Version July 2025
Parkinson disease: Oral: 50 mg once daily at bedtime.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling; use with caution in severe impairment. Avoid use in patients with end-stage renal disease (CrCl <15 mL/minute).
Mild (Child-Pugh class A): There are no dosage adjustments provided in the manufacturer's labeling.
Moderate (Child-Pugh class B): 25 mg once daily at bedtime.
Severe (Child-Pugh class C): Avoid use (has not been studied).
Refer to adult dosing.
New-onset or exacerbation of preexisting dyskinesia was the most common adverse effect of opicapone, in combination with levodopa, as well as the most common adverse event leading to discontinuation in clinical trials; most of the dyskinesia events occurred in patients already experiencing dyskinesia at baseline during clinical trials (Ref). During clinical trials, most of the gain of on-time with opicapone was without troublesome dyskinesia; in addition, there was no significant difference between placebo and opicapone with regards to the increase in on-time with troublesome dyskinesia (Ref).
Mechanism: Dose-related; related to the pharmacologic action (ie, potentiation of dopaminergic effects) (Ref).
Onset: Varied; most dyskinetic events occurred within the first 4 weeks of treatment in clinical trials (Ref).
Risk factors:
• Higher doses of levodopa
• Concomitant use of other dopaminergic drugs
• Preexisting dyskinesia (Ref)
Impulse control disorder (ICD) and/or compulsive behaviors, which may manifest as pathological gambling, hypersexuality, intense urges to spend money uncontrollably, and other intense urges, have been reported (Ref). In some cases, the behavior will subside with a dose reduction or discontinuation.
Mechanism: Dose-related; related to the pharmacologic action (ie, potentiation of dopaminergic effects) (Ref). The impact of the disease process and concurrent medications must be considered (Ref).
Onset: Variable; based on clinical experience, onset of dopaminergic adverse effects often occurs within the first several weeks following initiation of catechol-O-methyltransferase inhibitor therapy; onset may be dependent on the presence of patient risk factors and concomitant medications.
Risk factors:
• In general, the following are potentially associated with Parkinson disease-impulse control behaviors (Ref):
- Concomitant use of dopamine agonists
- Concomitant use of levodopa use; Note: Some studies have failed to find an association or strong association with the use of levodopa and the risk of ICD (Ref)
- Duration of treatment (Ref)
- Younger age
- Male patients
- Comorbid depression
- Comorbid anxiety
• Suspected or diagnosed dopamine dysregulation syndrome
Opicapone, in combination with levodopa, may cause orthostatic hypotension; orthostatic hypotension has resulted in treatment discontinuation (Ref). In addition, nonorthostatic hypotension, presyncope, and syncope have been reported.
Mechanism: Dose-related; related to the pharmacologic action (ie, potentiation of dopaminergic effects) (Ref).
Risk factors:
• Concomitant use of other hypotensive agents
• In general, the following risk factors may increase the likelihood of orthostatic hypotension in Parkinson disease (Ref)
- Age >68 years
- Polypharmacy (use of >5 medications)
- Concomitant use of amantadine or diuretics
Note: Concomitant use of entacapone, another catechol-O-methyltransferase inhibitor, appeared to reduce the risk of orthostatic hypotension in this study.
Use of opicapone, in combination with levodopa, may result in hallucinations, including auditory hallucinations, visual hallucinations, or mixed hallucinations; may also cause aggressive behavior, agitation, or delusions. During one clinical trial, visual hallucinations resulted in treatment discontinuation in several patients (Ref).
Mechanism: Dose-related; related to the pharmacologic action (ie, potentiation of dopaminergic effects) (Ref)
Onset: Variable; based on clinical experience, onset of dopaminergic adverse effects often occurs within the first several weeks following initiation of catechol-O-methyltransferase inhibitor therapy; onset may be dependent on the presence of patient risk factors and concomitant medications.
Risk factors:
• Prior history of a major psychotic disorder
• Age ≥70 years (Ref)
• Concomitant use of other agents known to cause psychiatric effects (eg, dopaminergic agonists, anticholinergic agents)
Opicapone, when added to levodopa, may result in a sudden onset of sleep while engaging in activities of daily living, including sleep driving; events have been reported to occur without significant warning signs and may result in accidents. Patients may report feeling alert immediately prior to events.
Mechanism: Dose-related; related to the pharmacologic action (ie, potentiation of dopaminergic effects).
Onset: Varied; based on clinical experience, onset may occur within the first several weeks of treatment with catechol-O-methyltransferase (COMT) inhibitors but may also develop years later in some patients. One case report described onset of irresistible sleep episodes 3 days following initiation of entacapone, another COMT inhibitor (Ref).
Risk factors:
• Preexisting sleep disorder
• Concomitant use of other sedating agents
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%: Neuromuscular & skeletal: Dyskinesia (20%) (table 1)
|
Drug (Opicapone) |
Placebo |
Dose |
Number of Patients (Opicapone) |
Number of Patients (Placebo) |
|---|---|---|---|---|
|
20% |
6% |
50 mg/day |
265 |
257 |
1% to 10%:
Cardiovascular: Hypertension (3%), hypotension (including orthostatic hypotension, presyncope, syncope: 5%) (table 2), increased serum creatine kinase (5%)
|
Drug (Opicapone) |
Placebo |
Dose |
Number of Patients (Opicapone) |
Number of Patients (Placebo) |
Comments |
|---|---|---|---|---|---|
|
5% |
1% |
50 mg/day |
265 |
257 |
Including orthostatic hypotension, presyncope, syncope |
Endocrine & metabolic: Weight loss (4%)
Gastrointestinal: Constipation (6%), xerostomia (3%)
Nervous system: Dizziness (3%), hallucination (including auditory hallucinations, visual hallucinations: 3% (table 3)), impulse control disorder (1%) (table 4), insomnia (3%), psychosis (including aggressive behavior, agitation, delusion: 1%) (table 5)
|
Drug (Opicapone) |
Placebo |
Dose |
Number of Patients (Opicapone) |
Number of Patients (Placebo) |
Comments |
|---|---|---|---|---|---|
|
3% |
1% |
50 mg/day |
265 |
257 |
Including auditory hallucination, visual hallucination, mixed hallucination |
|
Drug (Opicapone) |
Placebo |
Dose |
Number of Patients (Opicapone) |
Number of Patients (Placebo) |
|---|---|---|---|---|
|
1% |
0% |
50 mg/day |
265 |
257 |
|
Drug (Opicapone) |
Placebo |
Dose |
Number of Patients (Opicapone) |
Number of Patients (Placebo) |
Comments |
|---|---|---|---|---|---|
|
1% |
0% |
50 mg/day |
265 |
257 |
Including aggressive behavior, agitation, delusion |
Frequency not defined: Nervous system: Sleep driving, sudden onset of sleep
Postmarketing: Nervous system: Falling
Concomitant use of nonselective monoamine oxidase inhibitors; pheochromocytoma, paraganglioma, or other catecholamine secreting neoplasms.
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Disease-related concerns:
• Hepatic impairment: Use with caution in patients with mild to moderate hepatic impairment; avoid use in severe impairment.
• Renal impairment: Use caution in patients with severe renal impairment; discontinue opicapone if tolerability issues arise. Avoid use in patients with end-stage renal disease (CrCl <15 mL/minute).
Other warnings/precautions:
• Discontinuation of therapy: Dopaminergic agents have been associated with a syndrome resembling neuroleptic malignant syndrome upon withdrawal or abrupt dosage reduction; patients should be monitored closely if therapy is discontinued.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral:
Ongentys: 25 mg, 50 mg [contains fd&c blue #2 (indigotine,indigo carmine)]
No
Capsules (Ongentys Oral)
25 mg (per each): $29.47
50 mg (per each): $29.47
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Oral: Administer at bedtime; do not eat for 1 hour before and at least 1 hour after dose.
Parkinson disease: Adjunctive treatment to levodopa/carbidopa in patients with Parkinson disease experiencing “off” episodes.
Opicapone may be confused with entacapone or tolcapone.
Ongentys (brand name for opicapone) may be confused with Onglyza (brand name for saxagliptin).
Substrate of BCRP, MRP2, OATP1B1/1B3, OATP2B1, P-glycoprotein (Minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits COMT;
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
CNS Depressants: Opicapone may increase CNS depressant effects of CNS Depressants. Risk C: Monitor
COMT Substrates: COMT Inhibitors may increase serum concentration of COMT Substrates. Risk C: Monitor
Fluorodopa F18: Coadministration of COMT Inhibitors and Fluorodopa F18 may alter diagnostic results. Management: Discontinue medications used to treat Parkinson disease, including peripheral COMT inhibitors, 12 hours prior to fluorodopa F 18 administration if these medications can be safely withheld. Risk D: Consider Therapy Modification
Monoamine Oxidase Inhibitors: Opicapone may increase adverse/toxic effects of Monoamine Oxidase Inhibitors. Risk X: Avoid
Food decreases the rate and extent of absorption of opicapone. Management: Do not eat for 1 hour before and at least 1 hour after opicapone.
Based on data from animal reproduction studies, in utero exposure to opicapone may cause fetal harm. Opicapone is used in combination with levodopa/carbidopa. Also refer to the Levodopa/Carbidopa monographs for additional information.
It is not known if opicapone is present in breast milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Opicapone is used in combination with levodopa/carbidopa. Also refer to the Levodopa/Carbidopa monographs for additional information.
Liver and renal function tests (baseline and as clinically indicated); BP (baseline and as clinically indicated); mental alertness, daytime somnolence, preexisting sleep disorder.
Opicapone is a reversible and selective inhibitor of catechol-O-methyltransferase (COMT); COMT is the major degradation pathway for levodopa. When opicapone is taken with levodopa, the pharmacokinetics are altered, resulting in more sustained levodopa serum levels compared to levodopa taken alone. The resulting levels of levodopa provide for increased concentrations available for absorption across the blood-brain barrier, thereby providing for increased CNS levels of dopamine, the active metabolite of levodopa.
Absorption: With a moderate-fat/moderate-calorie meal, the mean Cmax decreased 62%, AUC decreased 31%, and the Tmax was delayed by 4 hours.
Protein binding: >99%.
Metabolism: Via sulphation (primarily), glucuronidation, methylation, reduction, and glutathione concentration.
Half-life elimination: 1 to 2 hours.
Time to peak: 2 hours (range: 1 to 4 hours).
Excretion: Feces: ~70% (22% as unchanged drug); expired air: 20%; urine: 5% (<1% as unchanged drug).
Hepatic function impairment: AUC increased by 35% in mild impairment (Child-Pugh class A) and 84% in moderate impairment (Child-Pugh class B).
