Medically reviewed on January 10, 2018.
Applies to the following strengths: 100 mg; 200 mg
Usual Adult Dose for:
Additional dosage information:
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
-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Patients who develop hepatocellular injury while on this drug and are withdrawn from this drug for any reason may be at increased risk for liver injury if this drug is restarted; therefore, restarting this drug is generally not recommended
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.
-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.
US BOXED WARNINGS: LIVER FAILURE
-Because of the risk of potentially fatal, acute fulminant liver failure, this drug should ordinarily be used 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.
-Because of the risk of liver injury and because this drug, 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 this drug.
-This drug should not be initiated if the patient exhibits clinical evidence of liver disease or if two SGPT/ALT or SGOT/AST values are 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 THIS DRUG, 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 to 100-fold higher than the general population (however, underreporting may mean there is a significant underestimation of the increased risk). All 3 cases of fatal fulminant hepatic failure were reported within the first 6 months of drug initiation. Analysis of the laboratory monitoring data in over 3,400 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.
-If used, it 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 classic signs of liver disease (e.g., clay colored stools, jaundice) and the nonspecific signs (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, appropriate tests to exclude the presence of liver disease should be performed. 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, thereafter, periodic monitoring is recommended at clinically relevant intervals. If the dose is increased to 200 mg 3 times a day, liver enzyme monitoring should take place before increasing the dose and then every 2 to 4 weeks for the following 6 months. After 6 months, periodic monitoring is recommended at clinically relevant intervals.
-This drug should be discontinued if SGPT/ALT or SGOT/AST levels exceed 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).
Safety and efficacy have not been established in patients younger than 18 years.
Consult WARNINGS section for additional precautions.
Hemodialysis: tolcapone is highly protein bound, therefore no significant removal of the drug is expected.
-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
-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.
-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.
-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.
More about tolcapone
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- Drug class: dopaminergic antiparkinsonism agents
Other brands: Tasmar