From the FDA Drug Label
In Study 2, ONGENTYS administration and food consumption were separated by 1 hour [see Dosage and Administration (2. 1), Clinical Studies (14)]. Distribution Opicapone is highly bound to plasma proteins (>99%), which is independent of concentration. Elimination The mean elimination half-life of opicapone is 1 to 2 hours. Metabolism Sulphation is the primary metabolic pathway of opicapone, based on clinical studies and in vitro assessments Other metabolic pathways include glucuronidation, methylation (by COMT), reduction, and glutathione conjugation. Excretion After administration of a single dose of radiolabeled opicapone 100 mg (2 times the recommended dosage) to healthy subjects, approximately 70% of the dose was recovered in feces (22% as unchanged), 20% in expired air, and 5% in urine (<1% as unchanged)
The main pharmacokinetic properties of opicapone are:
- High plasma protein binding (>99%)
- Short elimination half-life (1 to 2 hours)
- Primary metabolic pathway is sulphation
- Excretion is mainly through feces (70% of the dose) 1
From the Research
Opicapone should be prescribed at a dose of 50 mg taken once daily at bedtime for patients with Parkinson's disease experiencing "wearing-off" symptoms between their regular levodopa doses, as it has been shown to reduce OFF time by an average of about 60 minutes daily compared with placebo 2.
Key Points
- Opicapone is a catechol-O-methyltransferase (COMT) inhibitor that helps to prolong the effects of levodopa therapy by preventing its breakdown in the body 3.
- It is specifically used for patients experiencing "wearing-off" symptoms between their regular levodopa doses and should always be taken in combination with levodopa/carbidopa or levodopa/benserazide, not as a standalone treatment 4.
- Common side effects include dyskinesia (involuntary movements), constipation, dry mouth, and dizziness 5.
- Patients should be aware that opicapone may interact with certain medications like MAO inhibitors, COMT substrates, and some antidepressants 2.
- The medication works by inhibiting the COMT enzyme in peripheral tissues, which normally breaks down levodopa before it can reach the brain, thereby allowing more levodopa to cross the blood-brain barrier and be converted to dopamine, helping to control Parkinson's symptoms more consistently throughout the day 6.
Benefits and Risks
- The benefits of opicapone include a significant reduction in OFF time and an improvement in motor function 4, 2.
- The risks associated with opicapone include dyskinesia, constipation, dry mouth, and dizziness, as well as potential interactions with other medications 5, 6.
Clinical Evidence
- Clinical trials have demonstrated the efficacy and safety of opicapone in reducing OFF time and improving motor function in patients with Parkinson's disease 3, 4, 2.
- Post-hoc analyses and observational studies have also suggested the wider applicability of opicapone for different phenotypes of motor complications and for Parkinson's disease stages 6.