how to use estradiol sublingual ?

[KayXo]

Can you give more details?

Spironolactone whether taken sublingually or orally, the effect will be practically the same so there is no point in taking it sublingually. I personally also found that taking E both orally and sublingually had the same effect on me, as regards to feminization and breast growth so I just swallowed.

Estrone does in fact raise the risk of blood clotting.

The increase in coagulation (heightened/decreased production of certain proteins/factors) is triggered by estrogen activating estrogen receptors in the portal vein so if estrone is weaker than estradiol in activating receptors, the risk should be LESS with estrone, not higher. This, in addition to rapid metabolization/inactivation of estradiol, could account for why bio-identical estradiol, even taken orally, does not greatly increase the risk of DVT, especially relative to other forms of estrogen such as ethinyl estradiol.

Estrone and estriol both increase clotting factor. Estradiol does not.

Read the above. Estradiol would/should lead to a greater change in coagulation. The increase in coagulation is in direct proportion to how many times and how strongly (estriol and estrone are weak estrogens) estrogen receptors in the portal vein are activated.

The reason why estradiol triggers less coagulation changes when taken non-orally isn't because there is less conversion to estrone relative to oral but because there is less estrogen going into the portal vein and more into extrahepatic tissues. Higher doses non-orally lead to increasingly higher amounts going through the portal vein but the risk of DVT still remains very low, according to studies.

Estrone is a storable form of estrogen and can remain in fat and andipose tissues.

Estrone sulfate is actually the highest form of (inactive) estrogen found as a result of taking oral estradiol. This, along with estrone, constitute a reservoir from which estradiol can be later formed.

CLIMACTERIC 2005;8(Suppl 1):3–63

"estradiol, which is rapidly and extensively transformed in the intestinal tract and liver to estrone and estrone sulfate. Both metabolites are circulating in high concentrations and serve as a hormonally inert reservoir from which estradiol
is continuously delivered after reconversion"

Acta Endocrinol (Copenh). 1978 Aug;88(4):754-67.

"The levels of all oestrogens increased significantly following the ingestion of oestradiol, although to a greatly different extent. The largest and most prolonged increase was seen in the case of oestrone sulphate, the levels of which--depending on the dose ingested--were 20-50 times higher than the pre-treatment levels"

"The levels of oestrone and oestradiol sulphate exhibited smaller increases 3 h after ingestion, i.e. 4-10 and 2.5-5 times, respectively, and the plasma levels of oestradiol showed a minor increase only (1.4-1.8 times)."

I think the circular 28 day pack is a form of birth control pill and not bioidenticle hormones.

A few birth control pills actually contain bio-identical estradiol and you can find bio-identical hormones in circular packs.

[Cassi]

Wow, so much to learn.

Thank you!

[auroratrans]

I generally put the E under my tongue while I get my day going and put the Spiro in with my other daily vitamins to swallow after the E dissolves

My endo recommended the under the tongue method but I may try the upper cheek method with the E just to see if I like it

My best advise is to follow your Dr.'s recommendations

Hugs

but the upper cheek method  need a lot of time hour and half Maybe I don't know but tell me please what happen when you try that

Thank you
Love

[auroratrans]

Spironolactone whether taken sublingually or orally, the effect will be practically the same so there is no point in taking it sublingually. I personally also found that taking E both orally and sublingually had the same effect on me, as regards to feminization and breast growth so I just swallowed.

The increase in coagulation (heightened/decreased production of certain proteins/factors) is triggered by estrogen activating estrogen receptors in the portal vein so if estrone is weaker than estradiol in activating receptors, the risk should be LESS with estrone, not higher. This, in addition to rapid metabolization/inactivation of estradiol, could account for why bio-identical estradiol, even taken orally, does not greatly increase the risk of DVT, especially relative to other forms of estrogen such as ethinyl estradiol.

Read the above. Estradiol would/should lead to a greater change in coagulation. The increase in coagulation is in direct proportion to how many times and how strongly (estriol and estrone are weak estrogens) estrogen receptors in the portal vein are activated.

The reason why estradiol triggers less coagulation changes when taken non-orally isn't because there is less conversion to estrone relative to oral but because there is less estrogen going into the portal vein and more into extrahepatic tissues. Higher doses non-orally lead to increasingly higher amounts going through the portal vein but the risk of DVT still remains very low, according to studies.

Estrone sulfate is actually the highest form of (inactive) estrogen found as a result of taking oral estradiol. This, along with estrone, constitute a reservoir from which estradiol can be later formed.

CLIMACTERIC 2005;8(Suppl 1):3–63

"estradiol, which is rapidly and extensively transformed in the intestinal tract and liver to estrone and estrone sulfate. Both metabolites are circulating in high concentrations and serve as a hormonally inert reservoir from which estradiol
is continuously delivered after reconversion"

Acta Endocrinol (Copenh). 1978 Aug;88(4):754-67.

"The levels of all oestrogens increased significantly following the ingestion of oestradiol, although to a greatly different extent. The largest and most prolonged increase was seen in the case of oestrone sulphate, the levels of which--depending on the dose ingested--were 20-50 times higher than the pre-treatment levels"

"The levels of oestrone and oestradiol sulphate exhibited smaller increases 3 h after ingestion, i.e. 4-10 and 2.5-5 times, respectively, and the plasma levels of oestradiol showed a minor increase only (1.4-1.8 times)."

A few birth control pills actually contain bio-identical estradiol and you can find bio-identical hormones in circular packs.

Thank you so much
all my respect
Hug

[josie76]

Kay, I'll have to dig up the study but, estradiol and progesterone have zero increase in platelet aggregation. Progesterone metabolites directly decrease platelet aggregation. Estrone and estriol both trigger increased platelet aggregation.

This was due to direct and indirect influences on the availability and efficacy of thrombin on platelet physical shape profiles. Estradiol was shown to have no effect direct or indirect on the thrombin levels or response in the platelets. Three metabolites of progesterone did show by several mechanisms to reduce the efficacy of thrombin response in platelets. One has a direct reversal effect of thrombin's calcium ion influx. The calcium influx triggers the physical shape change in platelet cells that allow them to begin to aggregate.

[auroratrans]

Thanks josie76

[auroratrans]

Are we talking about "lil blue pill", the one that comes in 28 dial pack???

Have tried taking both ways and, if intermittent breast tenderness is any indication, feel sublingual leads to an "estrogen rush" with levels probably dropping off quicker whereas just swallowing gives the body time to more evenly metabolize between 'applications', taking over the course of a day.

Perhaps just my imagination??
Why can't 'they' design a higher mg estradiol pill that has a more consistent, slower level releasing 3-4 day half-life like bicalutamide??

Yes I talk about  blue pill, the one that comes in 28 dial pack

We are talking about the blue or blue green colored Estrace or generic version. This is bioidenticle estradiol. The reason we take it sublingual or buccally is because if you swallow the pill, the liver will convert the largest portion to estrone as all intestinal absorbtion passes by the liver on the way to the body.

Estrone is much weaker at activating estrogen receptors but also can compete for those receptors.
Estrone does in fact raise the risk of blood clotting. Estrone and estriol both increase clotting factor. Estradiol does not.
Estrone can be converted back and forth to estradiol but it is more desirable for the body to get it in estradiol form and let the body do its own conversion to estrone as needed.
Estrone is a storable form of estrogen and can remain in fat and andipose tissues.

I think the circular 28 day pack is a form of birth control pill and not bioidenticle hormones.


I think there is a rush of estrogen both sublingual or buccal absorbtion. When my doctor prescribed me a higher dose, my Rx bottle said 1-1/2 tablet twice daily. So instead I split it 1 blue-green tablet three times a day to spread it out more.

Thanks josie76 for answer

[KayXo]

Kay, I'll have to dig up the study but, estradiol and progesterone have zero increase in platelet aggregation. Progesterone metabolites directly decrease platelet aggregation. Estrone and estriol both trigger increased platelet aggregation.

Cardiovascular Endocrinology: September 2013 - Volume 2 - Issue 3 - p 50–54

"These results showed that estriol was one of the most potent inhibitors of platelet aggregation"

The Journals of Gerontology: Series A, Volume 55, Issue 4, 1 April 2000, Pages B183–B190

"We investigated the effects of estriol (E3) on endothelial function and bone mineral density (BMD) in very elderly women."

"E3 significantly improved BMD by inhibiting bone resorption. Endothelial function was improved in line with the antiatherosclerotic effects. E3 might be effective for use in HRT in elderly patients."

[josie76]

Here is a couple others. I don't have the links just the titles.

from some sources including these two
Both estrone(E1) and estiol(E3) increase platelet aggregation by synergistic effect on ADR and ADP effects.
Pregnanolone, pregnanediol, isopregnanediol can inhibit thrombin by 10-15%
Thrombin causes a Ca+2 egress and these metabolites cause a CA+2 influx.

Isn't it great how studies tend to prove each other wrong, or just wrong depending on the situation or tissues present. It'll drive you coo-coo after a while.       


American Journal of Hypertension, Volume 8, Issue 2, 1 February 1995, Pages 197–200,
17b-estradiol and progesterone may modulate platelet aggregation and atherosclerosis by attenuating calcium channel response

Progesterone metabolites rapidly stimulate calcium influx in human platelets by a src-dependent pathway.
Department of Physiological Sciences, Eastern Virginia Medical School, Norfolk, VA 23501-1980, USA. blackmPF@evms.edu

[KayXo]

Both estrone(E1) and estiol(E3) increase platelet aggregation by synergistic effect on ADR and ADP effects.

So did estradiol (E2). "the effects of E2 on the increased platelet aggregation by either ADR or ADP depended on internal factors such as endogenous estradiol and platelet aggregated state."

[josie76]

One of those studies specifically found E2 had zero effect raising clotting factor. Might be yet another one I read.

So much for studies. All they tell us is: it does something like so....most of the time. lol

[Laurie]

     Okay can we dispense with the 'my study is better than your study' war and let auroratrans have her thread back?

[V M]

but the upper cheek method  need a lot of time hour and half Maybe I don't know but tell me please what happen when you try that

Thank you
Love

I decided I prefered the under the tongue method

Hugs

[Cassi]

I decided I prefered the under the tongue method

Hugs

Thanks VM!  I have been doing it under the tongue as well and it seems to dissolve really quick. 

[Dani]

Spiro's bio-availability is quite high, around 90%, higher if taken with food (in contrast to the 5% for estradiol) so I don't see the point to taking it sublingually.

KayXo,

The bio availability of 5% for Estradiol is for ORAL administration.  With sublingual administration, the bio availability is about 5 times as much as oral administration and you avoid the first pass through the liver. The blood levels peak much higher but do not last as long.

So, take your pick of administration methods. Many women take their bio-identical Estradiol by sublingual method and they show results.