Tamoxifen is used to treat infertility in women with anovulatory disorders. A dose of 10–40 mg per day is administered in days 3–7 of a woman's cycle. In addition, a rare condition occasionally treated with tamoxifen is retroperitoneal fibrosis.
In men, tamoxifen "nolvaldex" is sometimes used by steroid-taking, weight-training athletes.An alternative and highly similar compound is clomaphene citrate "clomid".These drugs are used in as anti-aromatase therapy. In this regard, the drug is used for three purposes. The first purpose, is to reduce the amount of circulating estrogen. Abnormally high levels of estrogen in men, can be caused by taking highly aromatising anabolic steroids e.g. Trenbolone, dianabol, anadrol, deca durabolin or a long ester testosterone. In dosing with a dosing with 20 mg of Novaldex (Tamoxifen)for the duration of a steroid cycle, a reduction in water retention can be achieved. This prevents large fluctuations in water weight within the muscle.
Using Tamoxifen for the duration of a steroid cycle may or may not promote a preferable outcome for a weight training athlete, as the temporary increase in water weight within the muscle increases strength and allows larger weights to be used for the duration of the steroid cycle. Said water will dissipate once usage of steroids has ceased, and a dramatic loss in weight can be observed.
Tamoxifen is also used to prevent estrogen related gynomastia, resulting from said elevated estrogenic levels. It can be taken as a preventative measure in small doses, or used at the onset of any symptoms e.g. nipple soreness/sensitivity. In the latter case, dosing reverses the affliction.
Anti-aromatising drugs are used at the cessation of a steroid cycle. The half life of the steroids used within a cycle must be considered, so as to calculate the length of time before levels of testosterone have returned to a baseline level. Quick recovery of natural levels of testosterone production is highly important for the maintenance of muscle tissue. This is not possible unless the hypothalamus and Leydig cells sense a below baseline level of testosterone, due to the body's natural negative feedback loop. Levels of testosterone production from the testes can be inhibited by as much as 50% upon cessation of steroid intake, although this inhibition is dependent upon the amount, type ( hence relative anabolic and androgenic strength)and the length of time that the steroids have been used for. Tamoxifen has also been shown to have liver protecting/regenerative properties, hence another reason why a steroid taking athlete might wish to use it.
Tamoxifen citrate and clomiphene citrate are both commonly used at this point, although the latter has been shown to aggravate depressive mood.
Tamoxifen is also sometimes used to treat or prevent gynecomastia in sex offenders undergoing treatment by temporary chemical castration.
Tamoxifen has been shown to be effective in the treatment of mania in patients with bipolar disorder by blocking protein kinase C (PKC), an enzyme that regulates neuron activity in the brain. Researchers believe PKC is not over-active during the mania in bipolar patients.
Angiogenesis and cancer
Tamoxifen is one of three drugs in an anti-angiogenetic protocol developed by Dr. Judah Folkman, a researcher at Children's Hospital at Harvard Medical School in Boston. Folkman discovered in the 1970s that angiogenesis – the growth of new blood vessels – plays a significant role in the development of cancer. Since his discovery, an entirely new field of cancer research has developed. Clinical trials on angiogenesis inhibitors have been underway since 1992 using a myriad of different drugs. The Harvard researchers developed a specific protocol for a golden retriever named Navy who was cancer-free after receiving the prescribed cocktail of celecoxib, doxycycline, and tamoxifen – the treatment subsequently became known as the Navy Protocol. Furthermore tamoxifen treatment alone has been shown to have anti-angiogenetic effects in animal models of cancer which appear to be, at least in part, independent of tamoxifen's estrogen receptor antagonist properties.
Control of gene expression
Tamoxifen is used as a research tool to trigger tissue specific gene expression in many conditional expression constructs in genetically modified animals including a version of the Cre-Lox recombination technique.
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