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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. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the Phosphorus, (ˈfɒsfərəs is the Chemical element that has the symbol P and Atomic number 15 The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 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. For other uses of the words gram or gramme see Gram (disambiguation. The mole (symbol mol) is a unit of Amount of substance: it is an SI base unit, and almost the only unit to be used to measure this In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of A drug's efficiency may be affected by the degree to which it binds to the proteins within Blood plasma. Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The kidneys are complicated organs that have numerous biological roles The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The United States of America —commonly referred to as the The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction S. ) |
| Routes | Intravenous |
Zoledronate (INN: zoledronic acid, marketed by Novartis under the trade names Zometa,Zomera,Aclasta and Reclast) is a bisphosphonate. In Pharmacology and Toxicology, a route Intravenous therapy or IV therapy is the giving of Liquid substances directly into a Vein. An International Nonproprietary Name ( INN; also known as rINN, for recommended International Nonproprietary Name or pINN for proposed Novartis International AG is a multinational Pharmaceutical company based in Basel Switzerland that manufactures drugs such as Clozapine In Pharmacology, bisphosphonates (also called diphosphonates) are a class of drugs that inhibit Osteoclast action and the resorption of bone Zometa is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. In Biology, the skeleton is a strong and often a rigid framework that supports the body of an animal holding it upright and giving it shape and strength (Also skeletal A fracture is the (local separation of an object or material into two or more pieces under the action of stress. Cancer (medical term Malignant Neoplasm) is a class of Diseases in which a group of cells display uncontrolled Multiple myeloma (also known as MM, myeloma, plasma cell myeloma, or as Kahler's disease after Otto Kahler) is a type of It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. Hypercalcaemia (in American English '''Hypercalcemia''' is an elevated calcium level in the Blood.
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. Paget's disease, otherwise known as osteitis deformans, is a chronic disorder that typically results in enlarged and deformed bones In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis. Osteoporosis is a Disease of Bone that leads to an increased risk of fracture.
Contents |
Administration
The standard dose for zoledronate is 4 mg to be infused intravenously over 15 min every 3-4 weeks in cancer patients. Intravenous therapy or IV therapy is the giving of Liquid substances directly into a Vein. 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. [2] [3]
Side effects
Side effects can include fatigue, anemia, muscle aches, fever, and/or swelling in the feet or legs. Anemia ( AmE) or anæmia/anaemia ( BrE) (from the Ancient Greek grc-Latn anaîmia, meaning “without blood” is defined as a qualitative Myalgia means " Muscle Pain " and is a symptom of many diseases and disorders Fever (also known as pyrexia, from the Greek pyretos meaning fire or a febrile response, from the Latin word Febris Oedema (or Edema in American English formerly known as dropsy or hydropsy, is the increase of Interstitial fluid in any organ &mdash swelling 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. The kidneys are complicated organs that have numerous biological roles Renal function, in Nephrology, is an indication of the state of the Kidney and its role in Renal physiology.
A rare complication that has been recently observed in cancer patients being treated with bisphosphonates is osteonecrosis of the jaw. Osteonecrosis of the Jaws ( ONJ') is a severe Bone disease that affects the jaws including the Maxilla and the Mandible This has mainly been seen in patients with multiple myeloma treated with zoledronate who have had dental extractions. [4]
Contraindications
- Poor renal function (e. g. creatinine>3 mg/dL)
- Pregnancy
- Paralysis
References
- ^ Lyles K, et al. Creatinine is a break-down product of Creatine phosphate in Muscle, and is usually produced at a fairly constant rate by the body (depending on muscle mass (2007). "Zoledronic Acid and Clinical Fractures and Mortality after Hip Fracture". N. Engl. J. Med. 357: 1799. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 17878149.
- ^ 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 (2002). "Intravenous zoledronic acid in postmenopausal women with low bone mineral density". N. Engl. J. Med. 346 (9): 653-61. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 11870242.
- ^ Black et al. . Once-Yearly Zoledronic Acid for Treatment of Postmenopausal Osteoporosis. NEJM 2007;356;18;1809-1822. Abstract
- ^ Durie BG, Katz M, Crowley J (2005). "Osteonecrosis of the jaw and bisphosphonates". N. Engl. J. Med. 353 (1): 99-102; discussion 99-102. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 16000365.
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/
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