Zoledronic acid is a nitrogen-containing bisphosphonate that selectively inhibits osteoclast-mediated bone resorption. Its high affinity for mineralized bone allows rapid uptake following intravenous administration.
The principal molecular target in osteoclasts is farnesyl pyrophosphate synthase, an enzyme essential for osteoclast function and survival.
Clinical studies in tumor-induced hypercalcemia demonstrate significant reductions in serum and urinary calcium levels. Beyond its anti-resorptive effect, zoledronic acid exhibits anti-tumor, anti-angiogenic, analgesic, cytostatic, and pro-apoptotic activities, and may act synergistically with other anticancer agents.
Zoledronic acid is not metabolized, does not accumulate in plasma with repeated dosing every 28 days, and is excreted unchanged via the kidneys.
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Zoclast is indicated for the management and prevention of bone-related disorders, including:
Not recommended in patients with CrCl <30 mL/min
No dose adjustment required if CrCl >60 mL/min
Dose adjustment based on creatinine clearance:
| Creatinine Clearance | Dose |
|---|---|
| >60 mL/min | 4 mg |
| 50–60 mL/min | 3.5 mg |
| 40–49 mL/min | 3.3 mg |
| 30–39 mL/min | 3.0 mg |
Dilute the required dose in 100 mL of calcium-free infusion solution
(0.9% sodium chloride or 5% glucose)
Infusion duration must be at least 15 minutes
Use the solution immediately after preparation; if necessary, store at 2–8°C for up to 24 hours
Allow refrigerated solutions to reach room temperature before infusion
Do not mix with calcium-containing or divalent cation solutions (e.g., Lactated Ringer’s)
Administer as a single intravenous infusion via a separate line
Recommended dose: 4 mg as a single intravenous infusion
Indicated for patients with corrected serum calcium ≥12 mg/dL (3.0 mmol/L)
No dose adjustment is required in mild to moderate renal impairment
Retreatment may be considered if calcium levels do not normalize
A minimum interval of 7 days should elapse before retreatment
Recommended dose: 4 mg IV infusion every 3–4 weeks
Patients should receive daily supplementation with:
Calcium 500 mg
Vitamin D 400 IU
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No clinically significant interactions observed with commonly used anticancer agents, antibiotics, diuretics, or analgesics
Caution required with:
Aminoglycosides (prolonged hypocalcemia risk)
Loop diuretics (increased hypocalcemia risk)
Thalidomide (increased renal dysfunction risk in multiple myeloma)
Other potentially nephrotoxic agents
Commonly reported adverse reactions include:
Zoledronic acid is contraindicated during pregnancy and breastfeeding.
Use is not recommended in children and adolescents below 18 years of age.
Store below 30°C prior to opening
Protect from light and moisture
Keep out of reach and sight of children
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