Peringatan Keamanan

The oral LD50 of tolvaptan in rats and dogs is >2000 mg/kg. Most common adverse reactions (?5% placebo) are thirst, dry mouth, asthenia, constipation, pollakiuria or polyuria, and hyperglycemia.

Tolvaptan

DB06212

small molecule approved

Deskripsi

Tolvaptan is used to treat low blood sodium levels (hyponatremia) associated with various conditions like congestive heart failure, cirrhosis, and syndrome of inappropriate antidiuretic hormones (SIADH). FDA approved on May 19, 2009.

Struktur Molekul 2D

Berat 448.941
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Terminal half life, oral dose = 12 hours.
Volume Distribusi Healthy subjects: 3L/kg; slightly higher in heart failure patients.
Klirens (Clearance) 4 mL/min/kg (post-oral dosing).

Absorpsi

Tmax, Healthy subjects: 2 - 4 hours; Cmax, Healthy subjects, 30 mg: 374 ng/mL; Cmax, Healthy subjects, 90 mg: 418 ng/mL; Cmax, heart failure patients, 30 mg: 460 ng/mL; Cmax, heart failure patients, 90 mg: 723 ng/mL; AUC(0-24 hours), 60 mg: 3.71 ?g·h/mL; AUC(?), 60 mg: 4.55 ?g·h/mL; The pharmacokinetic properties of tolvaptan are stereospecific, with a steady-state ratio of the S-(-) to the R-(+) enantiomer of about 3. The absolute bioavailability of tolvaptan is unknown. At least 40% of the dose is absorbed as tolvaptan or metabolites. Food does not impact the bioavailability of tolvaptan.

Metabolisme

Metabolism exclusively by CYP3A4 enzyme in the liver. Metabolites are inactive.

Rute Eliminasi

Fecal- very little renal elimination (<1% is excreted unchanged in the urine)

Interaksi Makanan

4 Data
  • 1. Avoid excessive or chronic alcohol consumption. This may increase the risk of developing osmotic demyelination syndrome.
  • 2. Avoid grapefruit products. Grapefruit inhibits the CYP3A metabolism of tolvaptan, which may increase its serum concentration.
  • 3. Avoid St. John's Wort. This herb induces the CYP3A metabolism of tolvaptan and may reduce its serum concentration.
  • 4. Take with or without food.

Interaksi Obat

1350 Data
Desmopressin The therapeutic efficacy of Desmopressin can be decreased when used in combination with Tolvaptan.
Modafinil The metabolism of Tolvaptan can be increased when combined with Modafinil.
Armodafinil The metabolism of Tolvaptan can be increased when combined with Armodafinil.
Ranolazine The serum concentration of Tolvaptan can be increased when it is combined with Ranolazine.
Valsartan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Valsartan.
Olmesartan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Olmesartan.
Losartan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Losartan.
Candesartan cilexetil The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Candesartan cilexetil.
Eprosartan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Eprosartan.
Telmisartan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Telmisartan.
Irbesartan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Irbesartan.
Forasartan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Forasartan.
Saprisartan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Saprisartan.
Tasosartan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Tasosartan.
Saralasin The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Saralasin.
Azilsartan medoxomil The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Azilsartan medoxomil.
Fimasartan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Fimasartan.
Candesartan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Candesartan.
Ramipril Tolvaptan may increase the hyperkalemic activities of Ramipril.
Fosinopril Tolvaptan may increase the hyperkalemic activities of Fosinopril.
Trandolapril Tolvaptan may increase the hyperkalemic activities of Trandolapril.
Benazepril Tolvaptan may increase the hyperkalemic activities of Benazepril.
Enalapril Tolvaptan may increase the hyperkalemic activities of Enalapril.
Moexipril Tolvaptan may increase the hyperkalemic activities of Moexipril.
Lisinopril Tolvaptan may increase the hyperkalemic activities of Lisinopril.
Perindopril Tolvaptan may increase the hyperkalemic activities of Perindopril.
Quinapril Tolvaptan may increase the hyperkalemic activities of Quinapril.
Omapatrilat Tolvaptan may increase the hyperkalemic activities of Omapatrilat.
Rescinnamine Tolvaptan may increase the hyperkalemic activities of Rescinnamine.
Captopril Tolvaptan may increase the hyperkalemic activities of Captopril.
Cilazapril Tolvaptan may increase the hyperkalemic activities of Cilazapril.
Spirapril Tolvaptan may increase the hyperkalemic activities of Spirapril.
Temocapril Tolvaptan may increase the hyperkalemic activities of Temocapril.
Enalaprilat Tolvaptan may increase the hyperkalemic activities of Enalaprilat.
Imidapril Tolvaptan may increase the hyperkalemic activities of Imidapril.
Zofenopril Tolvaptan may increase the hyperkalemic activities of Zofenopril.
Delapril Tolvaptan may increase the hyperkalemic activities of Delapril.
Benazeprilat Tolvaptan may increase the hyperkalemic activities of Benazeprilat.
Fosinoprilat Tolvaptan may increase the hyperkalemic activities of Fosinoprilat.
Ramiprilat Tolvaptan may increase the hyperkalemic activities of Ramiprilat.
Trandolaprilat Tolvaptan may increase the hyperkalemic activities of Trandolaprilat.
Moexiprilat Tolvaptan may increase the hyperkalemic activities of Moexiprilat.
Perindoprilat Tolvaptan may increase the hyperkalemic activities of Perindoprilat.
Quinaprilat Tolvaptan may increase the hyperkalemic activities of Quinaprilat.
Cilazaprilat Tolvaptan may increase the hyperkalemic activities of Cilazaprilat.
Metreleptin The metabolism of Tolvaptan can be increased when combined with Metreleptin.
Crizotinib The metabolism of Tolvaptan can be decreased when combined with Crizotinib.
Sodium chloride The risk or severity of adverse effects can be increased when Sodium chloride is combined with Tolvaptan.
Lumacaftor The serum concentration of Tolvaptan can be decreased when it is combined with Lumacaftor.
Icosapent The risk or severity of hyperkalemia can be increased when Icosapent is combined with Tolvaptan.
Esmolol The risk or severity of hyperkalemia can be increased when Esmolol is combined with Tolvaptan.
Betaxolol The risk or severity of hyperkalemia can be increased when Betaxolol is combined with Tolvaptan.
Succinylcholine The risk or severity of hyperkalemia can be increased when Succinylcholine is combined with Tolvaptan.
Mesalazine The risk or severity of hyperkalemia can be increased when Mesalazine is combined with Tolvaptan.
Atenolol The risk or severity of hyperkalemia can be increased when Atenolol is combined with Tolvaptan.
Triamterene The risk or severity of hyperkalemia can be increased when Triamterene is combined with Tolvaptan.
Ardeparin The risk or severity of hyperkalemia can be increased when Ardeparin is combined with Tolvaptan.
Spironolactone The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Spironolactone.
Nabumetone The risk or severity of hyperkalemia can be increased when Nabumetone is combined with Tolvaptan.
Ketorolac The risk or severity of hyperkalemia can be increased when Ketorolac is combined with Tolvaptan.
Tenoxicam The risk or severity of hyperkalemia can be increased when Tenoxicam is combined with Tolvaptan.
Sotalol The risk or severity of hyperkalemia can be increased when Sotalol is combined with Tolvaptan.
Tolmetin The risk or severity of hyperkalemia can be increased when Tolmetin is combined with Tolvaptan.
Fenoprofen The risk or severity of hyperkalemia can be increased when Fenoprofen is combined with Tolvaptan.
Amiloride The risk or severity of hyperkalemia can be increased when Amiloride is combined with Tolvaptan.
Sulindac The risk or severity of hyperkalemia can be increased when Sulindac is combined with Tolvaptan.
Pentamidine The risk or severity of hyperkalemia can be increased when Pentamidine is combined with Tolvaptan.
Mefenamic acid The risk or severity of hyperkalemia can be increased when Mefenamic acid is combined with Tolvaptan.
Naproxen The risk or severity of hyperkalemia can be increased when Naproxen is combined with Tolvaptan.
Sulfasalazine The risk or severity of hyperkalemia can be increased when Sulfasalazine is combined with Tolvaptan.
Carprofen The risk or severity of hyperkalemia can be increased when Carprofen is combined with Tolvaptan.
Alprenolol The risk or severity of hyperkalemia can be increased when Alprenolol is combined with Tolvaptan.
Salicylic acid The risk or severity of hyperkalemia can be increased when Salicylic acid is combined with Tolvaptan.
Balsalazide The risk or severity of hyperkalemia can be increased when Balsalazide is combined with Tolvaptan.
Heparin The risk or severity of hyperkalemia can be increased when Heparin is combined with Tolvaptan.
Enoxaparin The risk or severity of hyperkalemia can be increased when Enoxaparin is combined with Tolvaptan.
Lumiracoxib The risk or severity of hyperkalemia can be increased when Lumiracoxib is combined with Tolvaptan.
Bevantolol The risk or severity of hyperkalemia can be increased when Bevantolol is combined with Tolvaptan.
Practolol The risk or severity of hyperkalemia can be increased when Practolol is combined with Tolvaptan.
Magnesium salicylate The risk or severity of hyperkalemia can be increased when Magnesium salicylate is combined with Tolvaptan.
Salsalate The risk or severity of hyperkalemia can be increased when Salsalate is combined with Tolvaptan.
Choline magnesium trisalicylate The risk or severity of hyperkalemia can be increased when Choline magnesium trisalicylate is combined with Tolvaptan.
Antrafenine The risk or severity of hyperkalemia can be increased when Antrafenine is combined with Tolvaptan.
Oxprenolol The risk or severity of hyperkalemia can be increased when Oxprenolol is combined with Tolvaptan.
Tiaprofenic acid The risk or severity of hyperkalemia can be increased when Tiaprofenic acid is combined with Tolvaptan.
Penicillin G Acyl-Serine The risk or severity of hyperkalemia can be increased when Penicillin G Acyl-Serine is combined with Tolvaptan.
Oxyphenbutazone The risk or severity of hyperkalemia can be increased when Oxyphenbutazone is combined with Tolvaptan.
Benoxaprofen The risk or severity of hyperkalemia can be increased when Benoxaprofen is combined with Tolvaptan.
Cimicoxib The risk or severity of hyperkalemia can be increased when Cimicoxib is combined with Tolvaptan.
Methsuximide The risk or severity of hyperkalemia can be increased when Methsuximide is combined with Tolvaptan.
Sulodexide The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Sulodexide.
Lornoxicam The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Lornoxicam.
Bufuralol The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Bufuralol.
Zaltoprofen The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Zaltoprofen.
Danaparoid The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Danaparoid.
Dalteparin The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Dalteparin.
Tinzaparin The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Tinzaparin.
Azapropazone The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Azapropazone.
Salicylamide The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Salicylamide.
Bopindolol The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Bopindolol.

Target Protein

Vasopressin V2 receptor AVPR2
Vasopressin V1a receptor AVPR1A

Referensi & Sumber

Synthesis reference: Bandi Parthasaradhi Reddy, "PROCESS FOR PREPARING TOLVAPTAN INTERMEDIATES." U.S. Patent US20130190490, issued July 25, 2013.
Artikel (PubMed)
  • PMID: 16181825
    Gheorghiade M, Teerlink JR, Mebazaa A: Pharmacology of new agents for acute heart failure syndromes. Am J Cardiol. 2005 Sep 19;96(6A):68G-73G.
  • PMID: 21401442
    Ambrosy A, Goldsmith SR, Gheorghiade M: Tolvaptan for the treatment of heart failure: a review of the literature. Expert Opin Pharmacother. 2011 Apr;12(6):961-76. doi: 10.1517/14656566.2011.567267. Epub 2011 Mar 15.
  • PMID: 22130104
    Yi S, Jeon H, Yoon SH, Cho JY, Shin SG, Jang IJ, Yu KS: Pharmacokinetics and pharmacodynamics of oral tolvaptan administered in 15- to 60-mg single doses to healthy Korean men. J Cardiovasc Pharmacol. 2012 Apr;59(4):315-22. doi: 10.1097/FJC.0b013e318241e89c.
  • PMID: 20637957
    Nemerovski C, Hutchinson DJ: Treatment of hypervolemic or euvolemic hyponatremia associated with heart failure, cirrhosis, or the syndrome of inappropriate antidiuretic hormone with tolvaptan: a clinical review. Clin Ther. 2010 Jun;32(6):1015-32. doi: 10.1016/j.clinthera.2010.06.015.

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