Zoledronate
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Zoledronate
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| Systematic (IUPAC) name | |
| (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid | |
| Identifiers | |
| CAS number | 118072-93-8 |
| ATC code | M05BA08 |
| PubChem | 68740 |
| DrugBank | APRD01294 |
| Chemical data | |
| Formula | C5H10N2O7P2 |
| Mol. weight | 272.09 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | 22% |
| Metabolism | Nil |
| Half life | 146 hours |
| Excretion | Renal (partial) |
| Therapeutic considerations | |
| Licence data | |
| Pregnancy cat. |
D (U.S.) |
| Legal status |
℞-only (U.S.) |
| Routes | Intravenous |
Zoledronate (INN: zoledronic acid, marketed by Novartis under the trade names Zometa® and Aclasta®) is a bisphosphonate. Zometa is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases.
Aclasta is a single 5 mg infusion for the treatment of Paget's disease of the bone and is being studied for the treatment of osteoporosis.
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[edit] Administration
The standard dose for Zometa is 4 mg to be infused intravenously over 15 min every 3-4 weeks in cancer patients. For Aclasta a single dose of 5 mg is used for the treatment of Paget's disease, and it is currently being studied as a once-yearly 5mg infusion for treatment of osteoporosis.
[edit] 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.
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 (Durie et al 2005).
[edit] Contraindications
- Poor renal function (e.g. creatinine>3 mg/dL)
- Pregnancy
- Paralysis
[edit] Reference
- Durie BG, Katz M, Crowley J. Osteonecrosis of the jaw and bisphosphonates. N Engl J Med 2005;353:99-102. PMID 16000365.
[edit] External links
- http://www.accessdata.fda.gov/scripts/cder/onctools/summary.cfm?ID=246
- http://www.multiplemyeloma.org/treatments/3.06.html
| Bisphosphonates (M05A)edit | ||
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| Nitrogenous: |
Pamidronic acid, Alendronic acid, Ibandronic acid, Risedronic acid, Zoledronic acid |
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| Non-nitrogenous: |
Etidronic acid, Clodronic acid, Tiludronic acid |
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