Clomifene Citrate (Clomid) is an antiestrogen which applies its linking to the hypothalamus and the gonads. The drug causes the pituitary gland to release hormones needed to stimulate ovulation (release of the egg from the ovary), thereby increasing the chances of women getting pregnant. Clomifene was also used to increase sperm count in male patients with idiopathic oligospermia (insufficient sperm count for egg fertilization). The FDA first approved clomifene in the US in 1967.
In addition to the use of the drug in medicine for the treatment of various diseases associated with infertility and problems with conception of the child in women, clomid is quite popular in strength sports and is used during the PCT. We can say that this is one of the main drugs that is needed during the cycle. It is used for starting hypothalamus-pituitary-testicular axis.
Unlike tamoxifen, clomid is a “new generation” drug. However, due to its selectivity, clomifene citrate, which is an antagonist of estrogens for some tissues, may be a real estrogen for others. But fortunately, this characteristic in the application of the drug by men was not seen.
The description of the drug Clomifene Citrate. Effects on the body
Clomifene citrate – the color of the drug can be white or pale yellow, essentially odorless. The substance dissolves freely in methanol, ethanol. It is insoluble in acetone, water and chloroform. Not dissolving in the air. Clomid is a mixture of two geometric isomers (zuclomifene and enclomifene) containing between 30 and 50% of zuclomifene. One tablet of the drug contains 50 mg of the active substance, as well as some inactive ingredients: corn starch, lactose, magnesium stearate, pregelatinized corn starch and sucrose.
Due to the ability to bind to estrogen receptors in the hypothalamus, Clomifene Citrate significantly increases the level of gonadoliberin (GnRH), follicle stimulating hormone (FSH) and luteinizing hormone (LH), thereby leading to greater testosterone production by testicles in men and estrogen in women. But, according to studies, this effect of clomid does not exceed, and sometimes is lower than the cheaper and more common analog – tamoxifen.
Clomid has no direct effect on the amount of estrogens. Its mechanism of action is to block their access to the pituitary gland and the subsequent increase in follicle stimulating and luteinizing hormone. Available evidence suggests that both estrogenic and antiestrogenic properties of clomifene may participate in the initiation of ovulation. Have been found that two clomifene isomers have mixed estrogenic and antiestrogenic effects, which can vary from one species to another. Some evidence suggests that zuclomifene has greater estrogenic activity than enclomifene.
Clomifene citrate has no apparent progestational, androgenic or antiandrogenic effects and does not appear to interfere with the function of the pituitary-adrenal or pituitary thyroid gland. Despite the absence of signs of “portable effect”, some patients after clomid therapy had spontaneous ovulatory menstruation.
Pharmacokinetics of Clomifene Citrate
Based on early studies with 14C-labeled clomifene citrate, it has been shown that the drug is easily absorbed orally in patients and is excreted primarily from the feces. Cumulative excretion in urine and faeces 14C is about 50% of the oral dose and 37% of the intravenous dose after 5 days. Some studies have shown that the substance was still present in the feces in patients even 6 weeks after taking. Subsequent single clinical studies in normal volunteers showed that zuclomifene has a longer half-life than enclomifene. Discovered levels of zuclomifene persisted for more than a month. This may indicate stereospecific enterohepatic recycling or sequestering of zuclomifene. Thus, it is possible that the active substance may remain in the body during early pregnancy in women.
Let’s sum up:
Clomid (Clomifene Citrate) is a drug that acts in the body as an antiestrogen. The sport used it to carry out post cycle therapy. Among athletes it is highly popular. In the medical field, it is used to treat infertility, amenorrhea and other diseases. Clomifene is available in most pharmacies.
This drug blocks estrogen receptors in the ovaries and the pituitary gland, allowing you to “save” them from exposure to estrogen, as well as contributes to the restoration of your own testosterone (by the way, Tamoxifen blocks estrogen receptors in the whole body, which is one of the differences in the mechanism of their action). Also in contrast to Tamoxifen, Clomifene Citrate can be used after the Progestin cycle.
How to take Clomid during PCT?
Athletes do not use it during AS cycles. It is advisable to take aromatase inhibitors during the cycle. Clomifene is used after a cycle of anabolic steroids, helping athletes to keep their muscular mass by a more rapid recovery of the level of your own “testosterone”.
The time when you should start using Clomid depends on the anabolic steroid that the athlete are taking, because they have different half-lives. Most often, athletes “wait” for the end of the AS effect, because at this time the steroid has an active effect on the hormonal system of the body. After this effect “fades”, the PCT starts. The taking starts with the highest dose and gradually decrease.
Clomid side effects
Its action can have a negative impact on vision. This drug has a toxic effect on the liver, but it is less than from Tamoxifen. Also in athletes who use Clomifene may experience side effects such as headache, dizziness, insomnia, drowsiness, upset digestive system, nausea and vomiting.
In most cases, all the side effects end after the end of its use. It should be noted that the use of clomifene citrate increases the risk of thrombosis. In order to minimize this risk, during the period of use of the drug, it is necessary to increase the amount of water consumption per day by at least 1 liter.