What is Tolvaptan?

Commonly Used Brand Name(s)Jynarque, Samsca

Therapeutic ClassificationsEndocrine-Metabolic Agent

Pharmacologic ClassificationsVasopressin Receptor Antagonist, V2

Blackbox WarningTOP

Oral route (Tablet)

Samsca (R) should be initiated and re-initiated in patients only in a hospital where serum sodium can be monitored closely. Too-rapid correction of hyponatremia (eg, greater than 12 mEq/L/24 hours) can cause osmotic demyelination resulting in dysarthria, mutism, dysphagia, lethargy, affective changes, spastic quadriparesis, seizures, coma, and death. Slower rates of correction may be advisable in susceptible patients (eg, those with severe malnutrition, alcoholism, or advanced liver disease) .Samsca (R) Not For Use For Autosomal Dominant Polycystic Kidney Disease (ADPKD): Because of the risk of hepatoxicity, tolvaptan should not be used for ADPKD outside of the FDA-approved REMS .

Oral route (Tablet)

Warning: Risk Of Serious Liver Injury:Jynarque (TM) (tolvaptan) can cause serious and potentially fatal liver injury. Acute liver failure requiring liver transplantation has been reported.Measure ALT, AST and bilirubin before initiating treatment, at 2 weeks and 4 weeks after initiation, then monthly for the first 18 months and every 3 months thereafter. Prompt action in response to laboratory abnormalities, signs, or symptoms indicative of hepatic injury can mitigate, but not eliminate, the risk of serious hepatotoxicity.Because of the risks of serious liver injury, Jynarque (TM) is available only through a restricted distribution program under a Risk Evaluation and Mitigation Strategy (REMS) called the Jynarque (TM) REMS Program .

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OverviewTOP

Tolvaptan is used to treat hyponatremia (low sodium in the blood) in patients with heart failure or syndrome of inappropriate antidiuretic hormone (SIADH).

Tolvaptan is also used to slow kidney function decline in adults who are at risk of rapidly progressing autosomal dominant polycystic kidney disease (ADPKD).

Sodium is a chemical that the body needs for it to function well. If you have a low sodium blood level, your body will not function normally and you may not feel well. Tolvaptan works in the kidneys to help maintain the right amount of sodium for the body.

Samsca® is available only with your doctor's prescription. Jynarque™ is available only under a restricted distribution program called the Jynarque™ REMS (Risk Evaluation and Mitigation Strategy) Program.

Proper UseTOP

Take this medicine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

It is important that you take your first dose or restart your treatment with this medicine in a hospital or medical facility. This will allow your doctor to check your response to this medicine and monitor any unwanted problems that may occur.

This medicine should come with a Medication Guide. Read and follow these instructions carefully. Ask your doctor if you have any questions.

You may take this medicine with or without food.

This medicine is not for long-term use. You should not take Samsca® for more than 30 days to lessen your risk of having liver injury.

DosingTOP

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

For oral dosage form (tablets):
- For hyponatremia:
  - Adults—At first, 15 milligrams (mg) once a day. Your doctor will adjust your dose as needed. However, the dose is usually not more than 60 mg per day.
  - Children—Use and dose must be determined by your doctor.
- For slowing kidney function decline in patients who are at risk of autosomal dominant polycystic kidney disease (ADPKD):
  - Adults—At first, 60 milligrams (mg) per day (45 mg upon waking, then 15 mg taken 8 hours after). Your doctor will adjust your dose as needed and tolerated.
  - Children—Use and dose must be determined by your doctor.

Missed DoseTOP

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

If you miss a dose of Jynarque™, skip the missed dose, and go back to your regular dosing schedule.

Use & StorageTOP

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Before UsingTOP

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

AllergiesTOP

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

PediatricTOP

Appropriate studies have not been performed on the relationship of age to the effects of tolvaptan in the pediatric population. Safety and efficacy have not been established.

GeriatricTOP

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of tolvaptan in the elderly. However, elderly patients are more likely to have age-related liver, kidney, or heart problems, which may require caution and an adjustment in the dose for patients receiving tolvaptan.

PregnancyTOP

	Pregnancy Category	Explanation
All Trimesters	C	Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast FeedingTOP

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Drug InteractionsTOP

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

Boceprevir
Clarithromycin
Cobicistat
Conivaptan
Delavirdine
Idelalisib
Indinavir
Itraconazole
Ketoconazole
Lopinavir
Nefazodone
Nelfinavir
Posaconazole
Ritonavir
Saquinavir
Telaprevir
Telithromycin
Tipranavir
Voriconazole

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

Acyclovir
Amobarbital
Amprenavir
Aprepitant
Atazanavir
Atorvastatin
Baricitinib
Bosentan
Butabarbital
Carbamazepine
Ceritinib
Ciprofloxacin
Crizotinib
Cyclosporine
Desmopressin
Digoxin
Diltiazem
Dronedarone
Efavirenz
Eliglustat
Enzalutamide
Erythromycin
Fluconazole
Fluvoxamine
Fosamprenavir
Fosaprepitant
Fosnetupitant
Fosphenytoin
Furosemide
Glyburide
Grazoprevir
Imatinib
Irinotecan
Letermovir
Lumacaftor
Methotrexate
Mitotane
Modafinil
Netupitant
Nevirapine
Nilotinib
Oxcarbazepine
Pentobarbital
Phenobarbital
Phenytoin
Pioglitazone
Pitavastatin
Repaglinide
Rifabutin
Rifampin
Rifapentine
Rosuvastatin
Secobarbital
Simeprevir
Simvastatin
St John's Wort
Sulfasalazine
Tenofovir Alafenamide
Topotecan
Valacyclovir
Verapamil
Vincristine
Vincristine Sulfate Liposome

Other InteractionsTOP

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

Grapefruit Juice

PrecautionsTOP

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly and to decide if you should continue to use it. Blood tests may be needed to check for unwanted effects.

You should not use tolvaptan together with clarithromycin (Biaxin®), indinavir (Crixivan®), itraconazole (Sporanox®), ketoconazole (Nizoral®), nefazodone (Serzone®), nelfinavir (Viracept®), ritonavir (Norvir®), saquinavir (Fortovase®, Invirase®), or telithromycin (Ketek®). Using these medicines together may increase risk for more serious side effects.

Check with your doctor right away if you have drowsiness, confusion, mood changes, muscle weakness in the arms or legs, seizures (convulsions), or trouble with speaking, swallowing, or controlling body movements. These may be symptoms of a serious and rare condition called osmotic demyelination syndrome (ODS). This may occur if the sodium blood level rises too fast.

Check with your doctor right away if you have pain or tenderness in the upper stomach, pale stools, dark urine, loss of appetite, nausea, vomiting, or yellow eyes or skin. These could be symptoms of a serious liver problem.

Certain medicines or illnesses, such as vomiting or diarrhea, may cause you to lose too much body water (dehydration). If you think you are dehydrated, tell your doctor right away. Always have water available to drink if you are thirsty, unless your doctor tells you otherwise.

Ask your doctor first before you use any medicine or salt substitutes that contain potassium.

You should not eat grapefruit or drink grapefruit juice while you are using this medicine. Grapefruit or grapefruit juice may increase the effects of tolvaptan in your body.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (eg, St. John's wort) or vitamin supplements.