Tolvaptan
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DRUG STATUS
Approvals
US(FDA), UK(BNF)
Essential Medicine
NO
Teratogenicity
N/A
Pharmaceutical Class
Vasopressin V2 Receptor Antagonist
Tolvaptan
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Click HereSummary
Tolvaptan is used to treat low sodium levels in the blood, a condition known as hyponatremia. It's primarily used in patients with heart failure or certain hormone imbalances that cause the body to retain too much water.
Tolvaptan works by blocking the action of a hormone called vasopressin in the kidneys. This hormone promotes water retention. By blocking its effects, Tolvaptan increases the amount of water excreted through urine without affecting sodium levels, thereby correcting hyponatremia and reducing fluid buildup.
The usual dose of Tolvaptan for adults is 15 mg once daily, which can be increased to a maximum of 60 mg per day. The tablet is swallowed whole and can be taken with or without food.
Common side effects of Tolvaptan include thirst, dry mouth, increased urination, and nausea. More serious side effects can include liver damage, dehydration, low blood pressure, and electrolyte imbalances.
Tolvaptan carries a risk of liver damage, so liver function should be monitored regularly. It should not be used by patients with liver disease or acute kidney injury. It's also not recommended for individuals with low blood volume or those who are not producing urine. Caution is advised in people with heart or kidney disease.
Indications and Purpose
What is Tolvaptan used for?
Tolvaptan is a medication that helps correct low sodium levels in the blood. It can be used in people with certain medical conditions, like heart failure or a condition called SIADH, where the body holds onto too much water and makes sodium levels low.
How does Tolvaptan work?
Tolvaptan works by blocking the action of a hormone called vasopressin in the kidneys. Vasopressin normally promotes water retention, so by blocking its effects, Tolvaptan increases the amount of water excreted through urine without affecting sodium levels. This helps correct conditions like hyponatremia (low sodium levels) and reduces fluid buildup in diseases like heart failure and kidney disorders.
Is Tolvaptan effective?
Clinical studies have shown that Tolvaptan effectively treats hyponatremia (low sodium levels) by increasing serum sodium levels through enhanced water excretion. In patients with heart failure or kidney disease, it helps reduce fluid retention, improving symptoms like swelling and shortness of breath. Studies have demonstrated that Tolvaptan significantly improves sodium balance and fluid management, supporting its effectiveness in these conditions.
How does one know if Tolvaptan is working?
The benefit of Tolvaptan is evaluated by monitoring serum sodium levels to assess the correction of hyponatremia. Doctors also track fluid balance (fluid intake versus output) and symptoms such as swelling, weight gain, and shortness of breath in patients with heart failure or kidney disease. Regular lab tests and clinical assessments help determine if the medication is effectively improving fluid retention and sodium levels.
Directions for Use
What is the usual dose of Tolvaptan?
The usual starting dose for Tolvaptan in adults is 15 mg once daily, which can be increased to 30 mg and then to a maximum of 60 mg once daily, as needed. Tolvaptan should be initiated and re-initiated in a hospital setting. The safety and effectiveness of Tolvaptan in children have not been established. Always follow your doctor's advice for dosing.
How do I take Tolvaptan?
Take tolvaptan tablets once a day, as prescribed by your doctor. You can take them with or without food, but avoid drinking grapefruit juice during treatment.
For how long do I take Tolvaptan?
Tolvaptan should not be used for more than 30 days to minimize the risk of liver injury. Always follow your healthcare provider's instructions regarding the duration of use.
How long does it take for Tolvaptan to start working?
Tolvaptan typically starts working within 2 to 4 hours after the first dose by promoting the excretion of excess water, helping to balance sodium levels. Its effects on fluid retention, particularly in conditions like hyponatremia or heart failure, can be seen within the first day of treatment, though full benefits may take a few days to be apparent.
How should I store Tolvaptan?
Tolvaptan should be stored at room temperature between 20°C to 25°C (68°F to 77°F). Keep the medication in its original packaging to protect it from moisture and light. Do not store it in the bathroom. Keep it out of reach of children and discard any unused medication after the expiration date.
Warnings and Precautions
Who should avoid taking Tolvaptan?
Important warnings for Tolvaptan include the risk of liver damage; liver function should be monitored regularly. It should be avoided in patients with liver disease or acute kidney injury. Tolvaptan is contraindicated in individuals with hypovolemia (low blood volume) or anuria (lack of urine production). It should also be used with caution in people with heart or kidney disease.
Can I take Tolvaptan with other prescription drugs?
Tolvaptan can interact with medications that affect liver enzymes, particularly CYP3A4 inhibitors like ketoconazole, clarithromycin, or ritonavir, which may increase Tolvaptan levels in the body and raise the risk of liver damage. Conversely, CYP3A4 inducers like rifampin or phenytoin can reduce Tolvaptan's effectiveness. It may also interact with diuretics or ACE inhibitors, which affect fluid and electrolyte balance. Always consult a healthcare provider before combining Tolvaptan with other medications.
Can I take Tolvaptan with vitamins or supplements?
There are no significant interactions between Tolvaptan and vitamins or supplements. However, caution is advised when taking potassium supplements or diuretics, as Tolvaptan may affect electrolyte balance, leading to imbalances in sodium, potassium, or other electrolytes. Always consult a healthcare provider before combining Tolvaptan with any supplements or medications that affect fluid balance.
Can Tolvaptan be taken safely while pregnant?
Tolvaptan is classified as Category C for pregnancy, meaning that animal studies have shown potential risks to the fetus, but there are no well-controlled studies in humans. It should only be used during pregnancy if the potential benefits outweigh the risks. Pregnant women should consult their healthcare provider before using Tolvaptan due to the lack of sufficient safety data.
Can Tolvaptan be taken safely while breastfeeding?
Tolvaptan is not recommended during breastfeeding, as it is unknown whether it passes into breast milk. Because of the potential risks to a nursing infant, healthcare providers generally advise against using Tolvaptan while breastfeeding. If treatment is necessary, alternatives should be considered, and breastfeeding may need to be discontinued. Always consult a healthcare provider for guidance.
Is Tolvaptan safe for the elderly?
In clinical studies, 42% of hyponatremic subjects treated with Tolvaptan were 65 years old and over, while 19% were 75 years old and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects. However, greater sensitivity of some older individuals cannot be ruled out. Always consult a healthcare provider for personalized advice.
Is it safe to exercise while taking Tolvaptan?
From all available and reliable information, there is no confirmed data on this. Please consult a doctor for personalized advice.
Is it safe to drink alcohol while taking Tolvaptan?
From all available and reliable information, there is no confirmed data on this. Please consult a doctor for personalized advice.
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