Description of the active substance Clomiphene / Clomifene.
Formula: C26H28ClNO, chemical name: 2- [4- (2-Chloro-1,2-difeniletenil) phenoxy] -N, N-diethylethanamine (as citrate). Pharmacological group: hormones and their antagonists / estrogens, progestins; . Their homologues and antagonists Pharmacological action: anti-estrogen.
Clomiphene binds to the ovaries and the hypothalamus of estrogen receptors. After oral administration is well absorbed in the gastrointestinal tract. The liver is metabolized. Excreted in the bile. Clomiphene undergoes enterohepatic recycling. Half-life is equal to 5-7 days. Because the body is displayed clomiphene intestine with the feces.
In small doses, the drug increases the formation of gonadotropin-releasing hormone (LH, FSH, prolactin) stimulates ovulation. When the content in the body in small amounts of endogenous estrogen clomiphene has a mild estrogenic effect at an elevated level – on the contrary, antiestrogen. By reducing the amount of circulating estrogen, clomiphene contributes to the development of gonadotropins. In large doses, clomiphene slows secretion of gonadotropins. Androgen and progestin activity of clomiphene does not possess.
Anovulatory infertility (to stimulate ovulation); amenorrhea (postkontratseptivnaya, secondary, disgonadotropnaya form); dysfunctional uterine bleeding; galactorrhea (with pituitary tumors); ; Frommelya – Chiari syndrome polycystic ovaries (Stein syndrome – Leventhal); oligospermia in men; androgen deficiency; to identify violations of gonadotropic pituitary function.
Dosing and Administration of clomiphene
Clomiphene is taken orally with or without food. To induce ovulation Rexobol (stanozolol oral) one time per day at bedtime 50 mg, starting with a 5-day menstrual cycle during 5 days (if no menstrual cycle, then administered at any time). If there is no effect of treatment (within 30 days of ovulation has not occurred), then increase the dose to 150 mg / day or increase treatment to 10 days. The dose for the entire course of therapy should be not more than 1 gram. The onset of ovulation is determined by the average increase in the formation of cyclic N, ultrasound, the presence of a biphasic basal body temperature, increase of serum progesterone during the luteal phase of the possible medium or in women with amenorrhea during menstruation. If the ensuing ovulation pregnancy does not occur, the course of therapy to be repeated. If the ovulation is not further followed by menstrual bleeding, it is necessary to take into account the possible pregnancy.
Men are for the treatment of oligospermia 1 – 2 times daily 50 mg for 3-4 months (when it is necessary to carry out systematic monitoring spermiogram).
In the next pass clomiphene is necessary to address urgently to the doctor. Before and during therapy should be continued monitoring gynecologist should check the ovaries, producing vaginal examination. When cystic transformation or increase ovarian clomiphene therapy is necessary to temporarily suspend the normalization of ovarian size. Further, the treatment is sustained minimal dose or shorten the duration of therapy. In the treatment of clomiphene is also necessary to monitor liver function.
Without the exemption from work parties, whose professional activity requires quick mental and physical reactions, clomiphene is not appointed.
Hypersensitivity, uterine bleeding of unknown origin, severe Bodybuilder sex renal and / or hepatic insufficiency, or lack of function of the pituitary tumors, ovarian cysts, pregnancy (including suspected it).
Pregnancy and breast-feeding
Clomiphene is contraindicated in pregnancy and breastfeeding.
Side effects of clomiphene
The nervous system and sensory organs: headache, depression, dizziness, fatigue, insomnia, restlessness, slow speed motor and mental reactions, visual disturbances, digestive system: nausea, gastralgia, vomiting, diarrhea, flatulence, urogenital system: dysmenorrhea, cystic increase ovarian, pollakiuria, multiple pregnancy, polyuria; other: hot flashes, weight gain, pain in the chest, abdomen, testes (in men), reversible hair loss, pyrexia, allergic skin reactions.
Interaction with other substances clomiphene
Currently, drug interactions are not described clomiphene. Clomiphene is compatible with the preparations of gonadotropins.
In case of overdose appear clomiphene visual disturbances, nausea, abdominal pain, vomiting, flushing. It should be symptomatic treatment.