Classes
DEA Class; Rx
Common Brand Names; Tasmar
- Antiparkinson Agents, COMT Inhibitors
Description
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
Indications
Indicated for use as adjunctive treatment to levodopa and carbidopa for the treatment of signs and symptoms of idiopathic Parkinson’s disease.
Contraindications
Hypersensitivity
Liver disease or history of tolcapone-induced hepatotoxicity
History of: non-traumatic rhabdomyolysis, drug-related hyperpyrexia & confusion
Adverse Effects
- 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%)
Warnings
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 and Lactation
Pregnancy Category: C
Lactation: not known if secreted in breast milk, use caution
Maximum Dosage
600 mg/day PO.
600 mg/day PO.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
Not indicated.
How supplied
Tolcapone
tablet
- 100mg