Clomifene used to stimulate ovary in female infertility and male hypogonadism but illegal use in bodybuilding

SOURCE:Clomifene. From Wikipedia, the free encyclopedia

Clomifene (INN) or clomiphene (USAN and former BAN) or Clomid or Clomifert is a selective estrogen receptor modulator (SERM) that increases production of gonadotropins by inhibiting negative feedback on the hypothalamus. It is used mainly for ovarian stimulation in female infertility due to anovulation (e.g., infertility in polycystic ovary syndrome). Clomiphene citrate is marketed under various trade names including Clomid, Serophene, and Milophene.

Mode of action

In normal physiologic female hormonal cycling, at 7 days past ovulation, high levels of estrogen and progesterone produced from the corpus luteum inhibit GnRH, FSH and LH at the hypothalamus and anterior pituitary. If fertilization does not occur in the post-ovulation period the corpus luteum disintegrates due to a lack of beta-hcg. This would normally be produced by the embryo in the effort of maintaining progesterone and oestrogen levels during pregnancy.

Therapeutically, clomiphene is given at day 2 of menses. By that time, FSH level is rising steadily, causing development of a few follicles. Follicles in turn produce the estrogen, which circulates in serum. Clomiphene acts by inhibiting the action of estrogen on the pituitary. Zuclomifene, the more active isomer (see below), binds to estrogen receptors and stays bound for long periods of time. This prevents normal receptor recycling and causes an effective reduction in hypothalamic estrogen receptor number. As a result, the body perceives a low level of estrogen, similar to day 22 in the previous cycle. Since estrogen can no longer effectively exert negative feedback on the hypothalamus, GnRH secretion becomes more pulsatile, which results in increased pituitary gonadotropin (FSH, LH) release. Increased FSH level causes growth of more ovarian follicles, and subsequently rupture of follicles resulting in ovulation.

Off-label use in the treatment of male hypogonadism (Low T)

Clomiphine citrate has been found very effective in the treatment of secondary male hypogonadism in many cases.[2] This has shown to be a much more attractive option than testosterone replacement therapy (TRT) in many cases because of the reduced cost and convenience of taking a pill as opposed to testosterone injections or gels.[3] Unlike traditional TRT it also does not shrink the testes and as a result can enhance fertility. Traditional TRT can render a man sterile.[4] Because clomiphene citrate has not been FDA approved for use in males it is prescribed off-label. According to Professor Craig Niederberger, because this drug is now generic, no drug company would pursue FDA approval for use in men now because there would be no profit incentive.[5] However, the single isomer of clomiphine “enclomiphene” under the brand name Androxal is currently under phase 2 trials for use in men.[6][7]

Prohibited use in sports and use in bodybuilding

Clomifene is commonly used by male anabolic steroid users to bind the estrogen receptors in their bodies, thereby blocking the effects of estrogen, such as gynecomastia. It also restores the body’s natural production of testosterone. It is commonly used as a “recovery drug” and taken toward the end of a steroid cycle.[citation needed] It is included on the World Anti-Doping Agency list of illegal doping agents in sport.

Tags: , , , , , , ,

3 Responses to “Clomifene used to stimulate ovary in female infertility and male hypogonadism but illegal use in bodybuilding”

  1. Clomifene could be use illegally in male bodybuilders « Dr Ko Ko Gyi’s Blog Says:

    […] Clomifene use to stimulate ovary in female infertility and male hypogonadism but illegal use in body… (drkokogyi.wordpress.com) […]

  2. Clomifene could be used illegally in male bodybuilders « Dr Ko Ko Gyi’s Blog Says:

    […] Clomifene use to stimulate ovary in female infertility and male hypogonadism but illegal use in body… (drkokogyi.wordpress.com) […]

  3. Infertility « Dr Ko Ko Gyi’s Blog Says:

    […] Clomifene use to stimulate ovary in female infertility and male hypogonadism but illegal use in body… (drkokogyi.wordpress.com) […]

Leave a Reply

Fill in your details below or click an icon to log in:

WordPress.com Logo

You are commenting using your WordPress.com account. Log Out /  Change )

Google photo

You are commenting using your Google account. Log Out /  Change )

Twitter picture

You are commenting using your Twitter account. Log Out /  Change )

Facebook photo

You are commenting using your Facebook account. Log Out /  Change )

Connecting to %s


%d bloggers like this: