Zoledronic acid 5 mg/100 mL bottle; solution for IV infusion.
Treatment of Paget’s disease of bone in men and women.
Paget’s disease of bone is characterized by greatly increased and disorderly bone remodeling. Excessive osteoclastic bone resorption is followed by irregular osteoblastic new bone formation, leading to the replacement of normal bone with disorganized, enlarged, and weakened bone structure.
Zoledronic acid is a bisphosphonate that works primarily on bone by inhibiting osteoclast-mediated bone resorption. It rapidly partitions to bone and localizes preferentially at sites of high bone turnover. The relatively long duration of action is attributable to its strong binding affinity to bone mineral.
Treatment with Reclast is indicated in patients with Paget’s disease of bone with elevations in serum alkaline phosphatase (SAP) of two times or higher than the upper limit of the age-specific normal reference range, or those who are symptomatic, or those at risk for complications from their disease to induce remission (normalization of SAP).
After a single treatment with Reclast in Paget’s disease, an extended remission period is observed. Re-treatment with Reclast may be considered in patients who have relapsed, based on increases in SAP, or in those who failed to achieve normalization of their SAP, or in those with symptoms, as dictated by medical practice.
Patients being treated with Zometa (also from Novartis) should not be treated with Reclast because the two medications contain the same active ingredient.
The efficacy of one infusion of Reclast 5 mg versus oral daily doses of risedronate 30 mg for two months was evaluated in two identical six-month, randomized, double-blind trials.
Therapeutic response was defined as either normalization of SAP or a reduction of ≥75% from baseline in total SAP excess at the end of six months. In both trials Reclast demonstrated a superior and more rapid therapeutic response compared with risedronate and returned more patients to normal levels of bone turnover as shown by biochemical markers of formation and resorption.
The six-month combined data from both trials showed that 96% of Reclast-treated patients achieved therapeutic response compared to 74% of patients treated with risedronate. Also at the six-month point, 89% of the Reclast-treated patients achieved normalization of SAP levels, compared to 58% of risedronate-treated patients. Most Reclast patients achieved a therapeutic response by the day 63 visit.
In patients previously treated with oral bisphosphonates, therapeutic response rates were 96% and 55% for Reclast and risedronate, respectively. The low risedronate response was due to the low response rate (30%) in those previously treated with risedronate.
Give by IV infusion over at least 15 minutes. Creatinine clearance ≥35 mL/min: 5 mg. Supplement with calcium 1,500 mg daily in divided doses and vitamin D 800 IU daily.
Not recommended for use in patients with severe renal impairment.
Uncorrected hypocalcemia. Pregnancy (Cat. D). Nursing mothers.
Severe renal impairment: not recommended. Ensure adequate hydration, vitamin D and calcium intake.
Additive hypocalcemic effect with aminoglycosides, loop diuretics. Caution with other nephrotoxic drugs.
Hypocalcemia, headache, dizziness, flulike syndrome, fatigue, pyrexia, rigors, peripheral edema, asthenia, bone pain, myalgia, GI upset; possible osteonecrosis of the jaw.