Clomiphene citrate, its chemical name is: N,N-diethyl-2-[4-(1,2-diphenyl-2-chlorovinyl)-phenoxy]ethylamine cis-trans-iso Citrate of a mixture of structures. Clomiphene citrate (Clomiphene citrate, CC) is the first-line drug for ovulation stimulation in patients with PCOS so far. Because of its weak estrogenic effect, it is a non-steroidal anti-estrogen preparation that can competitively bind to hypothalamic cells. The estrogen receptor reduces the negative feedback of estrogen to the hypothalamus, which stimulates the release of hypothalamic GnRH, promotes the increase of FSH and LH levels, and promotes follicular development.

Application

Clomiphene citrate is a non-steroidal anti-estrogen drug, the first choice for the treatment of ovulatory infertility, and it is currently recognized as an effective ovulation-inducing drug at home and abroad. Its structure is similar to diethylstilbestrol and tamoxifen, and it has an anti-estrogen effect. It competes with endogenous estradiol for estrogen receptors in the hypothalamus, blocks the negative feedback effect on the hypothalamus, increases the secretion of gonadotropin releasing hormone, and makes the pituitary gland secrete FSH and LH to promote follicular development the goal of.

Clomiphene citrate is mainly used to treat: (1) treatment of anovulatory female infertility, suitable for those with a certain level of estrogen in the body; (2) treatment of insufficient corpus luteum function; (3) testing of ovarian function; (4) ) To detect the abnormal function of the male hypothalamic pituitary gland axis; (5) To treat male infertility due to oligospermia.

Pharmacological action

 This product is an anti-estrogen drug with weak estrogenic activity. When the product is used in a small dose, it can stimulate the pituitary to secrete gonadotropins and induce ovulation; when used in a large dose, the product will have the effect of inhibiting the secretion of gonadotropins by the pituitary. This product can also promote sperm maturation.

Pharmacokinetics

After oral administration, it is absorbed through the intestine and enters the hepatic blood circulation. Tl/2 is generally 5 to 7 days. This product is metabolized in the liver. It enters the intestines with bile, then is eliminated from the feces, and part of it is re-absorbed through the hepato-intestinal circulation. Half of it is excreted from the feces within 5 days. It can still be detected in feces within 6 weeks.

Adverse reactions

(1) Swelling, stomach pain, pelvic or lower abdominal pain (cyst formation) are common.

(2) Blurred vision, double vision, flashes in front of eyes, sensitivity to light, vision loss, yellowish skin and sclera are rare.

(3) Pay attention when the following reactions persist: hot flashes, breast discomfort, constipation or diarrhea, dizziness or dizziness, headache, menstrual flow or irregular bleeding, appetite and weight gain, hair loss, mental depression, mental depression Nervousness, restlessness, insomnia, fatigue, nausea and vomiting, skin rash, allergic dermatitis, rubella, frequent urination, etc., may also have weight loss. There are very few reports of breast cancer and testicular cancer in foreign countries.