Zoledronic acid belongs to the class of nitrogen-containing bisphosphonates and acts primarily on bone. It is an inhibitor of osteoclast-mediated bone resorption. The action of bisphosphonates on bone is based on their high affinity for mineralized bone. Intravenously administered Zoledronic acid is rapidly distributed to bone. The main molecular target of Zoledronic acid in the osteoclast is the enzyme farnesyl pyrophosphate synthase, but this does not exclude other mechanisms. Clinical studies in tumour-induced hypercalcemia demonstrated that the effect of Zoledronic acid is characterized by decreases in serum calcium and urinary calcium excretion. In addition to its inhibitory activity against bone resorption, Zoledronic acid also possesses anti-tumour activity, anti-angiogenic activity, anti-pain activity, cytostatic and pro-apoptotic activity on tumour cells and synergistic cytostatic effect with other anti-cancer drugs. There was no accumulation of the active substance in plasma after multiple doses given every 28 days. Zoledronic acid is not metabolized and is excreted unchanged via the kidney.
Drometa IV Infusion
Hypercalcaemia of malignancy: 4 mg as a single infusion over at least 15 min. Re-treatment: 4 mg after at least 7 days if necessary. Co-admin oral Ca 500 mg and vit D 400 IU daily.
Bone metastases associated with solid tumours, Osteolytic lesions associated with multiple myeloma: 4 mg by infusion over at least 15 min 3-4 wkly. Co-admin oral Ca 500 mg and vit D 400 IU daily.
Corticosteroid-induced osteoporosis, Increase bone mass in men with osteoporosis, Osteoporosis in postmenopausal women: 5 mg as a single infusion over at least 15 min, once yrly, with adequate Ca and vit D intake. Patients with low-trauma hip fracture: Start 2 or more wk after hip fracture repair with a loading dose of vit D 50,000-125,000 IU given orally or by IM route prior to 1st infusion.
Paget’s disease of bone: 5 mg as a single infusion over 15 min. Patients should receive elemental Ca 1,500 mg and vit D 800 IU daily particularly within 2 wk after admin. Patients who have relapsed: May be given an additional infusion of 5 mg after an interval of at least 1 yr from the initial dose.
Prophylaxis of postmenopausal osteoporosis: 5 mg as a single infusion once every 2 yr.
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