tolcapone (Rx)

Brand and Other Names:Tasmar
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 100mg

Parkinson Disease

100 mg PO q8hr

May increase dose to 200 mg q8hr, but increased ALT occurred more frequently

Failure to show the expected incremental benefit on the 200-mg dose after a total of 3 weeks of treatment (regardless of dose), tolcapone should be discontinued

Always use as an adjunct to levodopa/carbidopa

Monitor

Baseline AST, ALT at initiation of treatment, then q2Weeks for 1 year, then q4Weeks for next 6 months, thereafter q8Weeks

Any symptoms of liver injury

Hepatic Impairment

Two SGPT/ALT or SGOT/AST baseline values >ULN: Do not initiate

ALT/AST >2 xULN while taking tolcapone: Discontinue drug

Renal Impairment

CrCl<25 mL/min: Caution, safety and efficacy not established

Amyloidosis (Orphan)

Orphan designation for treatment of transthyretin amyloidosis

Orphan sponsor

  • SOM Innovation Biotech SL (SOM Biotech); Baldiri Reixac 4, 08028; Barcelona, Spain

Safety and efficacy not established

Parkinson disease

100-200 mg PO q8hr

Always as an adjunct to levodopa/carbidopa

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Interactions

Interaction Checker

and tolcapone

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Contraindicated (3)

            • isocarboxazid

              tolcapone, isocarboxazid. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Both nonselective MAO inhibitors and tolcapone inhibit catecholamine metabolism, leading to increased levels of catecholamines. Potential for dangerously high HR or BP.

            • phenelzine

              tolcapone, phenelzine. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Both nonselective MAO inhibitors and tolcapone inhibit catecholamine metabolism, leading to increased levels of catecholamines. Potential for dangerously high HR or BP.

            • tranylcypromine

              tolcapone, tranylcypromine. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Both nonselective MAO inhibitors and tolcapone inhibit catecholamine metabolism, leading to increased levels of catecholamines. Potential for dangerously high HR or BP.

            Serious - Use Alternative (1)

            • metoclopramide intranasal

              tolcapone, metoclopramide intranasal. Either increases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Avoid use of metoclopramide intranasal or interacting drug, depending on importance of drug to patient.

            Monitor Closely (8)

            • dobutamine

              tolcapone will increase the level or effect of dobutamine by decreasing metabolism. Use Caution/Monitor. Tolcapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • dopamine

              tolcapone will increase the level or effect of dopamine by decreasing metabolism. Use Caution/Monitor. Tolcapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • epinephrine

              tolcapone will increase the level or effect of epinephrine by decreasing metabolism. Use Caution/Monitor. Tolcapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • epinephrine inhaled

              tolcapone will increase the level or effect of epinephrine inhaled by decreasing metabolism. Use Caution/Monitor. Tolcapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • epinephrine racemic

              tolcapone will increase the level or effect of epinephrine racemic by decreasing metabolism. Use Caution/Monitor. Tolcapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • isoproterenol

              tolcapone will increase the level or effect of isoproterenol by decreasing metabolism. Use Caution/Monitor. Tolcapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • methyldopa

              tolcapone will increase the level or effect of methyldopa by decreasing metabolism. Use Caution/Monitor. Tolcapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            • norepinephrine

              tolcapone will increase the level or effect of norepinephrine by decreasing metabolism. Use Caution/Monitor. Tolcapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.

            Minor (0)

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              Adverse Effects

              >10%

              Dyskinesia (45-50%)

              Nausea (30-35%)

              Insomnia (21-25%)

              Hallucinations (8-24%)

              Excessive dreaming (16-21%)

              Diarrhea (16-20%)

              Anorexia (16-20%)

              Dystonia (16-20%)

              Muscle cramping (16-20%)

              Somnolence (16-20%)

              Orthostatic hypotension (11-15%)

              Confusion (10-11%)

              Headache (10-11%)

              1-10%

              Vomiting (8-10%)

              Constipation (6-8%)

              URI (5-7%)

              Fatigue (3-7%)

              Abdominal pain (5-6%)

              Xerostomia (5-6%)

              UTI (5%)

              Hematuria (4-5%)

              Syncope (4-5%)

              Dyspnea (3%)

              Loss of balance (2-3%)

              Urine discoloration (2-3%)

              Chest pain (1-3%)

              Hyper/hypokinesia (1-3%)

              Parasthesia (1-3%)

              Transaminases increased (1-3%, usually 3x ULN in first 6 mos of therapy)

              Hypotension (2%)

              Neck pain (2%)

              Stiffness (2%)

              Sinus congestion (1-2%)

              <1%

              Dysphagia

              GI hemorrhage

              Gastroenteritis

              Mouth ulceration

              Salivation increase

              Esophagitis

              Cholelithiasis

              Colitis

              Dopaminergic side effects due to increased dopamine levels

              Hepatocellular injury, including liver failure

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              Warnings

              Black Box Warnings

              Because of risk of potentially fatal, acute fulminant liver failure, reserve use for in patients with Parkinson’s disease on l-dopa/carbidopa who are experiencing symptom fluctuations and are not responding satisfactorily to or are not appropriate candidates for other adjunctive therapies

              If substantial benefit not observed within 3 weeks following initiation, withdraw therapy

              Do not initiate if clinical evidence of liver disease or two SGPT/ALT or SGOT/AST values >ULN

              Discontinue if SGPT/ALT or SGOT/AST levels exceed 2 xULN 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)

              Patients with severe dyskinesia or dystonia should be treated with caution

              Patients who develop hepatocellular injury while taking tolcapone and are withdrawn from the drug are at increased risk for liver injury if tolcapone reintroduced

              Contraindications

              Hypersensitivity

              Liver disease or history of tolcapone-induced hepatotoxicity

              History of: non-traumatic rhabdomyolysis, drug-related hyperpyrexia & confusion

              Cautions

              Risk of potentially fatal hepatotoxicity; withdraw drug if no improvement in 3 wk

              Do not initiate treatment if AST/ALT >ULN; discontinue if liver enzymes >2 xULN

              Impulse control/compulsive behaviors: Risk of uncontrollable sexual, gambling or other urges

              Orthostatic hypotension, diarrhea, hallucinations, psychotic-like behavior, rhabdomyolysis, renal/hepatic impairment, hematuria, hyperpyrexia, confusion, and fibrotic complications may occur

              May be linked to higher melanoma risk in Parkinson's patients

              Avoid abrupt withdrawal

              May increase risk for falling asleep during activities of daily living

              Do not coadminister with nonselective MAO inhibitor (ie, MAO-A inhibitors); combination may result in result in inhibition of the majority of the pathways responsible for normal catecholamine metabolism

              Discontinued in Canada

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              Pregnancy & Lactation

              Pregnancy Category: C

              Lactation: not known if secreted in breast milk, use caution

              Pregnancy Categories

              A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

              B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

              C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

              D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

              X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

              NA: Information not available.

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              Pharmacology

              Mechanism of Action

              Reversible catechol-O-methyltransferase (COMT) inhibitor that prolongs the half-life of levodopa

              Pharmacokinetics

              Peak Plasma Time: 2 hr

              Concentration (100/200 mg q8hr for7 days): 3.5/6.4 mcg/mL

              Excretion: Urine (60%); feces (40%)

              Bioavailability: 65-85%

              Protein Bound: >99.9%

              Half-life elimination: 2-3hr

              Vd: 9 L

              Metabolism: Liver glucuronidation

              Total body clearance: 7 L/hr

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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              tolcapone oral
              -
              100 mg tablet
              tolcapone oral
              -
              100 mg tablet
              Tasmar oral
              -
              100 mg tablet

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Patient Education
              tolcapone oral

              TOLCAPONE - ORAL

              (TOLL-cup-own)

              COMMON BRAND NAME(S): Tasmar

              WARNING: Rarely, tolcapone has caused a severe (sometimes fatal) liver problem (liver failure). Tolcapone should not be used if you have even mild liver disease. You should only use tolcapone if you are experiencing problems with your levodopa wearing off between doses. If you show no benefit from tolcapone after 3 weeks of using it, your doctor may choose to stop it.Before and during treatment with tolcapone, you will have certain blood tests (liver function tests) every few weeks to monitor for liver problems. Keep all medical and lab test appointments. Tell your doctor right away if you experience symptoms of liver problems (such as persistent nausea/vomiting, abdominal pain, dark urine, severe tiredness, loss of appetite, itchiness). If you experience liver problems from taking tolcapone, you should not take it again.Your doctor may ask you to sign a consent form after telling you about the possible side effects of this medication.

              USES: This medication 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 TO USE: 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 your doctor 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).

              SIDE EFFECTS: See also Warning section.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.Many people using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.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.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: See also Warning section.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 (cannabis) 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 (cannabis). 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.

              DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some of the products that may interact with this drug include: certain MAO inhibitors (isocarboxazid, linezolid, metaxalone, 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 (cannabis), antihistamines (such as cetirizine, diphenhydramine), drugs for sleep or anxiety (such as alprazolam, diazepam, zolpidem), muscle relaxants, and opioid 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.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

              NOTES: Do not share this medication with others.Laboratory and/or medical tests (such as liver function tests) should be performed before you start tolcapone and periodically during your treatment to monitor your progress or check for side effects. Consult your doctor for more details.People with Parkinson's disease may have an increased risk for developing skin cancer (melanoma). Tell your doctor promptly if you notice a change in the appearance or size of moles or other unusual skin changes. Ask your doctor if you should have regular skin exams.

              MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

              STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

              Information last revised September 2021. Copyright(c) 2021 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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