The drug enclomiphene citrate is a derivative of clomiphene citrate. Enclomiphene is a relatively new drug that is not only more effective than just clomiphene (clomid), but also avoids a lot of side effects that its predecessor has.
Clomiphene consists of two isomers zuclomiphene (zuclomiphene) and enclomiphene (enclomiphene). Zuclomiphene is an estrogen agonist, it is associated with a number of side effects, such as a decrease in libido, while enclomiphene has an antiestrogenic effect in the same tissues.
Encomiphene is an antagonist of estrogen receptors. It blocks estrogen, causing the body to increase LH and FSH levels. This stimulates the testicles to produce more testosterone and sperm. And unlike testosterone replacement therapy (TRT), which replaces your body's natural testosterone production with a synthetic version, enclomiphene helps your body produce more of its own natural testosterone. This will help you avoid the side effects associated with synthetic testosterone, such as testicular contraction, prostate enlargement, cardiovascular problems.
Enclomiphene can be used to boost testosterone levels, regardless of whether you have a low level or you just want to get an advantage when it comes to your energy, self-confidence, sexual function and athletic performance.
Mechanism of action
Enclomiphene has a selective estrogen receptor modulator (SERM) action, which means that it interacts with estrogen receptors in the body, but has a different effect in different tissues. As a result, it can have a blocking effect on estrogens in some tissues, such as mammary glands, but not in others, such as bone tissue. This allows the use of enclomiphene for the treatment of various conditions associated with an imbalance of estrogens in the body.
Encomiphene is a selective antagonist of estrogen receptors, counteracting estrogen receptors in the pituitary gland, disrupting the negative feedback loop of estrogen in relation to the hypothalamic-pituitary-gonadal axis, which ultimately leads to an increase in the secretion of gonadotropins – LH and FSH and a subsequent increase in the level of testosterone circulating in the blood.
Enclomiphene vs Clomiphene
Clomiphene consists of two isomers: enclomiphene and zuclomiphene.
While enclomiphene blocks the binding of estrogen to estrogen receptors in the hypothalamus and pituitary gland of the brain, zuclomiphene increases the level of estrogen and accumulates over time.
Enclomiphene is superior to Clomiphene because it has fewer side effects and stays in the body for a shorter period of time.
Clomiphene is a selective estrogen receptor modulator (SERM), a class of drugs that affect estrogen production. By blocking the production of estrogen, clomiphene "deceives" the body, making it think that it does not receive enough estrogen, thereby stimulating the production of hormones luteinizing hormone (LH) and follicle stimulating hormone (FSH). In women, it helps to stimulate ovulation. In men, an increase in LH and FSH levels helps stimulate testosterone production and spermatogenesis.
Despite its popularity in the treatment of low testosterone levels, some studies show that the use of clomiphene may have disadvantages, mainly due to the inclusion of zuclomiphene in it. Zuclomiphene has side effects that go beyond the therapeutic effect of the drug. For these reasons, the researchers concluded that since the two isomers have completely different biochemical and toxicological properties, there is “a need to develop a pure selective estrogen receptor antagonist” for the treatment of men with low testosterone levels.
When comparing clomid with enclomiphene, the researchers found that enclomiphene wins. With fewer side effects and greater benefits, encomiphene is the preferred choice for safely increasing testosterone levels. Zuclomiphene has been shown to have a “detrimental” effect on the male reproductive tract. Along with a significant decrease in the size of the testes during testicular degeneration, zuclomiphene also caused the loss of Leydig cells, the absence of spermatozoa in the seminal tubules and a decrease in the size of the epididymis, seminal vesicles and kidneys.
Because of its mixed estrogenic and antiestrogenic effects, clomiphene can also cause emotional regulation disorders such as mood swings and depression. It is believed that this is due to an estrogenic imbalance caused by the fact that zuclomiphene remains in the body longer than enclomiphene.
Other reported side effects of clomiphene include irritability, anxiety, and decreased libido.
Hypogonadism in men
Encomiphene was developed as an alternative to testosterone for the treatment of hypogonadism in men in order to maintain sperm production and reduce the risk of negative side effects associated with taking testosterone. This helps to restore normal testosterone levels in the body and improve the quality of sperm.Hypogonadism in men
Enclomiphene was developed as an alternative to testosterone for treating hypogonadism in men, with the goal of maintaining sperm production and reducing the risk of negative side effects associated with testosterone use. It helps to restore normal testosterone levels in the body and improve the quality of sperm.
Clomiphene can be used in combination with other medications to stimulate ovulation in women who have problems getting pregnant.
Enclomiphene can be used to treat breast tumors that are estrogen-dependent. It helps to reduce the level of estrogen in the body, which can slow down the growth of the tumor.
Treatment of hypogonadism
Hypogonadism is a pathological process provoked by a lack of male sex hormones, in particular, testosterone, which entails a large number of consequences for the male body.
As you know, with reduced testosterone, many body functions suffer, such as fertility, and fatigue appears, muscle mass decreases, the percentage of fat increases, depression develops, erectile dysfunction. Most often, the level of testosterone in a man's body begins to fall after 30 years, but the situation can be aggravated by obesity, diabetes and vascular diseases.
One of the treatment options for hypogonadism is the use of drugs of the SERMs class.
During clinical trials, enclomiphene was tested on men with secondary hypogonadism. As a result of the research, it turned out that enclomiphene citrate increased the level of testosterone, the level of follicle-stimulating hormone and luteinizing hormone, important for reproductive health, while the number of spermatozoa did not decrease.
In men with secondary hypogonadotropic hypogonadism, an increase in LH and FSH improves testosterone levels and sperm motility. Men with secondary hypogonadotropic hypogonadism have abnormally low testosterone levels due to low normal levels of luteinizing hormone (LH) and follicle stimulating hormone (FSH). The biological role of these hormones is to stimulate the endogenous production of testosterone by the testes.
Treatment with enclomiphene works differently than traditional testosterone replacement therapy, which replaces testosterone using an exogenous source and has a number of advantages – such as improving, rather than reducing fertility, stimulating the production of enodogenic testosterone, rather than introducing exogenous, which ultimately does not lead to suppression of the production of own testosterone, as well as the absence of negative effects on cholesterol and increased hematocrit levels.
Moreover, testosterone levels in those who take enclomiphene remain elevated even after discontinuation of treatment.
The efficacy and safety of encomiphene citrate in the treatment of male hypogonadism have been studied in several clinical trials. One such study, published in the Journal of Clinical Endocrinology and Metabolism in 2014, showed that encomiphene citrate improves testosterone levels and sperm parameters in men with hypogonadism.
Another study published in the Journal of Sexual Medicine in 2016 also showed that encomiphene citrate improves testosterone levels and sperm production in men with hypogonadism without significant side effects.
Although encomiphene citrate is not a first-line drug for the treatment of male hypogonadism, it may be an effective alternative treatment option for men who are unable or unwilling to use testosterone.
Therapy to increase testosterone levels
Enclomiphene acts as an antiestrogen, which means it helps block the action of estrogens in the body. This can lead to an increase in testosterone levels not only for the treatment of low testosterone levels, but also can increase its level beyond the limits of the norm, which can give some advantages in terms of accelerated recovery after training and an increase in the psycho-emotional background.
An increase in testosterone levels can also lead to increased athletic performance, increased energy, some muscle mass, and even greater self-confidence.
If you use enclomiphene for these purposes, then during the reception you will need to monitor the level of hormones such as estradiol and SHBG. A high level of testosterone will lead to an increase in these hormones, which can create both undesirable side effects and nullify all the benefits of increased testosterone.
After 10 days of using enclomiphene, take a blood test for estradiol. When increasing it, use aromatase inhibitors such as anastrazole. You should choose the dosage and reduce the level of estradiol to the middle of the norm. This should definitely be done, because elevated estradiol can create problems with your psycho-emotional state and also lower libido. If you have started to feel these phenomena when taking enclomiphene, then it's time to reduce your estradiol level. We recommend lowering to the middle of the reference values, but perhaps you will feel better with its other values. These parameters are determined individually, since estrogens can suppress its production. It can improve muscle growth and increase strength.
Also, when using enclomiphene, you should monitor the level of SHBG. If this protein goes beyond the highest limit of the norm, you should reduce it with the help of such a remedy as mesterolone. The fact is that a high level of this protein binds your testosterone and prevents it from freely circulating in the blood and joining androgen receptors, which also reduces the effectiveness of using enclomiphene if your goal is to raise testosterone levels above the normal limits. The dosage of proviron can be 25-50 mg per day, every other day or several times a week, depending on the level of SHBG in the blood. Higher dosages can negatively affect the level of endogenous testosterone.
The study showed that a single dose of 12.5 mg of enclomiphene increased the testosterone level from 217.2 ng / dl to 471.9 ng / dl and allowed to keep the concentration of elevated testosterone for quite a long time.
The efficacy and safety of enclomiphene citrate in treating male hypogonadism have been studied in several clinical trials. One such trial, published in the Journal of Clinical Endocrinology & Metabolism in 2014, showed that enclomiphene citrate improved testosterone levels and semen parameters in men with hypogonadism.
Using in sports
Some studies show that enclomiphene may be effective for improving athletic performance. For example, one study published in the International Journal of Sports Medicine in the International Journal of Sports Medicine showed that the use of enclomiphene in men improved results in weightlifting. Of course, taking enclomiphene will not replace a full cycle of anabolic steroids in any way, but this may be an intermediate step when a novice athlete is still afraid to use AS, but already needs accelerated recovery or wants to accelerate progress a little beyond the values of a "natural athlete".
The use of enclomiphene for PCT
Enclomiphene can be used as a drug for post-course therapy (PCT) after taking anabolic steroids. This is the effect effect that is of the greatest interest to fans of PEDs. Anabolic steroids, such as testosterone, can suppress the body's natural testosterone production. At the end of the cycle of taking anabolic steroids, the testosterone level in the body can be very low, which can lead to undesirable effects, such as loss of muscle mass, a drop in the psycho-emotional background and a decrease in sexual function.
Post-course therapy is aimed at restoring the natural production of testosterone in the body. Enclomiphene can be an effective drug for PCT, as it helps restore natural testosterone production by stimulating the hypothalamus-pituitary-testicular axis.
- Increases testosterone levels in both hypogonadal men and healthy men with the ability to
- Increases in testosterone levels above the normal limits without negative estrogenic effects that may be caused by taking its predecessor - clomiphene citrate
The typical recommended enclomiphene dosage is 6.25–25 mg per day
Increasing the level of endogenous testosterone
- Abdominal discomfort
- Hot Flushes
- Pregnant women,
- Breastfeeding women,
- wWomen with unexplained uterine bleeding
- Women with ovarian growths or cysts unrelated to polycystic ovary syndrome
- Patients with a history of liver disease
- Patients with uncontrolled adrenal or thyroid dysfunction
- Patient with known allergy to enclomiphene or clomiphene
How to store
- Keep away from children
- Keep in a cool, dry place, away from direct sunlight
- Store at room temperature
- Do not use after the expiry date
Half-life: 10 hours
Frequency of intake: 1 time per day
Active ingredient: Enclomiphene citrate
Type: Selective estrogen receptor modulator
Form: Oral (pills)