Medication Description: Clomiphenicitrate (Clomiphen citras)
CLOMIFENZITRAT (Clomiphen citras). 1- [4- (2-Diethylaminoethoxy) phenyl] -1, 2-diphenyl-2-chloroethylene, citrate.
Synonyms: Klostilbegit, Ardomon, Chloramiphene, Clomid, Clomifeni citras, Clomivid, Clostilbergyt, Dyneric, Fertilin, Fertomid, Genozym, Gravosan, Nefimol, Omifin, Pergolime, Prolifen, Serofen, etc.
White or white with a creamy tinge crystalline powder, slightly soluble in water, moderately soluble in alcohol.
The drug is a mixture of the cis and trans forms of this compound; the cis isomer is more active, the content of which in the preparation is at least 50%.
The chemical structure is related to chlorotrienisene (see) - a drug with estrogenic activity, and tamoxifen (antiestrogenic drug).
Clomifentirate belongs to a group of drugs called antiestrogens. Drugs in this group specifically bind to estrogen-dependent receptors (estrogen receptors) in the hypothalamus and ovaries. In small doses, they enhance the secretion of gonadotropins (prolactin, follicle-stimulating and luteinizing hormones) and stimulate ovulation. With a low content of endogenous estrogens in the body, these drugs have a moderate estrogenic effect; however, with a high level of estrogens, they have an anti-estrogenic effect. By reducing the level of circulating estrogens (which inhibit the secretion of gonadotropic hormones in high concentrations), they increase the secretion of gonadotropins. In large doses, these drugs can inhibit the secretion of gonadotropins. They do not possess progestogenic and androgenic activity.
In connection with these properties, clomifencytrate in appropriate doses is used as a means of stimulating ovulation in anovulatory dysfunction of the ovaries and related infertility, as well as in dysfunctional uterine bleeding, dysgonadotropic forms of amenorrhea, and other types of pathology associated with endocrine ovulation disorders.
Clomifentirate is also used in breast cancer.
In connection with the stimulation of gonadotropin secretion, clomifentirate is also used for androgen deficiency, for oligospermia in men, and for delayed sexual and physical development in male adolescents.
Used to diagnose disorders of the gonadotropic function of the pituitary gland.
Clomifentirate can be used in combination with gonadotropic hormone preparations. It is well absorbed when taken orally and slowly excreted from the body; the half-life of the drug in the body is 5 - 7 days.
Take clomifentirate inside (regardless of the time of the meal).
To stimulate ovulation, a dose of 50 mg (0.05 g) is administered orally once a day (at bedtime), starting from the 5th day of the menstrual cycle, for 5 days.
Pre-determine the content of estrogen in the body. In the absence of an effect, the treatment is repeated, conducting 3–5 courses, while increasing the daily dose to 75–100 mg or increasing the duration of the course up to 10 days. The course dose of the drug should not be more than 500 mg.