The Chemistry and Usage of Clomid or Clomiphene Citrate
Clomid is a derivative of diphenyl ethylene stilbene and depending on its target tissues, it functions either as an estrogen agonist or an estrogen antagonist. Essentially, Clomiphene Citrate, Clomid is a Selective Estrogen Receptor Modulator (SERM). SERMs in their own right are anti-estrogens, substances which inhibit the production, use, or effects of estrogens.
While Clomid is the trademark name used in common practice, the International Nonproprietary Name given to the compound is Clomifene. The United States Adopted Name calls it Clomiphene. Clomid is also popularly known by the trade names, Androxal and Omifin.
A brief history of Clomid and its use as a fertility drug
Clomid has been in medical use since the late 1960s. It was primarily used in the treatment of Oligomenorrhea in women. When medical practitioners realized that women who were being treated for the disease with Clomid showed pregnancy rates higher than the normal average, the drug’s fertility uses became clearer.
Soon, Clomid began to be used to treat anovulation and female fertility problems. By the early 1970s, Clomid’s use as a female fertility drug gained immense popularity and its use quickly spread across the world.
Today, Clomid is available in the market in the form of round tablets, white in color and 50 milligrams in strength. It is easily the most popular female fertility drug. Clomid is also widely used off-label in similar treatment of males. The drug enjoys huge popularity with both medical professionals and individuals using anabolic steroids – athletes and body builders. It is sold in the majority of countries and regions under a multitude of brand names and for different uses. Apart from its effectiveness as a female fertility drug, the cheap cost and ready availability of Clomid worldwide have made it a popular off-label drug for men too.
The chemistry of Clomid
Clomid, as Clomiphene Citrate, has the chemical formula of C26H28ClNO. It belongs to the triphenylethylene group and shares closely related properties with Nolvadex, another compound from the triphenylethylene group. Clomid is composed of two cis-trans isomers viz. E-clomiphene and Z-clomiphene.
The working mechanism of Clomid
As a Selective Estrogen Receptor Modulator, Clomid alters the effects of estrogen in the human body. It forms one of the two categories of anti-estrogens, the other category being aromatase inhibitor (AI).
One rumor which has been doing its rounds in the medical and body-building community is that on account of being a Selective Estrogen Receptor Modulator, Clomid is essentially an anti-estrogen; it reduces estrogen levels in the blood.
This is, however, not the truth. Clomids do not reduce estrogen levels in blood; they only alter its effects. The lowering of estrogen levels is done by the second category of anti-estrogens, the aromatase inhibitors (AI).
SERMs, including Clomid, only impede estrogen’s action in breast tissue. They prevent estrogens from binding at receptor sites by occupying the sites themselves. Estrogens are unable to break the strong bond with which Clomid binds to the receptor sites. This prevents estrogens from working their effects on the breast tissue. Gynecomastia does not formulate at the receptor cells since estrogens are not attached to the receptor sites and cannot trigger gene transcription in those cells. Clomid also forcibly occupies the receptor sites already taken up by estrogens, causing the same end result – inhibition of estrogen’s action on the breast tissue.
Aromatase Inhibitors on the other hand lower estrogen levels in two ways – they inhibit the production of estrogen and they paralyze the aromatase enzyme which inhibits androgen’s conversion into estrogen.
As a Selective Estrogen Receptor Modulator, Clomid restricts negative feedback inside the brain’s hypothalamus. This boosts the production of gonadotropins by the body. The antagonistic effects include inhibition or complete blockage of estrogen’s effects on the different tissues and parts of the body – the hypothalamus, endometrium, the pituitary glands as well as the ovaries, vagina, and cervix. On account of being a SERM, Clomid also functions as an estrogen agonist in certain tissues of the body, like the liver. Instead of inhibiting the action of estrogens here, it itself functions as an estrogen.
Comparison of Clomid with Nolvadex
Nolvadex is another popular drug from the Selective Estrogen Receptor Modulator category. Clomid is often compared to Nolvadex because of the operational and functional similarities that exist between the two. Since both belong to the SERM category, they share common antagonist and agonist effects on body tissues.
Both Nolvadex and Clomid either inhibit or entirely block estrogen’s effect on various parts of the body, like the hypothalamus, ovaries, and pituitary gland as mentioned earlier.
Similarly, both act as estrogen agonist in the liver. Rather than inhibiting the action of estrogens in the liver, they themselves function as estrogens. This results in Clomid and Nolvadex depicting a positive impact on blood cholesterol levels in the body.
One important point of difference between the two is their efficiency as estrogen antagonists. While both show basic antagonist effects, Nolvadex is more efficient than Clomid. Clomid’s action in inhibiting the effects of estrogen on breast tissues is mild, so to block estrogen’s effect, Nolvadex is preferred.
Use of Clomid as a female fertility drug
Earlier, when Clomid was being used for the treatment of Oligomenorrhea in women, it was noticed that women treated with Clomid showed higher pregnancy rates. This is because it stimulates the hypothalamus to release hormones which are necessary for ovulation in women, also known as the gonadotropins.
This estrogen antagonistic action of Clomid on the hypothalamus triggers the release of two signaling hormones (or the gonadotropins) in both men and women. The gonadotropins consist of the Luteinizing Hormone (LH) and the Follicle Stimulating Hormone (FSH). They are known as signaling hormones because in men, these hormones signal the testicles, either to start or to increase the production of Testosterones – a process which is known as the Hypothalamic Pituitary Testicular Axis.
With the release of the FSH and LH in women, the follicle in the ovary begins to develop and mature. In due course of time, it leads to ovulation. Next, the corpus luteum is developed, which results in women being able to successfully achieve pregnancy.
The FSH and LH are released in any of the following two ways: one is when the hypothalamic and pituitary axis gets stimulated directly. The other instance is when the hypothalamic and pituitary axis registers a reduced influence of the inhibitory estrogens. This happens when estrogens have to compete with endogenous estrogens in the pituitary, the hypothalamus, or the uterus.
They are used in cases of reduced and insufficient hormonal stimulation in women whose ovaries can produce follicle but cannot ovulate due to insufficient hormonal stimulation. Clomid, in its citrate form, is used to cause ovulation. Clomid is also used in the hyperstimulation of the ovary, typically in the in vitro fertilization process.
Common side effects associated with the use of Clomid
The steroid side effects related to the use of Clomid typically occur in less than one percent of the total number of patients it is administered to. Some of the most common signs that your body is reacting adversely to the drug include hot flashes, blurring of the vision, discomfort and pain in the abdomen, cyst formation or enlargement of the ovarian region, which is reversible.
In some rare cases, individuals on Clomid may also experience unnatural bleeding from the uterus, nausea, or vomiting. These adverse effects can be seen in only about 0.1 to 1 percent of the total patients. Even fewer, less than 0.1 percent of the total patients may experience alopecia or hyperstimulation syndrome in the ovary.
The dose of Clomid, which may turn toxic for humans, is not exactly known. There have been cases of severe overdosage with Clomid, but even for acute cases, no toxic effects have been reported. However, when suspected over dosage happens or any of the following systems come up after the use of Clomid in doses exceeding the recommended size, immediate medical attention must be administered. The identifying signs and symptoms are changes in vision, particularly blurring, flashes and spots, vasomotor flushes, nausea or vomiting, and any enlargement in the ovarian or pelvic region accompanied by abdominal pain.
Off-label uses of Clomid for body builders and athletes
Clomid can help body builders and athletes suffering from gynecomastia, the side effect that most males face when using steroids which are aromatizable and anabolic.
Gynecomastia is the condition when use of steroids like Boldenone results in the enlargement of male breast tissue because of the excessive action of estrogens. Since Clomid inhibits the action of estrogen on breast tissue, it is widely used by male athletes and body builders to keep gynecomastia at bay.
Individuals who administer anabolic steroids can find great relief with Clomid during the Post Cycle Therapy. Increased testosterone production in men helps restore normal hormonal function after the end of the anabolic steroid cycle.
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