Zoledronic acid
1846280
223556698
2008-07-04T16:30:20Z
Fvasconcellos
1051513
oops
{{drugbox
| IUPAC_name = (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid
| image = Zoledronic acid.svg
| image2 = Zoledronate-3D-balls.png
| width = 180px
| CAS_number = 118072-93-8
| ATC_prefix = M05
| ATC_suffix = BA08
| PubChem = 68740
| DrugBank = APRD01294
| C = 5 |H = 10 |N = 2 |O = 7 |P = 2
| molecular_weight = 272.09 [[Gram|g]]/[[Mole (unit)|mol]]
| bioavailability =
| protein_bound = 22%
| metabolism = Nil
| elimination_half-life = 146 hours
| excretion = [[Kidney|Renal]] (partial)
| licence_EU = Reclast
| licence_US = Zoledronic_acid
| pregnancy_category = D <small>([[United States|U.S.]])</small>
| legal_status = ℞-only <small>(U.S.)</small>
| routes_of_administration = [[Intravenous therapy|Intravenous]]
}}
'''Zoledronic acid''' ([[International Nonproprietary Name|INN]]) or '''zoledronate''' (marketed by [[Novartis]] under the trade names '''Zometa''', '''Zomera''', '''Aclasta''' and '''Reclast''') is a [[bisphosphonate]]. Zometa is used to prevent [[skeletal]] [[fracture]]s in patients with [[cancer]]s 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.<ref>{{cite journal |author= Lyles K, et al.|title=Zoledronic Acid and Clinical Fractures and Mortality after Hip Fracture |journal=N. Engl. J. Med. |volume= 357|issue= |pages= 1799|year=2007 |pmid=17878149|doi=10.1056/NEJMoa074941}}</ref>
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 [[intravenous]]ly 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 fracture]]s and improved markers of bone density.<ref>{{cite journal |author=Reid IR, Brown JP, Burckhardt P, Horowitz Z, Richardson P, Trechsel U, Widmer A, Devogelaer JP, Kaufman JM, Jaeger P, Body JJ, Brandi ML, Broell J, Di Micco R, Genazzani AR, Felsenberg D, Happ J, Hooper MJ, Ittner J, Leb G, Mallmin H, Murray T, Ortolani S, Rubinacci A, Saaf M, Samsioe G, Verbruggen L, Meunier PJ |title=Intravenous zoledronic acid in postmenopausal women with low bone mineral density |journal=N. Engl. J. Med. |volume=346 |issue=9 |pages=653–61 |year=2002 |pmid=11870242 |doi=10.1056/NEJMoa011807}}</ref><ref>Black et al.. Once-Yearly Zoledronic Acid for Treatment of Postmenopausal Osteoporosis. NEJM 2007;356;18;1809-1822. [http://content.nejm.org/cgi/content/short/356/18/1809 Abstract]</ref>
==Side effects==
Side effects can include [[fatigue (physical)|fatigue]], [[anemia]], [[muscle pain|muscle aches]], [[fever]], and/or [[Edema|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 [[gamma/delta T cells|γδ T cells]].
Zoledronate is rapidly processed via the [[kidney]]s; consequently its administration is not recommended for patients with reduced [[renal function]] or kidney disease.{{Fact|date=April 2008}}
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 extraction]]s.<ref>{{cite journal |author=Durie BG, Katz M, Crowley J |title=Osteonecrosis of the jaw and bisphosphonates |journal=N. Engl. J. Med. |volume=353 |issue=1 |pages=99–102; discussion 99–102 |year=2005 |pmid=16000365 |doi=10.1056/NEJM200507073530120}}</ref>
==Contraindications==
*Poor renal function (e.g. [[creatinine]]>3 mg/dL)
*Pregnancy
*Paralysis
==References==
<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/
{{Bisphosphonates}}
[[Category:Bisphosphonates]]
[[Category:Imidazoles]]
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[[zh:唑來磷酸]]