quote from: Lady_Oracle on September 01, 2016, 03:09:58 PM
Sublingual just cuts the half life even shorter but you experience a higher peak (higher levels) because of its direct absorption. I havent been on pills in years but swallowing vs sublingual didn't really matter from what I remember, I still had a great deal of positive effects.

It does, but the estradiol 24-hour AUC for sublingual administration is nearly three times higher than for oral administration. The difference is significantly reduced first-pass liver oxidation to estrone. There is evidence that the bioavailability AUC is more important clinically than peak plasma levels.

Single-Dose Pharmacokinetics of Sublingual Versus Oral Administration of Micronized 17-Beta-Estradiol
Obstetrics and Gynecology, 89:340-345 (1997)

Quote from: rwOnnaDesuKa on September 01, 2016, 01:55:01 PM
You need to take the med as its designed to be taken and as instructed by your doc.   A higher number, or different absorption or availability curve, for whatever reason is not better.   If the doc is worried about your liver, he'll change the meds and method as appropriate.

If you trust the doc enough to let him radically alter your world, trust him enough to follow directions.

Perhaps, but I just switched endocrinologists because he seemed indifferent to the fact that he kept my estradiol levels so low I was starting to have menopausal symptoms (night sweats, heart palpitations, etc.) because of both low T and low E.  After ten months of HRT, my E2 levels were barely above the male range.  Now, two months later, and on a different drug regimen, my serum estradiol is 191 pg/mL, up from 47 pg/mL, and I feel much better.

With kindness,

Terri

I think switching docs is an entirely reasonable thing to do any time you are in any way unsatisfied with their performance.

Firing a doctor is not a big deal.

Quote from: rwOnnaDesuKa on September 01, 2016, 04:17:45 PM
I think switching docs is an entirely reasonable thing to do any time you are in any way unsatisfied with their performance.

Firing a doctor is not a big deal.

Actually getting an appointment with an endocrinologist has been a big deal for me. With the practice I was with in the '99 timeframe it wasn't too bad at 2 months. This go around it was initially scheduled at 4 months wait, the only endo they could refer me out to would have been 5. I was actually seen at 3 months because of a cancellation.

A 3 month delay when my COBRA coverage only lasts for 18 months is a VERY BIG DEAL.

As for the doc I had to wait 3 months on, she'd never heard of sublingual administration of estrogen and had never actually prescribed for IM injection for an mtf before. I've been misdiagnosed or misdirected by various physicians enough times to prefer to take their recommendations with a healthy dose of salt and plenty of my own research. I absolutely take an active role in my health care and have been glad of it at many turns.

I also never took the prescribed  Spiro because I'm extremely wary of taking meds that may not be necessary and some of Spiro's side effects would be problematic for me and it was entirely clear to me that E alone was resulting in feminisation at a pace faster than I'd hoped for. Naturally said endocrinologist was a bit nonplussed at this and sure enough, my levels came back at E too high if anything and T right at the low end of the cis female range. Score one for knowing my body well :-).

Understandable.

But dang I hate the complications our twisted health care reimbursement model produces.

It makes the financial aspect of saying yes/no to a treatment, or saying "you're fired" to a doctor more important than quality of care decisions.

Thanks girls for your comments. I'm under supervision of an endo, but this one who is new said that I may take my pills with a glass of water, I have not checked my estradiol levels, but some of you said that I should take my medicines as the instructions indicate, but I remember some years ago taking estrofem which are designed to be taken with a glass of water and I took them sublingually and the feminization was better than the ones I take now which are estradiol valerate pills. My endo says the advantage of taking my pills sublingually is that it enters more quicky into the bloodstream but he never told me about a higher estradiol levels. I'm from South America and I told him that I have read about the advantages of taking estradiol sublingual in some american forums and he told me that they were other pills not available here. So sublingual pills must be designed for sublingual use or any pill can be taken sublingually? I'm a little bit confused!!!

I have 3 intakes per 24 hours. 6am is sublingual estradiol valerate. 1pm is low dose oestrogel on the skin and 9pm is sublingual ev again. I like the idea of two different intake methods and spreading them out through the 24 hours. I can't post anything here about dosages but all three are low for that reason.

Quote from: fefi on September 01, 2016, 10:41:09 PM
Thanks girls for your comments. I'm under supervision of an endo, but this one who is new said that I may take my pills with a glass of water, I have not checked my estradiol levels, but some of you said that I should take my medicines as the instructions indicate, but I remember some years ago taking estrofem which are designed to be taken with a glass of water and I took them sublingually and the feminization was better than the ones I take now which are estradiol valerate pills. My endo says the advantage of taking my pills sublingually is that it enters more quicky into the bloodstream but he never told me about a higher estradiol levels. I'm from South America and I told him that I have read about the advantages of taking estradiol sublingual in some american forums and he told me that they were other pills not available here. So sublingual pills must be designed for sublingual use or any pill can be taken sublingually? I'm a little bit confused!!!

If I have this right, pills like estrace are estradiol and can be taken sublingually. The advantage of doing this is it avoids the liver getting into the blood stream so it remains at a higher level in the blood stream. Estradiol valerate has a few extra atoms tacked on it so the liver doesn't act on it but latter in the body it's converted to estradiol. As such there is no advantage to taking it sublingually. One issue is that estrace is manufactured by several companies and is really cheap. Estradiol valerate is manufactured by only one company and is more expensive.

Quote from: Dena on September 02, 2016, 01:44:31 AM
If I have this right, pills like estrace are estradiol and can be taken sublingually. The advantage of doing this is it avoids the liver getting into the blood stream so it remains at a higher level in the blood stream. Estradiol valerate has a few extra atoms tacked on it so the liver doesn't act on it but latter in the body it's converted to estradiol. As such there is no advantage to taking it sublingually. One issue is that estrace is manufactured by several companies and is really cheap. Estradiol valerate is manufactured by only one company and is more expensive.

Yes, sublingual route avoids first pass metabolism which converts 90% of the dose to estrone which is less effective hence the need for higher doses when swallowing the pills.

The valerate ester form does not affect metabolism and the primary reason for the valerate form is to make the estrogen more soluble in the oil used to make the injected form.

As far as I know the pharmacokinetics of the valerate form are identical to plain estradiol.

I noticed no difference taking estradiol orally vs sublingually. Orally was more convenient.

On EV vs E2

Maturitas. 1982 Dec;4(4):315-24.

"Natural oestrogenic hormones are the appropriate substances for the therapy of climacteric complaints. After oral or parenteral administration, oestradiol valerate, the synthesis compound contained in various commercially available preparations, is completely converted into the natural substances 17 beta-oestradiol and valeric acid. The 17 beta-oestradiol produced on cleavage of the ester behaves in the organism like the endogenous steroid hormone. Oestradiol valerate and 17 beta-oestradiol are virtually dose-equivalent. No differences in the spectrum of action of the oestrogen and its ester have been found either in animal experiments or man. The pharmacokinetic behaviour and the biotransformation of the 17 beta-oestradiol originating from oestradiol valerate are no different from those of natural 17 beta-oestradiol."

A study actually found lower levels in the blood with similar dose of EV vs. E2

Zentralbl Gynakol. 2001 Sep;123(9):505-12.

"During treatment with (...) micronized estradiol the serum concentrations are significantly higher than with (...) estradiol valerate."

Also, it seems because of the higher molecular weight of EV, you get fewer moles from a gram of EV than you do
from a gram of oestradiol. Hence, EV being slightly weaker than E2.

My doctor said take it sublingual, so that's what I've done.  I split my dose morning and evening, so other than a pill slipping every once and a while, it has worked well.  Been on the right dose since may now, E level rolling at 220.

Plus ... they taste good, knowing the good they're doing.

On sublingual, levels fluctuate a lot during the first few hours after taking it so really, measuring levels serves no purpose.

The remark above could be misleading. Sublingual administration does give a higher peak, it's true, but it also delivers a higher overall dosage than oral. The reasons for this are well documented: oral administration loses a significant proportion compared to sublingual owing to gastric digestion and liver metabolism.

'One very good study (Price) compared the peak and average estradiol in the bloodstream from taking estradiol pills either orally or sublingually. Six women took a variety of doses of estradiol via both methods, and their blood serum estradiol levels were measured at 0, 1, 2, 3, 4, 6, 8, 12, and 24 hours after they took their dose.

The graph is well worth studying: http://transascity.org/wp-content/uploads/2013/06/Price_Estradiol.jpg

'Assuming the 1-mg dose is taken, then in the case of oral administration the product of time and estradiol level is approximately 480 pg/ml*hr. Calculating the area under the sublingual curve is more difficult. I plotted points from the sublingual estradiol curve, and came up with an estimate of the estradiol function from 1 hr to 24 hours as being 350.54*(HOURS^-0.907). From 0 to 1 hours, I estimated the estradiol level linearly, as 451*HOURS. The area under the curve from 0 to 1 hour is therefore 225.5 pg/ml*hr. To find the area under the more complicated curve from 1 to 24 hours, I used a little calculus and integrated, and ended up with a value of 1,296 pg/ml*hr. Summing the two values gives a result of 1,521.5 pg/ml*hr.

For those keeping score, the total estradiol absorbed by your body when taking the same pill sublingually as opposed to orally is about 3.2 times the dose received when taking oral estradiol.'

If you spread the sublingual administration evenly you are overall getting a much more effective reception of estrogen:
http://transascity.org/wp-content/uploads/2013/06/Estradiol_Dose_Comparison.jpg

The full academic paper is here: http://www.sciencedirect.com/science/article/pii/S0029784496005133
and here: http://www.ncbi.nlm.nih.gov/pubmed/9052581

However in order to even out the peaking issue I use two different methods of administration: sublingual and gel.

Hi Richenda, I agree with you and I knew all the studies and graphics about oral vs sublingual estradiol, and the estradiol levels and everything is clear but we have to take into account that all the studies you published are all based on micronized estradiol. What about estradiol valerate, which are the pills that we take sublingual? I never found a study comparing women taking estradiol valerate pills and if there is a difference in the estradiol levels with estradiol valerate unless they work the same way which I do not think!!! Micronized estradiol is more potent than estradiol valerate, but I will continue taking mi pills sublingual!!!! Cross fingers they work!!!

Hi Terri,

My estradiol / estrogen levels were 85 on estradiol taken sublingually, and now on a higher level is 75.  I seem to be doing well, maybe because my T was 6, but I had to back off the daily Spiro dose to stop getting up at night and because I had not energy.  I assume my T will remain low, as I have always had low T anyway.  Can I go higher?  PS.  I tried to PM you, but this site will not allow it.  Can you give me your thoughts to help me for my next visit to my doctor? 

Sarah

How long have you been on HRT?  The reason I ask is because my E level rose kind of gradually but eventually reached 187 pg/ml at my last visit at about 20 months.  I was on a lower E dose and started with pretty high T.

I'm not sure what's going on in the body that makes it rise so gradually over time though.


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Welcome to Susan's Place Sarah. It is a little difficult to answer your question without knowing the units in your blood test as there are several measurement standards. It would be best to discuss this with your doctor because often doctors have treatment goals and once you understand them, you will know if your treatment is going according to plan.

As for the PM function, included in the links, you will find that you require 15 quality posts before the PM function works. We do this to learn about you and to eliminate spammers.

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