Clomiphene

Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.

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The active ingredient clomiphene is used to induce ovulation in women who want to have children. As a so-called selective estrogen receptor modulator, it acts at the natural docking points for the female hormones in the human body. Clomiphene can also be used in certain cases of missing menstrual bleeding. Here you can read everything interesting about the effect of clomiphene, side effects and use.

This is how clomiphene works

Hormonal regulation of the gonads

The function of the gonads in women (ovaries) and in men (testicles) are controlled by the so-called hypothalamus-pituitary-gonadal system. The hypothalamus is part of the diencephalon and an important control center in the endocrine system. Via the messenger substance GnRH (gonadotropin-releasing hormone), it stimulates the pituitary gland to release gonadotropins, i.e. the hormones LH (luteinizing hormone) and FSH (follicle-stimulating hormone). These reach the gonads with the blood and ensure their correct functioning: In women, the gonadotropins stimulate egg cell maturation in the ovaries, ovulation and the formation of the sex hormones estrogen and progestin. In men, the gonadotropins ensure the formation and maturation of sperm and the production of the male sex hormone testosterone.

Normally, the blood level of the sex hormones signals to the hypothalamus whether the hormone production is optimal, because the hormones bind to certain docking points (receptors) of the hypothalamus.

However, if the sex hormone level is too low because the gonads produce too few hormones, there is no positive feedback. The hypothalamus then activates the release of LH and FSH in the pituitary gland via an increased GnRH release - the gonads increase the production of sex hormones. In the opposite case - for example in doping, where sex hormones are supplied from the outside to stimulate muscle growth - the pituitary gland greatly reduces the release of gonadotropins in response to the increased levels in order to lower the body's own sex hormone production so that normal levels are restored.

Clomiphene corrects disorder

A disruption of this hormonal system in the area of ​​the hypothalamus and pituitary gland can lead, among other things, to a missed menstrual period and a lack of ovulation in women. Active substances such as clomiphene can then be administered: Clomiphene blocks the docking sites for sex hormones on the hypothalamus and pituitary gland without activating them. This simulates a deficiency in the body, even though there is a “normal” level of sex hormones. The hypothalamus reacts with increased GnRH release, the pituitary gland with increased LH and FSH release. The ovaries are therefore given the order to produce more sex hormones in order to remedy the deficiency that has been pretended to be. The increased estrogen levels achieved in this way lead to ovulation or the restart of the menstrual period.

In men, clomiphene is used for doping purposes without approval ("off-label") in order to maintain the body's own production of testosterone in the event of an external testosterone supply.

Clomiphene uptake, breakdown and excretion

The active ingredient clomiphene is quickly absorbed in the intestine after oral ingestion, with the highest blood levels four to seven hours after ingestion. The time until half of the active ingredient is excreted is very long at five days. The active ingredient is partly broken down in the liver, but leaves the body largely unchanged with the stool.

When is clomiphene used?

The active ingredient is used to treat women who are sterile due to the lack of ovulation. However, it must be clarified beforehand whether other causes in women or men are responsible for the infertility. Therapy can also be used in the absence of menstruation. In both cases, women can get pregnant with the help of clomiphene.

All applications in men take place without authorization.

This is how clomiphene is used

Therapy with clomiphene takes the form of cycles of five days each. If there was no menstruation for a long time prior to clomiphene therapy, therapy can be started at any time. If, on the other hand, the patient has regular menstrual periods (without ovulation), therapy should be started on or around the fifth day of the cycle.

In the first course of treatment, one tablet containing 50 milligrams of clomiphene is taken for five days. If ovulation was not triggered in the first cycle, another cycle is started 30 days later, but with 100 milligrams of clomiphene. A total of up to six such therapy cycles can be carried out.

What are the side effects of clomiphene?

Clomiphene intake causes ovarian enlargement, flushing (reddening of the face) and hot flashes in more than one in ten people treated. However, these clomiphene side effects are limited to the duration of use.

Side effects that occur in every tenth to hundredth woman are headache, visual disturbances, abdominal discomfort, flatulence, nausea, vomiting and a feeling of tightness in the chest.

What should be considered when taking clomiphene?

The use of clomiphene is only indicated in women of childbearing potential. This means that the active ingredient is not intended for men, children and adolescents as well as women during and after the menopause.

Furthermore, clomiphene should not be used by women with pre-existing liver disease or impaired liver function.

Interactions with other drugs are not yet known.

After successful fertilization, experts strongly advise discontinuing clomiphene. Experience shows that continuing to take the active ingredient could otherwise have a negative effect on the child.

How to get clomiphene medication

Therapy with clomiphene should only be carried out by an experienced doctor. The drug therefore requires a prescription and can only be purchased in pharmacies.

Since when is clomiphene known?

Clomiphene has been known since the 1960s and has been used medicinally ever since. At first, the active ingredient was only used for menstrual disorders. It was later discovered that it increases the pregnancy success rate. Since then, clomiphene has also been used to treat the absence of ovulation.

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