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Hrt (Pharmacokinetics)

#81

(25-10-2015, 09:26 PM)bobie Wrote:  Thanks, i actually got my progesterone tested back in june, it was low at 2.4 nmol/l then, i wasnt sure when to add it but i have a stash of utrogestan which is bio identical, i think i also have a couple of jars of pc somewhere too

Super, give it a try, it might help. DHEA could useful too, 25-50mg. I like it because it's a precursor to androstenedione. In other words, shove it back (upstream) to androstenedione, where it can be synthesized to more E1/E2, this is useful as it upregulates E/2 whilst andro levels are low at female range.
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#82

I dont know where i read it but within the last week im sure i read that the gnrh analogues (which im on) effect both androstenedione and progesterone negatively, i will try progesterone first and see how things go, thanks lotus
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#83

I have to say looking back at this study I find this particularly important:

. 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 what's interesting is how Serum concentrations of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) were significantly decreased within 6 hours. Meaning during those 6 hours, a reduction of T (testosterone) signal is being turned off to the hypothalamus (negative feedback)............that's good new in my opinion.



(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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