Pharmacological action

Pharmacological action - antiestrogenic.

Pharmacodynamics

An antiestrogen of non-steroidal structure, the action of which is due to specific binding to estrogen receptors of the ovaries and pituitary gland. In small doses, it enhances the secretion of gonadotropins: prolactin, FSH and LH. Stimulates ovulation. With a low content of estrogenic hormones in the body, it exhibits a moderate estrogenic effect. With a high content of estrogen, it has an antiestrogenic effect. In large doses, it inhibits the secretion of gonadotropins. Does not possess gestagenic and androgenic activity.

Pharmacokinetics

When taken orally, it is well absorbed from the gastrointestinal tract. Metabolized in the liver. Undergoes enterohepatic recirculation. T1/2 - 5-7 days. It is excreted mainly with bile.

Indications of the drug Clomiphene

• anovulatory infertility (induction of ovulation);
• dysfunctional metrorrhagia;
• amenorrhea (disgonadotropic form); secondary amenorrhea; post-contraceptive amenorrhea;
• galactorrhea (against the background of a pituitary tumor);
• polycystic ovary syndrome (Stein-Leventhal syndrome);
• Chiari-Frommel syndrome;
• androgen deficiency;
• oligospermia;
• diagnosis of violations of the gonadotropic function of the pituitary gland.

Dosing and Administration

Inside.

To stimulate ovulation , 50 mg is prescribed 1 time per day before bedtime, starting from the 5th day of the menstrual cycle, for 5 days (in the absence of a cycle, at any time). In the absence of effect (ovulation does not develop within 30 days), the dose is increased to 150 mg / day or the course is lengthened to 10 days. The course dose should not exceed 1 g. The development of ovulation is determined by the presence of a biphasic basal temperature, an average cyclical increase in LH production, an increase in serum progesterone during the likely middle phase of luteinization or during menstrual bleeding in women with amenorrhea. If ovulation occurs, but there is no pregnancy, then the same dose should be repeated at the next treatment course. If, after a likely ovulation, menstrual bleeding did not follow, the possibility of pregnancy should be taken into account, and this possibility must be excluded before a new course of treatment.

Men are prescribed 50 mg 1-2 times a day for 3-4 months (systematic monitoring of spermogram is required).

Overdose

Symptoms: nausea, vomiting, flushing, blurred vision.

Treatment: drug withdrawal (overdose symptoms go away on their own).

Special instructions

Increases the likelihood of developing multiple pregnancies.

The drug is effective when the level of endogenous estrogens is sufficient, less effective when the level of estrogen is low and practically ineffective when the concentration of pituitary gonadotropic hormones is low. In the course of treatment, it is necessary to constantly monitor the gynecologist, control the function of the ovaries, vaginal examinations, observe the phenomenon of the "pupil".

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Side effects

From the nervous system: dizziness, headache, drowsiness, slowing down of the speed of mental and motor reactions, depression, hyperexcitability, insomnia.

From the digestive system: nausea, vomiting, gastralgia, flatulence, diarrhea.

Allergic reactions: rarely - rash, allergic dermatitis, vasomotor disorders.

From the genitourinary system: rarely - polyuria, increased urination, lower abdominal pain, dysmenorrhea, menorrhagia, an increase in the size of the ovary (including cystic).

Others: weight gain, flushing of the face, rarely - decreased visual acuity, alopecia, soreness in the breast area.

The appearance of signs of ovarian hyperstimulation and general side effects requires dose reduction or drug withdrawal.