Zoledronic acid

Features

Zoledronic acid is a bisphosphonate and acts primarily on bone. It is an inhibitor of osteoclast-mediated bone resorption. The selective action of bisphosphonates on bone is based on their high affinity for mineralized bone. Intravenously administered zoledronic acid rapidly partitions to bone and localizes preferentially at sites of high bone turnover. The main molecular target of zoledronic acid in the osteoclast is the enzyme farnesyl pyrophosphate synthase. The relatively long duration of action of zoledronic acid is attributable to its high binding affinity to bone mineral.

Dosage

Treatment of Osteoporosis in Postmenopausal Women

The recommended regimen is a 5 mg infusion once a year given intravenously over no less than 15 minutes. For osteoporosis treatment, and to reduce the risk of hypocalcemia, patients must be adequately supplemented with calcium and vitamin D if dietary intake is not sufficient. Postmenopausal women require an average of at least 1200 mg calcium and 800-1000 IU vitamin D daily.

Prevention of Osteoporosis in Postmenopausal Women

The recommended regimen is a 5 mg infusion given once every 2 years intravenously over no less than 15 minutes. Patients must be adequately supplemented with calcium and vitamin D if dietary intake is not sufficient. Postmenopausal women require an average of 1200 mg calcium and 800-1000 IU vitamin D daily.

Osteoporosis in Men

The recommended regimen is a 5 mg infusion once a year given intravenously over no less than 15 minutes. Patients must be adequately supplemented with calcium and vitamin D if dietary intake is not sufficient. An average of at least 1200 mg calcium and 800-1000 IU vitamin D daily is recommended.

Treatment and Prevention of Glucocorticoid-Induced Osteoporosis

The recommended regimen is a 5mg infusion once a year given intravenously over no less than 15 minutes. Patients must be adequately supplemented with calcium and vitamin D if dietary intake is not sufficient. An average of at least 1200 mg calcium and 800-1000 IU vitamin D daily is recommended.

Treatment of Paget’s Disease of Bone

The recommended dose is a 5 mg infusion. The infusion time must not be less than 15 minutes given over a constant infusion rate. To reduce the risk of hypocalcemia, all patients with Paget’s disease should receive 1500 mg elemental calcium daily in divided doses (750 mg two times a day, or 500 mg three times a day) and 800 IU vitamin D daily, particularly in the 2 weeks following Zoledronic acid administration. All patients should be instructed on the importance of calcium and vitamin D supplementation in maintaining serum calcium levels, and on the symptoms of hypocalcemia .

Indications

Treatment of Osteoporosis in Postmenopausal Women

Zoledronic acid is indicated for treatment of osteoporosis in postmenopausal women. In postmenopausal women with osteoporosis, diagnosed by bone mineral density (BMD) or prevalent vertebral fracture, Zoledronic acid reduces the incidence of fractures (hip, vertebral and non-vertebral osteoporosis-related fractures). In patients at high risk of fracture, defined as a recent low-trauma hip fracture, Zoledronic acid reduces the incidence of new clinical fractures.

Prevention of Osteoporosis in Postmenopausal Women

Zoledronic acid is indicated for prevention of osteoporosis in postmenopausal women.

Osteoporosis in Men

Zoledronic acid is indicated for treatment to increase bone mass in men with osteoporosis.

Glucocorticoid-Induced Osteoporosis

Zoledronic acid is indicated for the treatment and prevention of glucocorticoidinduced osteoporosis in men and women who are either initiating or continuing systemic glucocorticoids in a daily dosage equivalent to 7.5 mg or greater of prednisone and who are expected to remain on glucocorticoids for at least 12 months.

Paget's Disease of Bone

Zoledronic acid is indicated for treatment of Paget's disease of bone in men and women. Treatment is indicated in patients with Paget’s disease of bone with elevations in serum alkaline phosphatase 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.

Product Information

Zoledronic Acid for Injection 4 mg is available as a sterile lyophilised powder for injection in a 5 ml vial containing 4 mg of anhydrous Zoledronic Acid.

 

For the use only of a Registered Medical Practitioner or a Hospital or a Laboratory