Leuprorelin Acetate Microspheres for Injection

Pharmacological action: 1 Mechanism of action Repeated administration of large doses of LH-RH or its highly active derivative leuprorelin acetate can produce a transient excitatory effect on the pituitary-gonadal system (acute effect) immediately after the first administration, and then inhibit the pituitary from producing and releasing gonadotropins. It also further inhibits the response of the ovaries and testicles to gonadotropins, thereby reducing the production of estradiol and testosterone (chronic effect). The LH release activity of leuprorelin acetate is about 100 times that of LH-RH, and its effect of inhibiting the function of the pituitary-gonadal system is also stronger than that of LH-RH. Leuprorelin acetate is a highly active LH-RH derivative. Because its resistance to proteolytic enzymes and its affinity for LH-RH receptors are stronger than LH-RH, it can effectively inhibit the function of the pituitary-gonadal system. In addition, leuprorelin acetate is also a sustained-release preparation that constantly releases leuprorelin acetate into the blood, so it can effectively reduce the response of the ovaries and testicles and produce a highly effective inhibitory effect on the pituitary-gonadal system. 2. Inhibitory effect on gonadal hormone concentration (1) For patients with endometriosis, uterine fibroids or premenopausal breast cancer, subcutaneous injection of leuprolide acetate once every 4 weeks can reduce serum estradiol to a level close to that of menopause. Therefore, this product has an ovarian function inhibitory effect, which can inhibit normal ovulation and stop menstruation. (2) Subcutaneous injection of leuprolide acetate once every 4 weeks in patients with prostate cancer can reduce serum testosterone concentration to below the castration level, indicating that this product has a drug-induced castration effect. (3) After subcutaneous injection of leuprolide acetate once every 4 weeks in boys and girls with central precocious puberty, the level of serum gonadotropin drops to the pre-pubertal level, indicating that it has a progressive inhibitory effect on secondary sexual characteristics.

Main ingredient: Leuprorelin acetate (pregnancy classification: X) 『Category』 Androgens Related Synthetic Drugs/Antineoplastics

This product is white or off-white granules or powder.

Endometriosis; uterine fibroids with menorrhagia, lower abdominal pain, back pain, and anemia; premenopausal breast cancer with estrogen receptor-positive disease; prostate cancer; central precocious puberty

Endometriosis: Usually, adults receive 3.75 mg of leuprolide acetate subcutaneously once every 4 weeks. However, when the patient weighs less than 50 kg, a 1.88 mg preparation can be used. The first dose should be started from the 1st to 5th day of the menstrual cycle. Uterine fibroids: Usually, adults receive 1.88 mg of leuprolide acetate subcutaneously once every 4 weeks. However, for patients who are overweight or have a significantly enlarged uterus, 3.75 mg should be injected. The first dose should be started from the 1st to 5th day of the menstrual cycle. Prostate cancer and premenopausal breast cancer: Usually, adults receive 3.75 mg of leuprolide acetate subcutaneously once every 4 weeks. Central precocious puberty: Usually, 30 g/kg of leuprolide acetate subcutaneously once every 4 weeks, which can be increased to 90 g/kg according to the patient's symptoms. Before administration, the drug in the bottle should be fully suspended with an additional 2 ml of solvent, and be careful not to foam.

Endocrine system: fever, facial flushing, sweating, loss of libido, impotence, gynecomastia in men, testicular atrophy, perineal discomfort, etc. Musculoskeletal system: bone pain, pain in the shoulders, waist and limbs. Urinary system: urination disorder, hematuria, etc. Circulatory system: abnormal electrocardiogram, increased heart-chest ratio, etc. Digestive system: nausea, vomiting, loss of appetite, etc. Allergic reaction: rash and itching, etc. Pain, nodules and redness at the injection site. Others: edema, chest oppression, chills, fatigue, weight gain, abnormal perception, hearing loss, tinnitus, excessive hair on the head, uric acid, BUN, LDH, GOT, GPT increase, etc. Menopausal syndrome-like mental depression due to the effect of estrogen reduction.

Those who have a history of allergy to the ingredients of this preparation, synthetic LH-RH or LH-RH derivatives. Pregnant women or women who may become pregnant, or breastfeeding women; those with unidentified, abnormal vaginal bleeding [possibly a malignant disease].

Precautions for children: Central precocious puberty: The safety of this product for low-birth-weight infants, newborns and infants has not been determined. Precautions during pregnancy and lactation: Pregnant women, women who may become pregnant or breastfeeding women should not use this drug (there have been reports of GnRH analogs causing miscarriage. In animal studies of this drug, increased fetal mortality and reduced fetal weight were observed (rats and rabbits), and there was a trend toward increased abnormalities in fetal bone formation (rabbits). It was also observed in rats that leuprolide acetate can be secreted into breast milk). Precautions for the elderly: There is currently a lack of research data on the effectiveness and safety of this product for the elderly.

Precautions for drug compatibility for endometriosis and uterine fibroids (When this product is used in combination with the following drugs, it should be used with caution) Drug phenomena, symptoms, treatment mechanisms and risk factors Sex hormone compounds The efficacy of this product will be reduced This product achieves clinical effects by reducing the secretion of sex hormones, so giving sex hormone triol derivatives will reduce the clinical efficacy of this product. Compounds changed from estrogen Combination compounds of estrogen and progesterone, sex hormone mixtures, etc.

Store sealed at room temperature.

3.75mg

24 months

Shanghai Livzon Pharmaceutical Co., Ltd.

• Founded in:

  1995-04-11

• Address:

  No. 1150, Guiqiao Road, China (Shanghai) Pilot Free Trade Zone

• Tax NO.:

  913100001338549664

• Registered Funds:

  87.3289 million yuan

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