FDA-filed SPL labeling · retrieved through openFDA

Tolvaptan

Tolvaptan is an oral tablet used to treat low blood sodium levels (hyponatremia) and, under a special safety program, to slow kidney cyst growth in autosomal dominant polycystic kidney disease (ADPKD).

Brand names JynarqueSamsca
Drug class ⓘ Vasopressin V2 Receptor Antagonist
Rx Form 1 Route Oral
Dr. Brian Staiger, PharmD, BCPS
Reviewed by Last reviewed Jul 10, 2026
🧬 Where this information comes from Click to expand

The clinical label records used on this page are FDA-filed Structured Product Labeling (SPL) retrieved through openFDA. We identified 10 clinical label sets within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. Forms, routes, brands, labelers, strengths, and NDC product-record counts are built separately from matching FDA National Drug Code Directory records. The linked DailyMed document is a representative official source for verification, not the page’s only clinical source. View the linked label on DailyMed →

At a glance
Linked label effectiveNov 6, 2025
Clinical labels in scope ⓘ10
AvailabilityRx
Earliest approval/marketing year ⓘ2009
FDA-listed product records ⓘ89
Boxed warningYes
How we combine label and product data →
✓No current FDA shortage listed · checked Sep 19, 2026
⭐ Tolvaptan at a glance The quick version — the full detail is in the Patient Information Guide below.
💊
HelloPharmacist Editorial Team Bottom Line
Tolvaptan is a prescription tablet that raises low blood sodium or slows ADPKD kidney cyst growth, depending on which product is prescribed. It carries serious risks — including dangerously fast sodium correction and liver injury — so it must be started under close medical supervision and monitored regularly. Always follow your prescriber's dosing and monitoring plan, drink fluids as directed, and report any liver-related symptoms right away.
How we write & review this content — our editorial policy →
⚠️ FDA Boxed Warning — the FDA’s strongest safety alert ▾

This medication carries two critical boxed warnings from the FDA.

First: When you first start tolvaptan (or restart it), you must be in a hospital so that your blood sodium can be closely monitored. If sodium rises too fast in the blood, it can cause a rare but life-threatening nerve condition called osmotic demyelination — leading to difficulty speaking, swallowing, or moving, and in severe cases, coma or death. People who are severely malnourished, have alcoholism, or have advanced liver disease face the highest risk.

Second: Tolvaptan should NOT be used for ADPKD outside of the FDA-approved restricted safety program (REMS) because it can cause serious liver damage. Only products enrolled in this program — such as Jynarque — are approved for ADPKD use.

Read the full warning on DailyMed →

📖 Tolvaptan: Patient Information Guide

A plain-language walkthrough of Tolvaptan — what it treats, how it works, how it’s taken, side effects, warnings and interactions. Tap any section to expand it.

🎯What it's used for▾

Tolvaptan tablets are used for two distinct conditions, depending on the specific product prescribed.

  • Samsca is indicated for the treatment of clinically significant hyponatremia (low blood sodium) that occurs with too much fluid in the body or normal fluid levels — for example, in people with heart failure, liver cirrhosis, or a condition called SIADH (syndrome of inappropriate antidiuretic hormone).
  • Jynarque (and the tolvaptan tablet REMS product) is used to slow the worsening of kidney function in adults with autosomal dominant polycystic kidney disease (ADPKD). Because of serious liver risks, it is only available through a strict FDA-approved restricted access program.
⚙️How it works▾

Tolvaptan works by blocking the vasopressin V2 receptor — a docking site in the kidneys that the hormone vasopressin uses to signal the body to hold onto water. When tolvaptan blocks this receptor, the kidneys release more water in the urine (a process called aquaresis), which helps raise blood sodium levels. In ADPKD, blocking this receptor also lowers levels of a chemical messenger called cAMP inside kidney cells, which slows the growth and enlargement of fluid-filled kidney cysts.

💊How it's taken▾

Tolvaptan is taken by mouth as a tablet and can be taken with or without food — a high-fat meal may increase peak levels but does not change overall exposure. The dosing schedule is different depending on which product you use.

  • Samsca is taken once daily and must be started in a hospital; it should not be taken for more than 30 days.
  • Jynarque is taken as two separate doses each day — one in the morning when you wake up, and one about 8 hours later. Doses are increased gradually over time if tolerated.

If you miss a dose of Jynarque, skip it and take your next scheduled dose at the usual time — do not double up. Always drink enough fluids to satisfy your thirst while on tolvaptan.

🤒Side effects — in detail▾

The most commonly reported side effects with tolvaptan include:

  • Increased thirst
  • Dry mouth
  • More frequent or larger amounts of urination
  • Weakness or fatigue
  • Constipation
  • High blood sugar (hyperglycemia)

More serious reactions — including signs of liver damage (yellowing skin or eyes, dark urine, severe stomach pain) or dangerous nerve problems from sodium rising too quickly (trouble speaking, swallowing, or moving limbs) — require immediate medical attention.

⚠️Warnings & precautions▾
  • Sodium correction must not happen too fast. If blood sodium rises more than 12 mEq/L in 24 hours, it can cause osmotic demyelination syndrome — a potentially fatal nerve condition. Symptoms include difficulty speaking, swallowing, weakness, seizures, or coma. This risk is higher in people with malnutrition, alcoholism, or advanced liver disease.
  • Liver injury risk is serious. Tolvaptan can cause significant or permanent liver damage. Samsca is limited to 30 days of use. Jynarque requires liver blood tests before starting and at regular intervals throughout treatment. Stop the medication and call your doctor immediately if you develop yellowing of the skin or eyes, dark urine, unusual tiredness, or stomach pain.
  • Dehydration and low blood volume can occur — drink enough to satisfy thirst and contact your doctor if you feel severely dizzy or faint.
  • High potassium (hyperkalemia) may develop, especially when tolvaptan is taken with certain blood pressure or heart medications; monitoring may be needed.
🔀What it interacts with▾

Tolvaptan's levels in the body are strongly affected by certain other medications and foods. Key interactions to know:

  • Strong CYP3A inhibitors (e.g., ketoconazole): Dramatically raise tolvaptan levels — combining these is contraindicated (forbidden).
  • Moderate CYP3A inhibitors: Can substantially increase tolvaptan exposure; dose reduction or temporary stopping may be needed.
  • Strong CYP3A inducers: Lower tolvaptan levels significantly, potentially reducing effectiveness — avoid combining.
  • Grapefruit juice: Should be avoided while taking tolvaptan, as it can raise tolvaptan levels.
  • ACE inhibitors, ARBs, and potassium-sparing diuretics: When used together with tolvaptan, these can raise blood potassium levels — monitoring is recommended.
  • Desmopressin (dDAVP) and other V2-receptor agonists: Tolvaptan blocks the receptor these drugs rely on, so combining them is not recommended.

This is not a complete list of interactions. Always talk with your doctor or pharmacist before starting, stopping, or changing any medication.

📋Before taking it▾
  • Do not take tolvaptan if you have a history of significant liver disease or liver injury (does not apply to uncomplicated polycystic liver disease).
  • Do not take it if you are unable to sense or respond to thirst — you need to be able to drink fluids to stay safe.
  • Do not take it if you have low blood volume (hypovolemia), a blockage in your urinary tract, or produce no urine (anuria).
  • Do not take it if your blood sodium is already abnormally high or low and has not been corrected.
  • Avoid tolvaptan if you have a known allergy or serious reaction to tolvaptan or any ingredient in the product.
  • Pregnancy: Tolvaptan may harm an unborn baby. Tell your doctor right away if you are pregnant or planning to become pregnant.
  • Breastfeeding: Breastfeeding is not recommended while taking tolvaptan due to the potential for serious harm to the infant, including liver toxicity and electrolyte problems.
  • Children: Safety and effectiveness in pediatric patients have not been established.
  • Older adults: Use with caution; older adults are more likely to have liver, kidney, or heart conditions that can affect safety. Dosing should be started conservatively.
🚑If you take too much▾

Taking too much tolvaptan can cause a sharp rise in blood sodium, excessive urination, severe thirst, and dehydration. There is no specific antidote. If an overdose is suspected, medical staff will monitor vital signs, electrolyte levels, heart rhythm, and fluid status, and replace fluids and electrolytes as needed until the effects wear off. Dialysis is unlikely to help because tolvaptan binds very tightly to proteins in the blood.

📡Pharmacodynamics — effects in the body▾

Tolvaptan starts increasing urine water output (aquaresis) within 1 to 2 hours of taking a dose. This excess water loss raises sodium levels in the blood, unless fluid intake is increased enough to match urine output. During treatment, the kidneys' filtration rate decreases slightly (by about 6–10%) and the ability to clear uric acid also decreases — both effects reverse when tolvaptan is stopped. The medication does not affect the heart's electrical rhythm at studied doses.

🔬Pharmacokinetics — how your body processes it▾

After an oral dose, tolvaptan reaches peak blood levels within 2 to 4 hours. It can be taken with or without food, though a high-fat meal can double peak concentrations without affecting overall absorption. Tolvaptan is more than 98% bound to proteins in the blood, which is why dialysis is not effective in overdose situations. It is broken down primarily through the CYP3A enzyme system in the liver, which is why certain medications and grapefruit juice that affect this enzyme can significantly change tolvaptan levels in the body.

📦How to store it▾

Store at 20°C to 25°C (68°F to 77°F); excursions permitted from 15°C to 30°C (59°F to 86°F) . Keep out of reach of children.

📄 Written from Tolvaptan’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Every point is grounded in that labeling — nothing is invented. How we use AI →

🩺 Pharmacist Counseling Corner

Quick, plain-English answers to the questions patients ask most about Tolvaptan — the kind of thing our pharmacy team would talk through with you at the counter.

Why do I have to start this medication in a hospital? ▾
This is a safety requirement — not just a formality. When tolvaptan raises your blood sodium levels, it has to happen gradually. If sodium goes up too fast, it can cause a rare but serious brain and nerve condition that can lead to seizures, coma, or even death. Starting in the hospital means doctors can watch your sodium levels closely and adjust things right away if needed. Once you're stable, you can continue the medication at home.
Why do I need regular liver blood tests if I'm on Jynarque? ▾
Tolvaptan can cause liver damage — and with Jynarque, which is used long-term for kidney disease, that risk needs to be watched carefully. Liver blood tests check for signs of injury before you have any symptoms. If the tests show a problem, your doctor can stop the medication early and prevent serious harm. This is why the testing schedule — before you start, then at set intervals — isn't optional. It's there to protect you.
I feel really thirsty and I'm urinating a lot. Is that normal? ▾
Yes, those are actually the most common side effects of tolvaptan — and they happen because the medication is doing its job of getting your kidneys to release extra water. The thirst is your body's signal to drink, and you should follow it. Don't try to restrict fluids on your own while taking this medication unless your doctor specifically tells you to. If the thirst or urination feels extreme or unmanageable, let your doctor know.
What signs of liver problems should I watch for? ▾
The ones to act on quickly are: yellowing of your skin or the whites of your eyes, very dark or tea-colored urine, unusual fatigue that feels different from your usual tiredness, nausea, and pain in the upper right part of your stomach. If any of these appear, stop taking tolvaptan and call your doctor or go to the emergency room. Don't wait to see if it gets better on its own — liver injury from tolvaptan can be serious and sometimes irreversible if not caught early.
Can I take tolvaptan with my other medications? ▾
Some medications can be a real problem with tolvaptan. Certain antifungals, antibiotics, and other drugs that affect a liver enzyme called CYP3A can raise tolvaptan levels dangerously high — the combination with strong inhibitors of this enzyme is actually forbidden. Even grapefruit juice can interfere. Blood pressure medications like ACE inhibitors or potassium-sparing diuretics can raise your potassium levels when combined with tolvaptan. Always give your pharmacist and doctor a full list of everything you take — including over-the-counter drugs and supplements — before starting tolvaptan.
Is it safe to take this medication if I'm pregnant or want to become pregnant? ▾
Tolvaptan is not considered safe during pregnancy. Animal studies showed harm to developing fetuses, and there isn't enough data from human pregnancies to confirm it's safe. If there's any chance you could become pregnant, talk to your doctor before starting this medication. Breastfeeding is also not recommended while you're on tolvaptan, because the drug could pass into breast milk and potentially harm your baby.
Is Tolvaptan available over the counter? ▾
Tolvaptan is dispensed by prescription according to its FDA labeling, so it isn't sold over the counter. Your prescriber and pharmacist will determine if it's appropriate for you.
When was Tolvaptan first available? ▾
Tolvaptan has been available in the United States since at least 2009, based on FDA approval history (Drugs@FDA) and product marketing records.
Who makes Tolvaptan? ▾
Tolvaptan is supplied by 18 manufacturers listed in the FDA NDC Directory, including Ascend Laboratories, LLC, Otsuka America Pharmaceutical, Inc., Teva Pharmaceuticals, Inc..

💬 Answers drafted from Tolvaptan’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Grounded in that labeling — nothing is made up. How we use AI →

🧰 Keep exploring

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💊 How Tolvaptan comes

Tolvaptan is available in 1 form. Different forms and brands can have different approved uses, doses, schedules, and directions. Follow the instructions for your exact product, and do not switch forms without guidance from your prescriber or pharmacist.

Tablet

By mouth
Brands Jynarque Samsca
How this form is used
What it may be used for
  • Samsca tablets are used to treat clinically significant low blood sodium (hyponatremia) with excess or normal body fluid
  • Jynarque tablets are used to slow kidney function decline in adults with autosomal dominant polycystic kidney disease (ADPKD) through the FDA-approved REMS program
  • Tolvaptan tablets (REMS formulation) are used for ADPKD under the same restricted safety program as Jynarque
Important instructions
  • Samsca tablets are taken once daily by mouth, with or without food, and must be started in a hospital
  • Samsca should not be taken for more than 30 days to reduce liver injury risk
  • Jynarque tablets are taken as two doses per day — one on waking and one about 8 hours later — by mouth, with or without food
  • Jynarque requires regular liver blood tests before starting and throughout treatment; if a dose is missed, skip it and take the next dose at its scheduled time
Available strengths 5 strengths
15 mg 30 mg 45 mg 60 mg 90 mg
52 FDA-listed product records ⓘ

📊 Tolvaptan across the U.S. market

How Tolvaptan appears in the FDA’s National Drug Code Directory — including its dosage forms, strengths, brand names, manufacturers, and FDA-listed product records. These are directory records, not sales or prescription volume.

1
Dose forms ⓘ
18
Manufacturers
3
Brand names
89
FDA-listed product records ⓘ
2009
First marketed ⓘ

Also listed with the FDA, not a patient dose form: Kit (30) · Powder (7) — bulk drug substance sold to compounders/manufacturers and multi-item kits. These aren’t counted in the dose-form total above.

Ascend Laboratories, LLC26%
Otsuka America Pharmaceutical, Inc.20%
Teva Pharmaceuticals, Inc.11%
Lupin Pharmaceuticals, Inc.8%
Apotex Corp.8%
Otsuka Pharmaceutical Co., Ltd.6%
Other makers21%

Share of FDA-listed product records by manufacturer — FDA National Drug Code Directory. Record counts are not sales or prescription volume.

📈 How widely Tolvaptan is used

A general measure of how commonly Tolvaptan is prescribed, based on Medicaid — one of the largest public drug programs. The figure below is prescriptions filled in Q1–Q4 2025, summed across every form and brand of the drug.

Think of this as a proxy for how widely Tolvaptan is used, drawn from freely available public data. Medicaid is just one program — these numbers don’t include Medicare, other government coverage, or commercial and cash-pay prescriptions, so real-world use is higher than what’s shown here.

5,692
Medicaid prescriptions filled (Q1–Q4 2025)
$113M gross Medicaid reimbursement (before mandatory rebates — net cost is lower)

How commonly is Tolvaptan prescribed? Of the 1,596 medications we measure, Tolvaptan ranks #1,027 by Medicaid prescriptions — more than 36% of them.

Where Tolvaptan ranks among the drugs we measure · Q1–Q4 2025 · neighbors ±5
Total prescriptions — #1,027 of 1,596
#1,022 Lasmiditan 5,898 Rx #1,023 Sarilumab Injection 5,765 Rx #1,024 Isavuconazonium 5,727 Rx #1,025 Deferoxamine 5,720 Rx #1,026 Doravirine, Lamivudine... 5,704 Rx #1,027 Tolvaptan (low blood s... 5,692 Rx #1,028 Tolvaptan (kidney dise... 5,692 Rx #1,029 Tolvaptan 5,692 Rx #1,030 Aminocaproic Acid 5,657 Rx #1,031 Ceftazidime Injection 5,585 Rx #1,032 Methylergonovine 5,549 Rx

Utilization by Tolvaptan product

Pick a product to see its own Medicaid numbers. Each chip is one clinical product — a specific strength & dosage form as defined by RxNorm — with brand-name and generic versions combined.

The 15 mg oral tablet is the most-dispensed Tolvaptan product — about 3% of these Medicaid prescriptions.

Hyponatremia tolvaptan 15 MG Oral Tablet Most dispensed

179 Medicaid prescriptions (Q1–Q4 2025) 3% of Tolvaptan prescriptions shown $191,023 gross reimbursement (before rebates) ≈ $1,067 per prescription (gross)

Summed across the 3 of 17 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 849827

Hyponatremia tolvaptan 30 MG Oral Tablet

11 Medicaid prescriptions (Q1–Q4 2025) <1% of Tolvaptan prescriptions shown $27,101 gross reimbursement (before rebates) ≈ $2,464 per prescription (gross)

Summed across the 1 of 17 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 849833

Other Tolvaptan products — combination packs and listings not yet matched to a specific clinical product (kept visible so every prescription is accounted for)

5,502 Medicaid prescriptions (Q1–Q4 2025) 97% of Tolvaptan prescriptions shown $112.8M gross reimbursement (before rebates) ≈ $20,502 per prescription (gross)

Summed across the 9 of 20 listed NDC products with Medicaid activity.

Shares are of the Medicaid prescriptions shown here. Product grouping follows RxNorm (the National Library of Medicine’s drug terminology), so “one product” means one strength & dosage form regardless of manufacturer. Dollar figures are gross Medicaid reimbursement before mandatory rebates — rebates (often large, especially for brand-name drugs) are confidential, so actual net cost to Medicaid is lower than shown.

Source: Medicaid State Drug Utilization Data (CMS), aggregated by generic ingredient — summed across every NDC (all brands, strengths, salt forms and dosage forms) of Tolvaptan, and across all states and both fee-for-service and managed-care claims. A general popularity signal; it excludes Medicare, commercial insurance and cash prescriptions, so it is not total U.S. use. Based on the 13 of 54 listed Tolvaptan NDCs with Medicaid activity.

🔍 Compare Tolvaptan products

A representative set of FDA-listed product records for Tolvaptan — across manufacturers, strengths, and dosage forms, grouped by form with each product’s manufacturer and how the FDA approved it. The same medicine may be made and packaged by different companies, so a single drug can have many directory entries. (It’s also why a refill can look different — a new shape, color, or box — even though it contains the same medication.)

Showing 89 of 89 products — FDA National Drug Code Directory. See every product, package size and price: browse all 89 Tolvaptan NDCs →

RxNorm Concept Web — From Ingredient to Every Form and Strength

This page starts with one ingredient concept (IN). The branches below show its dose-form concepts (SCDF), then the available clinical drug and strength concepts (SCD). Combination products remain separate concepts with their own pages.

Ingredient (IN) Tolvaptan RxCUI 358257 1 dose form · 7 strengths

Look up RxCUI 358257 in the RxCUI Atlas →

RxNorm is the U.S. National Library of Medicine’s normalized drug vocabulary. Its concept hierarchy can include forms that are not currently marketed; the status on each branch compares that concept with current FDA listings. RxCUIs identify vocabulary concepts, not individual packages or manufacturers.

🏷️ Sold under these brand names

Jynarque Samsca

🏭 Manufacturers & labelers

Ascend Laboratories, LLC 23 Otsuka America Pharmaceutical, Inc. 18 Teva Pharmaceuticals, Inc. 10 Lupin Pharmaceuticals, Inc. 7 Apotex Corp. 7 Otsuka Pharmaceutical Co., Ltd. 5 MSN Laboratories Private Limited 2 Par Pharmaceutical, Inc. 2 Par Health USA, LLC 2 Novadoz Pharmaceuticals LLC 2 Northstar Rx LLC 2 Endo USA, Inc. 2 Camber Pharmaceuticals, Inc. 2 Jiangsu Hengrui Pharmaceuticals Co., Ltd. 1 Hetero Labs Limited 1 Hetero Drugs Limited 1 Aurore Pharmaceuticals Private Limited 1 Tyche Industries Limited 1

RxNorm drug class

Tolvaptan belongs to the Vasopressin V2 Receptor Antagonist class.

Pharmacologic class Vasopressin V2 Receptor Antagonist
Drug family (ATC) Vasopressin antagonists
How it works Vasopressin V2 Receptor Antagonists

Classified by RxNorm RxClass — the U.S. National Library of Medicine's standardized drug-classification service (Established Pharmacologic Class from the FDA, the ATC drug family from the WHO, and mechanism of action). Reference only, not medical advice.

🔬 Where this comes from

Core label, product, RxNorm, safety, and utilization data on this page come from the sources identified below. AI-written, editorial, and licensed sections are labeled separately.

📄
FDA-filed drug labels (SPL) Uses, dosing, warnings & side effects from SPL records retrieved through openFDA; the linked representative set can be verified on DailyMed. ✓ Linked label effective Nov 6, 2025
🏭
Forms, brands & labelersAggregated from ingredient-matched FDA National Drug Code Directory product records for Tolvaptan.
📈
Real-world reportsThe FDA Adverse Event Reporting System (FAERS), served through openFDA.
🚨
Recalls & shortagesopenFDA drug-enforcement reports and the FDA drug-shortage database.
🧾 Clinical label set — FDA-filed SPL labels retained for Tolvaptan after exact ingredient or ingredient-combination matching and applicable route/form matching
Clinical labels in scope
10
NDC products indexed
89
Distinct labelers/manufacturers represented
18
Linked representative label ⓘ
Otsuka America Pharmaceutical, Inc.
Linked label effective
Nov 6, 2025
Composite sections available
24
Linked SPL Set ID
3febc0a1-9e5a-4ce0-843d-210f21d862c4
Linked SPL Document ID
3be8a6fe-a8d0-43ca-a84d-183b522a3cf4
Open the linked representative label on DailyMed ↗

How we combine label and product data

HelloPharmacist combines public FDA and NLM records; we don’t author the underlying clinical facts. We identified 10 FDA-filed SPL label sets within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. The representative label is the starting point for the displayed reference monograph; the 12 largest stored in-scope SPL records, which may include that representative, are compared section by section, and the longest available version of each section is retained. Forms, routes, brands, labelers, product-listed strengths, and product-record counts are aggregated separately from ingredient-matched FDA NDC Directory records; package records listed above are associated with the linked SPL; and the normalized concept hierarchy comes from NLM RxNorm.

For canonical ingredient pages, bounded product-attributed indication and administration excerpts may be added to the AI evidence, and the generator is instructed to preserve available product, brand, route, and form qualifiers instead of treating one label as universal. Where a section is identified as AI-written, its plain-language text is generated from bounded label evidence. New draft drug pages remain in the admin review queue before first publication. Otsuka America Pharmaceutical, Inc. is the representative DailyMed label linked for verification and dates; it is not the sole source used for the page.

This is general education, not medical advice — always consult your doctor or pharmacist about your medications and any medical condition. For the exact wording of the linked representative label, view that label on DailyMed; some displayed composite sections may come from other in-scope SPL labels. Learn how we use AI and our data sources & update cadence.