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

1. Endometriosis; 2. For uterine fibroids accompanied by menorrhagia, lower abdominal pain, back pain and anemia, it can reduce the size of the fibroids and/or improve the symptoms; 3. Premenopausal breast cancer and estrogen receptor-positive patients; 4. Prostate cancer; 5. 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.

1 Clinically important adverse reactions Common points for all indications 1) Due to the possibility of interstitial pneumonia (0.1%), the patient's condition should be closely observed. 2) Due to the possibility of allergic-like symptoms (0.1%), a careful medical consultation should be conducted and close observation should be performed after medication. 3) Due to the possibility of liver dysfunction or jaundice with elevated AST (GOT) and ALT (GPT) values (the probability of occurrence is unknown), the patient's condition should be closely observed, and appropriate measures should be taken if such conditions occur. 4) Due to the possibility of inducing or aggravating diabetes symptoms (the probability of occurrence is unknown), appropriate measures should be taken if such conditions occur. Endometriosis Mental depression similar to menopausal syndrome due to the effect of estrogen reduction (0.1~5%), the patient's condition should be closely observed. Premenopausal breast cancer 1) Due to the possibility of mental depression, the patient's condition should be closely observed. 2) Due to the temporary increase in serum testosterone concentration caused by the stimulation of this product on the pituitary-gonadal system, the bone pain of prostate cancer is transiently aggravated, urinary tract obstruction or spinal cord compression (ge; 5%). In this case, symptomatic treatment and other appropriate treatments should be carried out. 2 Other adverse reactions Indications for endometriosis, uterine fibroids, premenopausal breast cancer, central precocious puberty ge; 5% 0.1~5% 0.1% Hot flashes, hot sensations, hot flashes, loss of libido, chills, visual disturbances, emotional instability 1) Low estrogen symptoms Shoulder stiffness, headache, insomnia, dizziness, sweating Uterine bleeding, vaginal dryness, dyspareunia, vaginitis, leucorrhea 2) Increased female genitalia, ovarian hyperstimulation syndrome, breast pain, swelling or atrophy pain, such as joint pain and joint stiffness, low back pain, muscle spasms, bone loss, serum 3) Musculoskeletal system bone pain Increased phosphorus or hypercalcemia Acne, dry skin, hair loss, hirsutism, fingers (toes) ) Isopropylamine 4) Skin: drowsiness, irritability, memory loss, decreased concentration, feeling 5) Abnormal mental and nervous system 6) Allergic rash or itching Note) 7) Liver: increased GOT, GPT, ALP, LDH, gamma-GTP or bilirubin, jaundice, nausea, vomiting, loss of appetite, abdominal pain, abdominal distension, abdominal 8) Digestive system: diarrhea, constipation, oral inflammation, thirst 59) Circulatory system: palpitations, increased blood pressure, increased red blood cells, anemia, leukopenia, thrombocytopenia, 10) Prolonged partial coagulation of blood, resulting in prolonged peptidase time 11) Urinary system: frequent urination, difficulty urinating or increased BUN 12) Administration site: pain, nodules or redness at the injection site, abscesses, fatigue, Fatigue, weakness, numbness of lips or limbs, carpal tunnel, weight loss, syndrome, tinnitus, deafness, chest discomfort, edema, abnormal taste, 13) Other increases, lower limb pain, dyspnea, fever, total cholesterol, thyroid function, increased LDL cholesterol or triglycerides, abnormal hyperkalemia Note) Prostate cancer should be closely observed ge; 5% 0.1~5% 0.1% Note) 1) Liver LDH increased jaundice, GOT, GPT, gamma; -GTP, AL-P increased orgasm redness, heat headache, facial flushing, dizziness, sweating, loss of libido, impotence, male 2) Endocrine system sensor breast feminization, testicular atrophy or perineum discomfort joint pain, bone pain, Shoulder, waist, limbs, etc. pain, difficulty walking, muscle pain, bone loss 3) Musculoskeletal system 4) Skin dermatitis or hair growth on the head 5) Urinary system Frequent urination, hematuria or increased BUN 6) Circulatory system Abnormal electrocardiogram or increased cardiothoracic ratio 7) Blood anemia or thrombocytopenia 8) Digestive tract Nausea, vomiting, loss of appetite, diarrhea 9) Allergic rash or itching 10) Administration site Pain, nodules or redness at the injection site, abscesses, edema, chest pressure, chills, fatigue, numbness and weakness of the lips and limbs 11) Others Weight gain, paresthesia, deafness, tinnitus, fever, increased total cholesterol, triglycerides or uric acid, hyperkalemia, increased blood sugar level Note) Close observation is required

The following patients are contraindicated to use this product: Endometriosis Uterine fibroids Central precocious puberty (1) Patients with a history of allergy to the ingredients of this product, synthetic LH-RH or LH-RH derivatives. (2) Pregnant women or women who may become pregnant, or breastfeeding women (see [Use of drugs in pregnant and breastfeeding women]) (3) Patients with unidentified, abnormal vaginal bleeding [possibly a malignant disease] Premenopausal breast cancer (1) Patients with a history of allergy to the ingredients of this product, synthetic LH-RH or LH-RH derivatives. (2) Pregnant women or women who may become pregnant, or breastfeeding women Prostate cancer Patients with a history of allergy to the ingredients of this product, synthetic LH-RH or LH-RH derivatives.

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.

1.88 mg