tolcapone (Rx)

Brand and Other Names:Tasmar
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 100mg
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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

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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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

            Contraindications

            Hypersensitivity

            Liver disease or history of tolcapone-induced hepatotoxicity

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

            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

            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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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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