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-4%
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.
Zoclast is indicated for the management and prevention of bone-related disorders, including:
- Hypercalcaemia of malignancy
- Bone metastases associated with solid tumors
- Osteolytic lesions in patients with multiple myeloma
- Corticosteroid-induced osteoporosis
- Increasing bone mass in men with osteoporosis
- Osteoporosis in postmenopausal women
- Paget’s disease of bone
- Prophylaxis of postmenopausal osteoporosis
Renal Impairment
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 |