opicapone

Contraindicated in:

Concurrent use of nonselective MAO inhibitors;
Pheochromocytoma, paraganglioma, or other catecholamine secreting neoplasms;
Major psychotic disorders;
End-stage renal disease (CCr <15 mL/min);
Severe hepatic impairment.

Use Cautiously in:

Severe renal impairment;
Moderate hepatic impairment (↓ dose);
OB: Safety not established in pregnancy;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults may have ↑ risk of adverse reactions.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension, hypotension, presyncope, syncope

GI: constipation, dry mouth

Metab: ↓weight

MS: ↑creatine kinase

Neuro: dyskinesia, aggressive behavior, agitation, delusions, dizziness, hallucinations, impulse control disorders (gambling, sexual, uncontrolled spending, binge/compulsive eating), insomnia, psychosis, somnolence

Interactions ⬆ ⬇

Drug-drug:

Nonselective MAO inhibitors, including isocarboxazid, phenelzine, or tranylcypromine may significantly ↑ risk of arrhythmias, tachycardia, and ↑ BP; concurrent use contraindicated (can concomitantly use selective MAO-B inhibitors with opicapone).
Concurrent use of drugs that are metabolized by COMT, including dopamine, dobutamine, epinephrine, isoproterenol, and norepinephrine, may ↑ risk of arrhythmias, tachycardia, and ↑ BP; closely monitor.

Availability ⬆ ⬇

Capsules: 25 mg; 50 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 50 mg once daily at bedtime.

Hepatic Impairment

PO (Adults ): Moderate hepatic impairment: 25 mg once daily at bedtime.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as a selective and reversible inhibitor of the enzyme, catechol-O-methyltransferase (COMT), which prevents the metabolism of levodopa, increasing its availability to the CNS.

Therapeutic effects:

Reduction in “off” episodes.

Classifications ⬆ ⬇

Therapeutic Classification: antiparkinson agents

Pharmacologic Classification: catechol o methyltransferase comt inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: Moderate fat/calorie meal delays and reduces extent of absorption.

Distribution: Unknown.

Protein Binding: >99%.

Metabolism/Excretion: Primarily metabolized via sulfation, and to a lesser extent by glucuronidation, methylation, reduction, and glutathione conjugation; primarily excreted in feces (77%; 22% as unchanged drug), with 20% in expired air, and 5% in urine (<1% as unchanged drug).

Half-Life: 1–2 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2 hr	unknown

Patient/Family Teaching ⬆ ⬇

Instruct patient to take opicapone as directed on an empty stomach. Omit missed doses and take next scheduled dose next day. Caution patient not to discontinue opicapone without consulting health care professional. Abrupt discontinuation or rapid dose reduction may result in neuroleptic malignant syndrome (fever, muscular rigidity, altered consciousness, autonomic instability). Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
Caution patient to make position changes slowly to minimize orthostatic hypotension, especially at start of therapy. Notify health care professional if orthostatic hypotension occurs.
May cause sudden onset of sleep, drowsiness, or dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Advise patient to avoid taking alcohol or other CNS depressants concurrently with opicapone.
Inform patient and caregiver that hallucinations, nausea, dyskinesia, or dystonia may occur during opicapone therapy. Notify health care professional if hallucinations occur; may need to discontinue therapy.
Advise patient to notify health care professional if new or increased gambling, sexual, or other intense urges or hallucinations occur. Dose reduction may be required.
Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Indications ⬇

Contraind./Precautions ⬆ ⬇