Clomiphene citrate in the form of (Clomid, klostilbegit, ardomon, gravozan, serofen, serpafar, fertilin, fertomid et al.) Is close to non-steroidal estrogen dietistilbestrolu, however, does not exhibit estrogenic activity. The chemical structure similar to clomiphene main representative of a class of anti-estrogen drugs Imre – tamoxifen is 1- [4- (2-diethylaminoethoxy) phenyl] -1,2-diphenyl-2-chloroethylene citrate.
Clomiphene relates to anti-estrogen drugs, as specifically binds to estrogen dependent receptors in the hypothalamus and ovaries. In small doses through a negative feedback mechanism, clomiphene and its analogues enhance the secretion of gonadotropins (prolactin, luteinizing hormone and follicle-stimulating hormone) and to stimulate ovulation. At a low content of endogenous estrogen clomiphene body shows a mild estrogenic effect, however, in high concentrations estrogen has its own anti-estrogen effect. By reducing the content of circulating estrogen, induces a transient increase in the release of gonadotropins; large doses may inhibit it. Details
Another feature of clomiphene is that under certain conditions it does not act as a blocker, and as an activator of the estrogen receptors. All depends on whether the joining simultaneously with the drug to a particular receptor cofactor. Type cofactor is tissue-specific, that is, in the same tissue (hypothalamus, mammary gland) is clomiphene estrogen receptor blocker, and other (bone) -.. The same receptor activator. The last action of clomiphene on the body is a positive as it helps prevent osteoporosis.
Such antiesrogennye drugs like clomiphene in appropriate doses are used to stimulate ovulation in anovulatory ovarian dysfunction, infertility, uterine bleeding dysfunctional origin, some forms of amenorrhea, and others. Because of the gonadotropic influence of this drug is used during androgen nedstatochnosti, oligospermia in males and delayed sexual and physical development in adolescents.
Product: tablets 50 mg. If ingestion is well absorbed. It is metabolized in the liver and excreted in the bile and undergoes enterohepatic recycling. The half-life of 5-7 days.
Acceptance of the drug in women for six cycles even in therapeutic doses (50 mg for 5 days) can lead to visual impairment, and menorrhagia syndrome ovarian hyperstimulation (on withdrawal); accompanied by hot flashes, discomfort in the stomach and intestine, nausea, vomiting, depression, seizures, and disorders of the eye. In addition, clomiphene quite neurotoxic, which is reflected in the appearance of insomnia, headache, dizziness. Contraindications for taking the drug are expressed human natural detoxification systems (liver, kidney), uterine bleeding unclear etiology, including a history of ovarian cysts, pituitary tumor or pituitary insufficiency, pregnancy.
Given that the hypothalamus of male genotype full receptor having affinity for estrogen, quite a bit, the use of clomiphene in the power sport is theoretically possible to stimulate the production of gonadotropins and increase production of endogenous testosterone. The use of the same drug in women, in connection with the multi-faceted impact on hormonal homeostasis, will lead to pereproduktsii estrogen and progesterone, which is extremely negative impact on the physical shape Female athletes. Therefore, even in bodybuilding women receiving clomiphene at therapeutic doses is limited to a two-week period, followed by a break of the same duration.
Clomiphene citrate has the same function in the FCT as tamoxifen – restores the production of endogenous testosterone, but the clomiphene and tamoxifen, there are certain differences in the properties.
Clomid (clomiphene) and Nolvadex (Tamoxifen) is antiestrogen trifeniletilenov belonging to the same group. They are structurally similar and are classified as selective estrogen receptor modulators with mixed agonistic and antagonistic properties. This means that in certain tissue, they block the action of estrogen receptors by binding, while in other tissues could act as a real estrogen receptors activating. In men, both drugs act as anti-estrogens in their ability to interfere with estrogen negative feedback on the hypothalamus and stimulate the increased production of GnRH (GnRH). This will result in increased production of luteinizing hormone by the pituitary gland, which in turn can increase the production of testosterone by the testes. This makes both drugs, but for some reason bodybuilders continue to think that only good for Clomid testosterone stimulation. Read more
Studies conducted in the late ’70s in the University of Ghent in Belgium make clear the advantages of tamoxifen before Clomid to increase testosterone levels. Researchers looked at the effect of Nolvadex and Clomid on the endocrine system of healthy men, as well as those who have suffered from low sperm counts (oligospermia). It was also found that Nolvadex when used for 10 days at a dosage of 20mg per day increased testosterone levels in serum of 142% of the initial level that was comparable with the effect of 150mg Clomid per day over the same period of time (an increase in testosterone levels were slightly but not significantly greater with Clomid). We must remember that this is the effect of three 50mg tablets of Clomid. At about the same price 50mg Clomid and 20mg Nolvadex we can already see a difference in relation to the price / benefit result in Nolvadex.
Clomid acts on the estrogen receptors in the pituitary and ovaries. By linking estrogen receptors in the pituitary gland, Clomid breaks a negative feedback mechanism, ie. E. If the usual estrogen, acting on the pituitary gland, reduce the production of FSH and LH last one, when taking Clomid does not happen. Directly on blood levels of estrogen Clomid does not work.
Tamoxifen also has no effect on estrogen levels, ie. K. Mechanism of action reduces the blockade of various types of estrogen receptors, including the pituitary gland. Thus, we can talk about Clomid as selective (selective) blocker of estrogen receptors as well as of Nolvadex is not selective (non-selective). If Clomid selectively binds to the estrogen receptors, namely in the pituitary and testis, the Nolvadex associated with them throughout the body. In this case, Clomid acts as an estrogen antagonist and eliminates their inhibitory effect on the hypothalamus and pituitary gland, contributing to a more rapid recovery of their functions. Nolvadex by blocking the receptors in the body, also contributes to the fact that the body began to rebuild its own testosterone. Importantly, Nolvadex capable of blocking estrogen receptors in the pituitary less than Clomid. Details
The main differences of Tamoxifen and Clomid:
- In spite of the less impact on the pituitary gland, Nolvadex has the same ability to restore testosterone levels as Clomid
- Tamoxifen blocks the effects of estrogen in the body, including the pituitary and hypothalamus, which means that it will not only contribute to the restoration of testosterone secretion, but also prevent fluid retention in the body.
- Tamoxifen significantly cheaper than Clomid
- Tamoxifen has fewer side effects
- Tamoxifen reduces the level of cholesterol, which is important in the use of steroids (AAS during the course, the level of “bad” cholesterol increases)
- Clomid increases the level of globulin, which binds to testosterone, which adversely affects the set weight.
- tamoxifen has one serious side effect, which is absent in Clomid – a thrombophlebitis, risk voznikonveniya thrombus (blood-thinning leveled preparatmi)