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Cycling Estradiol

#1

As a male who only wants to grow breasts, I've had a lot of progress over the last 4 years using herbals, creams and massage.
I decided to finally ask my doctor for estrogen, and he has put me on 2mg/day of estradiol, a prescription for 100 pills. I am on day 34.
My idea was to go through the prescription then evaluate to see if I wanted to go further, possibly renewing the prescription.
The idea of cycling the estradiol also occurred to me - just a bodybuilders cycle steroids.
A friend told me however, that I need to stay on the estradiol for at least a year or I will lose whatever I have gained.
Does anyone who has taken estradiol have advice on this?
Input would be greatly appreciated!

Thanks!
Joey
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#2

I think that question you should ask your doctor.. The only reason I would cycle like that is if you were going to use PC.
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#3

Congratulations! That's a big step, I hope you're enjoying the experience and taking it all into consideration after your other NBE experiences. I'd love to hear how they compare
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#4

I've gone off of E2 for a few days and still had +800 pg/mL of E2 in my system after lab tests. I believe certain metabolites of estradiol stay active up to +48 hrs, possibly up to 96 hours.



(08-06-2015, 09:06 PM)Lotus Wrote:  Two postmenopausal studies on E2, which in comparison they relate to most genetic males here at BN, (hormone levels).

Single-dose pharmacokinetics of sublingual versus oral administration of micronized 17 beta-estradiol.

Price TM1, Blauer KL, Hansen M, Stanczyk F, Lobo R, Bates GW.
Author information
Abstract
OBJECTIVE
To investigate the pharmacokinetic profiles of different doses of micronized 17 beta-estradiol administered by oral or sublingual routes.
METHODS:
Single doses of micronized 17 beta-estradiol were administered orally (1 mg, 0.5 mg) or sublingually (1 mg, 0.5 mg, 0.25 mg) to six postmenopausal women in a randomized clinical trial. We calculated pharmacokinetic parameters for estradiol (E2) and estrone (E1) of maximum serum concentration, time to maximum serum concentration, terminal half-life, area under the concentration curve, and oral clearance. Serum levels of E1 sulfate also were compared at 4, 12, and 24 hours after dosing.
RESULTS:
Sublingual administration resulted in rapid absorption with significantly higher E2 levels than did comparable oral dosing. Estrone levels did not vary with route of administration but correlated with the dosage administered. Estrone sulfate levels correlated with the dosage administered and also tended to be higher with sublingual administration. Sublingual administration resulted in a significantly lower E1 to E2 ratio during the 24 hours than did oral administration.
CONCLUSION:
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.

____________________________________

17beta-estradiol.

Burnier AM, Martin PL, Yen SS, Brooks P.
Abstract
The sublingual absorption rates, the sustained effects, te biologic activity, and the metabolism of micronized 17beta-estradiol (E2) were measured in 10 postmenopausal women. E2 (0.5 mg) was administered in a single sublingual dose to five of the patients. An alternate-day schedule with the same dosage was used for the other five patients. In the single-dose study, a twenty-six fold increase in serum E2 and a ninefold increase in serum estrone (E1) concentrations were observed 1 hour after the sublingual deposition of E2 (0.5 mg). Serum concentrations of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) were significantly decreased within 6 hours. The rise in E2 was early and peaked in the first 2 hours. The rise in E1 was slower and progressive, reaching its maximum thirteenfold increase at 4 hours, and remained two and one half times the baseline of 29 pg/ml at 24 hours, whereas E2 returned to the baseline level of 24 pg/ml. When micronized E2 was given in a dosage of 0.5 mg sublingually every other night, increased circulating levels of estrogens continued to be elevated at a minimum two and one-half fold baseline level for the week of study.

Mean levels (CMax) after 1 hour in this study were 773.6 pg/ml. Estrace 1 mg, cut in half (0.5 mg).
http://www.ncbi.nlm.nih.gov/pubmed/6786097
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#5

I look at this study and see a glaring fact, FSH is downregulated, LH is lowered too (but that's ok because how it reduces T signal from the hypothalamus). FSH (follicle stimulating hormone) is what concerns me, meaning we lose its ability to stimulate aromatase, (or its ability to synthesize it). So, in other words, one would still need to add pro-aromatase............I do have a prossible solution.

Another thing is how E2 does given every other night, now this is peaking my curiosity.

Quote:When micronized E2 was given in a dosage of 0.5 mg sublingually every other night, increased circulating levels of estrogens continued to be elevated at a minimum two and one-half fold baseline level for the week of study.



Serum concentrations of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) were significantly decreased within 6 hours. The rise in E2 was early and peaked in the first 2 hours. The rise in E1 was slower and progressive, reaching its maximum thirteenfold increase at 4 hours, and remained two and one half times the baseline of 29 pg/ml at 24 hours, whereas E2 returned to the baseline level of 24 pg/ml. When micronized E2 was given in a dosage of 0.5 mg sublingually every other night, increased circulating levels of estrogens continued to be elevated at a minimum two and one-half fold baseline level for the week of study.
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#6

Dear guy with lingerie,

I do understand about cycling, hormone receptors can get desensitized, thereby slowing progress. I don't see cycling off of E2 for a few days hurting, in fact it could be beneficial, (my opinion from experience though). PC (progesterone cream) can help restore lost receptor sensitivity, that means applying PC to the breasts, (inhibits DHT too) and helps prevent cancer, all of which is beneficial for the breasts.
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#7

Personally, I don't think cycling on and off of estrogen is good. It's rough on the mind and the body. If I go off E too long, just one day, I get major pms bitchiness and emotional upheval. Needlesz to say, I stay consistant!
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#8

Thanks for the responses!
So going back to Lotus' response, am I better off swallowing the dose or letting it melt under the tongue?
Someone had said that under the tongue is a better option to ingest it.
I will of course have to talk to my doctor as the end of my prescription comes to see how he feels about staying on it. I was interested in other members experiences with the drug.

Joey
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#9

(13-07-2016, 10:49 AM)guy_and_lingerie Wrote:  I will of course have to talk to my doctor as the end of my prescription comes to see how he feels about staying on it. I was interested in other members experiences with the drug.

While I was taking 2mg a day (1st six months) I took .5mg 4 times a day and my clinician had me take it sublingually under the tongue. Now I am taking 3mg a day (2nd six months) 1mg three times a day under the tongue.
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#10

(13-07-2016, 02:45 AM)Lotus Wrote:  I've gone off of E2 for a few days and still had +800 pg/mL of E2 in my system after lab tests. I believe certain metabolites of estradiol stay active up to +48 hrs, possibly up to 96 hours.



(08-06-2015, 09:06 PM)Lotus Wrote:  Two postmenopausal studies on E2, which in comparison they relate to most genetic males here at BN, (hormone levels).

Single-dose pharmacokinetics of sublingual versus oral administration of micronized 17 beta-estradiol.

Price TM1, Blauer KL, Hansen M, Stanczyk F, Lobo R, Bates GW.
Author information
Abstract
OBJECTIVE
To investigate the pharmacokinetic profiles of different doses of micronized 17 beta-estradiol administered by oral or sublingual routes.
METHODS:
Single doses of micronized 17 beta-estradiol were administered orally (1 mg, 0.5 mg) or sublingually (1 mg, 0.5 mg, 0.25 mg) to six postmenopausal women in a randomized clinical trial. We calculated pharmacokinetic parameters for estradiol (E2) and estrone (E1) of maximum serum concentration, time to maximum serum concentration, terminal half-life, area under the concentration curve, and oral clearance. Serum levels of E1 sulfate also were compared at 4, 12, and 24 hours after dosing.
RESULTS:
Sublingual administration resulted in rapid absorption with significantly higher E2 levels than did comparable oral dosing. Estrone levels did not vary with route of administration but correlated with the dosage administered. Estrone sulfate levels correlated with the dosage administered and also tended to be higher with sublingual administration. Sublingual administration resulted in a significantly lower E1 to E2 ratio during the 24 hours than did oral administration.
CONCLUSION:
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.

____________________________________

17beta-estradiol.

Burnier AM, Martin PL, Yen SS, Brooks P.
Abstract
The sublingual absorption rates, the sustained effects, te biologic activity, and the metabolism of micronized 17beta-estradiol (E2) were measured in 10 postmenopausal women. E2 (0.5 mg) was administered in a single sublingual dose to five of the patients. An alternate-day schedule with the same dosage was used for the other five patients. In the single-dose study, a twenty-six fold increase in serum E2 and a ninefold increase in serum estrone (E1) concentrations were observed 1 hour after the sublingual deposition of E2 (0.5 mg). Serum concentrations of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) were significantly decreased within 6 hours. The rise in E2 was early and peaked in the first 2 hours. The rise in E1 was slower and progressive, reaching its maximum thirteenfold increase at 4 hours, and remained two and one half times the baseline of 29 pg/ml at 24 hours, whereas E2 returned to the baseline level of 24 pg/ml. When micronized E2 was given in a dosage of 0.5 mg sublingually every other night, increased circulating levels of estrogens continued to be elevated at a minimum two and one-half fold baseline level for the week of study.

Mean levels (CMax) after 1 hour in this study were 773.6 pg/ml. Estrace 1 mg, cut in half (0.5 mg).
http://www.ncbi.nlm.nih.gov/pubmed/6786097

http://www.ask.novartispharma.ca/download.htm?res=estradot_scrip_e.pdf&resTitleId=739

This PDF quotes a few studies too, its concerning the Estrodot patches, but most of it still applies to what we should expect with tablets. ( half life ect )
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