The highest dose of tolcapone administered to humans was 800 mg tid, with and without levodopa/carbidopa coadministration. This was in a 1-week study in elderly, healthy volunteers. The peak plasma concentrations of tolcapone at this dose were on average 30 μg/mL (compared to 3 μg/mL and 6 μg/mL with 100 mg and 200 mg tolcapone, respectively). Nausea, vomiting and dizziness were observed, particularly in combination with levodopa/carbidopa.

THE THRESHOLD FOR THE LETHAL PLASMA CONCENTRATION FOR TOLCAPONE BASED ON ANIMAL DATA IS > 100 μG/ML. RESPIRATORY DIFFICULTIES WERE OBSERVED IN RATS AT HIGH ORAL (GAVAGE) AND INTRAVENOUS DOSES AND IN DOGS WITH RAPIDLY INJECTED INTRAVENOUS DOSES.

Management of Overdose

Hospitalization is advised. General supportive care is indicated. Based on the physicochemical properties of the compound, hemodialysis is unlikely to be of benefit.

TASMAR (tolcapone) tablets are contraindicated in patients with liver disease, in patients who were withdrawn from TASMAR (tolcapone) because of evidence of TASMAR (tolcapone) -induced hepatocellular injury or who have demonstrated hypersensitivity to the drug or its ingredients.

TASMAR (tolcapone) is also contraindicated in patients with a history of non-traumatic rhabdomyolysis or hyperpyrexia and confusion possibly related to medication (see PRECAUTIONS: Events Reported With Dopaminergic Therapy).

Last reviewed on RxList: 3/12/2009
This monograph has been modified to include the generic and brand name in many instances.