Zoledronic Acid is a potent bisphosphonate that inhibits osteoclast-mediated bone resorption. Its action is due to a strong affinity for mineralized bone, particularly at sites of high turnover. The primary molecular target is farnesyl pyrophosphate synthase in osteoclasts, leading to reduced bone breakdown. Its long duration of effect is attributed to strong binding with bone mineral.
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Zoldix is prescribed for:
Limitations of use: The optimal duration of therapy is not clearly established. For patients at low fracture risk, discontinuation should be considered after 3–5 years of use.
- Pediatric: Not indicated.
- Geriatric: Monitor renal function closely.
- Renal impairment: Contraindicated if CrCl <35 mL/min.
- Hepatic impairment: No adjustment needed (not metabolized hepatically).
- Pregnancy & Lactation: Contraindicated – may cause fetal harm and not recommended during breastfeeding.
Postmenopausal Osteoporosis (treatment): 5 mg IV infusion once yearly (≥15 minutes).
Postmenopausal Osteoporosis (prevention): 5 mg IV infusion every 2 years.
Osteoporosis in Men: 5 mg IV infusion once yearly.
Glucocorticoid-Induced Osteoporosis: 5 mg IV infusion once yearly.
Paget’s Disease: A single 5 mg IV infusion (≥15 minutes).
Re-treatment may be required if symptoms return or serum alkaline phosphatase fails to normalize.
Supplementation:
Patients should receive Calcium (≥1200–1500 mg/day) and Vitamin D (800–1000 IU/day), particularly during the first 2 weeks after infusion.
Administration guidelines:
Common (>10%): Pyrexia, myalgia, headache, arthralgia, extremity pain
Others: Flu-like illness, nausea, vomiting, diarrhea, eye inflammation
Serious: Osteonecrosis of the jaw (ONJ), atypical femur fractures, renal impairment
Overdosage may result in renal failure, hypocalcemia, hypophosphatemia, and hypomagnesemia. Treat with IV supplementation (calcium gluconate, phosphate, magnesium sulfate). Maximum single dose: 5 mg IV over ≥15 minutes.
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