Lupin-Tolvaptan: Uses, Side Effects and Dosage

ABOUT THIS MEDICATION

What the medication is used for:

LUPIN-TOLVAPTAN is used in adults to treat autosomal dominant polycystic kidney disease (ADPKD).

ADPKD is a genetic disorder which leads to the growth of multiple cysts (sacs filled with fluid) on the kidneys. Over time, the cysts grow in size, which can damage the way your kidneys work, and may ultimately lead to kidney failure.

LUPIN-TOLVAPTAN should only be prescribed by a doctor experienced in the diagnosis and treatment of ADPKD.

What it does:

LUPIN-TOLVAPTAN works by blocking the effects of a hormone called vasopressin, which promotes cyst growth in the kidneys in patients with ADPKD. By blocking the effects of the hormone, LUPIN-TOLVAPTAN is able to reduce the growth of the cysts in the kidneys and slow the decline of kidney function. This should help protect your kidneys from damage and failure.

Because of the way that LUPIN-TOLVAPTAN works, you will produce more urine causing you to urinate more frequently during the day and at night. This may become less pronounced over time.

Before starting this medication:

Before taking LUPIN-TOLVAPTAN you should discuss carefully with your doctor if this medication is suitable for you, taking into consideration the potential benefits and risks involved. Once you and your doctor have agreed that LUPIN-TOLVAPTAN is suitable for you, your doctor will ask that you sign a patient-prescriber agreement form (PPAF), stating that you understand the benefits and risks of treatment and that you agree to take blood tests as prescribed by your doctor to start and remain on treatment. For more information on LUPIN-

TOLVAPTAN controlled hepatic safety monitoring and distribution programme, please call 1-866-488-6017.

When it should not be used:

Do not take LUPIN-TOLVAPTAN if:

• you have been asked to permanently discontinue tolvaptan in the past

• you are allergic to tolvaptan, benzazepine or benzazepine derivatives (e.g. REMERON^®), or any non-medicinal ingredients in the formulation.

  • you cannot replace fluids by drinking or you can not feel if you are thirsty
  • you have elevated sodium (salt) in your blood
  • you have a condition associated with a low blood volume
  • your liver is not functioning properly and in a way that is of concern to your doctor. The presence of hepatic cysts in and of themselves should not be an impediment to initiation of LUPIN-TOLVAPTAN treatment.

  • you are pregnant or plan to become pregnant. It is not known if LUPIN-TOLVAPTAN will harm your unborn baby.

  • you are breast-feeding. It is not known if tolvaptan passes into your breast milk. You and your healthcare provider should decide if you will take LUPIN-TOLVAPTAN or breast-feed. You should not do both.
  • your body is not able to make any urine. LUPIN-TOLVAPTAN will not help your condition.

  • you take certain medicines. These medicines could cause you to have too much LUPIN-TOLVAPTAN in your blood:

    • the antibiotic medicines, clarithromycin or telithromycin
    • the antifungal medicines, ketoconazole or itraconazole
    • the anti-HIV medicines, ritonavir, indinavir, nelfinavir, and saquinavir
    • the antidepressant medicine, nefazodone

    • you have one of the following rare hereditary diseases:

      • Galactose intolerance
      • Lapp lactase deficiency
      • Glucose-galactose malabsorption because lactose is a non-medicinal ingredient in LUPIN-TOLVAPTAN.

What the medicinal ingredient is:

tolvaptan

What the non-medicinal ingredients are:

Corn starch, dehydrated alcohol, hydroxypropyl cellulose, lactose monohydrate, low substituted hydroxypropyl cellulose, magnesium stearate, microcrystalline cellulose, and ferric oxide (Red iron), traces of methylene chloride and ethanol maybe present.

IMPORTANT: PLEASE READ

What dosage forms it comes in:

Weekly combination blister packs of 15+15 mg, 30+15 mg, 45+15 mg, 60+30 mg, and 90+30 mg tablets.

WARNINGS AND PRECAUTIONS

To prevent pregnancy while on LUPIN-TOLVAPTAN treatment, women of childbearing potential must have effective contraceptive measures in place before and during treatment.

BEFORE you use LUPIN-TOLVAPTAN talk to your doctor, nurse or pharmacist if you:

• have difficulty urinating or have an enlarged prostate
• are dehydrated or suffer from excessive vomiting, diarrhea or sweating
• have low levels of sodium in your blood
• have high potassium levels in your blood
• have high levels of uric acid in your blood or gout
• are taking medication to treat high blood pressure
• are less than 18 years old
• have been asked to permanently discontinue tolvaptan in the past

Driving and using machines: Before doing tasks which require special attention, wait until you know how you respond to LUPIN-TOLVAPTAN. Dizziness, weakness and fainting can occur.

INTERACTIONS WITH THIS MEDICATION

As with most medicines, interactions with other drugs are possible. Tell your doctor, nurse, or pharmacist about all the medicines you take, including drugs prescribed by other doctors, vitamins, minerals, natural supplements, or alternative medicines.

The following may interact with LUPIN-TOLVAPTAN: clarithromycin, ketoconazole, ritonavir, saquinavir, rifampicin, phenytoin, carbamazepine, St. John’s Wort, cyclosporin, quinidine, verapamil, erythromycin, fluconazole, hypertonic saline solutions, drugs that increase serum sodium concentrations, drugs known to increase serum potassium levels (such as spironolactone), digoxin, consuming grapefruit juice, or vasopressin drugs, such as desmopressin, used to control bleeding.

PROPER USE OF THIS MEDICATION

Always take LUPIN-TOLVAPTAN exactly as your doctor has prescribed. Check with your doctor, nurse or pharmacist if you are not sure.

You can take LUPIN-TOLVAPTAN with or without food.

While taking LUPIN-TOLVAPTAN you will produce more urine, urinate more frequently, and urinate at night. If this causes you concern, consult your doctor, nurse or pharmacist. This side- effect should become less pronounced with time.

To prevent becoming dehydrated, have water available to drink at all times while taking LUPIN-TOLVAPTAN. Unless your doctor tells you otherwise, drink plenty of water during the day and one or two glasses before going to bed. If you suffer from vomiting, diarrhea or any other condition that might cause you to become dehydrated while taking LUPIN-TOLVAPTAN call your doctor.

Blood tests:

During treatment with LUPIN-TOLVAPTAN, your doctor will arrange blood tests to check for changes in your liver function, as follows:

• before starting treatment with LUPIN-TOLVAPTAN
• every month for the first 18 months, then
• every 3 months thereafter during treatment for the next 12 months, and every 3-6 months thereafter during treatment

Usual adult dose:

• LUPIN-TOLVAPTAN is to be taken twice a day in two different doses. There are three possible dose combinations that your doctor may prescribe:

  • 45+15 mg, for a total daily dose of 60 mg, or
  • 60+30 mg, for a total daily dose of 90 mg, or
  • 90+30 mg, for a total daily dose of 120 mg.
• Take one tablet of the higher dose (45 mg, 60 mg or 90 mg) in the morning.
• 8 hours later take one tablet of the lower dose (15 mg or 30 mg).
• This schedule was designed to give you the best balance between the amount of medicine in your body and possible side effects (especially night time urination).
• Do not drink grapefruit juice during treatment with LUPIN-TOLVAPTAN. This could cause you to have too great of a drug effect, while taking LUPIN-TOLVAPTAN.

Adjusted dose if you are taking certain medicines:

Your doctor will tell you to reduce your usual dose of LUPIN-TOLVAPTAN if you take certain medicines as these medicines could cause you to have too much LUPIN-TOLVAPTAN in your blood. Your doctor may reduce your dose to the following:

IMPORTANT: PLEASE READ

• 15 mg + 15 mg, for a total daily dose of 30 mg.

  or

• 30 mg +15 mg, for a total daily dose of 45 mg.

Overdose:

Missed Dose:

Do not miss or skip doses of LUPIN-TOLVAPTAN. If you miss a dose, take your next dose at the scheduled time and prescribed level. Do not take 2 doses at the same time.

SIDE EFFECTS AND WHAT TO DO ABOUT THEM

Side effects may include:

• Thirst
• Increased amount of urine
• Increased frequency of urination during the day and at night
• Headache
• Constipation, diarrhea, dry mouth, indigestion, decreased appetite
• Fatigue, weakness, dizziness
• Trouble sleeping
• Muscle spasms
• Rash, itching
• Abdominal pain

If any of these affects you severely, tell your doctor, nurse or pharmacist.

Serious side effects and what to do about them

Serious side effects and what to do about them

This is not a complete list of side effects. For any unexpected effects while taking LUPIN-TOLVAPTAN contact your doctor, nurse or pharmacist.

IMPORTANT: PLEASE READ

HOW TO STORE IT

Store LUPIN-TOLVAPTAN between 15^oC to 30^oC.

Keep LUPIN-TOLVAPTAN out of reach and sight of children.

Reporting Side Effects

MORE INFORMATION

If you want more information about LUPIN-TOLVPATAN:

• Talk to your healthcare professional
• Find the full product monograph that is prepared for healthcare professionals and includes this Patient Medication Information by visiting the Health Canada Drug Product Database website: (https://www.canada.ca/en/health-canada/services/drugs-health-products/drug-products/drug-product-database.html ); the manufacturer’s website www.lupinpharma.ca or by calling 1-844-587-4623.

Last Revised: APR 25, 2025