Clomiphene has mainly antiestrogenic effects and some estrogenic effects. The mechanism in stimulating ovulation is unknown but is believed to be related to its antiestrogenic properties. By clomiphene competing with estrogen for binding sites at the hypothalamic level, the gonadotropins, follicle-stimulating hormone (FSH) and luteinizing hormone (LH), secretion is increased, which results in ovarian follicle maturation, followed by the preovulatory LH surge, ovulation, and the subsequent development of the corpus luteum. Usefulness in male infertility is also likely related to the increases in FSH and LH secretion.

Clomiphene citrate is chiefly indicated for the treatment of ovulatory failure in female patients who wish to become pregnant. This therapy will not be successful unless the patient though unovulatory, is capable of ovulation & her partner is fertile.

Clomiphene citrate is also indicated for the Polycystic ovary syndrome, Menorrhagia caused by hyperplastic endometrium, Amenorrhea with galactorrhea syndrome, Psychogenic amenorrhea syndrome, Secondary amenorrhea of unknown cause, Amenorrhea during post oral contraceptive period

The usual dose for the first course of Clomiphene is 50 mg (1 tablet) a day for 5 days in the early follicular phase of the cycle, following normal menstruation or a progestagen-induced withdrawal bleeding. Many regimes have been used, but most common begin either on day 2 or day 5. If this dose induces ovulation, there is no need to increase the dose in the following courses. If this dose induces ovulation, but pregnancy does not occur, stimulation with Clomiphene Citrate is to be continued, but up to 6 stimulative courses. If the first course does not induce ovulation, the second course should be started with 100 mg a day (2 tablets of 50 mg taken in a single dose) for 5 days. If ovulation is not induced, 2 more stimulative courses of the same dose should be given. If the next three stimulative courses do not produce a successful result, the therapeutic trial is considered to be finished. If ovulation is induced, but pregnancy does not occur, maximum 6 courses with Clomiphene are recommended. However, if menstrual bleeding does not occur, the patient should be examined carefully for the possible pregnancy, and the next course of therapy should be delayed until the correct diagnosis has been determined.

Clomiphene citrate is contraindicated during pregnancy, in patients with liver diseases, ovarian cysts, bleeding of undetermined origin, patients with neoplasm of endometrium.

Clomiphene Citrate is well tolerated. However a few side effects like dizziness, headache, nausea, vomiting, depression, fatigue, insomnia, vasomotor flushing, and allergic reaction may occur. Rarely ovarian enlargement and cyst formation may occur. All these effects disappear promptly after the treatment is discontinued.

Overdose Effects

No such effects of acute over dosage of Clomiphene citrate have been reported. However, in case of over dosage, a few sign symptoms of nausea, vomiting, vasomotor flushes, scotoma, and ovarian enlargement with pelvic or abdominal pain may occur. In the event of over dosage appropriate supportive measures should be employed.

Clomiphene citrate should be used with caution in longer maintenance therapy, with alcoholic drinks & antidepressants.

Pregnancy & Lactation

This is not recommended in pregnancy. In some cases Clomiphene citrate may reduce lactation, if it is administered to a woman during lactating period. So it should be avoided during lactational period.