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
- anaphylactic shock
- anorexia
- asthenia
- bleeding
- colitis
- constipation
- dehydration
- diabetic ketoacidosis
- diarrhea
- disseminated intravascular coagulation (DIC)
- dizziness
- dyspepsia
- elevated hepatic enzymes
- fatigue
- fever
- GI bleeding
- hepatic failure
- hepatotoxicity
- hyperbilirubinemia
- hyperglycemia
- hyperkalemia
- hypernatremia
- hyperuricemia
- hypovolemia
- nausea
- osmotic demyelination syndrome
- palpitations
- polydipsia
- polyuria
- prolonged bleeding time
- pulmonary embolism
- rash
- respiratory depression
- rhabdomyolysis
- stroke
- thrombosis
- vaginal bleeding
- ventricular fibrillation
- 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
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- Bendroflumethiazide; Nadolol
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- Cabozantinib
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- Eluxadoline
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
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- Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
- Emtricitabine; Tenofovir disoproxil fumarate
- Enalapril, Enalaprilat
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- Ethinyl Estradiol
- Ethinyl Estradiol; Desogestrel
- Ethinyl Estradiol; Ethynodiol Diacetate
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- Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
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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
- Etravirine
- Ezetimibe; Simvastatin
- Fedratinib
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- Gemcitabine
- Gentamicin
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- Glyburide
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- grapefruit juice
- Heparin
- Hetastarch
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- Hydrochlorothiazide, HCTZ; Methyldopa
- Hydrochlorothiazide, HCTZ; Metoprolol
- Hydrochlorothiazide, HCTZ; Moexipril
- Hydrochlorothiazide, HCTZ; Olmesartan
- Hydrochlorothiazide, HCTZ; Propranolol
- Hydrochlorothiazide, HCTZ; Quinapril
- Hydrochlorothiazide, HCTZ; Spironolactone
- Hydrochlorothiazide, HCTZ; Telmisartan
- Hydrochlorothiazide, HCTZ; Triamterene
- Hydrochlorothiazide, HCTZ; Valsartan
- Ibritumomab Tiuxetan
- Ibrutinib
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- Imatinib
- Indinavir
- Irbesartan
- Isavuconazonium
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- Mitotane
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- Nafcillin
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- Nefazodone
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- Nevirapine
- Niacin; Simvastatin
- Nicardipine
- Nilotinib
- Olmesartan
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- Omeprazole; Amoxicillin; Rifabutin
- Ondansetron
- Osimertinib
- Oxcarbazepine
- Paclitaxel
- Pazopanib
- Perindopril
- Perindopril; Amlodipine
- Phenobarbital
- Phentermine; Topiramate
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- Pitavastatin
- Ponatinib
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- Potassium Chloride
- Potassium-sparing diuretics
- Pravastatin
- Primidone
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- Ribociclib
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- Simvastatin; Sitagliptin
- Sodium Chloride
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- St. John’s Wort, Hypericum perforatum
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- Testosterone
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- Tipranavir
- Tobramycin
- Topiramate
- Topotecan
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- Tranexamic Acid
- Triamterene
- Tucatinib
- Valsartan
- Vancomycin
- Vemurafenib
- Venetoclax
- Verapamil
- Voriconazole
- Zonisamide
