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 | |
| ATC code | M05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C5H10N2O7P2 |
| Mol. mass | 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 |
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Zoledronate (INN: zoledronic acid, marketed by Novartis under the trade names Zometa and Reclast) 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.
An annual dose of zoledrinic acid may also prevent recurring fractures in patients with a previous hip fracture. [1]
Reclast is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the 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.[1] [1]
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.[1]
Contraindications
- Poor renal function (e.g. creatinine>3 mg/dL)
- Pregnancy
- Paralysis
References
External links
- http://www.accessdata.fda.gov/scripts/cder/onctools/summary.cfm?ID=246
- http://www.multiplemyeloma.org/treatments/3.06.html
- http://www.us.zometa.com/info/index.jsp
- http://www.zometa.com/index.jsp
- http://www.reclast.com/
Drugs for treatment of bone diseases (M05) | |
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| Bisphosphonates | Nitrogenous (Pamidronic acid, Alendronic acid, Ibandronic acid, Risedronic acid, Zoledronic acid) - Non-nitrogenous (Etidronic acid, Clodronic acid, Tiludronic acid) |
| Bone morphogenetic proteins | Dibotermin alfa - Eptotermin alfa |
| Other | Ipriflavone - Aluminium chlorohydrate - Strontium ranelate |
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
