tolcapone: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
tolcapone: clinical details
Prescribing considerations
- Initiation and supervision should be by a physician experienced in advanced Parkinson’s disease after discussion of hepatic risk.
- Reserve for levodopa-responsive motor fluctuations after failure or intolerance of other COMT inhibitors.
- Review levodopa-related adverse effects and symptom control when tolcapone is introduced or withdrawn.
- Use caution in severe renal impairment because tolerability data are limited.
- Monitor patients and carers for impulse-control disorders and sudden sleep episodes.
Contraindications and cautions
- Liver disease or increased liver enzymes
- Severe dyskinesia
- Previous neuroleptic malignant syndrome, non-traumatic rhabdomyolysis or hyperthermia
- Phaeochromocytoma
- Concomitant non-selective MAO inhibition
- Hypersensitivity to tolcapone or an excipient
Monitoring
- Check liver function before treatment; do not initiate if results are abnormal or hepatic impairment is suspected.
- Monitor liver enzymes regularly throughout treatment.
- Stop treatment immediately if ALT or AST exceeds the upper limit of normal or clinical features suggest hepatic failure.
- Monitor coagulation parameters during concomitant warfarin treatment.
- Review blood pressure, dyskinesia, neuropsychiatric effects, diarrhoea and overall clinical benefit.
Clinical pharmacology
Tolcapone is an orally active, selective, reversible COMT inhibitor. It reduces levodopa conversion to 3-O-methyldopa, prolongs levodopa elimination and increases its bioavailability. It is highly protein-bound and extensively metabolised, principally by glucuronidation.
Formulation and product differences
- The selected UK product is a pale-to-light-yellow film-coated tablet intended to be swallowed whole.
- It contains lactose monohydrate and is essentially sodium-free.
- It can be combined with immediate- or sustained-release formulations of levodopa/benserazide or levodopa/carbidopa.
tolcapone preparations and strengths
Tablet
Route: Oral
Strengths: 100 mg
tolcapone interactions
Important interactions include:
Levodopa combinations
Tolcapone increases levodopa exposure and may worsen dyskinesia, nausea, hallucinations, faintness or drowsiness.
Non-selective monoamine oxidase inhibitors
Concomitant use is contraindicated; combined MAO-A and MAO-B inhibition is treated as non-selective inhibition.
Warfarin
The interaction is insufficiently characterised, so coagulation measurements require closer monitoring.
Potent noradrenaline-reuptake inhibitors
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.