Tolcapone

TASMAR

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Pronunciation: TOEL-ka-poen

Tolcapone ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Tolcapone ballicule

Tolcapone TASMAR mascot mnemonic cartoon — Visual mnemonic: Tolcapone mascot
**“Total Capone Taskbar”**

What it isCentral and peripheral catechol-O-methyltransferase inhibitor used with levodopa/carbidopa for Parkinson disease with motor fluctuations.

Why this oneCrosses the blood-brain barrier and extends levodopa effect more strongly than peripheral-only COMT inhibitors.

What limits itReserved for patients who fail or cannot use other adjuncts; monitor liver tests and stop within 3 weeks if there is no substantial benefit.

Tolcapone molecular structure (skeletal formula) — Molecular structure: Tolcapone

FDA-approved for

Parkinson disease with motor fluctuations (1998)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Risk of potentially fatal acute fulminant liver failure; reserve for fluctuating Parkinson's not responding to other adjuncts; withdraw if no benefit within 3 weeks; do not initiate with liver disease or ALT/AST >2x ULN.

FDA dosing	Population	Start	Target	Max
Parkinson's disease (adjunct to levodopa/carbidopa)	Adult	100 mg TID	100 mg TID	200 mg TID

Renal Undefined

Hepatic Contraindicated in liver disease; do not initiate if ALT/AST >2x ULN

Instructions

Only prescribe with concomitant carbidopa/levodopa.
Withdraw if no substantial clinical benefit within 3 weeks.
Do not retreat patients withdrawn for hepatocellular injury.

Available strengths

tab 100 mg

Contraindications

Liver disease
Prior tolcapone-induced hepatocellular injury (withdrawn from drug)
History of nontraumatic rhabdomyolysis or hyperpyrexia and confusion possibly medication-related

Cautions

Hepatocellular injury / fulminant liver failure - monitor LFTs
Rhabdomyolysis
Use caution with severe dyskinesia or dystonia
Events reported with dopaminergic therapy (hallucinations, hypotension)

Adverse reactions

Severe hepatocellular injury incl. fatal fulminant liver failure
Elevated ALT/AST

Pregnancy No adequate human data; animal embryo-fetal toxicity; given with levodopa/carbidopa (teratogenic in rabbits)

Lactation Undefined

Cost

Tolcapone (TASMAR)

Strength		#/mo	generic $/mo	CostPlus
100 mg	tab	90 TID		out of stock

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Tolcapone is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2015

⚠ BOXED WARNINGS

Potentially fatal acute fulminant liver failure
Use only for levodopa-treated Parkinson disease with fluctuations not adequately managed by other adjuncts
Stop if substantial benefit is absent within 3 weeks

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability1 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk1 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityOrthostasis, hallucinations, dyskinesia and impulse-control symptoms; abrupt withdrawal can be hazardous.

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Memory aids: interaction avatars

no kinetic interactions

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