CLOMIPHENE CITRATE

Clomiphene Citrate is medication used mainly in the treatment of infertility in women by safely increasing the quantity of hormones in charged of the growth and release of a fertilizable mature egg. It can also be used to treat irregular or absent menstrual periods in premenopausal women.

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What is Clomiphene

Clomiphene Citrate is a fertility agent that is used to induce ovulation in women who do not ovulate periodically and anovulatory women. This includes patients with a polycystic ovary syndrome. This medication is very effective in inducing ovulation in women who have ovaries that do not function normally, as long as they have an intact hypothalamic –pituitary-ovarian axis.


It is usually prescribed as a first line medication for women suffering from infertility because, apart from its low economic expenses, it induces ovulation in more than 80% of the chosen patients and roughly 40% of them become pregnant within the first six cycles of the treatment. Clomiphene should not be used to increase the rates of ovulation in women who ovulate normally and on a regular cycle. It can be used to increase the sperm count in male patients suffering from oligospermia.


Clomiphene was approved for clinical use by the FDA in 1976.


Clomiphene is classified as a selective estrogen receptor modulator because it has the ability to compete with estradiol for estrogen receptors at the hypothalamus levels. Clomiphene blocks a negative feedback of circulating estradiol in the hypothalamus, which prevents estrogen from reducing the output of the gonadotropin-releasing hormones. During a therapy with clomiphene, the amplitude, and frequency of the GNRH increases which stimulates the pituitary glands to secrete more follicle stimulating hormones and Luteinizing hormones. These hormones then stimulate the ovaries to develop oocyte follicles. Clomiphene may facilitate the development of multiple oocytes to maturity in some patients. The estrogen produced by these follicles leads to the thinning of the cervical mucus and the proliferation of the endometrium. As the levels of estradiol produced by the follicles rise, a positive feedback is facilitated which causes a surge of the LH and the FSH which is followed by the release of mature oocytes/ovulation. Once ovulation occurs, a corpus lutetium forms and the levels of progesterone rise just as they should in a normal ovulatory cycle. The traditional timing of administering this medication is from the follicular phase cycle of day 5 through day 9.


Clomiphene citrate is prescribed as an option for increasing a woman’s chances of getting pregnant by increasing her ability to produce mature eggs during a menstrual cycle. Its functions are to inhibit the effects of estrogen and to increase its production. In men, this drug can be used as a partial antiestrogen and it can also be used to counter the side effects of aromatizing steroids. These include excessive water retention and gynecomastia. As an antiestrogenic medication, it can be used to facilitate an increased production of the LH and the FSH, which in turn elevated the production of sperms and testosterone.

Benefits
  • Induces ovulation in anovulatory women.
  • Regulates periods
  • Improves sperm motility.
  • Increases testosterone.
  • Counteracts some side effects of steroid use in men.
Precautions when using Clomiphene Citrate

    Your health care provider should be informed if you are suffering from the following health conditions:


    • Blood clots, blood vessel disease, adrenal gland disease.
    • Liver disease, ovarian cysts, ovarian cancer.
    • Pituitary gland disease, endometriosis, vaginal bleeding that has not been diagnosed.
    • Allergic reactions to clomiphene, other medications, dyes, and preservatives.
    • Your healthcare provider should also know if you are pregnant or if you are breastfeeding.

    Clomiphene is only effective at inducing ovulation in women with a normal ovarian function and an intact hypothalamic-pituitary tract. Patients with any untreated pituitary conditions, primary ovarian failure, and thyroid diseases will not respond to treatment using this therapy. A reduced response to this therapy may occur in females with hirsutism, diabetes mellitus, obesity, hyperinsulinemia and lower levels of endogenous estrogens. In many cases, a combination of clomiphene and other drugs may be necessary to increase the chances of conception. Clomiphene is contraindicated in patients with a dysfunctional uterine and abnormal uterine bleeding which has not been diagnosed. Before its administration, all possibilities of ovarian carcinomas should be ruled out. This is mainly because clomiphene can stimulate the growth and development of tumors. Clomiphene should be used carefully in patients with fibroids and other associated conditions for the same reason.


    Clomiphene should be used cautiously in patients with psychosis and depression. There is a possibility that it can worsen these conditions. Depression is very common in women who are infertile because they lack some cycles where ovulation should occur.

Interactions

Letrozole/Tamoxifen should not be taken with anastrozole. Estrogen containing therapies should never be used with anastrozole as they diminish pharmacological action. Herbal supplements that have estrogen-like properties should also not be used in conjunction with anastrozole.

ADVERSE REACTIONS AND SIDE EFFECTS
  • Clomiphene is associated with increased rates of multiple births.
  • Hot flashes, mild pelvic discomfort, breast tenderness.
  • Dizziness, fatigue, headaches, nausea/vomiting.
  • Abnormal uterine bleeding, bowel pain, menstrual irregularities, diarrhea and weight gain.
  • Vaginal dryness, enlargement of the ovaries, ovarian hyperstimulation syndrome, and visual impairment.
  • Rash, dermatitis, alopecia, acne, Acne Vulgaris, allergic dermatitis and hypertrichosis.
  • Depression, anxiety, insomnia, restlessness, light-headedness, psychosis, emotional lability, and irritability.

This list may not contain all the possible side effects, so it is very important that you contact your health service provider immediately in case you experience any negative reactions that may include; skin rashes, swelling of the face, dizziness, blue tints on your skin, chest tightness, chest pains, itching and red painful swollen areas on your body.

Conclusions

Clomiphene Citrate is usually indicated for: Increasing the chances of pregnancy by helping women ovulate during their menstrual cycle, it can also Increase the production of testosterone in males by Inhibiting the effects of estrogen in them.



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