Peringatan Keamanan

Patients experiencing an overdose may present with hypocalcemia.L4763 Patients given doses of 6mg/kg/day for 2 days have experienced acute renal failure and death.L4763 Treat overdose with symptomatic and supportive care.L4763 Dialysis will not be useful for removal of the drug from serum.L4763

Tiludronic acid

DB01133

small molecule approved investigational vet_approved

Deskripsi

Tiludronate, or (4-chlorophenyl)thio-methylene-1,1-bisphosphonate, is a first generation bisphosphonate similar to etidronic acid and clodronic acid.A1923,A203111 These drugs were developed to mimic the action of pyrophosphate, a regulator of calcification and decalcification.A1923 Tiludronic acid was first described in the literature in 1988 as a potential treatment for Paget's disease of bone.A202235

Tiludronic acid was granted FDA approval on 7 March 1997.L4763

Struktur Molekul 2D

Berat 318.608
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean plasma elimination half-life is 150 hours, though the elimination rate from bone is unknown.[L4763] The terminal phase half life is approximately 40h after a single IV dose of 10-30mg.[A1923]
Volume Distribusi The volume of distribution of tiludronic acid is estimated to be between 30L and 60L.[A1923] Due to the unknown clearance rate from bone, this may underestimate the true volume of distribution.[A1923]
Klirens (Clearance) Tiludronic acid has a renal clearance of 0.68L/h in healthy subjects and 0.47L/h in subjects with Paget's disease.[A1923,L4763] Approximately 50% of tilurdronic acid binds to bone but the rate of clearance from the bone is unknown.[A1923]

Absorpsi

A single 400mg dose of tiludronic acid reaches a Cmax of 3.35±1.07mg/L, with a Tmax of 1.7—0.9h, and and AUC of 27.2±9.0mg\*h/L.A1923 Tiludronic acid has an oral bioavailability of 2-11% with an average of 6%.A1923

Metabolisme

Tiludronic acid is not metabolized in vitro in human liver microsomes.L4763

Rute Eliminasi

Tiludronic acid is 60% eliminated in the urine as the unchanged parent drug.L4763

Interaksi Makanan

4 Data
  • 1. Take at least 2 hours before or after calcium supplements.
  • 2. Take on an empty stomach. Take at least 2 hours before or after meals.
  • 3. Take separate from antacids. Take at least 2 hours before or after antacids. The bioavailability of this medication is significantly reduced when administered with aluminum or magnesium containing antacids.
  • 4. Take with a full glass of water.

Interaksi Obat

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

Target Protein

Hydroxylapatite
Adenosine triphosphate (ATP)
Tyrosine-protein phosphatase non-receptor type 12 PTPN12
Tyrosine-protein phosphatase non-receptor type 6 PTPN6
Receptor-type tyrosine-protein phosphatase epsilon PTPRE
V-ATPase Subunits ATP6V0A1

Referensi & Sumber

Synthesis reference: William Rocco, Sharon M. Laughlin, "Stable pharmaceutical compositions containing tiludronate hydrates and process for producing the pharmaceutical compositions." U.S. Patent US5656288, issued April, 1995.
Artikel (PubMed)
  • PMID: 8573422
    Sansom LN, Necciari J, Thiercelin JF: Human pharmacokinetics of tiludronate. Bone. 1995 Nov;17(5 Suppl):479S-483S.
  • 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: 22652318
    Qin A, Cheng TS, Pavlos NJ, Lin Z, Dai KR, Zheng MH: V-ATPases in osteoclasts: structure, function and potential inhibitors of bone resorption. Int J Biochem Cell Biol. 2012 Sep;44(9):1422-35. doi: 10.1016/j.biocel.2012.05.014. Epub 2012 May 29.
  • 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: 3073800
    Reginster JY, Jeugmans-Huynen AM, Albert A, Denis D, Deroisy R, Lecart MP, Fontaine MA, Collette J, Franchimont P: Biological and clinical assessment of a new bisphosphonate, (chloro-4 phenyl) thiomethylene bisphosphonate, in the treatment of Paget's disease of bone. Bone. 1988;9(6):349-54. doi: 10.1016/8756-3282(88)90115-9.
  • PMID: 30555553
    Duan X, Yang S, Zhang L, Yang T: V-ATPases and osteoclasts: ambiguous future of V-ATPases inhibitors in osteoporosis. Theranostics. 2018 Oct 26;8(19):5379-5399. doi: 10.7150/thno.28391. eCollection 2018.
  • 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.

Contoh Produk & Brand

Produk: 1 • International brands: 0
Produk
  • Skelid
    Tablet • 200 mg/1 • Oral • US • Approved

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