Tolcapone(toll kap’ own)
Tasmar
PREGNANCY CATEGORY C
Drug Classes
Antiparkinsonian
COMT inhibitor
Therapeutic Actions
Selectively and reversibly inhibits COMT, an enzyme that eliminates biologically active catecholamines including dopa, dopamine, norepinephrine, epinephrine; when given with levodopa, tolcapone’s inhibition of COMT is believed to increase the plasma concentrations and duration of action of levodopa.
Indications
Adjunct with levodopa and carbidopa in the treatment of the signs and symptoms of idiopathic Parkinson disease
Contraindications and Cautions
Contraindicated with hypersensitivity to drug or its components, lactation, liver disease, patients with a history of nontraumatic rhabdomyolysis or hyperpyrexia and confusion.
Use cautiously with hypertension, hypotension, or renal impairment; pregnancy.
Available Forms
Tablets—100 mg
Dosages
Adults
Initial maintenance dosage, 100 mg PO tid. Maximum daily dose, 600 mg. 200 mg tid is
more associated with liver enzyme elevation and is only recommended when benefit outweighs risk. However, 200 mg tid can be used if benefit is justified. If patient does not show a clinical benefit within 3 wk of treatment with 200 mg tid, tolcapone should be discontinued.
more associated with liver enzyme elevation and is only recommended when benefit outweighs risk. However, 200 mg tid can be used if benefit is justified. If patient does not show a clinical benefit within 3 wk of treatment with 200 mg tid, tolcapone should be discontinued.
Pediatric patients
Safety and efficacy not established.
Patients with renal or hepatic impairment
Discontinue drug if liver enzyme values are greater than twice upper limit of normal. Patients with moderate to severe hepatic impairment should not exceed 100 mg PO tid; patients with liver enzyme values greater than the upper limit of normal at initiation should not receive this drug. Use caution in patients with renal impairment.
Pharmacokinetics
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