Zoledronic Acid (4 brand names, 2 dosage forms, 3 routes)
Available dosage forms: INJECTABLE, SOLUTION.
Routes of administration: INTRAVENOUS, INJECTION, IV (INFUSION).
Brand Names
- RECLAST
- ZOLEDRONIC
- ZOLEDRONIC ACID
- ZOMETA
Related Health Topics
Related Conditions
Contraindications
Zoledronic acid injection is contraindicated in patients with the following conditions: •Hypocalcemia [see Warnings and Precautions (5.2)] •Creatinine clearance less than 35 mL/min and in those with evidence of acute renal impairment due to an increased risk of renal failure [see Warnings and Precautions (5.3)]. •Known hypersensitivity to zoledronic acid or any components of zoledronic acid injection. Hypersensitivity reactions, including urticaria, angioedema, and anaphylactic reaction/shock have been reported [see Adverse Reactions (6.2)].
Adverse Reactions
The following clinically significant adverse drug reactions are described elsewhere in the labeling: •Drugs with Same Active Ingredient [see Warnings and Precautions (5.1)] •Hypocalcemia and Mineral Metabolism [see Warnings and Precautions (5.2)] •Renal Impairment [see Warnings and Precautions (5.3)] •Osteonecrosis of the Jaw [see Warnings and Precautions (5.4)] •Atypical Fractures Including Femoral Fractures [see Warnings and Precautions (5.5)] •Musculoskeletal Pain [see Warnings and Precautions (5.6)] •Patients with Asthma [see Warnings and Precautions (5.7)]
Drug Interactions
No in vivo drug interaction studies have been performed for zoledronic acid injection. In vitro and ex vivo studies showed low affinity of zoledronic acid for the cellular components of human blood. In vitro mean zoledronic acid protein binding in human plasma ranged from 28% at 200 ng/mL to 53% at 50 ng/mL. In vivo studies showed that zoledronic acid is not metabolized, and is excreted into the urine as the intact drug.
Mechanism of Action
Zoledronic acid injection 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.
Overdosage
Clinical experience with acute overdosage of zoledronic acid injection solution for intravenous infusion is limited. Patients who have received doses higher than those recommended should be carefully monitored. Overdosage may cause clinically significant renal impairment, hypocalcemia, hypophosphatemia, and hypomagnesemia. Clinically relevant reductions in serum levels of calcium, phosphorus, and magnesium should be corrected by intravenous administration of calcium gluconate, potassium or sodium phosphate, and magnesium sulfate, respectively. Single doses of zoledronic acid injection should not exceed 5 mg and the duration of the intravenous infusion should be no less than 15 minutes [see Dosage and Administration (2)].