Tamoxifen Citrate

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Tamoxifen Citrate

Nolvadex is the brand name for Tamoxifen. 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 receptoragonists 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.

Tamoxifen essentially blocks the action of estrogen in certain tissues like breast tissue. This is advantageous to males 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. Do not use Tamoxifen without a doctors prescription.

In addition to blocking the action of estrogen, Tamoxifen also increases testosterone, LH, FSH and estrogen. Estrogen is of course blocked in certain tissues leaving a circulating amount that may be beneficial to lipids. I personally would use a low dose aromatase inhibitor alongside or immediately following Tamoxifen if employing it for PCT as Tamoxifen may raise E2 so much that it causes an abnormal T/E2 ratio. Users with an abnormal T/E2 ratio may benefit from a long-term cotreatment with aromatase inhibitors.

Tamoxifen is a versatile compound that may be prescribed for breast cancer, gynocomastia, testosterone recovery and even for fertility in males.

Information is for educational purposes ONLY. Consult a medical doctor before using any medication. heavyiron does not advocate readers engage in any illegal activity. Research chemicals are not meant for human consumption.

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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]

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Stimulation of calcitonin secretory capacity by increased serum levels of testosterone in men treated with tamoxifen.

Schopman W, Slager E, Hackeng WH, Mulder H.
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]

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Hormonal effects of an antiestrogen, tamoxifen, in normal and oligospermic men.

Vermeulen A, Comhaire F.

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]

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Hormonal changes in tamoxifen treated men with idiopathic oligozoospermia.


Hampl R, Heresová J, Lachman M, Sulcová J, Stárka L.
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]

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Tamoxifen, serum lipoproteins and cardiovascular risk.

Bruning PF, Bonfrer JM, Hart AA, de Jong-Bakker M, Linders D, van Loon J, Nooyen WJ.
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]

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Urol Int. 2009;83(4):446-51. Epub 2009 Dec 8.

Role of testosterone/estradiol ratio in predicting the efficacy of tamoxifen citrate treatment in idiopathic oligoasthenoteratozoospermic men.

Cakan M, Aldemir M, Topcuoglu M, Altuğ U.
Department of 2nd Urology, SB Ankara Dişkapi Training Hospital, Ankara, Turkey. muratcakandr@yahoo.com

Abstract

AIM: It was the aim of this study to investigate the effect of a low testosterone/estradiol (T/E2) ratio and the normalization of this ratio by an aromatase inhibitor, anastrozole, on the treatment results of tamoxifen citrate (TAM) in idiopathic oligoasthenoteratozoospermic patients with a normal T/E2 ratio.
PATIENTS AND METHODS: 127 normogonadotropic men were included in this study. TAM (10 mg twice daily) was applied to 103 of the patients (group 1). The control group consisted of 25 patients who did not receive any treatment (group 2). After 3 months, TAM therapy was continued in 42 of the patients with a normal T/E2 ratio (group 1A). Of the remaining 61 patients with low ratios, 30 continued with TAM (group 1BTAM), while the remaining 31 patients underwent additional anastrozole therapy (1 mg/day) to TAM (group 1BANA).
RESULTS: In the 3rd month of the study, while the sperm concentration and motility were found significantly improved in group 1 (p < 0.05), they were significantly lower in groups 1BTAM and 1BANA than in group 1A (p < 0.01). In the 6th month of the study, the mean T/E2 ratio was normal in group 1A and group 1BANA, but was lower than normal ranges in group 1BTAM. The sperm concentration and motility significantly increased in groups 1A and 1BANA (p < 0.05).
CONCLUSIONS: A significant decrease in the T/E2 ratio was seen in the majority of the patients during TAM treatment. Normalization of this ratio by addition of anastrozole to the treatment regimen improved the treatment outcomes. However, a placebo-controlled study is needed to confirm our results.

PMID: 19996653 [PubMed - indexed for MEDLINE]

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Treatment of gynecomastia with tamoxifen: A double-blind crossover study

Lawrence N. Parker a, b, c, , David R. Gray b, c, a, Michael K. Lai b, c, a and Ellis R. Levin b, c, a

a Medicine, Service, University of California at Irvine, USA
b Pharmacy Service, University of California at Irvine, USA
c Long Beach Medical Program, Veterans Administration Medical Center, Long Beach, Calif., USA

Abstract

Benign asymptomatic or painful enlargement of the male breast is a common problem, postulated to be due to an increased estrogen/testosterone ratio or due to increased estrogenic or decreased androgenic stimulation via estrogen or androgen receptor interactions. Treatment at present consists of analgesic medication or surgery. However, treatment directed against the preponderance of estrogenic stimulation would seem to represent a more specific form of therapy. In the present double-blind crossover study, one-month courses of a placebo or the antiestrogen tamoxifen (10 mg given orally bid) were compared in random order. Seven of ten patients experienced a decrease in the size of their gynecomastia due to tamoxifen (P < 0.005). Overall, the decrease for gynecomastia for the whole group was significant (P < 0.01). There was no beneficial effect of placebo (P > 0.1). Additionally, all four patients with painful gynecomastia experienced symptomatic relief. There was no toxicity. The reduction of breast size was partial and may indicate the need for a longer course of therapy. A followup examination was performed in eight out of ten patients nine months to one year after discontinuing placebo and tamoxifen. There were no significant changes from the end of the initial study period except for one tamoxifen responder who developed a recurrence of breast tenderness after six months, and one nonresponder who demonstrated an increase in breast size and a new onset of tenderness after ten months. Therefore, antiestrogenic treatment with tamoxifen may represent a safe and effective mode of treatment for selected cases of cosmetically disturbing or painful gynecomastia.

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[Influence of size and duration of gynecomastia on its response to treatment with tamoxifen]

[Article in Spanish]
Devoto C E, Madariaga A M, Lioi C X, Mardones N.
Sección EndocrinologÃ*a, Servicio de Medicina, Hospital ClÃ*nico San Borja Arriarán, Santiago, Chile. edevoto@vtr.net

Abstract

BACKGROUND: Gynecomastia is treated when it is painful, there are psychosocial repercussions or it does not revert in less than two years. It is treated with the antiestrogenic drug tamoxifen, but there are doubts about its effectiveness in high volume gynecomastias or in those lasting more than two years.

AIM: To assess the effectiveness and safety of tamoxifen for gynecomastia and the influence of its volume and duration on the response to treatment.

PATIENTS AND METHODS: Forty three patients with gynecomastia, aged 12 to 62 years, were studied. Twenty seven patients had a pubertal physiological gynecomastia, in eight it was caused by medications, in four it was secondary to hypogonadism, in three it was idiopathic and in one it was due to toxic exposure. Twenty patients had mastodynia and in 33, gynecomastia had a diameter over 4 cm. It lasted less than two years in 30 patients, more than two years in nine and four did not recall its duration. All were treated with tamoxifen 20 mg/day for 6 months. A follow up evaluation was performed at three and six months of treatment.

RESULTS: Mastodynia disappeared in all patients at three months. At six months gynecomastia disappeared in 26 patients (62%), but relapsed in 27%. All gynecomastias caused by drugs with antiandrogen activity disappeared. Fifty two percent of gynecomastias over 4 cm and 90% of those of less than 4 cm in diameter disappeared (p<0.05). Fifty six percent of gynecomastias lasting more than two years and 70% of those of a shorter duration disappeared (p=NS). Two patients had diarrhea or flushes associated to the therapy.

CONCLUSIONS: Tamoxifen is safe and effective for the treatment of gynecomastia. Larger lesions have a lower response to treatment.

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J Clin Oncol. 1996 Mar;14(3):1018-26.

Tamoxifen-associated eye disease. A review.

Nayfield SG, Gorin MB.
Chemoprevention Branch, National Cancer Institute, Bethesda, MD, 20892, USA.

Abstract

PURPOSE: The oral antiestrogen tamoxifen has demonstrated efficacy in the treatment of metastatic breast cancer and as adjuvant therapy in early-stage disease. Clinical trials of tamoxifen in chemoprevention of breast cancer among high-risk women have focused attention on potential adverse effects of long-term tamoxifen use, including the possibility of ocular toxicity. This review evaluates the published case reports, clinical series, and clinical trial data on ocular toxicities attributed to tamoxifen. Clinical issues of surveillance, differential diagnosis, and management of tamoxifen-related eye disease are discussed.

DESIGN: National Library of Medicine online bibliographic services were used to identify case reports and clinical studies of ocular adverse effects that occurred in patients receiving tamoxifen published through the fall of 1994. The medical literature relevant to issues raised by the reports and studies was similarly identified and reviewed.

RESULTS: Case reports and case series identify crystalline retinal deposits, macular edema, and corneal changes as potential tamoxifen ocular toxicities. Extensive retinal lesions and macular edema with visual impairment have been reported in a few patients receiving high-dose tamoxifen. Less extensive retinal changes may occur in patients receiving low doses for long periods, and isolated retinal crystals may be observed in patients without visual symptoms.

CONCLUSION: Ocular toxicity is uncommon in the current clinical setting of long-term, low-dose tamoxifen use. Physicians should be aware of the potential for ocular toxicity among patients receiving the drug and should assure appropriate surveillance and prompt evaluation of visual complaints.


PMID: 8622006 [PubMed - indexed for MEDLINE]

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[Treatment of marked gynecomastia in puberty with tamoxifen].

[Article in German]
König R, Schönberger W, Neumann P, Benes P, Grimm W.
Source

Kinderklinik, Universität Mainz.

Abstract

Based on the good results of another author 10 boys with marked pubertal gynecomastia were treated with the antioestrogen Tamoxifen (Nolvadex) at a dose of 20-40 mg/d orally for 2-12 months. In most cases the gynecomastia decreased totally, only two patients experienced palpable subareolar glandular tissue at the end of therapy. Side effects were not noted. During therapy levels of estradiol and testosteron increased, with a more pronounced elevation of estradiol. Basal values of LH and FSH remained nearly unchanged, but LH showed an increased response to LH-RH, which could be explained by the antioestrogenic effect of Tamoxifen at the hypothalamic level. The reduction of breast size in spite of increased estradiol levels on the other hand, suggests that the mean therapeutic effect of tamoxifen is through estrogen receptor blockade of breast tissue.

PMID:3123765 [PubMed - indexed for MEDLINE]

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In the cancer subjects that upregulation of PGR occurs, 100% see down regulation after 4 weeks of Tamoxifen.

Cancer Res. 1981 May;41(5):1984-8.

Effects of tamoxifen on estrogen and progesterone receptors in human breast cancer.

Waseda N, Kato Y, Imura H, Kurata M.

Abstract

Twenty patients with primary breast cancer were treated with tamoxifen (10 mg p.o. twice a day) for 1 to 4 weeks. Before and after the tamoxifen administration, tumor specimens were obtained and assayed for estrogen receptors and progesterone receptors (PGR). Total cytosol estrogen receptor (ERC) and occupied nuclear estrogen receptor (ERN) were measured by hydroxylapatite assay, and unoccupied PGR was measured by the dextran-coated charcoal assay. ERC, ERN, and PGR were detectable in 11, 8, and 6 tumors, respectively, before tamoxifen administration. After tamoxifen treatment, ERC decreased in 10 of 11 ERC-positive tumors. Occupied ERN increased in three of five ERN-positive tumors treated with tamoxifen for a short period (1 to 2 weeks), but they decreased in all of three ERN-positive tumors after longer administration (3 to 4 weeks). PGR increased in three of five ERN-positive tumors after short-term tamoxifen treatment, but they decreased in all of three tumors treated by the drug for a longer period. Increased PGR responses were accompanied by an increase of ERN in two of three ERN-positive tumors. These results suggest that tamoxifen interacts with the estrogen receptor system in human breast cancer tissue and may be estrogenic during short treatment, while longer treatment results in an antiestrogenic response.

PMID:7214366 [PubMed - indexed for MEDLINE]