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Clomiphene citrate

Generic Name: clomiphene citrate
Clomiphene Citrate is typically prescribed for women to aid in ovulation. In men, the application of Clomid causes an elevation of follicle stimulating hormone and luteinizing hormone. As a result, natural testosterone production is also increased.

This effect is obviously beneficial to the athlete, especially at the conclusion of a steroid cycle when endogenous testosterone levels are subnormal. When an athlete discontinues the use of steroids, his testosterone levels will most likely be suppressed. If endogenous testosterone levels are not brought to normal, a dramatic loss in size and strength may occur. Clomid plays a crucial role in preventing this crash in athletic performance.

Bodybuilders find that a daily intake of 50-100 mg of clomiphene citrate over a two week period will bring endogenous testosterone production back to an acceptable level. Clomid will gradually raise testosterone levels over its period of intake. Since an immediate boost in testosterone is often desirable, athlete will commonly use HCG (human choronic gonadotropin) for a couple of weeks, and the continue treatment with Clomid.

Clomid is also effective as an anti-estrogen. Most athletes will suffer from an elevated estrogen level at the conclusion of a cycle. A high estrogen level combined with a low testosterone level puts an athlete in serious risk of developing gynocomastia. With the intake of Clomid, the athlete gets the dual effect of blocking out some of the effects of estrogen, while also increasing endogenous testosterone production.



Clomiphene Citrate (Clomid®)

Description :
by Bill Roberts - Clomid is the anti-estrogen of choice for improving recovery of natural testosterone production after a cycle, improving testosterone production of endurance athletes, and is also effective in reducing risk of gynecomastia during a cycle employing aromatizable steroids.

While it has been claimed that Clomid "stimulates" production of LH and therefore of testosterone, in fact Clomid's activity is achieved not by stimulation of the hypothalamus and pituitary, but by blocking their inhibition by estrogen.

Clomid is a mixed estrogen agonist/antagonist (activator/blocker) which, when bound to the estrogen receptor, puts it in a somewhat different conformation (shape) than does estradiol. The estrogen receptor requires binding of an estrogen or drug at its binding site and also the binding of any of several cofactors at different sites. Without the binding of the cofactor, the estrogen receptor is inactive. Different tissues use different cofactors. Some of these cofactors are able to bind to the estrogen receptor/Clomid complex, but others are blocked due to the change in shape. The result is that in some tissues Clomid acts as an antagonist -- the cofactor used in that tissue cannot bind and so the receptor remains inactive -- and in others Clomid acts as an agonist (activator), because the cofactors used in that tissue are able to bind.

Clomid is an effective antagonist in the hypothalamus and in breast tissue. It is an effective agonist in bone tissue, and for improving blood cholesterol.

Clomid also has the property of reducing the adverse effect of exercise-induced damage of muscle tissue. This is very significant for endurance athletes but is not very significant, if at all significant, with reasonable weight training. Clomid does not perceptibly affect gains of the weight trainer either favorably or adversely in my experience.

The drug seems to have estrogenic effects on mood, which can be beneficial (improving relationships with women by improving empathy) or can yield depression or PMS-like symptoms, but for most users there is no significant effect either way.

The claim that duration of intake should not exceed 10-14 days is incorrect. Clinical studies with male patients have been for periods of a year or longer. This error probably originates from the fact that, for use in women, due to the menstrual cycle there would obviously be no point in trying to stimulate ovulation all four weeks of the month. Thus, use in women is limited to 10-14 days. That limitation is not because of toxicity.

Clomid is in fact useful throughout a cycle if aromatizable drugs are being used. I do think however that to be conservative, one should use it no more than 2/3 of the time throughout the year or a little less.



Common uses and directions for Clomid

Clomid is indicated for the treatment of ovulatory dysfunction in women desiring pregnancy. Impediments to achieving pregnancy must be excluded or adequately treated before beginning Clomid therapy.

The workup and treatment of candidates for Clomid therapy should be supervised by physicians experienced in management of gynecolic or endocrine disorders. Patients should be chosen for therapy with Clomid only after careful diagnostic evaluation.

Treatment of the selected patient should begin with a low dose, 50 mg. daily for 5 days. The dose should be increased only in those patients who do not ovulate in response to cyclic 50 mg. Clomid tablets.

Clomid, at recommended dosages, is generally well tolerated. Adverse reactions are usually mild and transient and most disappear promptly after treatment is discontinued.

Male athletes also find Clomid interesting. In men using Clomid, the elevation in both follicle stimulating hormone and (primarily) luteinizing hormone will cause natural testosterone production to increase. This effect is especially beneficial to the athlete at the conclusion of a steroid cycle when endogenous testosterone levels are depressed. If endogenous testosterone levels are not brought beck to normal, a dramatic loss in size and strength is likely to occur once the anabolics have been removed. Clomid can play a crucial role in preventing this crash in athletic performance.

More information about Clomid (Clomiphene citrate):


Clomid (Clomiphene citrate) additional information

Common uses
Clomid tablets, containing clomiphene citrate, is a non steroidal ovulatory stimulant.

Clomid is indicated for the treatment of ovulatory dysfunction in women desiring pregnancy.

Male athletes also find Clomid interesting. In men using Clomid, the elevation in both follicle stimulating hormone and (primarily) luteinizing hormone will cause natural testosterone production to increase. This effect is especially beneficial to the athlete at the conclusion of a steroid cycle when endogenous testosterone levels are depressed. If endogenous testosterone levels are not brought beck to normal, a dramatic loss in size and strength is likely to occur once the anabolics have been removed. Clomid can play a crucial role in preventing this crash in athletic performance.

Directions

Clomid comes as a tablet containing 50 mg. clomiphene citrate, to take by mouth. Impediments to achieving pregnancy must be excluded or adequately treated before beginning Clomid therapy.

The workup and treatment of candidates for Clomid therapy should be supervised by physicians experienced in management of gynecolic or endocrine disorders. Patients should be chosen for therapy with Clomid only after careful diagnostic evaluation.

Treatment of the selected patient should begin with a low dose, 50 mg. daily for 5 days. The dose should be increased only in those patients who do not ovulate in response to cyclic 50 mg. Clomid tablets.

For athletes using anabolic steroids, Clomid can normalize the testosterone level and the spermatogenesis (sperm development)within 10-14 days. For this reason Clomid is primarily taken after steroids are discontinued. At this time it is extremely important to bring the testosterone production to a normal level as quickly as possible so that the loss of strength and muscle mass is minimized.

50-100 mg./day seems is a sufficient dosage for athletes. Clomid is usually taken with fluids after meals. If several tablets are taken it is recomended that they be administered in equal doses distributed throughout the day. The duration of Clomid intake should not exceed 10 to 14 days. Most athlets begin with 100 mg./day taking one 50 mg. tablet every morning and evening after meals. After the fifth day the dosage is often reduced to only one 50 mg. tablet per day.

If you miss a dose, take it as soon as remembered if it is within an hour or so. If you do not remember until later, skip the missed dose and resume your usual dosing schedule. Do not "double-up" the dose to catch up.

Precautions

Blurring or other visual symptoms such as spots or flashes may occasionally occur during therapy with Clomid. These visual symptoms increase in incidence with increasing total dose or therapy duration and generally disappear within a few days or weeks after Clomid is discontinued. These visual symptoms may render such activites as driving a car or operating machinery more hazardous than usual, particularly under conditions of variable lighting.
If experiencing visual symptom, treatment should be discontinued and complete ophthalmologic evaluation performed.
There is an increased chance of multiple pregnancy, including bilateral tubal pregnancy and coexisting tubal and intrauterine pregnancy, when conception occurs in relation to Clomid therapy.
It is not known whether Clomid is excreted in human milk. Caution should be exercised if Clomid is administered to a nursing woman. In some individuals, Clomid may reduce lactation.
Prolonged use of Clomid may increase the risk of a borderline or invasive ovarian tumor.

Possible side effects

Clomid at recommended dosages, is generally well tolerated. Adverse reactions usually have been mild and transient and most have disappeared promptly after treatment has been discontinued.

Side effects include ovarian enlargement, vasomotor flushes, abdominal-pelvic discomfort/distention/bloating, nausea and vomiting, breast discomfort, visual symptoms, headache and abnormal uterine bleeding. If you notice other effects not listed above, contact your doctor.

Overdose

If overdose of Clomid is suspected, contact your local poison control center or emergency room immediately. Toxic effects accompanying acute overdosage of Clomid have not been reported. Signs and symptoms of overdosage as a result of the use of more than the recommended dose during Clomid therapy include nausea, vomiting, vasomotor flushes, visual blurring, spots or flashes, scotomata, ovarian enlargement with pelvic or abdominal pain.

Additional information

Keep Clomid in a tightly closed container and out of reach of children. Store Clomid at room temperature and away from excess heat and moisture (not in the bathroom).

Note

The above information is intended to supplement, not substitute for, the expertise and judgment of your physician, or other healthcare professional. It should not be construed to indicate that use of Clomid is safe, appropriate, or effective for you. Consult your healthcare professional before using Clomid.







Alternative Description :

clomifene citrate (clomifene, clomid)

In this article



What is clomifene citrate?

Clomifene citrate is a drug treatment that stimulates your ovaries to release eggs.

Ovulation stimulation using clomifene citrate is a well-established, effective treatment (Brown et al 2009). Clomifene citrate is the most widely used of all fertility drugs.

Other drugs that may be used to treat ovulation disorders include metformin and bromocriptine.



What's the success rate of clomifene citrate?

About 70 per cent of women will ovulate in response to a fairly low dose of clomifene citrate (Homburg 2005). Of those who ovulate, about 40 per cent will become pregnant (Homburg 2005).




Other factors that can affect the pregnancy rate include:

A low dose of clomifene may not be enough. Your doctor may increase the dose to help you conceive. Studies suggest that about 29 per cent of women who start taking the drug go on to have a live birth (NCCWCH 2013:147-8).



Is clomifene citrate right for me?

Clomifene citrate is a recommended treatment for ovulation disorders caused by problems such as polycystic ovaries or polycystic ovary syndrome (NCCWCH 2013:18). It may be used on its own or in combination with another drug called metformin, which you take daily in several doses (NCCWCH 2013:147-8).

It used to be used in some cases of unexplained infertility. However, it's no longer recommended for this, as there's a lack of evidence that it makes any difference compared to trying to get pregnant naturally (Hughes et al 2010, NCCWCH 2013:18).

Clomifene citrate may also be used in cases of unexplained infertility (NCCWCH 2004: 58), although there's a lack of evidence that it really helps (Hughes et al 2010).

You might be prescribed clomifene citrate before you undergo a fertility treatment such as intrauterine insemination (IUI), to boost your egg production (HFEA 2009a).



How does clomifene citrate work?

Clomifene citrate blocks the effect of the hormone oestrogen in your body. This blocking effect tricks your body into bumping up levels of two other hormones that are essential for ovulation. These two other hormones are:

FSH causes the eggs in your ovaries to ripen, ready for release. LH triggers the release of one or more mature eggs from the ovary follicles. The egg or eggs then move down into one of your fallopian tubes.



How long will I have to take clomifene citrate for?

You usually take clomifene in pill form for five days early in your cycle, for up to six months at a time (NCCWCH 2013:142,179). A low dose of 50 mg is often used to start with.

If you have regular cycles, you'll start taking the pills within five days of your period starting, preferably on about day two.

If you're not menstruating at all or if your cycle is very irregular, your doctor will check that you're not pregnant. She'll then give you a synthetic version of the hormone progesterone, a progestogen called Provera.

Progesterone works with oestrogen to keep your reproductive cycle regular. Provera will re-establish your periods. Once you're having periods, you can then start taking clomifene citrate (BNF 2011).

Ovulation generally occurs between five days and nine days after you've taken your last pill. Your fertility specialist may monitor your ovaries using ultrasound, at least during the first cycle (NCCWCH 2013: 180). She'll look to see how your ovaries are responding and whether one egg follicle or more is preparing to release a mature egg into one of your fallopian tubes.

You might ovulate and conceive in the first month of taking clomifene citrate. Or it can take a month or two of drug therapy for you to start ovulating regularly.

Treatment may be continued for up to six cycles, as this is thought to be long enough to see whether your body is responding to the drug (NCCWCH 2013:179-80).

Unfortunately, some women don't respond to clomifene citrate at all. If you don't ovulate on low dose clomifene, your doctor may suggest increasing the dose over the next two months (NCCWCH 2013:142, 178). If you're still not ovulating at doses of 100 to 150 mg a day, then you'll be termed "clomifene resistant" (NCCWCH 2013:142). This can usually be identified within three monitored cycles, so ask your doctor what other drug or surgical options may be open to you.



Does clomifene citrate have any side-effects?

Clomifene citrate can cause a wide range of minor side-effects, including:

Clomifene citrate can also cause your cervical mucus to become drier, so you may want to use a sperm-friendly vaginal lubricant.

Ovarian hyperstimulation syndrome (OHSS) is another potential side-effect of clomifene citrate (BNF 2011). OHSS occurs when you respond too well to fertility drugs and your ovaries become very swollen. Watch out for your tummy swelling up, giving you a full, bloated feeling.

OHSS can develop into a serious condition. However, most cases of OHSS in response to clomifene citrate are mild and are resolved after a few days (Homburg 2005).

Human chorionic gonadotrophin (hCG) is the main fertility drug thought to be responsible for severe cases of OHSS. This means that your chances of getting severe OHSS are increased if you're taking clomifene citrate with hCG. If you do develop severe OHSS, your doctor will monitor you closely (Balen 2008).



I have polycystic ovary syndrome. Will clomifene citrate work for me?

If you have polycystic ovary syndrome (PCOS), there is a chance that clomifene citrate won't work for you. About 30 per cent of women with PCOS are resistant to clomifene citrate (Homburg 2005). This is more common if you have a body mass index (BMI) greater than 25.

If that's the case, your doctor may recommend that you try to lose some weight before you even start taking clomifene (NCCWCH 2013:180). Getting nearer to your ideal weight may be just enough for you to start ovulating regularly.

Your doctor may prescribe medication to help your body to respond to clomifene citrate. The medication is an insulin-sensitising drug called metformin. Metformin can help you respond to clomifene citrate and has been shown to increase your chances of ovulation and pregnancy (NCCWCH 2013:180, Tang et al 2012).



Is there anything else I should know about clomifene citrate?

There is a theory that clomifene citrate's anti-oestrogen effect may increase the risk of miscarriage. It's estimated that about one in five pregnancies conceived after treatment with clomifene citrate miscarry (Homburg 2005, NCCWCH 2013:149-58). However, this is a similar rate to that found in couples who haven't had any fertility treatment.

There's been some ongoing concern that using clomifene citrate may be linked with ovarian cancer. However, reviews of the evidence haven't supported this (NCCWCH 2013:424-5). Findings suggest that it's the fertility problem itself that may increase the risk, rather than the drugs used to treat it.

Drugs that stimulate ovulation can result in more than one egg being released. This increases your chance of multiple pregnancy, which is why ultrasound monitoring is recommended to check how strongly your ovaries respond to the drug (NCCWCH 2013:142). If you take clomifene citrate, you have about a one in 10 chance of a multiple pregnancy, most likely twins (Homburg 2005, NCCWCH 2013:142).

Want to talk with others about taking fertility drugs? Go to BabyCentre's community.

Last reviewed: May 2013



References

Balen A. 2008. Ovarian hyperstimulation syndrome (OHSS): a short report for the HFEA. www.hfea.gov.uk [pdf file, accessed May 2013]

BNF. 2011. Clomifene citrate. British National Formulary. www.bnf.org [Accessed May 2013]

Brown J, Farquhar C, Beck J, et al. 2009. Clomiphene and anti-oestrogens for ovulation induction in PCOS. Cochrane Database of Systematic Reviews. (4): CD002249. onlinelibrary.wiley.com [pdf file, accessed May 2013]

Homburg R. 2005. Clomiphene citrate - end of an era? A mini review. Hum Reprod. 20(8): 2043-51. humrep.oxfordjournals.org [pdf file, accessed May 2013]

Hughes E, Brown J, Collins JJ, et al. 2010. Clomiphene citrate for unexplained subfertility in women. Cochrane Database of Systematic Reviews (1): CD000057. onlinelibrary.wiley.com [pdf file, accessed May 2013]

NCCWCH. 2013. Fertility: assessment and treatment for people with fertility problems. National Collaborating Centre for Women's and Children's Health, NICE Clinical Guideline. London: RCOG Press. guidance.nice.org.uk [pdf file, accessed April 2013]

NHS Choices. 2011. IVF. NHS Choices Health A-Z. www.nhs.uk [Accessed April 2013]

Tang T, Lord JM, Norman RJ, et al. 2012. Insulin-sensitising drugs (metformin, rosiglitazone, pioglitazone, D-chiro-inositol) for women with polycystic ovary syndrome, oligo amenorrhoea and subfertility. Cochrane Database of Systematic Reviews (5): CD003053 onlinelibrary.wiley.com [pdf file, accessed April 2013]







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