Zoledronic acid injection

The pharmacological action of zoledronic acid is mainly to inhibit bone resorption. Its mechanism of action is not fully understood and may be related to multiple effects. Zoledronic acid can inhibit osteoclast activity in vitro, induce osteoclast apoptosis, and block osteoclast resorption of mineralized bone and cartilage by binding to bone. Zoledronic acid can also inhibit the enhanced osteoclast activity and bone calcium release caused by various stimulating factors released by tumors. Toxicological studies Genetic toxicity: The results of the Ames bacterial reverse mutation test, the Chinese hamster ovary cell chromosome aberration test, the Chinese hamster gene mutation test and the rat micronucleus test were all negative. Reproductive toxicity: Female rats were subcutaneously injected with 0.01, 0.03 or 0.1 mg/kg/day of this product from 15 days before mating to the end of pregnancy (AUC is 0.07, 0.2 and 1.2 times that of 4 mg when injected intravenously in humans). Animals in the high-dose group showed ovulation inhibition and decreased pregnancy rate. Animals in the medium-dose and high-dose groups showed increased pre-implantation loss, decreased number of implanted embryos and live fetuses, and decreased survival rate of newborn mice. All dose groups of mothers experienced dystocia and increased perinatal mortality. The cause of maternal death may be related to the drug's inhibition of bone calcium mobilization, leading to perinatal hypocalcemia, which may be a common effect of bisphosphonates. Female rats were subcutaneously injected with 0.1, 0.2 or 0.4 mg/kg/day of this product during pregnancy (AUC is 1.2, 2.4 or 4.8 times that of human intravenous injection of 4 mg). Animals in the medium- and high-dose groups showed increased pre- or post-implantation loss, decreased number of live fetuses, and fetal skeletal, visceral and external deformities. The skeletal deformities of the fetuses in the high-dose group were manifested as unossified and incomplete ossification, thickened, bent or shortened bones, etc. In the high-dose group, toxic reactions such as reduced lens size, incomplete cerebellar development, reduced or absent liver lobules, deformed lung lobes, vascular dilation, cleft palate, and edema were also observed. Fetuses in the low-dose group also showed skeletal deformities. In this test, the body weight and food intake of maternal animals in the high-dose group decreased, indicating that the test has reached the highest drug exposure level. Pregnant rabbits were subcutaneously administered 0.01, 0.03, and 0.1 mg/kg/day of this product (AUC is less than or equal to 0.5 times the human intravenous dose of 4 mg), and no toxicity to the fetus was observed. Maternal death and abortion occurred in animals in each medication group (the dose was greater than or equal to 0.05 times the human intravenous dose of 4 mg based on relative body surface area), which may be related to drug-induced hypocalcemia. Carcinogenicity: Conventional lifelong carcinogenicity studies were conducted using mice and rats. Mice were orally administered 0.1, 0.5, and 2.0 mg/kg/day of this product (the dose was greater than or equal to 0.002 times the human intravenous dose of 4 mg based on relative body surface area), and the incidence of Harderian (accessory lacrimal gland) adenoma increased in all drug-treated groups. Rats were orally administered 0.1, 0.5, and 2.0 mg/kg/day of this product (calculated based on relative body surface area, the dose is less than or equal to 0.2 times the human intravenous dose of 4 mg), and no increase in tumor incidence was observed.

Zoledronic acid

This product is a colorless clear liquid.

Bone pain caused by osteolytic bone metastases of malignant tumors.

Intravenous drip. For adults, 4 mg each time, diluted with 100 ml 0.9% sodium chloride injection or 5% glucose injection, then intravenously dripped. The drip time should be no less than 15 minutes. Administer once every 3 to 4 weeks as directed by the doctor.

The most common adverse reaction of this product is fever. Other adverse reactions mainly include: systemic reactions: fatigue, chest pain, leg edema, conjunctivitis; digestive system: nausea, vomiting, constipation, diarrhea, abdominal pain, dysphagia, anorexia; cardiovascular and cerebrovascular system: hypotension; blood and lymphatic system: anemia, hypokalemia, hypomagnesemia, hypophosphatemia, hypocalcemia, granulocytopenia, thrombocytopenia, pancytopenia; muscle and bone: bone pain, bone joints, muscle pain; kidney: increased serum creatinine value (related to the time of administration); nervous system: insomnia, anxiety, excitement, headache, lethargy; respiratory system: dyspnea, cough, pleural effusion; infection: urinary tract infection, upper respiratory tract infection; metabolic system: anorexia, weight loss, dehydration; others: flu-like symptoms, redness and swelling at the injection site, rash, itching, etc. The toxic and side effects of zoledronic acid are mostly mild and transient. In most cases, they will automatically subside within 24 to 48 hours without special treatment.

1. Patients who are allergic to this product or other bisphosphonates are contraindicated. 2. Patients with severe renal insufficiency are not recommended to use this product. 3. Pregnant and lactating women are contraindicated to use this product.

Precautions for children: The safety and effectiveness of this product in children have not been established, and its use is not recommended. Precautions for pregnancy and lactation: It is not clear whether this product will be secreted into breast milk. Because this product can bind to bones for a long time, pregnant and lactating women are prohibited from using this product. Precautions for the elderly: Same as adults. However, elderly patients often have lower renal function, and renal function should be closely monitored during administration.

This product should be used with caution when used in combination with aminoglycosides, because aminoglycosides have a synergistic effect in lowering blood calcium, which may prolong the duration of hypoglycemia; when used in combination with diuretics, it may increase the risk of hypocalcemia; when used in combination with thalidomide, it will increase the risk of renal abnormalities in patients with multiple myeloma.

Store in a cool, dry place.

1ml:1mg (based on C5H10N2O7P2)

24 months

Chengdu Tiantai Mountain Pharmaceutical Co., Ltd.

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  2000-09-29

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  No. 88 Tianxing Avenue, Qionglai City, Sichuan Province

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  915101832024104543

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