Zoledronic Acid 118072-93-8
Zoledronic acid or zoledronate (marketed by Novartis under the trade names Zometa, Zomera, Aclasta and Reclast) is a bisphosphonate. Zometa is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer, as well as for treating osteoporosis. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of zoledronic acid may also prevent recurring fractures in patients with a previous hip fracture. Reclast is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the U. S. Food and Drug Administration (FDA) also approved Reclast for the treatment of postmenopausal osteoporosis.
Administration
The standard dose for zoledronate is 4 mg to be infused intravenously over 15 min every 3–4 weeks in cancer patients. For Reclast a single dose of 5 mg is used for the treatment of Paget's disease. Zoledronate has been approved as a once-yearly 5 mg infusion for treatment of osteoporosis and shown significant benefits versus placebo over three years, with a reduced number of vertebral fractures and improved markers of bone density.
Side effects
Side effects can include fatigue, anemia, muscle aches, fever, and/or swelling in the feet or legs. Flu-like symptoms are commonly experienced after the first zoledronate infusion, although not subsequent infusions, and are thought to occur because of its potential to activate human γδ T cells (gamma/delta T cells). Zoledronate is rapidly processed via the kidneys; consequently its administration is not recommended for patients with reduced renal function or kidney disease. A rare complication that has been recently observed in cancer patients being treated with bisphosphonates is osteonecrosis of the jaw. This has mainly been seen in patients with multiple myeloma treated with zoledronate who have had dental extractions.
Contraindications
*Poor renal function (e. g. CrCl<30 mL/min)*Hypocalcemia*Pregnancy*Paralysis
| Systematic (IUPAC) name: | 1-hydroxy-2-(1H-imidazol-1-yl)ethane-1,1-diyldiphosphonic acid |
|---|---|
| Zoledronic Acid CAS number: | 118072-93-8 |
| ATC code: | M05BA08 |
| PubChem: | 68740 |
| DrugBank: | APRD01294 |
| Formula: | C5 H10 N2 O7 |
| Molecular mass: | 272.09 g/mol |
| Zoledronic Acid Assay/Purity: | Typically NLT 98% |
