Because of the risk of potentially fatal, acute fulminant liver failure, tolcapone should ordinarily be used in patients with Parkinson's disease on levodopa/carbidopa who are experiencing symptom fluctuations and are not responding satisfactorily to or are not appropriate candidates for other adjunctive therapies.
Because of the risk of liver injury and because tolcapone, when it is effective, provides an observable symptomatic benefit, the patient who fails to show substantial clinical benefit within 3 weeks of initiation of treatment, should be withdrawn from tolcapone.
Tolcapone therapy should not be initiated if the patient exhibits clinical evidence of liver disease or two SGPT/ALT or SGOT/AST values greater than the upper limit of normal. Patients with severe dyskinesia or dystonia should be treated with caution.
Patients who develop evidence of hepatocellular injury while on tolcapone and are withdrawn from the drug for any reason may be at increased risk for liver injury if tolcapone is reintroduced. Accordingly, such patients should not ordinarily be considered for retreatment.
Cases of severe hepatocellular injury, including fulminant liver failure resulting in death, have been reported in postmarketing use. As of May 2005, 3 cases of fatal fulminant hepatic failure have been reported from more than 40,000 patient years of worldwide use. This incidence may be 10-fold to 100-fold higher than the background incidence in the general population. Under-reporting of cases may lead to significant underestimation of the increased risk associated with the use of tolcapone. All 3 cases were reported within the first six months of initiation of treatment with tolcapone. Analysis of the laboratory monitoring data in over 3,400 tolcapone-treated patients participating in clinical trials indicated that increases in SGPT/ALT or SGOT/AST, when present, generally occurred within the first 6 months of treatment with tolcapone.
A prescriber who elects to use tolcapone in face of the increased risk of liver injury is strongly advised to monitor patients for evidence of emergent liver injury. Patients should be advised of the need for self-monitoring for both the classical signs of liver disease (eg, clay colored stools, jaundice) and the nonspecific ones (eg, fatigue, loss of appetite, lethargy).
Although a program of periodic laboratory monitoring for evidence of hepatocellular injury is recommended, it is not clear that periodic monitoring of liver enzymes will prevent the occurrence of fulminant liver failure. However, it is generally believed that early detection of drug-induced hepatic injury along with immediate withdrawal of the suspect drug enhances the likelihood for recovery. Accordingly, the following liver monitoring program is recommended.
Before starting treatment with tolcapone, the physician should conduct appropriate tests to exclude the presence of liver disease. In patients determined to be appropriate candidates for treatment with tolcapone, serum glutamic-pyruvic transaminase (SGPT/ALT) and serum glutamic-oxaloacetic transaminase (SGOT/AST) levels should be determined at baseline and periodically (i.e. every 2 to 4 weeks) for the first 6 months of therapy. After the first six months, periodic monitoring is recommended at intervals deemed clinically relevant. Although more frequent monitoring increases the chances of early detection, the precise schedule for monitoring is a matter of clinical judgement. If the dose is increased to 200 mg three times a day, liver enzyme monitoring should take place before increasing the dose then be conducted every 2 to 4 weeks for the following 6 months of therapy. After six months, periodic monitoring is recommended at intervals deemed clinically relevant.
Tolcapone should be discontinued if SGPT/ALT or SGOT/AST exceeds 2 times the upper limit of normal or if clinical signs and symptoms suggest the onset of hepatic dysfunction (persistent nausea, fatigue, lethargy, anorexia, jaundice, dark urine, pruritus, and right upper quadrant tenderness) .
Tolcapone use has been associated with a risk of potentially fatal, acute fulminant liver failure. Avoid use in patients with liver disease and monitor liver enzymes before starting treatment with tolcapone and periodically during therapy. Discontinue therapy if liver dysfunction is present or if a patient fails to show substantial clinical benefit within 3 weeks of initiation of treatment .
Commonly used brand name(s):
In the U.S.
Available Dosage Forms:
Therapeutic Class: Antiparkinsonian
Pharmacologic Class: Catechol-O-Methyltransferase Inhibitor
Tolcapone is used in combination with levodopa and carbidopa for the treatment of the symptoms of Parkinson's disease.
tolcapone is available only with your doctor's prescription.
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 tolcapone, the following should be considered:
Tell your doctor if you have ever had any unusual or allergic reaction to tolcapone 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.
Studies on tolcapone have been done only in adult patients. There is no identified potential use of tolcapone in children.
The risk of hallucinations (seeing, hearing, or feeling things that are not there) may be increased in patients older than 75 years of age.
|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.|
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.
Using tolcapone 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.
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. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.
The presence of other medical problems may affect the use of tolcapone. Make sure you tell your doctor if you have any other medical problems, especially:
Take tolcapone only as directed by your doctor, to help your condition as much as possible. Do not take more or less of it, and do not take it more or less often than your doctor ordered.
It is important that you and your doctor discuss the risks of tolcapone and that you read and sign a written informed consent before you begin taking tolcapone.
The dose of tolcapone 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 tolcapone. 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.
If you miss a dose of tolcapone, 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.
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.
It is important that your doctor check your progress at regular visits. Tolcapone may have serious effects on your liver. You must have regular blood tests done to make sure tolcapone is not affecting your liver.
Because tolcapone may have serious effects on your liver, you should watch for any signs of these effects. Signs include dark urine; itching; light-colored stools; loss of appetite; nausea (continuing); tenderness in upper right part of abdomen; unusual drowsiness, dullness, or feeling sluggish; unusual tiredness or weakness; or yellow eyes or skin. If you notice any of these signs, contact your doctor.
Do not stop taking tolcapone without first checking with your doctor. Your doctor may want you to gradually reduce the amount you are taking before stopping completely.
Tolcapone may cause dizziness or lightheadedness, drowsiness, weakness, or trouble in thinking or concentrating. Make sure you know how you react to tolcapone before you drive, use machines, or do anything else that could be dangerous if you are not alert, well-coordinated, or able to think clearly.
Dizziness, lightheadedness, or fainting may occur, especially when you get up from a lying or sitting position. Getting up slowly may help. If you should have this problem, check with your doctor.
Hallucinations (seeing, hearing, or feeling things that are not there) may occur in some patients. This is more common in elderly patients.
You may experience nausea, especially when you first begin taking tolcapone.
Tolcapone causes the urine to turn bright yellow. This is to be expected while you are taking it. This effect is harmless and will go away after you stop taking the medicine.
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur:Incidence not known
Check with your doctor as soon as possible if any of the following side effects occur:More common
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:More common
After you stop using tolcapone, it may still produce some side effects that need attention. During this period of time, check with your doctor immediately if you notice the following side effects:
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
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