Tianqing Yitai Zoledronic Acid Concentrated Solution for Injection

1. Indications and Usage
Malignancy-Associated Hypercalcemia: Treatment of hypercalcemia of malignancy.
Bone Metastases: Treatment to prevent skeletal-related events (such as pathologic fractures, spinal cord compression, or need for radiation or surgery to bone) in patients with multiple myeloma or bone metastases from solid tumors.
2. Dosage and Administration
Standard Dose: The recommended dose is 4 mg.
Preparation: The concentrated solution must be further diluted in 100 mL of 0.9% Sodium Chloride or 5% Glucose Injection.
Infusion Protocol: It must be administered as a single intravenous infusion over no less than 15 minutes.
Renal Adjustments: In bone metastasis patients with mild to moderate renal impairment (Creatinine Clearance 30-60 mL/min), the dose must be reduced (e.g., to 3.5 mg, 3.3 mg, or 3.0 mg).
3. Mechanism of Action
Inhibition of Osteoclasts: Zoledronic acid is a potent inhibitor of osteoclast-mediated bone resorption.
FPPS Inhibition: It binds to bone mineral and, upon osteoclast uptake, inhibits farnesyl pyrophosphate synthase (FPPS), a key enzyme in the mevalonate pathway, thereby preventing post-translational modification of small GTPases and inducing osteoclast apoptosis.
4. Safety and Warnings
Renal Toxicity: Renal impairment can occur. Renal function must be monitored before each dose.
Hypocalcemia: Significant hypocalcemia, hypophosphatemia, and hypomagnesemia may occur.
Osteonecrosis of the Jaw: Rare cases have been reported, mostly in cancer patients.
Infusion-Related Reactions: Acute phase reactions (fever, myalgia, flu-like symptoms) are common after the first infusion.
5. Adverse Reactions and Clinical Research
Common Adverse Reactions: Pyrexia, asthenia, bone pain, headache, nausea, vomiting, and constipation.
Clinical Research: Clinical trials have demonstrated significant delays in the time to first-onset of skeletal-related events and reductions in hypercalcemia of malignancy.
6. Drug Interactions
Nephrotoxic Drugs: Concomitant use with aminoglycosides or nonsteroidal anti-inflammatory drugs should be avoided or monitored closely.
Diuretics: Concurrent use with diuretics may increase the risk of hypocalcemia.
Calcium/Vitamin D: Calcium and vitamin D supplements should be administered to maintain normal calcium levels.
7. Pharmaceutical Information
Active Ingredient: Zoledronic Acid.
Appearance: Colorless, clear liquid.
Storage: Store at controlled room temperature. Do not freeze.