Generic Name: Tolcapone Brand Name(s): Generics only. No brands available.

Uses

What is Tolcapone used for?

Tolcapone is used with other medications (levodopa/carbidopa) to treat Parkinson’s disease. Tolcapone belongs to a class of drugs known as COMT inhibitors. Many people taking levodopa for Parkinson’s have problems with the effects of the levodopa wearing off between scheduled doses, causing symptoms to return or worsen. Tolcapone blocks a certain natural substance (COMT enzyme) that breaks down levodopa in the body. This effect allows the levodopa to last longer in the system so that it doesn’t wear off before the next dose.

How should I take Tolcapone?

Take this medication by mouth with or without food, usually 3 times daily or as directed by your doctor. You will start on a low dose. Your doctor may increase your dosage after 3 weeks if he or she thinks that you will benefit from a higher dose.

Dosage is based on your medical condition and response to therapy.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day. Do not suddenly stop taking this medication unless instructed to do so by your doctor. Doing so may cause your Parkinson’s symptoms to become much worse.

Tell your doctor if your condition persists or worsens (such as your Parkinson’s symptoms are not controlled).

How do I store Tolcapone?

Tolcapone is best stored at room temperature away from direct light and moisture. To prevent drug damage, you should not store Tolcapone in the bathroom or the freezer. There may be different brands of Tolcapone that may have different storage needs. It is important to always check the product package for instructions on storage, or ask your pharmacist. For safety, you should keep all medicines away from children and pets.

You should not flush Tolcapone down the toilet or pour them into a drain unless instructed to do so. It is important to properly discard this product when it is expired or no longer needed. Consult your pharmacist for more details about how to safely discard your product.

Precautions & warnings

What should I know before using Tolcapone?

Before taking tolcapone, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: alcoholism, low blood pressure, Parkinson’s with severe movement problems, liver problems, mental/mood disorders (such as psychosis, schizophrenia), history of a certain muscle problem (rhabdomyolysis), fever and confusion caused by any drug.

This drug may make you dizzy or drowsy. Alcohol or marijuana can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana. See also Side Effects section.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Older adults may be more sensitive to the side effects of this drug, especially drowsiness, confusion, and hallucinations.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

It is not known if this medication passes into breast milk. Consult your doctor before breast-feeding.

Is it safe during pregnancy or breast-feeding?

There are no adequate studies in women for determining risk when using this Tolcapone during pregnancy or while breastfeeding. Please always consult with your doctor to weigh the potential benefits and risks before taking Tolcapone. Tolcapone is pregnancy risk category C according to the US Food and Drug Administration (FDA).

FDA pregnancy risk category reference below:

  • A=No risk,
  • B=No risk in some studies,
  • C=There may be some risk,
  • D=Positive evidence of risk,
  • X=Contraindicated,
  • N=Unknown

Side effects

What side effects can occur from Tolcapone?

Nausea/vomiting, unwanted/uncontrolled movements, diarrhea, headache, drowsiness, trouble sleeping, increased number of dreams, increased sweating, dry mouth, gas, and abdominal pain may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

To avoid dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication may develop serious side effects, but with frequent visits to your doctor, this risk can be minimized.

Some people taking tolcapone have fallen asleep suddenly during their usual daily activities (such as talking on the phone, driving). In some cases, sleep occurred without any feelings of drowsiness beforehand. This sleep effect may occur anytime during treatment with tolcapone even if you have used this medication for a long time. If you experience increased sleepiness or fall asleep during the day, do not drive or take part in other possibly dangerous activities until you have discussed this effect with your doctor. Your risk of this sleep effect is increased by using alcohol or other medications that can make you drowsy. See also Precautions section.

Your urine may change color (such as increased yellow color). This effect is harmless.

Tell your doctor right away if you have any serious side effects, including: easy bleeding/bruising, chest pain, fast/irregular heartbeat, fever, mental/mood changes (such as agitation, confusion, hallucinations), unusual strong urges (such as increased gambling, increased sexual urges), muscle pain/soreness/stiffness/weakness, pain/trouble with breathing.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

Not everyone experiences these side effects. There may be some side effects not listed above. If you have any concerns about a side-effect, please consult your doctor or pharmacist.

Interactions

What drugs may interact with Tolcapone?

Some of the products that may interact with this drug include: certain MAO inhibitors (isocarboxazid, linezolid, methylene blue, moclobemide, phenelzine, procarbazine, tranylcypromine).

Other MAO inhibitors (safinamide, selegiline, rasagiline) may be used cautiously with close monitoring by your doctor. If you are taking rasagiline or selegiline for Parkinson’s disease, ask your doctor if you should continue taking it.

Tolcapone can slow down the removal of other drugs from your body, thereby affecting how they work. These affected drugs include apomorphine, dobutamine, and methyldopa. This is not a complete list.

Tell your doctor or pharmacist if you are taking other products that cause drowsiness including alcohol, marijuana, antihistamines (such as cetirizine, diphenhydramine), drugs for sleep or anxiety (such as alprazolam, diazepam, zolpidem), muscle relaxants, and narcotic pain relievers (such as codeine).

Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.

Tolcapone may interact with other drugs that you are currently taking, which can change how your drug works or increase your risk for serious side effects. To avoid any potential drug interactions, you should keep a list of all the drugs you are using (including prescription drugs, nonprescription drugs and herbal products) and share it with your doctor and pharmacist. For your safety, do not start, stop, or change the dosage of any drugs without your doctor’s approval.

Does food or alcohol interact with Tolcapone?

Tolcapone may interact with food or alcohol by altering the way the drug works or increase the risk for serious side effects. Please discuss with your doctor or pharmacist any potential food or alcohol interactions before using this drug.

What health conditions may interact with Tolcapone?

Tolcapone may interact with your health condition. This interaction may worsen your health condition or alter the way the drug works. It is important to always let your doctor and pharmacist know all the health conditions you currently have.

Dosage

The information provided is not a substitute for any medical advice. You should ALWAYS consult with your doctor or pharmacist before using this Tolcapone.

What is the dose of Tolcapone for an adult?

Usual Adult Dose for Parkinson’s Disease

Initial dose: 100 mg orally 3 times a day

-Dose may be increased to 200 mg 3 times daily only if the anticipated incremental benefit is justified

-If substantial clinical benefit is not observed within 3 weeks of start of therapy, this drug should be discontinued

Comments:

-This drug should not be used until there has been a complete discussion of risks and the patient has provided written acknowledgement that the risks have been explained.

Renal Dose Adjustments

Mild to moderate renal impairment: No dose adjustment recommended

Severe renal impairment (CrCl less than 25 mL/min): Safety has not been established

Liver Dose Adjustments

Therapy should not be initiated:

-In patients with clinical evidence of liver disease, or

-If 2 ALT or AST values are greater than the upper limit of normal

Discontinue therapy if ALT or AST levels exceed 2 times the upper limit of normal or if clinical signs and symptoms suggest the onset of hepatic dysfunction.

Patients who develop hepatocellular injury while on this drug and are withdrawn from this drug for any reason may be at increased risk for liver injury if this drug is restarted; therefore, restarting this drug is generally not recommended

Dose Adjustments

Use with caution in patients with severe dyskinesia or dystonia

To optimize response to therapy, reductions in levodopa dose may be necessary. In clinical trials, the majority of patients whose levodopa dose was greater than 600 mg/day or who had moderate or severe dyskinesias before beginning treatment, decreased their daily levodopa dose.

Discontinuation:

-As with any dopaminergic drug, withdrawal or abrupt reduction may lead to emergence of signs and symptoms of Parkinson’s disease or hyperpyrexia and confusion, therefore, upon discontinuation monitor and adjust other dopaminergic treatments as needed.

Dialysis

Hemodialysis: tolcapone is highly protein bound, therefore no significant removal of the drug is expected.

Other Comments

Administration advice:

-May be taken with or without food

-In clinical trials, the first dose of the day was always taken together with the first dose of the day of levodopa/carbidopa; subsequent doses were taken approximately 6 and 12 hours later

General:

-Because of the risks of fatal, acute fulminant liver failure, this drug should only be used in patients with Parkinson’s disease on levodopa/carbidopa who are experiencing symptom fluctuations not responding satisfactorily to, or are not appropriate candidates for other adjunctive therapies; this drug should be discontinued if substantial clinical benefit is not observed within 3 weeks.

-Patients who develop hepatocellular injury and are withdrawn from this drug for any reason may be at increased risk for liver injury if this drug is reintroduced, therefore, restarting this drug in these patients is not advised.

Monitoring:

-Hepatic: Obtain liver enzymes (AST and ALT) at baseline, every 2 to 4 weeks for the first 6 months, then as clinically relevant; if the dose is increased to 200 mg three times a day, liver enzyme monitoring should be obtained prior to increase, every 2 to 4 weeks for 6 months, then as clinically relevant; monitor for signs and symptoms of hepatic dysfunction

-Cardiovascular: Monitor for signs and symptoms of orthostatic hypotension

-Nervous System: Monitor for somnolence and drowsiness

-Dermatologic: Monitor for melanomas; consider periodic skin examinations by dermatologists.

-Psychiatric: Question patients about new or increased gambling urges, sexual urges, uncontrolled spending, binge or compulsive eating, or other urges.

Patient advice:

-Patients should understand the risks of hepatic failure and immediately reports any symptoms of hepatic dysfunction.

-Patients should not drive a car or operate machinery or other potentially dangerous activities until it is determined how this drug affects their mental and/or motor performance.

-Patients should be instructed to report episodes of sudden onset of sleep, new or worsening dyskinesia, new or worsening compulsive behaviors and/or unusual urges.

-Patients should be instructed to report changes in the size, shape, or color of moles on their skin and should have their skin checked on a regular basis for melanomas.

-Patients should be aware that this drug may cause orthostatic blood pressure changes including fainting and dizziness and patients are advised to avoid standing rapidly after sitting or lying down.

-Patients should speak to their physician or health care provider if they become pregnant, intend to become pregnant, or are breastfeeding.

What is the dose of Tolcapone for a child?

The dosage has not been established in pediatric patients. It may be unsafe for your child. It is always important to fully understand the safety of the drug before using. Please consult with your doctor or pharmacist for more information.

How is Tolcapone available?

Tolcapone is available in the following dosage forms and strengths:

  • Oral tablet.

What should I do in case of an emergency or overdose?

In case of an emergency or an overdose, call your local emergency services or go to your nearest emergency room.

What should I do if I miss a dose?

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 take your regular dose as scheduled. Do not take a double dose.

 

Hello Health Group does not provide medical advice, diagnosis or treatment.

Sources

Review Date: June 2, 2018 | Last Modified: June 2, 2018

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