Clomiphene 50mg/ml, 60ML
Clomiphene (sometimes spelled clomifene) citrate, also known as Clomid or Serophene, is a selective androgen receptor modulator (SERM) used as an ovulation induction fertility drug in women, and sometimes off label as a testosterone enhancer, fertility treatment, or anti-estrogen in men. Clomiphene citrate’s property of increasing male androgen levels allows its off-label use as an alternative to testosterone replacement therapy (TRT) for men with hypogonadotropic (secondary) hypogonadism. Bodybuilders sometimes use Clomid as a way to treat gynecomastia occurring on steroid cycles or to recover normal hormone levels and sexual function afterwards. Clomiphene may have the favorable side-effect of decreasing fasting blood glucose and helping to prevent metabolic syndrome.
The mechanism of action of clomiphene is novel compared to tamoxifen, another SERM that can increase testosterone levels. Clomiphene’s two different isomers (enclomiphene and zuclomiphene) exert different effects in different tissue or cell types; the net effect of clomiphene interacting with the pituitary is to increase androgen levels, but this effect is achieved with different and selective effects coming from the two different isomers:
The direct effects of clomiphene citrate (Clomid), tamoxifen, and estradiol (E2) on the gonadotropin-releasing hormone (GnRH)-stimulated release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) were studied in cultured anterior pituitary cells obtained ... Tamoxifen...was without effect on the GnRH-stimulated LH release at a concentration of 10(-7) M. Furthermore, tamoxifen, unlike Clomid, caused an apparent but not statistically significant inhibition of the sensitizing effect of E2 on the GnRH-stimulated release of LH. Clomid and its Enclomid isomer, unlike tamoxifen, exert a direct estrogenic rather than an antiestrogenic effect on cultured pituitary cells by enhancing the GnRH-stimulated release of gonadotropin.
Zuclomiphene blocks or antagonizes estrogen receptors, leading the pituitary to falsely detect low estrogen and to increase release of LH and FSH, increasing downstream testosterone; however, enclomiphene exerts a near-opposite effect, while still ultimately contributing to increased LH/FSH and testosterone levels.
With clomiphene for hypogonadism, unlike TRT, typically the use is limited to a short period of time. In a comparison with testosterone replacement gel therapy (TGRT), Levine and Taylor found that clomiphene had an acceptable side-effect profile and lower cost, even for long-term use, for treating male hypogonadism and sexual dysfunction, concluding that “CC represents a treatment option for men with hypogonadism, demonstrating biochemical and clinical efficacy with few side effects and lower cost as compared with TGRT”.
Kanayama et al have recommended clomiphene as one facet of a pharmaceutical approach to recovery of anabolic-androgenic steroid (AAS) abuse stating “AS-induced hypogonadism may require treatment with human chorionic gonadotropin or clomiphene to reactivate neuroendocrine function, and may necessitate antidepressant treatments in cases of depression inadequately responsive to endocrine therapies alone.”
Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006.
Schellen TM. Clomiphene treatment in male infertility. Int J Fertil. 1982;27(3):136-45.
Kaminetsky J, Hemani ML. Clomiphene citrate and enclomiphene for the treatment of hypogonadal androgen deficiency. Expert Opin Investig Drugs. 2009 Dec;18(12):1947-55.
Tan RS, Vasudevan D. Use of clomiphene citrate to reverse premature andropause secondary to steroid abuse. Fertil Steril. 2003 Jan;79(1):203-5.
Hill S, Arutchelvam V, Quinton R. Enclomiphene, an estrogen receptor antagonist for the treatment of testosterone deficiency in men. IDrugs. 2009 Feb;12(2):109-19.
Adashi EY, Hsueh AJ, Bambino TH, Yen SS. Disparate effect of clomiphene and tamoxifen on pituitary gonadotropin release in vitro. Am J Physiol. 1981 Feb;240(2):E125-30.
Taylor F, Levine L. Clomiphene citrate and testosterone gel replacement therapy for male hypogonadism: efficacy and treatment cost. J Sex Med. 2010 Jan;7(1 Pt 1):269-76.
Kanayama G, Brower KJ, Wood RI, Hudson JI, Pope HG Jr. Treatment of anabolic-androgenic steroid dependence: Emerging evidence and its implications. Drug Alcohol Depend. 2010 Jun 1;109(1-3):6-13.