I was thinking about doing it with my pill tonight. Do I have to talk to my doctor first? Also what if you swallow some of the pill before it's all dissolved?

When I started taking tablets my Dr. told me to dissolve them under my tongue, something about it being good to circumvent the liver.

I've had my levels in the thousands and feel great, anything below 300 pg/ml and I feel terrible. My last two blood work appointments was at the end of my injection week (I'm on weekly) and both times they were between 120-180 pg/ml and was feeling like hell. My levels on pills were also in the 100s and didn't feel too great back then either, so I wasn't really surprised. My body just doesn't like being that low.

Estrace, Estrofem and Progynova contain micronized estradiol/estradiol valerate. As such, these can be absorbed sublingually through blood vessels which are abundant in that area. Please consult doctor before you change from oral to sublingual.

Am J Med. 1995 Aug;99(2):119-22.
Estrogen acutely increases peripheral blood flow in postmenopausal women.

"Subjects were given, in double-blind, randomized  fashion, a sublingual placebo tablet (Mead Johnson Laboratories, Evansville, Indiana) on 1 day and sublingual estradiol-17B (Estrace (...), Mead Johnson  Laboratories) on the other."

"Estradiol-17B plasma concentrations increased from 112 +/- 38 to 3,234 +/- 411 pmol/L (P <0.0001) after administration of sublingual estradiol-17B (normal postmenopausal plasma concentration less than 200 pmol/L; normal premenopausal physiologic ranges: luteal 368  to 1,100 pmol/L, midcycle 785 to 1,840 pmolIL, follicular 74 to 368 pmol/L). No subjects reported any adverse symptoms after administration of either estradiol-178 or placebo."

3,234 pmol/L = 881 pg/ml, 40 minutes after sublingual administration

Am J Cardiol. 1997 Sep 15;80(6):791-3.
Effect of acute administration of estradiol 17 beta on aortic blood flow in menopausal women.

"The study group consisted of 16 menopausal women (mean age 54 ± 5 years [range 45 to 63])."

"Each subject was studied at the same hour of the day in a quiet, darkened room. The study was a randomized, double-blind study with 1 crossover. After a baseline echocardiogram showed normal heart structure and function, all subjects had 2 echocardiograms recorded on 2 different days: 20 minutes after the sublingual administration of either estradiol 17 β (...) (Estrace (...), Mead Johnson Laboratories, Princeton, New Jersey) or placebo (...) (Mead Johnson, Princeton, New Jersey). The time elapsed between the 2 studies was 48 ± 4 hours. Ten milliliters of blood was withdrawn before and at the end of each test in order to evaluate plasma levels of ovarian hormones."

"Compared with baseline and placebo, plasma levels of estradiol increased 10-fold after sublingual administration of estradiol 17β (56 ± 21 vs 537 ± 210 pmol/L, p <0.001)." After 20 minutes.

537 pmol/L = 146 pg/ml

Obstet Gynecol. 1997 Mar;89(3):340-5.
Single-dose pharmacokinetics of sublingual versus oral administration of micronized 17 beta-estradiol.

"Sublingual administration of micronized 17 beta-estradiol results in a rapid, burst-like absorption into the systemic circulation, yielding high E2 levels that fall rapidly over the first 6 hours."

Estrace was used in this study.

J Clin Psychiatry. 2001 May;62(5):332-6.
Estrogen deficiency in severe postpartum depression: successful treatment with sublingual physiologic 17beta-estradiol: a preliminary study.

Estrofem sublingually in study.

Maturitas. 1999 Oct 24;33(2):145-52.
The acute effects of sublingual estradiol on left ventricular diastolic function in normotensive and hypertensive postmenopausal women.

"17β-estradiol (two tablets of Estrace (...), Mead Johnson Laboratories, Evansville, Indiana) were allowed to dissolve sublingually."

"Serum 17β-estradiol values reached 2227±1180 pg/ml at 60 min post dose. Compared with baseline values, the plasma levels of estradiol increased more than 10-fold for the whole group. It should be noted that hormone plasma concentration was substantially higher in the hypertensive subgroup: the estradiol levels were 1790±869 pg/ml in the normotensives and 2664±1490 in the hypertensives (P<0.05)."

Psychopharmacology (1999) 147:108–110
Role of estradiol in puerperal psychosis

Both women were treated with sublingual estradiol.

"treatment with micronized 17-b estradiol (Estrofem, Novo Nordisk, Bagsvaerd, Denmark) was started as monotherapy"

"Sublingual 17-b estradiol was given as monotherapy in the outpatient unit"

Quote from: Anastasija on December 02, 2016, 12:57:33 PM
as an injection has the highest concentration and is maintained for a long time, because E is released over about two weeks.

But half-life and how steady levels remain depend on ester. Estradiol valerate has a half-life of 4.5 days, estradiol cypionate, lower peaks but steadier levels.

QuoteThe same pill, depending on how you take, but I think E pills is released by 2h.

Or earlier or later depending on individual's metabolism and other factors. Levels may or may not be steady but usually are quite steady.

Quoteaccording to my study should be done the day before injection and completely fasting, then the result is the most reliable. but I can be wrong

Levels fluctuate quite a bit on injections so that this makes testing not really reliable.

Quote from: Mia on December 02, 2016, 12:22:52 PM
Hmmm, my numbers are radically different than anyone else's I've seen here.

I started HRT in 2014 - back then, E=19, T=668. About 6 months later, taking oral Estradiol, my levels were E=1457, T=46.

Fast forward to March, 2016 (about 2 years later). Now using Estradiol Valerate injections, E=2276.9, T=8. But the lab results state "Normal".

I'm not sure if there are different methods of determining E levels? This is Estrogen Total Serum, in pg/Ml.

Estrogens total include estradiol and estrone. Estradiol is the most potent of the two, about 10 x. My estradiol levels with injectable estradiol valerate range from 1,000-4,000 pg/ml.

Quote from: Anastasija on December 02, 2016, 11:42:55 AM
I just accept ANDROCUR x2 + flutamidx2

Flutamide (in addition to high doses of androcur-cyproterone acetate) may have adverse effects on liver whereas bicalutamide, a newer anti-androgen has shown (appears) to have a safer side-effect profile.

"As regard as pure antiandrogens clinically important adverse events including gastrointestinal events, particularly diarrhea and occasional disturbances of liver function related to flutamide treatment and antabuse effect, problems with light-dark adaptation and rare interstitial pneumonitis related to nilutamide indicates the bicalutamide, due to its better tolerability profile, together with its once-daily oral administration regimen, could be considered the antiandrogen of first choice in the treatment of prostatic cancer."

J Cancer Res Clin Oncol. 2006 Aug;132 Suppl 1:S17-26.

"CPA is associated with loss of libido and erectile dysfunction. CPA is also associated with cardiovascular risk and there have been occasional reports of fatal fulminant hepatitis and hepatocellular carcinoma. Gynecomastia is quite rare with CPA, which is in contrast to the non-steroidal antiandrogens." Although to be fair, this is at very high doses, not commonly prescribed to transsexual women.

"There are no direct comparisons between the three non-steroidal antiandrogens in terms of quality of life, but available evidence suggests that bicalutamide has a more favorable safety and tolerability profile than nilutamide and flutamide. Unlike CPA, non-steroidal antiandrogens appear to be better tolerated than castration, allowing patients to maintain sexual activity, physical ability, and bone mineral density, but these agents have a higher incidence of gynecomastia and breast pain (mild to moderate in > 90% of cases)." 

Androcur has also been associated with 5 of 8 cases of prolactinoma and with 7 of 8 cases of meningioma in transsexual women. It has a tendency to overstimulate prolactin. Also, it can cause extreme fatigue, depression,  and anxiety in some. Slightly raises risk of blood clots and can lead to excess weight gain in abdominal region due to glucocorticoid effects.

Regarding flutamide,

Fertil Steril. 2012 Oct;98(4):1047-52.

"Hepatotoxicity is a rare but possible event using low- and ultralow-dose regimens of flutamide."

I hope your doctor is keeping a good eye on all of this with regular blood tests.

Flutamide only blocks T, does not reduce it.

ok, from start its so many to read. But i will try explain few items wher are you wrong.

First you need not consult a doctor kwestaich take something under the tongue or swallowing, because it still means accepting and dosage is the same, the difference in the language that, in adopting the concentration is greater, and the liver does not get in the ass.

of course, that the concentration of each may be different, depending on age, weight, susceptibility to drugs.

I was doing my testing on an empty stomach, or estrofem 17 I took more than 10h before and 3 days before the next injection, that is, from the last 11 days have passed, my score estradiol amounted to 428

generally gets only study of estradiol, the estrogen alone is not tested, because it already contains estardiaol

Another thing ANDROCUR and flutamide also enjoy sublingually, why? the same reason as in the case estrofemu, the tablet is released into the body immediately, and juak will go to the stomach it will take her to 2h and the whole body gets in the ass, recently I did liver tests, and after 3 months on hṛt wątrąbę I am in very good condition, and I will tell you just that before hṛt lived very unwell, much fried, roasted, energy drinks

and the last thing flutamide, flutamide is not blocking testosterone does ANDROCUR. Flutamide blocking the development of male characteristics such as body hair.

ANDROCUR is the same as spiro, only ANDROCUR is probably banned in the US

not that I had read, no measure reduces T, only the blocks it. To the right there was a reduction of T, you need to take calcium, so it is called, and after some time the value of T in the body decreases. How do you imagine that the drug reduced the amount of hormone in your blood? it is not physically possible. I for example, I am against taking on the grid themselves blockers and only later on, eg for 3-4 months estrofemu. Why? so that, for example with me within two months testosterone levels went down from 1,178 to 28, if not brałabym at this time estrofemu that the body would not have had any hormones that regulate the activity of the whole organism.

I do not argue with research, but I think that they are not reliable

Quote from: Anastasija on December 03, 2016, 03:18:16 AM
Another thing ANDROCUR and flutamide also enjoy sublingually, why? the same reason as in the case estrofemu, the tablet is released into the body immediately, and juak will go to the stomach it will take her to 2h and the whole body gets in the ass, recently I did liver tests, and after 3 months on hṛt wątrąbę I am in very good condition, and I will tell you just that before hṛt lived very unwell, much fried, roasted, energy drinks

Cyproterone acetate (Brand: Androcur) is not intended to be taken sublingually. And all attempting to do so will do is give you a mouth full of tablet filler..

Quoteand the last thing flutamide, flutamide is not blocking testosterone does ANDROCUR. Flutamide blocking the development of male characteristics such as body hair.

Both these drugs are androgen blockers and will block both T and DHT at the receptor.. Taking both is pointless.

QuoteANDROCUR is the same as spiro, only ANDROCUR is probably banned in the US

No, they are not the same. Spironolactone does not block DHT, cyproterone acetate blocks DHT in addition to T.

Quotenot that I had read, no measure reduces T, only the blocks it. To the right there was a reduction of T, you need to take calcium, so it is called, and after some time the value of T in the body decreases. How do you imagine that the drug reduced the amount of hormone in your blood? it is not physically possible. I for example, I am against taking on the grid themselves blockers and only later on, eg for 3-4 months estrofemu. Why? so that, for example with me within two months testosterone levels went down from 1,178 to 28, if not brałabym at this time estrofemu that the body would not have had any hormones that regulate the activity of the whole organism.

I do not argue with research, but I think that they are not reliable

Actually, HRT will reduce T levels, firstly, increased levels of E will downregulate T production by the gonads. Also, cyrpoterone acetate will lower T levels by the same method. An androgen blocker is used mostly to get  T levels down quicker than relying on estrogen alone.

Apparently you are arguing with the research, despite sex hormones being very well understood and well researched. HRT is well researched and understood for menopausal women. HRT for trans women is a little less understood, but the principles are well known.

Quote from: kelly_aus on December 03, 2016, 06:30:00 AM
Cyproterone acetate (Brand: Androcur) is not intended to be taken sublingually. And all attempting to do so will do is give you a mouth full of tablet filler..

If micronized (I'm not sure), it could be indeed taken sublingually so that less of it would go through the liver and it could result in a somewhat different effect as the ratio of CPA to its major metabolite 15B OH-CPA (equally anti-androgenic but much less progestogenic) would be modified and lead to a stronger progestogenic (and antigonadotropic) effect. I have rarely come across anyone taking CPA this way. In any case, this should be discussed with her physician.

QuoteSpironolactone does not block DHT, cyproterone acetate blocks DHT in addition to T.

Spironolactone actually does block DHT and all androgens in addition to reducing its concentrations.

September 2012, Vol. 11, No. 5 , Pages 779-795

"Spironolactone acts as an anti-androgen by binding to the androgen receptors"

Br J Dermatol. 1988 May;118(5):687-91.

"Spironolactone was first noted to have anti-androgenic properties by Corvol. Since then,
spironolactone has been used successfully to treat hirsutism and acne. It is thought to exert its
anti-androgenic effect by suppression of androgen production by gonads by blocking the
enzyme cytochrome P450, and by competitive inhibition of dihydrotestosterone (DHT) at the
skin androgen receptor."

Endocrinology. 1975 Jul;97(1):52-8.

"It seems likely that spirolactones, besides their action on testosterone biosynthesis, exert their antiandrogenic activity via a peripheral androgen antagonism."

QuoteAn androgen blocker is used mostly to get  T levels down quicker than relying on estrogen alone.

Anti-androgens were initially proposed to be added to estrogen in the past because estrogen was non bio-identical and posed significant risks such as deep vein thrombosis, stroke and pulmonary embolism when used alone and taken at high doses to lower T but now that bio-identical estrogen is mostly, if not exclusively prescribed to transsexual women, and has shown to be quite safe, especially non-orally, it can be used instead of anti-androgens to lower T very effectively and just as rapidly (no reason why the effect of E would be slower).

In any case, it is up to the doctor to decide which protocol to use.

QuoteApparently you are arguing with the research, despite sex hormones being very well understood and well researched. HRT is well researched and understood for menopausal women. HRT for trans women is a little less understood, but the principles are well known.

Although there is still much to be discovered and learned.

Quote from: kelly_aus on December 03, 2016, 06:30:00 AM
Cyproterone acetate (Brand: Androcur) is not intended to be taken sublingually. And all attempting to do so will do is give you a mouth full of tablet filler..

You're completely wrong, really.

First, read each of the absorbability of ingestible tablets and these soluble, accurate data will not you give, but how to swallow tablet is a body begins przysfajać it after 2 hours and absorbs about 5%, if it rozpuścisz this assimilation begins immediately and is 25 % up.

Another thing is no such thing as a drug that can not be dissolved under the tongue, the usual demagogy, the only thing that can limit us in this is that the tablet is too bitter. If a doctor tells you that tablets can not dissolve under the tongue because it does not absorb, it is an ordinary liar or an ignoramus. Ask the people associated with the production of drugs, or medical laboratories.

the second thing, ANDROCUR is the same as spiro, spiro only that is allowed in the US, and ANDROCUR not, and yet ANDROCUR has stronger effects, but still their primary function is to block the production of T.

And one last thing, flutamide is completely on something else, it does not block the production testosteonu itself, to block the development of masculine characteristics in the body. For example, it ANDROCUR that block this does not mean that the hair is the body you begin to grow less, or will be weaker.

So it was not itself such a treatment I use and I know each other, after 3 months, disappeared me completely hair, underarm hair after depilation grow very slowly, already some two weeks and are barely visible, I had a goatee, now do not have it, after wydepilowaniu legs, hair begins to grow again after three days, he passed two weeks of hair removal and are barely visible

Quote from: Anastasija on December 03, 2016, 12:35:31 PMAnother thing is no such thing as a drug that can not be dissolved under the tongue, the usual demagogy, the only thing that can limit us in this is that the tablet is too bitter. If a doctor tells you that tablets can not dissolve under the tongue because it does not absorb, it is an ordinary liar or an ignoramus. Ask the people associated with the production of drugs, or medical laboratories.

To be efficiently absorbed sublingually, a drug needs to be micronized, in small enough particles so they can readily pass through the mucous membranes. Basic chemistry.

Quotethe second thing, ANDROCUR is the same as spiro, spiro only that is allowed in the US, and ANDROCUR not, and yet ANDROCUR has stronger effects, but still their primary function is to block the production of T.

Both these drugs reduce androgen synthesis and block androgens at receptors.

QuoteAnd one last thing, flutamide is completely on something else, it does not block the production testosteonu

Flutamide does block testosterone and all androgens.

Expert Opin. Drug Saf. (2014) 13(11)

"Flutamide, Nilutamide and Bicalutamide are non-steroidal compounds with a high affinity for the AR, which, by directly targeting the AR ligandbinding domain, ultimately prevent the transcription of AREs [18]."

https://en.wikipedia.org/wiki/Flutamide#Antiandrogen

"Flutamide acts as a selective, competitive, silent antagonist of the androgen receptor (AR).[2] Its active metabolite, 2-hydroxyflutamide, has between 10- to 25-fold higher affinity for the AR than does flutamide, and hence is a more powerful antiandrogen in comparison.[2][21][46][47]"

"Flutamide has far lower affinity for the AR than do steroidal antiandrogens like spironolactone and cyproterone acetate, and it is a relatively weak antiandrogen in terms of potency by weight, but the large dosages at which flutamide is used appear to compensate for this.[49]"

From package insert
http://hemonc.org/docs/packageinsert/flutamide.pdf

"Flutamide demonstrates potent antiandrogenic effects by inhibiting androgen uptake and/or inhibiting nuclear binding of androgen in target tissues."

This is why with flutamide, LH, T, DHT and E increase in comparison to cyproterone acetate.

J Clin Endocrinol Metab. 1984 Nov;59(5):963-9.

"After 14 days of FLU treatment, serum testosterone (T) increased significantly [17.4 +/- 1.4 (SE) vs. 26.9 +/- 1.5 nmol/liter, as well as estradiol (E2) concentrations (144 +/- 12 vs. 177 +/- 20 pmol/liter). Dihydrotestosterone increased slightly after 14 days of FLU administration (1.59 +/- 0.14 vs. 1.98 +/- 0.30 nmol/liter). At the same time basal LH concentrations were significantly elevated (5.9 +/- 0.5 vs. 8.6 +/- 0.6 ng/ml), whereas FSH levels were not affected (2.8 +/- 0.6 vs. 2.8 +/- 0.6 ng/ml). No changes in PRL values were detected throughout treatment with FLU. The effect of CPA was quite different. At the end of the treatment phase, serum T levels were reduced considerably (14.6 +/- 1.8 vs. 3.3 +/- 0.4 nmol/liter). Serum E2 decreased similarly (95 +/- 13 vs. 35 +/- 6 pmol/liter). Conversion of T to dihydrotestosterone was also diminished significantly (1.72 +/- 0.33 vs. 1.14 +/- 0.33 nmol/liter). Both gonadotropins were significantly depressed after 14 days of CPA administration (LH, 5.6 +/- 0.7 vs. 2.8 +/- 0.4 ng/ml; FSH, 2.4 +/- 0.3 vs. 1.4 +/- 0.2 ng/ml)."