Tolvaptan

What is Tolvaptan

Tolvaptan is an oral selective vasopressin V2-receptor antagonist. One tolvaptan product, Samsca, is indicated for the treatment of clinically significant hypervolemic and euvolemic hyponatremia (i.e., serum sodium less than 125 mEq/L or less marked hyponatremia that is symptomatic and has resisted correction with fluid restriction), including in patients with heart failure and syndrome of inappropriate antidiuretic hormone (SIADH).

Samsca use requires initiation or reinitiation in a hospital setting, and should not be used for longer than 30 days due to the risk for liver problems.

Tolvaptan can cause serious and potentially fatal liver injury. Due to the risk of hepatic injury associated with tolvaptan, the drug should be avoided in patients with preexisting hepatic disease, including cirrhosis.

A second product, Jynarque, is used chronically to slow kidney function decline in patients with rapidly progressing autosomal dominant polycystic kidney disease (ADPKD).

Routine monitoring of liver function is required with the use of tolvaptan for ADPKD; prescribers, pharmacies, and patients must register with the Jynarque REMs program. More information is available at www.jynarque.com/risks-and-rems.

Brand Names

  • JYNARQUE
  • Samsca

Indications

  • autosomal dominant polycystic kidney disease
  • hyponatremia
  • SIADH

For the treatment of clinically significant hypervolemic and euvolemic hyponatremia (i.e., serum sodium less than 125 mEq/L or hyponatremia that is symptomatic and has resisted correction with fluid restriction), including in patients with heart failure and syndrome of inappropriate antidiuretic hormone (SIADH)

Side Effects

  1. anaphylactic shock
  2. anorexia
  3. asthenia
  4. bleeding
  5. colitis
  6. constipation
  7. dehydration
  8. diabetic ketoacidosis
  9. diarrhea
  10. disseminated intravascular coagulation (DIC)
  11. dizziness
  12. dyspepsia
  13. elevated hepatic enzymes
  14. fatigue
  15. fever
  16. GI bleeding
  17. hepatic failure
  18. hepatotoxicity
  19. hyperbilirubinemia
  20. hyperglycemia
  21. hyperkalemia
  22. hypernatremia
  23. hyperuricemia
  24. hypovolemia
  25. nausea
  26. osmotic demyelination syndrome
  27. palpitations
  28. polydipsia
  29. polyuria
  30. prolonged bleeding time
  31. pulmonary embolism
  32. rash
  33. respiratory depression
  34. rhabdomyolysis
  35. stroke
  36. thrombosis
  37. vaginal bleeding
  38. ventricular fibrillation
  39. xerostomia

Monitoring Parameters

  • LFTs
  • serum bilirubin
  • serum potassium
  • serum sodium

Contraindications

  • alcoholism
  • anuria
  • autosomal dominant polycystic kidney disease
  • breast-feeding
  • dehydration
  • geriatric
  • hepatic disease
  • hepatotoxicity
  • hyperkalemia
  • hypernatremia
  • hyponatremia
  • hypovolemia
  • malnutrition
  • osmotic demyelination syndrome
  • pregnancy
  • requires a specialized care setting
  • urinary tract obstruction

Interactions

  • Abacavir; Dolutegravir; Lamivudine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Aliskiren; Hydrochlorothiazide, HCTZ
  • Aliskiren; Valsartan
  • Amiloride
  • Amiloride; Hydrochlorothiazide, HCTZ
  • Amiodarone
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amprenavir
  • Angiotensin-converting enzyme inhibitors
  • Apalutamide
  • Aprepitant, Fosaprepitant
  • Argatroban
  • Aspirin, ASA; Pravastatin
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atenolol; Chlorthalidone
  • Atorvastatin
  • Atorvastatin; Ezetimibe
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Azilsartan
  • Azilsartan; Chlorthalidone
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Benazepril
  • Benazepril; Hydrochlorothiazide, HCTZ
  • Bendroflumethiazide; Nadolol
  • Bexarotene
  • Bisoprolol; Hydrochlorothiazide, HCTZ
  • Bivalirudin
  • Boceprevir
  • Bosentan
  • Brigatinib
  • Bumetanide
  • Cabozantinib
  • Candesartan
  • Candesartan; Hydrochlorothiazide, HCTZ
  • Capmatinib
  • Captopril
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  • Carbamazepine
  • Carvedilol
  • Ceritinib
  • Chloramphenicol
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  • Chlorthalidone
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  • Cimetidine
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  • Clindamycin
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  • Conivaptan
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  • Cyclosporine
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  • Danazol
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  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
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  • Dronedarone
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  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Duvelisib
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  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elbasvir; Grazoprevir
  • Elexacaftor; tezacaftor; ivacaftor
  • Eliglustat
  • Eluxadoline
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
  • Emtricitabine; Tenofovir disoproxil fumarate
  • Enalapril, Enalaprilat
  • Enalapril; Felodipine
  • Enalapril; Hydrochlorothiazide, HCTZ
  • Encorafenib
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  • Eslicarbazepine
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  • Ethinyl Estradiol; Norelgestromin
  • Ethinyl Estradiol; Norethindrone
  • Ethinyl Estradiol; Norethindrone Acetate
  • Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
  • Ethinyl Estradiol; Norethindrone; Ferrous fumarate
  • Ethinyl Estradiol; Norgestimate
  • Ethinyl Estradiol; Norgestrel
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  • Glyburide
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  • grapefruit juice
  • Heparin
  • Hetastarch
  • Hydralazine; Hydrochlorothiazide, HCTZ
  • Hydrochlorothiazide, HCTZ
  • Hydrochlorothiazide, HCTZ; Irbesartan
  • Hydrochlorothiazide, HCTZ; Lisinopril
  • Hydrochlorothiazide, HCTZ; Losartan
  • Hydrochlorothiazide, HCTZ; Methyldopa
  • Hydrochlorothiazide, HCTZ; Metoprolol
  • Hydrochlorothiazide, HCTZ; Moexipril
  • Hydrochlorothiazide, HCTZ; Olmesartan
  • Hydrochlorothiazide, HCTZ; Propranolol
  • Hydrochlorothiazide, HCTZ; Quinapril
  • Hydrochlorothiazide, HCTZ; Spironolactone
  • Hydrochlorothiazide, HCTZ; Telmisartan
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  • Hydrochlorothiazide, HCTZ; Valsartan
  • Ibritumomab Tiuxetan
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  • Irbesartan
  • Isavuconazonium
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  • Istradefylline
  • Itraconazole
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  • Ketoconazole
  • Lamivudine; Tenofovir Disoproxil Fumarate
  • Ledipasvir; Sofosbuvir
  • Lefamulin
  • Lesinurad
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  • Lumacaftor; Ivacaftor
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  • Mifepristone
  • Mitotane
  • Modafinil
  • Moexipril
  • Moxifloxacin
  • Nafcillin
  • Nateglinide
  • Nebivolol; Valsartan
  • Nefazodone
  • Nelfinavir
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  • Niacin; Simvastatin
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  • Ondansetron
  • Osimertinib
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  • Perindopril
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  • Potassium Chloride
  • Potassium-sparing diuretics
  • Pravastatin
  • Primidone
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  • Quinapril
  • Quinidine
  • Quinine
  • Ramipril
  • Ranolazine
  • Regular Insulin
  • Repaglinide
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  • Rifampin
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  • Rimegepant
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  • Simvastatin; Sitagliptin
  • Sodium Chloride
  • Sofosbuvir; Velpatasvir
  • Sofosbuvir; Velpatasvir; Voxilaprevir
  • Sorafenib
  • Spironolactone
  • St. John’s Wort, Hypericum perforatum
  • Telaprevir
  • Telithromycin
  • Telmisartan
  • Temsirolimus
  • Tenofovir Alafenamide
  • Tenofovir, PMPA
  • Testosterone
  • Tezacaftor; Ivacaftor
  • Thiazide diuretics
  • Tipranavir
  • Tobramycin
  • Topiramate
  • Topotecan
  • Torsemide
  • Trandolapril
  • Trandolapril; Verapamil
  • Tranexamic Acid
  • Triamterene
  • Tucatinib
  • Valsartan
  • Vancomycin
  • Vemurafenib
  • Venetoclax
  • Verapamil
  • Voriconazole
  • Zonisamide
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