Mechanism of action
Anti-estrogen drug nonsteroidal structure. The mechanism of action is explained by the ability to specifically bind to estrogen receptors in the hypothalamus and ovaries. In small doses, the drug enhances the secretion of gonadotropic hormones (prolactin, follicle-stimulating and luteinizing hormones) and stimulates ovulation. Reducing the level of circulating estrogens (which inhibit the secretion of gonadotropic hormones in high concentrations), increases the secretion of gonadotropins.
After taking the drug inside clomiphene is well absorbed from the gastrointestinal tract.
Due to the strong binding to plasma proteins, the drug is slowly excreted from the plasma. Clomiphene and its metabolites undergo enterohepatic recirculation and accumulate in adipose tissue.
Clomiphene is metabolized to form metabolites with anti-estrogenic activity.
T1/2 Clomiphene is 5-7 days.
It is excreted unchanged and in the form of metabolites, mainly with feces (37-51%), usually within 3 weeks.
Indications and usage
- induction of ovulation in anovulatory dysfunction of the ovaries and related infertility;
- violation of ovulation with hypothalamus insufficiency;
- secondary amenorrhea of various genesis;
- dysfunctional uterine bleeding;
- galactorrhea of non-tumor origin;
- Stein-Leventhal syndrome;
- Chiari-Frommel syndrome;
Dose set individually in accordance with the reactivity of the ovaries of the patient. In case of cyclic bleeding, it is recommended to begin treatment on the 5th day of the cycle.
Scheme I: 50 mg / day for 5 days, during which the reaction of the ovaries should be monitored by clinical and laboratory studies. Ovulation usually occurs between 11 and 15 days of the cycle.
Scheme II should be used if Scheme I was unsuccessful. Assign 100 mg / day for 5 days, starting from the 5th day of the menstrual cycle. If this is not enough to induce ovulation, the same course (100 mg for 5 days) can be repeated in the next cycle.In case of continuing anovulation, after a 3-month break, 3 courses of treatment can be additionally performed in the same doses. If there is no effect after this, further treatment with Klostilbegit is not recommended. The total dose during 1 menstrual cycle should not exceed 750 mg.
At postcontraceptive amenorrhea the drug should be used at a dose of 50 mg / day daily, as a rule, when using Scheme I, a 5-day course of treatment is successful.
At oligospermia the drug should be used in a dose of 50 mg 1-2 times / day for 6 weeks under the systematic control of sperm.
From the side of the central nervous system: after use in high doses - dizziness, headache; possible depression, fatigue, anxiety, insomnia.
Gastrointestinal: after use in high doses - nausea, intermittent vomiting; possible pain in the epigastric region.
On the part of the endocrine system: there may be hot flushes similar to menopause symptoms; appearance of cystic enlargement of the ovaries (especially with Stein-Leventhal syndrome); rarely dysmenorrhea.
Dermatologic: With prolonged use, reversible hair loss is possible.
Metabolism: possible increase in body weight.
Allergic reactions: rarely - urticaria, allergic dermatitis.
Other: sensation of heat and visual disturbances (disappear after stopping treatment); rarely, chest pain, increased urination, and polyuria. In men, pain in the testicles is possible.
- abnormal liver function;
- ovarian cyst;
- Malignant neoplasms of the genital organs;
- Primary hypofunction of the pituitary gland;
- uterine bleeding of unknown origin;
- lactation (breastfeeding);
- hypersensitivity to the drug.
Pregnancy and breastfeeding
Klostilbegit strictly contraindicated during pregnancy and lactation (breastfeeding).
Before treatment, a thorough gynecological examination should be carried out. Treatment begins when the total content of gonadotropin in the urine is normal or below the normal level, the state of the ovaries on palpation is normal, the functions of the thyroid gland and the adrenal glands are well coordinated. In case of insufficiency of ovulation, prior to use of the drug, the scheme should exclude or cure all other possible forms of infertility.
If an ovarian increase or a cystic change occurs while taking the drug, treatment should be stopped until the size of the ovaries returns to normal. In the further treatment can be continued, but the drug should be prescribed in lower doses or reduce the period of treatment. During therapy in such patients, the condition of the ovaries should be monitored.
In order to prevent the development of deficiency in the function of the corpus luteum after treatment with Klostilbegit, it is recommended that prophylactic treatment with Progesterone be carried out after conception.
Klostilbegit used only with the constant supervision of a gynecologist.
As a result of treatment, multiple pregnancy may occur.
During treatment, it is recommended to monitor liver function.
Influence on ability to drive motor transport and control mechanisms
Since temporary visual impairment occurs at the beginning of treatment, it is not recommended to engage in driving vehicles and other potentially dangerous activities.
Symptoms: nausea, vomiting, hot flashes, blurred vision, abdominal pain.
Treatment: conduct symptomatic therapy.
Data on drug interactions drug Klostilbegit absent.
The drug should be stored at room temperature (15 ° to 25 ° C). Shelf life - 5 years.