Peringatan Keamanan

Patients experiencing an overdose may present with renal impairment, hypocalcemia, hypophosphatemia, and hypomagnesemia.L13712,L13715,L13721 Overdose should be managed through intravenous administration of the insufficient ions.L13712,L13715,L13721

Zoledronic acid

DB00399

small molecule approved

Deskripsi

Zoledronic acid, or CGP 42'446,A203120 is a third generation, nitrogen containing bisphosphonate similar to ibandronic acid, minodronic acid, and risedronic acid.A203111 Zoledronic acid is used to treat and prevent multiple forms of osteoporosis, hypercalcemia of malignancy, multiple myeloma, bone metastases from solid tumors, and Paget’s disease of bone.L13712,L13715,L13721 Zoledronic acid was first described in the literature in 1994.A203120

Zoledronic acid was granted FDA approval on 20 August 2001.L13712

Struktur Molekul 2D

Berat 272.0896
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Zoledronic acid has a terminal elimination half life of 146 hours.[L13712,L13715,L13721]
Volume Distribusi -
Klirens (Clearance) Zoledronic acid has a renal clearance of 3.7 ± 2.0 L/h.[L13712,L13715,L13721]

Absorpsi

A 4mg intravenous dose reaches a Cmax of 370±78.5ng/mL, with a Tmax of 0.317±0.014h, and an AUC of 788±181ng\*h/mL.A203099 A 5mg intravenous dose reaches a Cmax of 471±76.1ng/mL, with a Tmax of 0.368±0.005h, and an AUC of 917±226ng\*h/mL.A203099

Metabolisme

Zoledronic acid is not metabolized in vivio.L13712,L13715,L13721

Rute Eliminasi

Zoledronic acid is 39 ± 16% eliminated in the urine as the unmetabolized parent drug.L13712,L13715,L13721

Interaksi Obat

312 Data
Deferasirox The risk or severity of gastrointestinal bleeding and gastrointestinal ulceration can be increased when Zoledronic acid is combined with Deferasirox.
Thalidomide The risk or severity of jaw osteonecrosis can be increased when Thalidomide is combined with Zoledronic acid.
Bevacizumab The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Bevacizumab is combined with Zoledronic acid.
Lenalidomide The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Lenalidomide is combined with Zoledronic acid.
Sunitinib The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Sunitinib is combined with Zoledronic acid.
Ranibizumab The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Ranibizumab is combined with Zoledronic acid.
Fumagillin The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Fumagillin is combined with Zoledronic acid.
Resveratrol The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Resveratrol is combined with Zoledronic acid.
Halofuginone The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Halofuginone is combined with Zoledronic acid.
Anecortave acetate The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Anecortave acetate is combined with Zoledronic acid.
Endostatin The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Endostatin is combined with Zoledronic acid.
Semaxanib The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Semaxanib is combined with Zoledronic acid.
Squalamine The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Squalamine is combined with Zoledronic acid.
Pazopanib The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Pazopanib is combined with Zoledronic acid.
Volociximab The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Volociximab is combined with Zoledronic acid.
TNP-470 The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when TNP-470 is combined with Zoledronic acid.
Pomalidomide The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Pomalidomide is combined with Zoledronic acid.
Roquinimex The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Roquinimex is combined with Zoledronic acid.
Endostar The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Endostar is combined with Zoledronic acid.
Trebananib The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Trebananib is combined with Zoledronic acid.
Anecortave The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Anecortave is combined with Zoledronic acid.
Beloranib The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Beloranib is combined with Zoledronic acid.
Brolucizumab The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Brolucizumab is combined with Zoledronic acid.
Icosapent The risk or severity of gastrointestinal bleeding can be increased when Icosapent is combined with Zoledronic acid.
Mesalazine The risk or severity of nephrotoxicity and hypocalcemia can be increased when Mesalazine is combined with Zoledronic acid.
Indomethacin The risk or severity of gastrointestinal bleeding can be increased when Indomethacin is combined with Zoledronic acid.
Nabumetone The risk or severity of gastrointestinal bleeding can be increased when Nabumetone is combined with Zoledronic acid.
Ketorolac The risk or severity of gastrointestinal bleeding can be increased when Ketorolac is combined with Zoledronic acid.
Tenoxicam The risk or severity of gastrointestinal bleeding can be increased when Tenoxicam is combined with Zoledronic acid.
Celecoxib The risk or severity of gastrointestinal bleeding can be increased when Celecoxib is combined with Zoledronic acid.
Tolmetin The risk or severity of gastrointestinal bleeding can be increased when Tolmetin is combined with Zoledronic acid.
Rofecoxib The risk or severity of gastrointestinal bleeding can be increased when Rofecoxib is combined with Zoledronic acid.
Piroxicam The risk or severity of gastrointestinal bleeding can be increased when Piroxicam is combined with Zoledronic acid.
Fenoprofen The risk or severity of gastrointestinal bleeding can be increased when Fenoprofen is combined with Zoledronic acid.
Valdecoxib The risk or severity of gastrointestinal bleeding can be increased when Valdecoxib is combined with Zoledronic acid.
Diclofenac The risk or severity of gastrointestinal bleeding can be increased when Diclofenac is combined with Zoledronic acid.
Sulindac The risk or severity of gastrointestinal bleeding can be increased when Sulindac is combined with Zoledronic acid.
Flurbiprofen The risk or severity of gastrointestinal bleeding can be increased when Flurbiprofen is combined with Zoledronic acid.
Etodolac The risk or severity of gastrointestinal bleeding can be increased when Etodolac is combined with Zoledronic acid.
Mefenamic acid The risk or severity of gastrointestinal bleeding can be increased when Mefenamic acid is combined with Zoledronic acid.
Naproxen The risk or severity of gastrointestinal bleeding can be increased when Naproxen is combined with Zoledronic acid.
Sulfasalazine The risk or severity of gastrointestinal bleeding can be increased when Sulfasalazine is combined with Zoledronic acid.
Phenylbutazone The risk or severity of gastrointestinal bleeding can be increased when Phenylbutazone is combined with Zoledronic acid.
Meloxicam The risk or severity of gastrointestinal bleeding can be increased when Meloxicam is combined with Zoledronic acid.
Carprofen The risk or severity of gastrointestinal bleeding can be increased when Carprofen is combined with Zoledronic acid.
Diflunisal The risk or severity of gastrointestinal bleeding can be increased when Diflunisal is combined with Zoledronic acid.
Salicylic acid The risk or severity of gastrointestinal bleeding can be increased when Salicylic acid is combined with Zoledronic acid.
Meclofenamic acid The risk or severity of gastrointestinal bleeding can be increased when Meclofenamic acid is combined with Zoledronic acid.
Acetylsalicylic acid The risk or severity of gastrointestinal bleeding can be increased when Acetylsalicylic acid is combined with Zoledronic acid.
Oxaprozin The risk or severity of gastrointestinal bleeding can be increased when Oxaprozin is combined with Zoledronic acid.
Ketoprofen The risk or severity of gastrointestinal bleeding can be increased when Ketoprofen is combined with Zoledronic acid.
Balsalazide The risk or severity of gastrointestinal bleeding can be increased when Balsalazide is combined with Zoledronic acid.
Ibuprofen The risk or severity of gastrointestinal bleeding can be increased when Ibuprofen is combined with Zoledronic acid.
Olsalazine The risk or severity of nephrotoxicity and hypocalcemia can be increased when Olsalazine is combined with Zoledronic acid.
Lumiracoxib The risk or severity of gastrointestinal bleeding can be increased when Lumiracoxib is combined with Zoledronic acid.
Magnesium salicylate The risk or severity of gastrointestinal bleeding can be increased when Magnesium salicylate is combined with Zoledronic acid.
Salsalate The risk or severity of gastrointestinal bleeding can be increased when Salsalate is combined with Zoledronic acid.
Choline magnesium trisalicylate The risk or severity of gastrointestinal bleeding can be increased when Choline magnesium trisalicylate is combined with Zoledronic acid.
Antrafenine The risk or severity of gastrointestinal bleeding can be increased when Antrafenine is combined with Zoledronic acid.
Aminophenazone The risk or severity of gastrointestinal bleeding can be increased when Aminophenazone is combined with Zoledronic acid.
Antipyrine The risk or severity of gastrointestinal bleeding can be increased when Antipyrine is combined with Zoledronic acid.
Tiaprofenic acid The risk or severity of gastrointestinal bleeding can be increased when Tiaprofenic acid is combined with Zoledronic acid.
Etoricoxib The risk or severity of gastrointestinal bleeding can be increased when Etoricoxib is combined with Zoledronic acid.
Taxifolin The risk or severity of gastrointestinal bleeding can be increased when Taxifolin is combined with Zoledronic acid.
Oxyphenbutazone The risk or severity of gastrointestinal bleeding can be increased when Oxyphenbutazone is combined with Zoledronic acid.
Licofelone The risk or severity of gastrointestinal bleeding can be increased when Licofelone is combined with Zoledronic acid.
Nimesulide The risk or severity of gastrointestinal bleeding can be increased when Nimesulide is combined with Zoledronic acid.
Benoxaprofen The risk or severity of gastrointestinal bleeding can be increased when Benoxaprofen is combined with Zoledronic acid.
Metamizole The risk or severity of nephrotoxicity and hypocalcemia can be increased when Metamizole is combined with Zoledronic acid.
Zomepirac The risk or severity of gastrointestinal bleeding can be increased when Zomepirac is combined with Zoledronic acid.
Cimicoxib The risk or severity of gastrointestinal bleeding can be increased when Cimicoxib is combined with Zoledronic acid.
Lornoxicam The risk or severity of gastrointestinal bleeding can be increased when Lornoxicam is combined with Zoledronic acid.
Aceclofenac The risk or severity of gastrointestinal bleeding can be increased when Aceclofenac is combined with Zoledronic acid.
Zaltoprofen The risk or severity of gastrointestinal bleeding can be increased when Zaltoprofen is combined with Zoledronic acid.
Azapropazone The risk or severity of gastrointestinal bleeding can be increased when Azapropazone is combined with Zoledronic acid.
Parecoxib The risk or severity of gastrointestinal bleeding can be increased when Parecoxib is combined with Zoledronic acid.
Salicylamide The risk or severity of gastrointestinal bleeding can be increased when Salicylamide is combined with Zoledronic acid.
Kebuzone The risk or severity of gastrointestinal bleeding can be increased when Kebuzone is combined with Zoledronic acid.
Isoxicam The risk or severity of gastrointestinal bleeding can be increased when Isoxicam is combined with Zoledronic acid.
Indoprofen The risk or severity of gastrointestinal bleeding can be increased when Indoprofen is combined with Zoledronic acid.
Ibuproxam The risk or severity of gastrointestinal bleeding can be increased when Ibuproxam is combined with Zoledronic acid.
Floctafenine The risk or severity of gastrointestinal bleeding can be increased when Floctafenine is combined with Zoledronic acid.
Fenbufen The risk or severity of gastrointestinal bleeding can be increased when Fenbufen is combined with Zoledronic acid.
Etofenamate The risk or severity of gastrointestinal bleeding can be increased when Etofenamate is combined with Zoledronic acid.
Epirizole The risk or severity of gastrointestinal bleeding can be increased when Epirizole is combined with Zoledronic acid.
Benzydamine The risk or severity of gastrointestinal bleeding can be increased when Benzydamine is combined with Zoledronic acid.
Dexibuprofen The risk or severity of gastrointestinal bleeding can be increased when Dexibuprofen is combined with Zoledronic acid.
Dexketoprofen The risk or severity of gastrointestinal bleeding can be increased when Dexketoprofen is combined with Zoledronic acid.
Droxicam The risk or severity of gastrointestinal bleeding can be increased when Droxicam is combined with Zoledronic acid.
Tolfenamic acid The risk or severity of gastrointestinal bleeding can be increased when Tolfenamic acid is combined with Zoledronic acid.
Firocoxib The risk or severity of gastrointestinal bleeding can be increased when Firocoxib is combined with Zoledronic acid.
Clonixin The risk or severity of gastrointestinal bleeding can be increased when Clonixin is combined with Zoledronic acid.
Morniflumate The risk or severity of gastrointestinal bleeding can be increased when Morniflumate is combined with Zoledronic acid.
Propacetamol The risk or severity of gastrointestinal bleeding can be increased when Propacetamol is combined with Zoledronic acid.
Talniflumate The risk or severity of gastrointestinal bleeding can be increased when Talniflumate is combined with Zoledronic acid.
Robenacoxib The risk or severity of gastrointestinal bleeding can be increased when Robenacoxib is combined with Zoledronic acid.
Tepoxalin The risk or severity of gastrointestinal bleeding can be increased when Tepoxalin is combined with Zoledronic acid.
Flunixin The risk or severity of gastrointestinal bleeding can be increased when Flunixin is combined with Zoledronic acid.
Polmacoxib The risk or severity of gastrointestinal bleeding can be increased when Polmacoxib is combined with Zoledronic acid.
Nitroaspirin The risk or severity of gastrointestinal bleeding can be increased when Nitroaspirin is combined with Zoledronic acid.

Target Protein

Geranylgeranyl pyrophosphate synthase GGPS1
Hydroxylapatite
Farnesyl pyrophosphate synthase FDPS

Referensi & Sumber

Synthesis reference: Judith Aronhime, Revital Lifshitz-Liron, "Zoledronic acid crystal forms, zoledronate sodium salt crystal forms, amorphous zoledronate sodium salt, and processes for their preparation." U.S. Patent US20050054616, issued March 10, 2005.
Artikel (PubMed)
  • PMID: 17878149
    Lyles KW, Colon-Emeric CS, Magaziner JS, Adachi JD, Pieper CF, Mautalen C, Hyldstrup L, Recknor C, Nordsletten L, Moore KA, Lavecchia C, Zhang J, Mesenbrink P, Hodgson PK, Abrams K, Orloff JJ, Horowitz Z, Eriksen EF, Boonen S: Zoledronic acid and clinical fractures and mortality after hip fracture. N Engl J Med. 2007 Nov 1;357(18):1799-809. Epub 2007 Sep 17.
  • PMID: 11870242
    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: Intravenous zoledronic acid in postmenopausal women with low bone mineral density. N Engl J Med. 2002 Feb 28;346(9):653-61.
  • PMID: 16000365
    Durie BG, Katz M, Crowley J: Osteonecrosis of the jaw and bisphosphonates. N Engl J Med. 2005 Jul 7;353(1):99-102; discussion 99-102.
  • PMID: 28000034
    Shiraki M, Tanaka S, Suzuki H, Ueda S, Nakamura T: Safety, pharmacokinetics, and changes in bone metabolism associated with zoledronic acid treatment in Japanese patients with primary osteoporosis. J Bone Miner Metab. 2017 Nov;35(6):675-684. doi: 10.1007/s00774-016-0806-3. Epub 2016 Dec 20.
  • PMID: 30650219
    Cremers S, Drake MT, Ebetino FH, Bilezikian JP, Russell RGG: Pharmacology of bisphosphonates. Br J Clin Pharmacol. 2019 Jun;85(6):1052-1062. doi: 10.1111/bcp.13867. Epub 2019 Feb 28.
  • PMID: 18214569
    Russell RG, Watts NB, Ebetino FH, Rogers MJ: Mechanisms of action of bisphosphonates: similarities and differences and their potential influence on clinical efficacy. Osteoporos Int. 2008 Jun;19(6):733-59. doi: 10.1007/s00198-007-0540-8.
  • PMID: 9145236
    Murakami H, Takahashi N, Tanaka S, Nakamura I, Udagawa N, Nakajo S, Nakaya K, Abe M, Yuda Y, Konno F, Barbier A, Suda T: Tiludronate inhibits protein tyrosine phosphatase activity in osteoclasts. Bone. 1997 May;20(5):399-404.
  • PMID: 8053405
    Green JR, Muller K, Jaeggi KA: Preclinical pharmacology of CGP 42'446, a new, potent, heterocyclic bisphosphonate compound. J Bone Miner Res. 1994 May;9(5):745-51. doi: 10.1002/jbmr.5650090521.
Menampilkan 8 dari 13 artikel.

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