View Full Version : Nolvadex~Tamoxifen Citrate

01-03-2010, 05:38 PM

(Tamoxifen Citrate)

Tamoxifen is an antagonist of the estrogen receptor in breast tissue. It has been the standard endocrine (anti-estrogen) therapy for hormone-positive early breast cancer, although aromatase inhibitors have been proposed for postmenopausal women.
Some breast cancer cells require estrogen to grow. Estrogen binds to and activates the estrogen receptor in these cells. Tamoxifen is metabolized into compounds that also bind to the estrogen receptor but do not activate it. Furthermore tamoxifen prevents estrogen from binding to its receptor. Hence breast cancer cell growth is blocked.Tamoxifen is a SERM.

Selective Estrogen Receptor Modulators (SERMs) are a class of compounds that act on the estrogen receptor. A characteristic that distinguishes these substances from pure receptor agonists and antagonists is that their action is different in various tissues, thereby granting the possibility to selectively inhibit or stimulate estrogen-like action in various tissues.

Nolvadex essentially blocks the action of estrogen in certain tissues like breast tissue. This is advantageous to the male bodybuilder because Tamoxifen is an effective way to prevent gynocomastia. A daily dose of 20mg will typically protect a male from gyno. I always like to keep a bottle of Tamoxifen on hand for emergency gyno treatment as it is one of the fastest ways to mitigate gyno syptoms.

In addition to blocking the action of estrogen, Tamoxifen also increases testosterone, LH and FSH and estrogen. Estrogen is of course blocked in certain tissues leaving a circulating amount that may be beneficial to lipids. Higher circulating estrogen may produce a puffy or watery look so an aromatase inhibitor would be more suited for controlling estrogen and reducing bloat. Unfortunately there is some evidence that Tamoxifen reduces IGF-1 levels so it may not be the best choice for PCT when used alone. Post cycle is a fragile time so lower IGF-1 levels are not desirable along with the higher circulating estrogen. I personally would use a low dose aromatase inhibitor alongside Tamoxifen if employing it for PCT.


01-03-2010, 05:40 PM
Tamoxifen treatment in oligozoospermia.

Bartsch G, Scheiber K.

This study of the effects of long-term tamoxifen administration on semen analysis of oligospermic males confirms the potential therapeutic efficacy in normogonadotrophic oligospermia. 38 out of the 56 patients responded well to long-term treatment with 30 mg tamoxifen daily. According to the nomenclature of Eliasson, 32 patients reached normal sperm density and 16 patients normal sperm motility after tamoxifen treatment. In the group of responders a pregnancy rate of 34% is obtained. As far as the endocrinological parameters are concerned normogonadotrophic patients (responders and non-responders) showed an increase in testosterone, 17beta-estradiol, LH and FSH levels, whereas the levels of prolactin and testosterone/estradiol-binding globulin remained unchanged. No alterations at all were seen with regard to semen volume, during the time of tamoxifen treatment.

PMID: 7250160 [PubMed - indexed for MEDLINE]

01-06-2010, 12:39 PM
Stimulation of calcitonin secretory capacity by increased serum levels of testosterone in men treated with tamoxifen.

Schopman W (http://forums.rxmuscle.com/pubmed?term=%22Schopman%20W%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Slager E (http://forums.rxmuscle.com/pubmed?term=%22Slager%20E%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Hackeng WH (http://forums.rxmuscle.com/pubmed?term=%22Hackeng%20WH%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Mulder H (http://forums.rxmuscle.com/pubmed?term=%22Mulder%20H%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract).
Department of Internal Medicine, Eudokia Hospital, Bergsingel, Rotterdam, The Netherlands.

Previous studies have suggested that sex steroids, including both oestrogen and testosterone, influence calcitonin secretion. However, a negative effect of gonadotrophins on calcitonin has not been excluded. Twelve men with infertility and low-normal serum levels of testosterone were studied before and during tamoxifen therapy. Increases in the serum levels of LH, FSH, testosterone and calcitonin were observed after treatment. Our findings suggest that testosterone has a direct influence on calcitonin secretion.

PMID: 3123401 [PubMed - indexed for MEDLINE]

01-06-2010, 12:42 PM
Hormonal effects of an antiestrogen, tamoxifen, in normal and oligospermic men.

Vermeulen A (http://forums.rxmuscle.com/pubmed?term=%22Vermeulen%20A%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Comhaire F (http://forums.rxmuscle.com/pubmed?term=%22Comhaire%20F%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract).

The administration of tamoxifen, 20 mg/day for 10 days, to normal males produced a moderate increase in luteinizing hormone (LH), follicle-stimulating hormone (FSH), testosterone, and estradiol levels, comparable to the effect of 150 mg of clomiphene citrate (Clomid). However, whereas Clomid produced a decrease in the LH response to LH-releasing hormone (LHRH), no such effect was seen after the administration of tamoxifen. In fact, prolonged treatment (6 weeks) with tamoxifen significantly increased the LH response to LHRL. Treatment of patients with "idiopathic" oligospermia for 6 to 9 months resulted in a significant increase in gonadotropin, testosterone, and estradiol levels. A significant increase in sperm density was observed only in subjects with oligospermia below 20 X 10(6)/ml and normal basal FSH levels. When basal FSH levels were increased or oligospermia was moderate (greater than 20 X 10(6)/ml); no effect on sperm density was seen. As sperm density increased, FSH levels decreased, suggesting an inhibin effect. Sperm motility was not improved by tamoxifen treatment. In five boys with delayed puberty, tamoxifen treatment appeared to activate the pituitary-gonadal axis and pubertal development.

PMID: 640052 [PubMed - indexed for MEDLINE]

01-06-2010, 12:44 PM
Hormonal changes in tamoxifen treated men with idiopathic oligozoospermia.

Hampl R (http://forums.rxmuscle.com/pubmed?term=%22Hampl%20R%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Heresová J (http://forums.rxmuscle.com/pubmed?term=%22Heresov%C3%A1%20J%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Lachman M (http://forums.rxmuscle.com/pubmed?term=%22Lachman%20M%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Sulcová J (http://forums.rxmuscle.com/pubmed?term=%22Sulcov%C3%A1%20J%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Stárka L (http://forums.rxmuscle.com/pubmed?term=%22St%C3%A1rka%20L%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract).
Research Institute of Endocrinology, Prague/Czechoslovakia.

Three months of tamoxifen treatment of 43 men with idiopathic oligozoospermia, out of which 20 completed the study, resulted in a significant enhancement of sperm motility, but the improvement of sperm parameters was in no relation to the FSH response to short time tamoxifen treatment. There was a significant increase of testosterone, estradiol, LH, FSH, SHBG, 17 alpha-hydroxy-progesterone and also of 11 beta-hydroxyandrostenedione, an androgen of exclusively adrenal origin, during the treatment and (with the exception of the latter), on the first week after discontinuation of the therapy. Significantly elevated testosterone and SHBG concentrations were retained still 9 weeks after finishing of the therapy. The results confirm that tamoxifen treatment provides conditions more favourable for conception and demonstrate that also adrenal steroidogenesis is positively influenced by this antiestrogen.

PMID: 3243340 [PubMed - indexed for MEDLINE]

01-11-2010, 02:37 PM
Effect of tamoxifen on GH and IGF-1 serum level in stage I-II breast cancer patients.

Mandalŕ M, Moro C, Ferretti G, Calabro MG, Nolč F, Rocca A, Munzone E, Castro A, Curigliano G.

Division of Medical Oncology, European Institute of Oncology, Via Ripamonti 435, 20141-Milan, Italy. [email protected]

OBJECTIVE: Tamoxifen suppresses insulin-like growth factor-1 (IGF-1) plasma levels in early and advanced breast cancer patients. Relationships between tamoxifen (GH) and IGF-1 are complex and not completely described yet. The present investigation was performed to evaluate the effect of acute and chronic tamoxifen administration on GH response to growth hormone-releasing hormone (GHRH), as well as on IGF-1 serum levels. MATERIALS AND METHODS: Evaluation of GH after administration of GHRH was performed (a) at baseline, (b) 3 hours after 20 mg oral administration of tamoxifen and (c) after 12 weeks of 20 mg a day oral tamoxifen treatment, in fifteen postmenopausal stage I-II breast cancer patients. IGF-I was measured at baseline and after chronic tamoxifen administration. RESULTS: The GH response to GHRH was significantly reduced after 12 weeks of tamoxifen 10 mg administered twice a day orally (mean peak 3.2 +/- 0.2 micrograms/l, mean AUC 261.3 +/- 18.2 micrograms/minute p < 0.01 versus basal AUC). A concomitant significant reduction of IGF-1 was observed after 3 months of tamoxifen treatment. Basal pretreatment levels of 113.2 +/- 15.5 micrograms/l were suppressed to 70 +/- 7.9 micrograms/l (p < 0.01). CONCLUSION: Our study confirm the inhibitory effect of tamoxifen on IGF-I and suggested, as shown in previous in vitro data, that its suppression could be directly related to GH reduction in response to GHRH stimulation

01-12-2010, 03:48 AM
Women & Nolvadex
*Note: * caveat about this is general information & not medical recommendations *

Nolvadex, being a Selective Estrogen Receptor Moderator (SERM), is one of the only compounds that directly affects the estrogen produced by the ovaries. As opposed to most other "anti-estrogens", which are actually Aromatase Inhibitors (AIs), such as Arimidex, Aromasin, etc. These work to prevent convertion of testosterone to estrogen. The sources of such estrogen are things like exogenous testosterone (e.g. Deca) and adrenal androgens.

Typical Use
Nolvadex is often used for short-term manipulation of estrogen to control estrogen-driven bodyfat depositing such as around the waist, hips and thighs. This is not intended as a "maintenance protocol for fat loss" - meaning it should be used for a specific goal such as a photoshoot or a competition, where you expect to rebound some after coming off.

Typical Cycle
Dose: 20 mg / day - split the dose 1/2 in the AM, 1/2 in the PM
Duration: 4-8 weeks max
Suggested to taper down the dose over the last week to reduce estrogen rebound

Typical Sides
- interrupted period / flow - may take a few months for the flow to come back as normal.
- may still experience usual menstrual sides (cramps, bloating, etc.) on your regular menstrual schedule
- post-cycle estrogen rebound

01-22-2010, 02:11 PM
Tamoxifen, serum lipoproteins and cardiovascular risk.

Bruning PF (http://forums.rxmuscle.com/pubmed?term=%22Bruning%20PF%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Bonfrer JM (http://forums.rxmuscle.com/pubmed?term=%22Bonfrer%20JM%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Hart AA (http://forums.rxmuscle.com/pubmed?term=%22Hart%20AA%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), de Jong-Bakker M (http://forums.rxmuscle.com/pubmed?term=%22de%20Jong-Bakker%20M%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Linders D (http://forums.rxmuscle.com/pubmed?term=%22Linders%20D%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), van Loon J (http://forums.rxmuscle.com/pubmed?term=%22van%20Loon%20J%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Nooyen WJ (http://forums.rxmuscle.com/pubmed?term=%22Nooyen%20WJ%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract).
Department of Clinical Oncology, The Netherlands Cancer Institute, Amsterdam.

The influence of tamoxifen on plasma lipids and lipoproteins was monitored in 46 postmenopausal and 8 premenopausal women treated for advanced breast cancer up till 6 months. Total cholesterol (total-C) did not significantly change. However, high density lipoprotein cholesterol (HDL-C) and the HDL-C/total-C ratio rose significantly. Low density lipoprotein cholesterol was significantly decreased. Triglycerides and free fatty acids did not change markedly. The concomitant rise of sex hormone binding globulin and thyroxine binding globulin indicates that the increase of HDL-C with prolonged use of tamoxifen is compatible with an intrinsic oestrogenic effect of tamoxifen on the liver. The increased HDL-C/total-C ratio lends no support to the concern that long-term administration of this anti-oestrogenic drug might lead to an increased cardiovascular risk.

PMID: 3207604 [PubMed - indexed for MEDLINE]

08-21-2010, 03:42 PM
Since the Tamoxifen acts as the 'estrogen' blocker to the receptor site....or in some cases will actually metabolize into compounds that also bind to the estrogen receptor but do not activate it. What happens to all the estrogen in women? Where does it go? Does it convert back to something else? Metabolized by the body to?

08-22-2010, 03:44 PM
Since the Tamoxifen acts as the 'estrogen' blocker to the receptor site....or in some cases will actually metabolize into compounds that also bind to the estrogen receptor but do not activate it. What happens to all the estrogen in women? Where does it go? Does it convert back to something else? Metabolized by the body to?
The estrogen circulates in your body or attaches to other estrogen receptors since not all receptors are blocked by Nolvadex. Once you stop the SERM it is free to attach to the particular estrogen receptors that were formerly blocked.

08-02-2012, 02:24 AM
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