Tolcapone

DEA Class;  Rx

Common Brand Names; Tasmar

  • Antiparkinson Agents, COMT Inhibitors

Peripheral and centrally acting oral COMT inhibitor; improves levodopa availability in the CNS; more potent than entacapone
Used for adults with Parkinson’s disease as an adjunct to levodopa/carbidopa
Less favorable side effect profile vs. entacapone; boxed warning exists in labeling for hepatotoxicity and risk for hepatocellular injury and liver failure

Indicated for use as adjunctive treatment to levodopa and carbidopa for the treatment of signs and symptoms of idiopathic Parkinson’s disease.

Hypersensitivity

Liver disease or history of tolcapone-induced hepatotoxicity

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

  • 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%)
  • 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%)

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

Pregnancy Category: C

Lactation: not known if secreted in breast milk, use caution

Adults

600 mg/day PO.

Geriatric

600 mg/day PO.

Adolescents

Safety and efficacy have not been established. 

Children

Safety and efficacy have not been established. 

Infants

Not indicated.

Tolcapone

tablet

  • 100mg

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